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Howard I Maibach - One of the best experts on this subject based on the ideXlab platform.

  • effect of topical Laurocapram azone on the in vitro percutaneous permeation of sodium lauryl sulfate using human skin
    Acta Dermato-venereologica, 1996
    Co-Authors: C Szolarplatzer, Sunita Patil, Howard I Maibach
    Abstract:

    The probability of simultaneous cutaneous exposure to surfactants and penetration enhancers could occur frequently during routine skin treatment. This study ascertains whether pre-exposure of skin to Laurocapram would affect the penetration of a model surfactant, sodium lauryl sulfate (SLS). In vitro experiments with human skin were performed to compare the penetration of SLS after pretreatment with (1) different concentrations of Laurocapram, (2) after repeated SLS treatments, (3) untreated controls, and (4) water-control. Pre-exposure to Laurocapram enhanced penetration of SLS compared to all other treatments (p<0.05). Since subsequent pre-exposure of skin to Laurocapram increased SLS penetration, the chances of an elevated skin irritation reaction at the exposed site may therefore be possible. Pre-exposure of the skin with SLS did not increase the SLS flux values significantly, compared to the Laurocapram pretreated skin. From these results it can be proposed that proper care and precautions may be necessary after exposure of skin to Laurocapram and also to various other percutaneous enhancers. Further in vivo correlations are essential to define the clinical implications of this study, especially as related to irritant dermatitis. Key words : percutaneous penetration ; skin irritancy ; penetration enhancer ; topical application.

  • Effect of topical Laurocapram (Azone) on the in vitro percutaneous permeation of sodium lauryl sulfate using human skin.
    Acta dermato-venereologica, 1996
    Co-Authors: Szolar-platzer C, Sunita Patil, Howard I Maibach
    Abstract:

    The probability of simultaneous cutaneous exposure to surfactants and penetration enhancers could occur frequently during routine skin treatment. This study ascertains whether pre-exposure of skin to Laurocapram would affect the penetration of a model surfactant, sodium lauryl sulfate (SLS). In vitro experiments with human skin were performed to compare the penetration of SLS after pretreatment with (1) different concentrations of Laurocapram, (2) after repeated SLS treatments, (3) untreated controls, and (4) water-control. Pre-exposure to Laurocapram enhanced penetration of SLS compared to all other treatments (p

  • Effects of penetration enhancers on in vitro percutaneous absorption of low molecular weight heparin through human skin
    Journal of Controlled Release, 1996
    Co-Authors: Glen L. Xiong, Danyi Quan, Howard I Maibach
    Abstract:

    Abstract The influence of the penetration enhancers, Laurocapram (Azone®), 1,8-cineole, and nerolidol on the in vitro percutaneous absorption of low molecular weight heparin (LMWH) through human skin was investigated. The enhancing effectiveness of the enhancers decreased in the order: Laurocapram > nerolidol > 1,8-cineole. Compared to the control formulation (without enhancers), a 4.4-fold enhancement was observed with 2% Laurocapram and a 2-fold enhancement resulted with 2% nerolidol. There were no significant promoting effects at low concentrations of 1,8-cineole; however, a 3.5-fold increase in LMWH flux resulted with 10% 1,8-cineole. The highest enhancement factor was 5.6 with 5% Laurocapram. Cellophane tape-stripping of the stratum corneum did not affect drug flux compared to the control (full-thickness skin). Thus the epidermis and dermis, as well as the stratum corneum, may constitute major rate determining barriers for LMWH permeation across human skin.

  • An electron spin resonance study of human epidermal lipids using 5-doxyl stearic acid
    Journal of Controlled Release, 1995
    Co-Authors: Danyi Quan, Roger Cooke, Howard I Maibach
    Abstract:

    Abstract The effect of Laurocapram (1-dodecylazacycloheptan-2-one, Azone®) on the lipids of human epidermis was studied by electron spin resonance (ESR) of 5-doxyl stearic acid (5-DSA) intercalated into the epidermis. Order parameters S, polarities ao and S/Wratio (strongly immobilized/weakly immobilized spin label) from the ESR spectra demonstrate that Azone® increased the fluidity and the polarity of the local environment surrounding the spin label, and modified the conformation of epidermal lipid. Skin recovery from the disordered system was observed at a low Azone® concentration. Comparatively, Azone® showed a greater effect on stratum corneum lipid bilayers and a smaller effect on epidermal lipids. There was no direct relationship between the amount of enhancer used and the ESR parameters.

  • An electron spin resonance study : I. Effect of Azone on 5-doxyl stearic acid-labeled human stratum corneum.
    International Journal of Pharmaceutics, 1994
    Co-Authors: Danyi Quan, Howard I Maibach
    Abstract:

    Abstract An electron spin resonance study was performed to investigate the effect of Laurocapram (1-dodecylazacyclo-heptan-2-one, Azone®) on lipid bilayers of human stratum corneum. 5-Doxylstearic acid (5-DSA) was used as a lipid spin label and incorporated with the untreated and treated stratum corneum. Azone® led to a significant change in ESR spectra of human stratum corneum — from strongly immobilized to weakly immobilized spectra. The molecular motion of 5-DSA comprising the Azone®-treated stratum corneum showed an isotropic motion to some extent, which was totally different from the molecular motion of 5-DSA in the untreated stratum corneum. Azone® reduced order parameters (S) by 54–80% at different concentrations. The results suggest that Azone® affected the spin label binding to lipid bilayers and caused an increase in the flexibility and polarity of local bilayers surrounding 5-DSA. The concentration effect of Azone® and influence of ethanol on the stratum corneum were also investigated.

Allen Cato - One of the best experts on this subject based on the ideXlab platform.

