The Experts below are selected from a list of 132 Experts worldwide ranked by ideXlab platform
Fotios M. Plakogiannis - One of the best experts on this subject based on the ideXlab platform.
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Ketoprofen Suppository Dosage Forms: In Vitro Release and in Vivo Absorption Studies in Rabbits
Drug Development and Industrial Pharmacy, 1999Co-Authors: Ali Babar, T. Bellete, Fotios M. PlakogiannisAbstract:In vitro release of ketoprofen from suppository bases and in vivo absorption in rabbits were studied. Suppositories containing 50 mg of ketoprofen were prepared using Theobroma Oil, esterified (c10–c18) fatty acids, and polyethylene glycol 1000 bases. The displacement values of the drug were determined and found to be of the order of Theobroma Oil > esterified (c10–c18) fatty acids and polyethylene glycol 1000 bases. The suppository hardness data revealed that the Theobroma Oil base produced relatively brittle suppositories. Using the USP dissolution method, the release of ketoprofen was observed to be greatest from polyethylene glycol 1000 suppositories. With the dialysis technique, the maximum release of drug was obtained from Theobroma Oil suppository containing polysorbate 40 at a 6% level. Selected suppository formulations were evaluated for rectal absorption studies in rabbits. The in vivo data showed that the optimum drug absorption took place from the polyethylene glycol 1000 base and Theobroma oi...
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In Vitro Release of Testosterone from Suppository Bases and In Vivo Absorption Studies in Human Males
Journal of pharmaceutical sciences, 1993Co-Authors: Ali Babar, Hani M. Fares, Fotios M. PlakogiannisAbstract:Diffusion rates of testosterone from various suppository bases with and without surfactants were determined. In a limited study, selected suppository formulations were evaluated for efficiency of rectal absorption of testosterone in three male volunteers ranging in age from 25 to 30 years. Significant reductions in the ratios of urinary metabolites to free testosterone were observed with polyethylene glycol 1000, esterified (C10-C18) fatty acids, and Theobroma Oil-based samples.
Lip Yong Chung - One of the best experts on this subject based on the ideXlab platform.
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thermostability and polymorphism of Theobroma Oil and palm kernel Oil as suppository bases
Journal of Thermal Analysis and Calorimetry, 2009Co-Authors: Mohamed Ibrahim Noordin, Lip Yong ChungAbstract:Thermal stability of pharmaceutical ingredients is an important aspect. In this study, we adopted differential scanning calorimetry (DSC) to investigate thermal stability of suppository bases, Theobroma Oil (cocoa butter) and a palm kernel Oil (PKO) blend. The study shows Theobroma Oil possesses six polymorphic forms whilst the palm kernel Oil blend has three. Upon rescanning, the PKO blend does not show changes in the enthalpy of fusion and the melting point with time, whilst the Theobroma Oil shows significant reduction, and only regained its thermal stable state after 10 days. This indicates that PKO blend possesses better thermal stability.
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Robustness of Palm Kernel Oil Blend in Suppository Preparation Using Acetaminophen as a Model Drug
Journal of Pharmacy Technology, 2007Co-Authors: Mohamed Ibrahim Noordin, Lip Yong ChungAbstract:Background: Theobroma Oil suppository base has good characteristics for the delivery of most drugs, but its polymorphism renders it a difficult medium with which to work. Preparation of suppositories using Theobroma Oil must be carried out at a temperature below 36 °C to avoid formation of metastable polymorphs. Substitutes for Theobroma Oil are therefore desirable. Objective: To compare the characteristics of Theobroma Oil- and palm kernel Oil blend (PKOB)-based suppositories, each produced by 2 different techniques of preparation. Methods: Theobroma Oil and PKOB (consisting of hydrogenated palm kernel Oil and hydrogenated palm kernel stearin in an 8:2 ratio, with 5 stearic acid and 5 glyceryl monostearate) were used as a base. Suppositories were prepared by 2 different techniques, with acetaminophen used as the model drug. The standard technique used a water bath to melt the base preparation at 36 °C before incorporation of acetaminophen, while the second technique involved melting the base in an oven at 60 °C. The 2 types of suppositories produced by these techniques were then tested physically for appearance, hardness, liquefaction time, and melting characteristics using differential scanning calorimetry. Results: Satisfactory Theobroma Oil-based suppositories were produced by the water bath technique at 36 °C, but the oven technique at 60 °C failed to produce a good product. On the other hand, both techniques produced satisfactory PKOB-based suppositories that were similar in both physical and thermal characteristics. Conclusions: PKOB constituted with the above-mentioned ingredients can be exposed to a wider range of temperatures without risk of polymorphism.