  • Phase 1/2 Pilot Study of Methotrexate-Laurocapram Topical Gel for the Treatment of Patients With Early-Stage Mycosis Fungoides
    Archives of dermatology, 2003
    Co-Authors: Marie-france Demierre, Luc Vachon, Lynda Sutton, Allen Cato, Brian Leyland-jones
    Abstract:

    Objectives To assess the safety and tolerability of a topical gel formulation combining methotrexate and Laurocapram and to obtain preliminary information on the therapeutic potential of methotrexate-Laurocapram in patients with early-stage mycosis fungoides (stage IA or IB). Design An open-label, phase 1/2 pilot study. Setting Two academic referral centers. Patients Ten patients 18 years or older with histologically confirmed stage IA or IB mycosis fungoides. Intervention The gel formulation of methotrexate-Laurocapram was applied to the total body surface, excluding genital, perianal areas, nipples, face, and skin under the breasts, on an every-other-day basis for 24 consecutive weeks. Main Outcome Measures The safety of methotrexate-Laurocapram was assessed in this study by reviewing adverse events and laboratory data. Efficacy outcomes included changes in lesion condition and severity assessments, reduction in area of sample lesions, and the investigator's global evaluation. Results Adverse events consisted of skin reactions of mild severity. No clinically significant laboratory abnormalities were observed. Based on the investigator's global evaluation at the end of the treatment phase (week 24), 7 (78%) of 9 patients demonstrated a slight-to-moderate response to treatment with methotrexate-Laurocapram. Statistical significance ( P = .049) was reached for induration and pruritus, a trend ( P = .10) was observed for erythema, and no change was found for scaling ( P = .37). Conclusions These findings indicate that the topical administration of methotrexate-Laurocapram is safe and in general well tolerated. This treatment may represent a new therapeutic potential for patients with mycosis fungoides.

  • activity of a 0 05 triamcinolone acetonide Laurocapram formulation double blind randomized comparison with standard 0 1 triamcinolone acetonide creams and with mild class vi to potent class iii topical corticosteroids
    Current Therapeutic Research-clinical and Experimental, 2001
    Co-Authors: Allen Cato, Lynda Sutton, George N. Manning, Allan S. Kaplan
    Abstract:

    Abstract Background: The addition of Laurocapram, a skin penetration enhancer, to a 0.05% triamcinolone acetonide (TA) cream has been shown to improve the activity of the corticosteroid. Objective: The purpose of these studies was to compare the activity of a 0.05% TA/Laurocapram formulation (TNX) with that of standard 0.1% TA cream formulations and 3 topical corticosteroids classified as mild to potent—fluocinolone acetonide, amcinonide, and mometasone furoate. Methods: Sixty-one healthy adult subjects participated in 2 double-blind, randomized, single-point vasoconstriction studies. In each study, sites on subjects' forearms were exposed to the topical corticosteroid formulation for 6 or 16 hours. The degree of vasoconstriction (ie, skin blanching), a surrogate measure of the activity of the corticosteroid, was assessed 2 hours after the end of the exposure period using a 4-point scale (0 = none, 1=mild, 2=moderate, 3=marked). Results: The vasoconstriction activity of TNX was significantly greater than that of 4 marketed 0.1% TA topical formulations ( P ≤ 0.05), which are classified as mild to mid-strength corticosteroids. The activity of TNX was also greater than that of 0.01% and 0.025% fluocinolone acetonide and 0.1% amcinonide ( P = 0.05), classified as mild, mid-strength, and potent agents, respectively, and similar to that of 0.1% mometasone furoate, a Class IV mid-strength agent. Conclusions: Based on the correlation between the vasoconstriction activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram will enhance the clinical activity of corticosteroids and hence may improve treatments for corticosteroid-responsive dermatoses. Moreover, the TA/Laurocapram formulation can be differentiated therapeutically from conventional TA creams.

  • activity of a triamcinolone acetonide Laurocapram formulation double blind comparisons with triamcinolone acetonide placebo vehicle and mid strength class iv to potent class ii corticosteroids
    Current Therapeutic Research-clinical and Experimental, 2001
    Co-Authors: Allen Cato, Lynda Sutton, Allan S. Kaplan, George N. Manning
    Abstract:

    Background: The activity of corticosteroids is dependent on their ability to penetrate the skin. Laurocapram is a skin penetration enhancer that facilitates absorption of cutaneously applied substances. Objective: The purpose of these studies was to determine whether the addition of Laurocapram to a topical triamcinolone acetonide (TA) 0.05% cream formulation would improve the rate of percutaneous penetration and hence the activity of the corticosteroid, as measured by increased vasoconstriction (ie, skin blanching). Methods: Thirty healthy subjects participated in each of 2 double-blind, randomized, multiple-point vasoconstriction studies comparing the TA 0.05%/Laurocapram (TNX) formulation with the placebo vehicle (TNX without TA), the TNX formulation without Laurocapram (TN), and 3 mid-strength to potent corticosteroid formulations (fluocinolone acetonide 0.025% ointment, betamethasone dipropionate 0.05% cream, and fluocinonide 0.05% cream). Duplicate sites on subjects' forearms were exposed to ∼10 mg of each formulation for 4 or 6 hours. Sites were washed and evaluated 1 hour later (ie, 5 or 7 hours after application). Skin blanching activity, a surrogate marker of clinical activity and the rate of percutaneous penetration, was assessed 12 times over a 57-hour period using a 4-point scale (0 = none; 1 = mild; 2 = moderate; 3 = marked). Results: In the first study, the vasoconstriction effect of the TNX formulation after 4 hours of exposure to the cream was significantly greater than that of TN (P < 0.01). In the second study, after 6 hours of exposure, the skin blanching activity of TNX was significantly greater (P = 0.05) than that of fluocinolone acetonide 0.025% ointment, a mid-strength corticosteroid, and betamethasone dipropionate 0.05% cream, a potent corticosteroid, and slightly less than that of fluocinonide 0.05% cream, also classified as a potent corticosteroid. Conclusions: Based on the correlation between the vasoconstrictor activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram enhances the skin penetration of, and hence the activity of, topical corticosteroids and may improve treatments for corticosteroid-responsive dermatoses.

  • Azone® enhances clinical effectiveness of an optimized formulation of triamcinolone acetonide in atopic dermatitis
    International journal of dermatology, 2001
    Co-Authors: Allen Cato, Lynda Sutton, James M. Swinehart, Edmond I. Griffin, Allan S. Kaplan
    Abstract:

    Background  Atopic dermatitis is a chronic, relapsing condition affecting up to 14% of the population in Western countries. Topical corticosteroids are the mainstay of treatment. Triamcinolone acetonide, a corticoid of intermediate potency, has proven useful in the treatment of atopic dermatitis. Aim  To evaluate the effectiveness of a triamcinolone acetonide–Laurocapram combination in the treatment of atopic dermatitis. Methods  One hundred and fifty patients were enrolled in a three-arm, parallel group, controlled clinical trial evaluating the effectiveness of a triamcinolone acetonide (0.05%) and Laurocapram combination, applied twice daily for 2 weeks, in the treatment of atopic dermatitis. Fifty patients received triamcinolone acetonide–Laurocapram (TNX), 50 triamcinolone acetonide (TN), and 50 a vehicle control formulation (AN). Response to treatment was evaluated by change in disease severity at 6 h, at 3, 8, and 15 days after the start of treatment, and by the global change in disease status. Results  TNX effected a significantly higher degree of improvement in the signs and symptoms of atopic dermatitis (erythema, induration, and pruritus) and a greater overall improvement in disease status compared with treatment with TN or AN. Treatment-associated side-effects were local reactions, occurring in three, two, and six patients in the TNX, TN, and AN groups, respectively. Conclusions  The results suggest that the incorporation of Laurocapram in the formulation enhances the effectiveness of triamcinolone acetonide, without compromising its safety profile.

  • Activity of a triamcinolone acetonide/Laurocapram formulation: double-blind comparisons with triamcinolone acetonide, placebo vehicle, and mid-strength (Class IV) to potent (Class II) corticosteroids
    Current Therapeutic Research, 2001
    Co-Authors: Allen Cato, Lynda Sutton, Allan S. Kaplan, George N. Manning
    Abstract:

    Background: The activity of corticosteroids is dependent on their ability to penetrate the skin. Laurocapram is a skin penetration enhancer that facilitates absorption of cutaneously applied substances. Objective: The purpose of these studies was to determine whether the addition of Laurocapram to a topical triamcinolone acetonide (TA) 0.05% cream formulation would improve the rate of percutaneous penetration and hence the activity of the corticosteroid, as measured by increased vasoconstriction (ie, skin blanching). Methods: Thirty healthy subjects participated in each of 2 double-blind, randomized, multiple-point vasoconstriction studies comparing the TA 0.05%/Laurocapram (TNX) formulation with the placebo vehicle (TNX without TA), the TNX formulation without Laurocapram (TN), and 3 mid-strength to potent corticosteroid formulations (fluocinolone acetonide 0.025% ointment, betamethasone dipropionate 0.05% cream, and fluocinonide 0.05% cream). Duplicate sites on subjects' forearms were exposed to ∼10 mg of each formulation for 4 or 6 hours. Sites were washed and evaluated 1 hour later (ie, 5 or 7 hours after application). Skin blanching activity, a surrogate marker of clinical activity and the rate of percutaneous penetration, was assessed 12 times over a 57-hour period using a 4-point scale (0 = none; 1 = mild; 2 = moderate; 3 = marked). Results: In the first study, the vasoconstriction effect of the TNX formulation after 4 hours of exposure to the cream was significantly greater than that of TN (P < 0.01). In the second study, after 6 hours of exposure, the skin blanching activity of TNX was significantly greater (P = 0.05) than that of fluocinolone acetonide 0.025% ointment, a mid-strength corticosteroid, and betamethasone dipropionate 0.05% cream, a potent corticosteroid, and slightly less than that of fluocinonide 0.05% cream, also classified as a potent corticosteroid. Conclusions: Based on the correlation between the vasoconstrictor activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram enhances the skin penetration of, and hence the activity of, topical corticosteroids and may improve treatments for corticosteroid-responsive dermatoses.

Allan S. Kaplan - One of the best experts on this subject based on the ideXlab platform.

  • activity of a 0 05 triamcinolone acetonide Laurocapram formulation double blind randomized comparison with standard 0 1 triamcinolone acetonide creams and with mild class vi to potent class iii topical corticosteroids
    Current Therapeutic Research-clinical and Experimental, 2001
    Co-Authors: Allen Cato, Lynda Sutton, George N. Manning, Allan S. Kaplan
    Abstract:

    Abstract Background: The addition of Laurocapram, a skin penetration enhancer, to a 0.05% triamcinolone acetonide (TA) cream has been shown to improve the activity of the corticosteroid. Objective: The purpose of these studies was to compare the activity of a 0.05% TA/Laurocapram formulation (TNX) with that of standard 0.1% TA cream formulations and 3 topical corticosteroids classified as mild to potent—fluocinolone acetonide, amcinonide, and mometasone furoate. Methods: Sixty-one healthy adult subjects participated in 2 double-blind, randomized, single-point vasoconstriction studies. In each study, sites on subjects' forearms were exposed to the topical corticosteroid formulation for 6 or 16 hours. The degree of vasoconstriction (ie, skin blanching), a surrogate measure of the activity of the corticosteroid, was assessed 2 hours after the end of the exposure period using a 4-point scale (0 = none, 1=mild, 2=moderate, 3=marked). Results: The vasoconstriction activity of TNX was significantly greater than that of 4 marketed 0.1% TA topical formulations ( P ≤ 0.05), which are classified as mild to mid-strength corticosteroids. The activity of TNX was also greater than that of 0.01% and 0.025% fluocinolone acetonide and 0.1% amcinonide ( P = 0.05), classified as mild, mid-strength, and potent agents, respectively, and similar to that of 0.1% mometasone furoate, a Class IV mid-strength agent. Conclusions: Based on the correlation between the vasoconstriction activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram will enhance the clinical activity of corticosteroids and hence may improve treatments for corticosteroid-responsive dermatoses. Moreover, the TA/Laurocapram formulation can be differentiated therapeutically from conventional TA creams.

  • activity of a triamcinolone acetonide Laurocapram formulation double blind comparisons with triamcinolone acetonide placebo vehicle and mid strength class iv to potent class ii corticosteroids
    Current Therapeutic Research-clinical and Experimental, 2001
    Co-Authors: Allen Cato, Lynda Sutton, Allan S. Kaplan, George N. Manning
    Abstract:

    Background: The activity of corticosteroids is dependent on their ability to penetrate the skin. Laurocapram is a skin penetration enhancer that facilitates absorption of cutaneously applied substances. Objective: The purpose of these studies was to determine whether the addition of Laurocapram to a topical triamcinolone acetonide (TA) 0.05% cream formulation would improve the rate of percutaneous penetration and hence the activity of the corticosteroid, as measured by increased vasoconstriction (ie, skin blanching). Methods: Thirty healthy subjects participated in each of 2 double-blind, randomized, multiple-point vasoconstriction studies comparing the TA 0.05%/Laurocapram (TNX) formulation with the placebo vehicle (TNX without TA), the TNX formulation without Laurocapram (TN), and 3 mid-strength to potent corticosteroid formulations (fluocinolone acetonide 0.025% ointment, betamethasone dipropionate 0.05% cream, and fluocinonide 0.05% cream). Duplicate sites on subjects' forearms were exposed to ∼10 mg of each formulation for 4 or 6 hours. Sites were washed and evaluated 1 hour later (ie, 5 or 7 hours after application). Skin blanching activity, a surrogate marker of clinical activity and the rate of percutaneous penetration, was assessed 12 times over a 57-hour period using a 4-point scale (0 = none; 1 = mild; 2 = moderate; 3 = marked). Results: In the first study, the vasoconstriction effect of the TNX formulation after 4 hours of exposure to the cream was significantly greater than that of TN (P < 0.01). In the second study, after 6 hours of exposure, the skin blanching activity of TNX was significantly greater (P = 0.05) than that of fluocinolone acetonide 0.025% ointment, a mid-strength corticosteroid, and betamethasone dipropionate 0.05% cream, a potent corticosteroid, and slightly less than that of fluocinonide 0.05% cream, also classified as a potent corticosteroid. Conclusions: Based on the correlation between the vasoconstrictor activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram enhances the skin penetration of, and hence the activity of, topical corticosteroids and may improve treatments for corticosteroid-responsive dermatoses.

  • Azone® enhances clinical effectiveness of an optimized formulation of triamcinolone acetonide in atopic dermatitis
    International journal of dermatology, 2001
    Co-Authors: Allen Cato, Lynda Sutton, James M. Swinehart, Edmond I. Griffin, Allan S. Kaplan
    Abstract:

    Background  Atopic dermatitis is a chronic, relapsing condition affecting up to 14% of the population in Western countries. Topical corticosteroids are the mainstay of treatment. Triamcinolone acetonide, a corticoid of intermediate potency, has proven useful in the treatment of atopic dermatitis. Aim  To evaluate the effectiveness of a triamcinolone acetonide–Laurocapram combination in the treatment of atopic dermatitis. Methods  One hundred and fifty patients were enrolled in a three-arm, parallel group, controlled clinical trial evaluating the effectiveness of a triamcinolone acetonide (0.05%) and Laurocapram combination, applied twice daily for 2 weeks, in the treatment of atopic dermatitis. Fifty patients received triamcinolone acetonide–Laurocapram (TNX), 50 triamcinolone acetonide (TN), and 50 a vehicle control formulation (AN). Response to treatment was evaluated by change in disease severity at 6 h, at 3, 8, and 15 days after the start of treatment, and by the global change in disease status. Results  TNX effected a significantly higher degree of improvement in the signs and symptoms of atopic dermatitis (erythema, induration, and pruritus) and a greater overall improvement in disease status compared with treatment with TN or AN. Treatment-associated side-effects were local reactions, occurring in three, two, and six patients in the TNX, TN, and AN groups, respectively. Conclusions  The results suggest that the incorporation of Laurocapram in the formulation enhances the effectiveness of triamcinolone acetonide, without compromising its safety profile.

  • Activity of a triamcinolone acetonide/Laurocapram formulation: double-blind comparisons with triamcinolone acetonide, placebo vehicle, and mid-strength (Class IV) to potent (Class II) corticosteroids
    Current Therapeutic Research, 2001
    Co-Authors: Allen Cato, Lynda Sutton, Allan S. Kaplan, George N. Manning
    Abstract:

    Background: The activity of corticosteroids is dependent on their ability to penetrate the skin. Laurocapram is a skin penetration enhancer that facilitates absorption of cutaneously applied substances. Objective: The purpose of these studies was to determine whether the addition of Laurocapram to a topical triamcinolone acetonide (TA) 0.05% cream formulation would improve the rate of percutaneous penetration and hence the activity of the corticosteroid, as measured by increased vasoconstriction (ie, skin blanching). Methods: Thirty healthy subjects participated in each of 2 double-blind, randomized, multiple-point vasoconstriction studies comparing the TA 0.05%/Laurocapram (TNX) formulation with the placebo vehicle (TNX without TA), the TNX formulation without Laurocapram (TN), and 3 mid-strength to potent corticosteroid formulations (fluocinolone acetonide 0.025% ointment, betamethasone dipropionate 0.05% cream, and fluocinonide 0.05% cream). Duplicate sites on subjects' forearms were exposed to ∼10 mg of each formulation for 4 or 6 hours. Sites were washed and evaluated 1 hour later (ie, 5 or 7 hours after application). Skin blanching activity, a surrogate marker of clinical activity and the rate of percutaneous penetration, was assessed 12 times over a 57-hour period using a 4-point scale (0 = none; 1 = mild; 2 = moderate; 3 = marked). Results: In the first study, the vasoconstriction effect of the TNX formulation after 4 hours of exposure to the cream was significantly greater than that of TN (P < 0.01). In the second study, after 6 hours of exposure, the skin blanching activity of TNX was significantly greater (P = 0.05) than that of fluocinolone acetonide 0.025% ointment, a mid-strength corticosteroid, and betamethasone dipropionate 0.05% cream, a potent corticosteroid, and slightly less than that of fluocinonide 0.05% cream, also classified as a potent corticosteroid. Conclusions: Based on the correlation between the vasoconstrictor activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram enhances the skin penetration of, and hence the activity of, topical corticosteroids and may improve treatments for corticosteroid-responsive dermatoses.

  • Activity of a 0.05% triamcinolone acetonide/Laurocapram formulation: double-blind, randomized comparison with standard 0.1% triamcinolone acetonide creams and with mild (Class VI) to potent (Class III) topical corticosteroids
    Current Therapeutic Research, 2001
    Co-Authors: Allen Cato, Lynda Sutton, George N. Manning, Allan S. Kaplan
    Abstract:

    Abstract Background: The addition of Laurocapram, a skin penetration enhancer, to a 0.05% triamcinolone acetonide (TA) cream has been shown to improve the activity of the corticosteroid. Objective: The purpose of these studies was to compare the activity of a 0.05% TA/Laurocapram formulation (TNX) with that of standard 0.1% TA cream formulations and 3 topical corticosteroids classified as mild to potent—fluocinolone acetonide, amcinonide, and mometasone furoate. Methods: Sixty-one healthy adult subjects participated in 2 double-blind, randomized, single-point vasoconstriction studies. In each study, sites on subjects' forearms were exposed to the topical corticosteroid formulation for 6 or 16 hours. The degree of vasoconstriction (ie, skin blanching), a surrogate measure of the activity of the corticosteroid, was assessed 2 hours after the end of the exposure period using a 4-point scale (0 = none, 1=mild, 2=moderate, 3=marked). Results: The vasoconstriction activity of TNX was significantly greater than that of 4 marketed 0.1% TA topical formulations ( P ≤ 0.05), which are classified as mild to mid-strength corticosteroids. The activity of TNX was also greater than that of 0.01% and 0.025% fluocinolone acetonide and 0.1% amcinonide ( P = 0.05), classified as mild, mid-strength, and potent agents, respectively, and similar to that of 0.1% mometasone furoate, a Class IV mid-strength agent. Conclusions: Based on the correlation between the vasoconstriction activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram will enhance the clinical activity of corticosteroids and hence may improve treatments for corticosteroid-responsive dermatoses. Moreover, the TA/Laurocapram formulation can be differentiated therapeutically from conventional TA creams.

Lynda Sutton - One of the best experts on this subject based on the ideXlab platform.

  • Phase 1/2 Pilot Study of Methotrexate-Laurocapram Topical Gel for the Treatment of Patients With Early-Stage Mycosis Fungoides
    Archives of dermatology, 2003
    Co-Authors: Marie-france Demierre, Luc Vachon, Lynda Sutton, Allen Cato, Brian Leyland-jones
    Abstract:

    Objectives To assess the safety and tolerability of a topical gel formulation combining methotrexate and Laurocapram and to obtain preliminary information on the therapeutic potential of methotrexate-Laurocapram in patients with early-stage mycosis fungoides (stage IA or IB). Design An open-label, phase 1/2 pilot study. Setting Two academic referral centers. Patients Ten patients 18 years or older with histologically confirmed stage IA or IB mycosis fungoides. Intervention The gel formulation of methotrexate-Laurocapram was applied to the total body surface, excluding genital, perianal areas, nipples, face, and skin under the breasts, on an every-other-day basis for 24 consecutive weeks. Main Outcome Measures The safety of methotrexate-Laurocapram was assessed in this study by reviewing adverse events and laboratory data. Efficacy outcomes included changes in lesion condition and severity assessments, reduction in area of sample lesions, and the investigator's global evaluation. Results Adverse events consisted of skin reactions of mild severity. No clinically significant laboratory abnormalities were observed. Based on the investigator's global evaluation at the end of the treatment phase (week 24), 7 (78%) of 9 patients demonstrated a slight-to-moderate response to treatment with methotrexate-Laurocapram. Statistical significance ( P = .049) was reached for induration and pruritus, a trend ( P = .10) was observed for erythema, and no change was found for scaling ( P = .37). Conclusions These findings indicate that the topical administration of methotrexate-Laurocapram is safe and in general well tolerated. This treatment may represent a new therapeutic potential for patients with mycosis fungoides.

  • activity of a 0 05 triamcinolone acetonide Laurocapram formulation double blind randomized comparison with standard 0 1 triamcinolone acetonide creams and with mild class vi to potent class iii topical corticosteroids
    Current Therapeutic Research-clinical and Experimental, 2001
    Co-Authors: Allen Cato, Lynda Sutton, George N. Manning, Allan S. Kaplan
    Abstract:

    Abstract Background: The addition of Laurocapram, a skin penetration enhancer, to a 0.05% triamcinolone acetonide (TA) cream has been shown to improve the activity of the corticosteroid. Objective: The purpose of these studies was to compare the activity of a 0.05% TA/Laurocapram formulation (TNX) with that of standard 0.1% TA cream formulations and 3 topical corticosteroids classified as mild to potent—fluocinolone acetonide, amcinonide, and mometasone furoate. Methods: Sixty-one healthy adult subjects participated in 2 double-blind, randomized, single-point vasoconstriction studies. In each study, sites on subjects' forearms were exposed to the topical corticosteroid formulation for 6 or 16 hours. The degree of vasoconstriction (ie, skin blanching), a surrogate measure of the activity of the corticosteroid, was assessed 2 hours after the end of the exposure period using a 4-point scale (0 = none, 1=mild, 2=moderate, 3=marked). Results: The vasoconstriction activity of TNX was significantly greater than that of 4 marketed 0.1% TA topical formulations ( P ≤ 0.05), which are classified as mild to mid-strength corticosteroids. The activity of TNX was also greater than that of 0.01% and 0.025% fluocinolone acetonide and 0.1% amcinonide ( P = 0.05), classified as mild, mid-strength, and potent agents, respectively, and similar to that of 0.1% mometasone furoate, a Class IV mid-strength agent. Conclusions: Based on the correlation between the vasoconstriction activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram will enhance the clinical activity of corticosteroids and hence may improve treatments for corticosteroid-responsive dermatoses. Moreover, the TA/Laurocapram formulation can be differentiated therapeutically from conventional TA creams.

  • activity of a triamcinolone acetonide Laurocapram formulation double blind comparisons with triamcinolone acetonide placebo vehicle and mid strength class iv to potent class ii corticosteroids
    Current Therapeutic Research-clinical and Experimental, 2001
    Co-Authors: Allen Cato, Lynda Sutton, Allan S. Kaplan, George N. Manning
    Abstract:

    Background: The activity of corticosteroids is dependent on their ability to penetrate the skin. Laurocapram is a skin penetration enhancer that facilitates absorption of cutaneously applied substances. Objective: The purpose of these studies was to determine whether the addition of Laurocapram to a topical triamcinolone acetonide (TA) 0.05% cream formulation would improve the rate of percutaneous penetration and hence the activity of the corticosteroid, as measured by increased vasoconstriction (ie, skin blanching). Methods: Thirty healthy subjects participated in each of 2 double-blind, randomized, multiple-point vasoconstriction studies comparing the TA 0.05%/Laurocapram (TNX) formulation with the placebo vehicle (TNX without TA), the TNX formulation without Laurocapram (TN), and 3 mid-strength to potent corticosteroid formulations (fluocinolone acetonide 0.025% ointment, betamethasone dipropionate 0.05% cream, and fluocinonide 0.05% cream). Duplicate sites on subjects' forearms were exposed to ∼10 mg of each formulation for 4 or 6 hours. Sites were washed and evaluated 1 hour later (ie, 5 or 7 hours after application). Skin blanching activity, a surrogate marker of clinical activity and the rate of percutaneous penetration, was assessed 12 times over a 57-hour period using a 4-point scale (0 = none; 1 = mild; 2 = moderate; 3 = marked). Results: In the first study, the vasoconstriction effect of the TNX formulation after 4 hours of exposure to the cream was significantly greater than that of TN (P < 0.01). In the second study, after 6 hours of exposure, the skin blanching activity of TNX was significantly greater (P = 0.05) than that of fluocinolone acetonide 0.025% ointment, a mid-strength corticosteroid, and betamethasone dipropionate 0.05% cream, a potent corticosteroid, and slightly less than that of fluocinonide 0.05% cream, also classified as a potent corticosteroid. Conclusions: Based on the correlation between the vasoconstrictor activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram enhances the skin penetration of, and hence the activity of, topical corticosteroids and may improve treatments for corticosteroid-responsive dermatoses.

  • Azone® enhances clinical effectiveness of an optimized formulation of triamcinolone acetonide in atopic dermatitis
    International journal of dermatology, 2001
    Co-Authors: Allen Cato, Lynda Sutton, James M. Swinehart, Edmond I. Griffin, Allan S. Kaplan
    Abstract:

    Background  Atopic dermatitis is a chronic, relapsing condition affecting up to 14% of the population in Western countries. Topical corticosteroids are the mainstay of treatment. Triamcinolone acetonide, a corticoid of intermediate potency, has proven useful in the treatment of atopic dermatitis. Aim  To evaluate the effectiveness of a triamcinolone acetonide–Laurocapram combination in the treatment of atopic dermatitis. Methods  One hundred and fifty patients were enrolled in a three-arm, parallel group, controlled clinical trial evaluating the effectiveness of a triamcinolone acetonide (0.05%) and Laurocapram combination, applied twice daily for 2 weeks, in the treatment of atopic dermatitis. Fifty patients received triamcinolone acetonide–Laurocapram (TNX), 50 triamcinolone acetonide (TN), and 50 a vehicle control formulation (AN). Response to treatment was evaluated by change in disease severity at 6 h, at 3, 8, and 15 days after the start of treatment, and by the global change in disease status. Results  TNX effected a significantly higher degree of improvement in the signs and symptoms of atopic dermatitis (erythema, induration, and pruritus) and a greater overall improvement in disease status compared with treatment with TN or AN. Treatment-associated side-effects were local reactions, occurring in three, two, and six patients in the TNX, TN, and AN groups, respectively. Conclusions  The results suggest that the incorporation of Laurocapram in the formulation enhances the effectiveness of triamcinolone acetonide, without compromising its safety profile.

  • Activity of a triamcinolone acetonide/Laurocapram formulation: double-blind comparisons with triamcinolone acetonide, placebo vehicle, and mid-strength (Class IV) to potent (Class II) corticosteroids
    Current Therapeutic Research, 2001
    Co-Authors: Allen Cato, Lynda Sutton, Allan S. Kaplan, George N. Manning
    Abstract:

    Background: The activity of corticosteroids is dependent on their ability to penetrate the skin. Laurocapram is a skin penetration enhancer that facilitates absorption of cutaneously applied substances. Objective: The purpose of these studies was to determine whether the addition of Laurocapram to a topical triamcinolone acetonide (TA) 0.05% cream formulation would improve the rate of percutaneous penetration and hence the activity of the corticosteroid, as measured by increased vasoconstriction (ie, skin blanching). Methods: Thirty healthy subjects participated in each of 2 double-blind, randomized, multiple-point vasoconstriction studies comparing the TA 0.05%/Laurocapram (TNX) formulation with the placebo vehicle (TNX without TA), the TNX formulation without Laurocapram (TN), and 3 mid-strength to potent corticosteroid formulations (fluocinolone acetonide 0.025% ointment, betamethasone dipropionate 0.05% cream, and fluocinonide 0.05% cream). Duplicate sites on subjects' forearms were exposed to ∼10 mg of each formulation for 4 or 6 hours. Sites were washed and evaluated 1 hour later (ie, 5 or 7 hours after application). Skin blanching activity, a surrogate marker of clinical activity and the rate of percutaneous penetration, was assessed 12 times over a 57-hour period using a 4-point scale (0 = none; 1 = mild; 2 = moderate; 3 = marked). Results: In the first study, the vasoconstriction effect of the TNX formulation after 4 hours of exposure to the cream was significantly greater than that of TN (P < 0.01). In the second study, after 6 hours of exposure, the skin blanching activity of TNX was significantly greater (P = 0.05) than that of fluocinolone acetonide 0.025% ointment, a mid-strength corticosteroid, and betamethasone dipropionate 0.05% cream, a potent corticosteroid, and slightly less than that of fluocinonide 0.05% cream, also classified as a potent corticosteroid. Conclusions: Based on the correlation between the vasoconstrictor activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram enhances the skin penetration of, and hence the activity of, topical corticosteroids and may improve treatments for corticosteroid-responsive dermatoses.

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  • activity of a 0 05 triamcinolone acetonide Laurocapram formulation double blind randomized comparison with standard 0 1 triamcinolone acetonide creams and with mild class vi to potent class iii topical corticosteroids
    Current Therapeutic Research-clinical and Experimental, 2001
    Co-Authors: Allen Cato, Lynda Sutton, George N. Manning, Allan S. Kaplan
    Abstract:

    Abstract Background: The addition of Laurocapram, a skin penetration enhancer, to a 0.05% triamcinolone acetonide (TA) cream has been shown to improve the activity of the corticosteroid. Objective: The purpose of these studies was to compare the activity of a 0.05% TA/Laurocapram formulation (TNX) with that of standard 0.1% TA cream formulations and 3 topical corticosteroids classified as mild to potent—fluocinolone acetonide, amcinonide, and mometasone furoate. Methods: Sixty-one healthy adult subjects participated in 2 double-blind, randomized, single-point vasoconstriction studies. In each study, sites on subjects' forearms were exposed to the topical corticosteroid formulation for 6 or 16 hours. The degree of vasoconstriction (ie, skin blanching), a surrogate measure of the activity of the corticosteroid, was assessed 2 hours after the end of the exposure period using a 4-point scale (0 = none, 1=mild, 2=moderate, 3=marked). Results: The vasoconstriction activity of TNX was significantly greater than that of 4 marketed 0.1% TA topical formulations ( P ≤ 0.05), which are classified as mild to mid-strength corticosteroids. The activity of TNX was also greater than that of 0.01% and 0.025% fluocinolone acetonide and 0.1% amcinonide ( P = 0.05), classified as mild, mid-strength, and potent agents, respectively, and similar to that of 0.1% mometasone furoate, a Class IV mid-strength agent. Conclusions: Based on the correlation between the vasoconstriction activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram will enhance the clinical activity of corticosteroids and hence may improve treatments for corticosteroid-responsive dermatoses. Moreover, the TA/Laurocapram formulation can be differentiated therapeutically from conventional TA creams.

  • activity of a triamcinolone acetonide Laurocapram formulation double blind comparisons with triamcinolone acetonide placebo vehicle and mid strength class iv to potent class ii corticosteroids
    Current Therapeutic Research-clinical and Experimental, 2001
    Co-Authors: Allen Cato, Lynda Sutton, Allan S. Kaplan, George N. Manning
    Abstract:

    Background: The activity of corticosteroids is dependent on their ability to penetrate the skin. Laurocapram is a skin penetration enhancer that facilitates absorption of cutaneously applied substances. Objective: The purpose of these studies was to determine whether the addition of Laurocapram to a topical triamcinolone acetonide (TA) 0.05% cream formulation would improve the rate of percutaneous penetration and hence the activity of the corticosteroid, as measured by increased vasoconstriction (ie, skin blanching). Methods: Thirty healthy subjects participated in each of 2 double-blind, randomized, multiple-point vasoconstriction studies comparing the TA 0.05%/Laurocapram (TNX) formulation with the placebo vehicle (TNX without TA), the TNX formulation without Laurocapram (TN), and 3 mid-strength to potent corticosteroid formulations (fluocinolone acetonide 0.025% ointment, betamethasone dipropionate 0.05% cream, and fluocinonide 0.05% cream). Duplicate sites on subjects' forearms were exposed to ∼10 mg of each formulation for 4 or 6 hours. Sites were washed and evaluated 1 hour later (ie, 5 or 7 hours after application). Skin blanching activity, a surrogate marker of clinical activity and the rate of percutaneous penetration, was assessed 12 times over a 57-hour period using a 4-point scale (0 = none; 1 = mild; 2 = moderate; 3 = marked). Results: In the first study, the vasoconstriction effect of the TNX formulation after 4 hours of exposure to the cream was significantly greater than that of TN (P < 0.01). In the second study, after 6 hours of exposure, the skin blanching activity of TNX was significantly greater (P = 0.05) than that of fluocinolone acetonide 0.025% ointment, a mid-strength corticosteroid, and betamethasone dipropionate 0.05% cream, a potent corticosteroid, and slightly less than that of fluocinonide 0.05% cream, also classified as a potent corticosteroid. Conclusions: Based on the correlation between the vasoconstrictor activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram enhances the skin penetration of, and hence the activity of, topical corticosteroids and may improve treatments for corticosteroid-responsive dermatoses.

  • Activity of a triamcinolone acetonide/Laurocapram formulation: double-blind comparisons with triamcinolone acetonide, placebo vehicle, and mid-strength (Class IV) to potent (Class II) corticosteroids
    Current Therapeutic Research, 2001
    Co-Authors: Allen Cato, Lynda Sutton, Allan S. Kaplan, George N. Manning
    Abstract:

    Background: The activity of corticosteroids is dependent on their ability to penetrate the skin. Laurocapram is a skin penetration enhancer that facilitates absorption of cutaneously applied substances. Objective: The purpose of these studies was to determine whether the addition of Laurocapram to a topical triamcinolone acetonide (TA) 0.05% cream formulation would improve the rate of percutaneous penetration and hence the activity of the corticosteroid, as measured by increased vasoconstriction (ie, skin blanching). Methods: Thirty healthy subjects participated in each of 2 double-blind, randomized, multiple-point vasoconstriction studies comparing the TA 0.05%/Laurocapram (TNX) formulation with the placebo vehicle (TNX without TA), the TNX formulation without Laurocapram (TN), and 3 mid-strength to potent corticosteroid formulations (fluocinolone acetonide 0.025% ointment, betamethasone dipropionate 0.05% cream, and fluocinonide 0.05% cream). Duplicate sites on subjects' forearms were exposed to ∼10 mg of each formulation for 4 or 6 hours. Sites were washed and evaluated 1 hour later (ie, 5 or 7 hours after application). Skin blanching activity, a surrogate marker of clinical activity and the rate of percutaneous penetration, was assessed 12 times over a 57-hour period using a 4-point scale (0 = none; 1 = mild; 2 = moderate; 3 = marked). Results: In the first study, the vasoconstriction effect of the TNX formulation after 4 hours of exposure to the cream was significantly greater than that of TN (P < 0.01). In the second study, after 6 hours of exposure, the skin blanching activity of TNX was significantly greater (P = 0.05) than that of fluocinolone acetonide 0.025% ointment, a mid-strength corticosteroid, and betamethasone dipropionate 0.05% cream, a potent corticosteroid, and slightly less than that of fluocinonide 0.05% cream, also classified as a potent corticosteroid. Conclusions: Based on the correlation between the vasoconstrictor activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram enhances the skin penetration of, and hence the activity of, topical corticosteroids and may improve treatments for corticosteroid-responsive dermatoses.

  • Activity of a 0.05% triamcinolone acetonide/Laurocapram formulation: double-blind, randomized comparison with standard 0.1% triamcinolone acetonide creams and with mild (Class VI) to potent (Class III) topical corticosteroids
    Current Therapeutic Research, 2001
    Co-Authors: Allen Cato, Lynda Sutton, George N. Manning, Allan S. Kaplan
    Abstract:

    Abstract Background: The addition of Laurocapram, a skin penetration enhancer, to a 0.05% triamcinolone acetonide (TA) cream has been shown to improve the activity of the corticosteroid. Objective: The purpose of these studies was to compare the activity of a 0.05% TA/Laurocapram formulation (TNX) with that of standard 0.1% TA cream formulations and 3 topical corticosteroids classified as mild to potent—fluocinolone acetonide, amcinonide, and mometasone furoate. Methods: Sixty-one healthy adult subjects participated in 2 double-blind, randomized, single-point vasoconstriction studies. In each study, sites on subjects' forearms were exposed to the topical corticosteroid formulation for 6 or 16 hours. The degree of vasoconstriction (ie, skin blanching), a surrogate measure of the activity of the corticosteroid, was assessed 2 hours after the end of the exposure period using a 4-point scale (0 = none, 1=mild, 2=moderate, 3=marked). Results: The vasoconstriction activity of TNX was significantly greater than that of 4 marketed 0.1% TA topical formulations ( P ≤ 0.05), which are classified as mild to mid-strength corticosteroids. The activity of TNX was also greater than that of 0.01% and 0.025% fluocinolone acetonide and 0.1% amcinonide ( P = 0.05), classified as mild, mid-strength, and potent agents, respectively, and similar to that of 0.1% mometasone furoate, a Class IV mid-strength agent. Conclusions: Based on the correlation between the vasoconstriction activity of corticosteroids and their clinical activity, the results suggest that the addition of Laurocapram will enhance the clinical activity of corticosteroids and hence may improve treatments for corticosteroid-responsive dermatoses. Moreover, the TA/Laurocapram formulation can be differentiated therapeutically from conventional TA creams.