Nashiru Billa - One of the best experts on this subject based on the ideXlab platform.
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Lyophilized Drug-Loaded Solid Lipid Nanoparticles Formulated with Beeswax and Theobroma Oil.
Molecules (Basel Switzerland), 2021Co-Authors: Hilda Amekyeh, Nashiru BillaAbstract:Solid lipid nanoparticles (SLNs) have the potential to enhance the systemic availability of an active pharmaceutical ingredient (API) or reduce its toxicity through uptake of the SLNs from the gastrointestinal tract or controlled release of the API, respectively. In both aspects, the responses of the lipid matrix to external challenges is crucial. Here, we evaluate the effects of lyophilization on key responses of 1:1 beeswax-Theobroma Oil matrix SLNs using three model drugs: amphotericin B (AMB), paracetamol (PAR), and sulfasalazine (SSZ). Fresh SLNs were stable with sizes ranging between 206.5-236.9 nm. Lyophilization and storage for 24 months (4-8 °C) caused a 1.6- and 1.5-fold increase in size, respectively, in all three SLNs. Zeta potential was >60 mV in fresh, stored, and lyophilized SLNs, indicating good colloidal stability. Drug release was not significantly affected by lyophilization up to 8 h. Drug release percentages at end time were 11.8 ± 0.4, 65.9 ± 0.04, and 31.4 ± 1.95% from fresh AMB-SLNs, PAR-SLNs, and SSZ-SLNs, respectively, and 11.4 ± 0.4, 76.04 ± 0.21, and 31.6 ± 0.33% from lyophilized SLNs, respectively. Thus, rate of release is dependent on API solubility (AMB < SSZ < PAR). Drug release from each matrix followed the Higuchi model and was not affected by lyophilization. The above SLNs show potential for use in delivering hydrophilic and lipophilic drugs.
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A Gastrointestinal Transit Study on Amphotericin B-Loaded Solid Lipid Nanoparticles in Rats
AAPS PharmSciTech, 2015Co-Authors: Hilda Amekyeh, Nashiru Billa, Kah-hay Yuen, Sherlyn Lim Sheau ChinAbstract:The gastrointestinal (GI) transit behavior of and absorption from an amphotericin B (AmB) solid lipid nanoformulation (SLN) in rats was investigated. We aimed to estimate the gastric emptying time (GET) and cecal arrival time (CAT) of AmB SLN in rats as animal models. From these two parameters, an insight on the absorption window of AmB was ascertained. Three types of SLNs, AmB, paracetamol (PAR), and sulfasalazine (SSZ), were similarly formulated using beeswax/Theobroma Oil composite as the lipid matrix and characterized with regard to size, viscosity, density, migration propensity within agarose gel, in vitro drug release, morphology, gastrointestinal transit, and in vivo absorption. The GET and CAT were estimated indirectly using marker drugs: PAR and sulfapyridine (SP). All three types of SLNs exhibited identical properties with regard to z-average, viscosity, relative density, and propensity to migrate. PAR was absorbed rapidly from the small intestine following emptying of the SLNs giving the T_50E (time for 50% absorption of PAR) to be 1.6 h. SP was absorbed after release and microbial degradation of SSZ from SLN in the colon with a lag time of 2 h post-administration, serving as the estimated cecal arrival time of the SLNs. AmB within SLN was favorably absorbed from the small intestine, albeit slowly.
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Properties of An Oral Nanoformulation of A Molecularly Dispersed Amphotericin B Comprising A Composite Matrix of Theobroma Oil and Bee’S Wax
Nanomaterials (Basel Switzerland), 2014Co-Authors: Chloe See Wei Tan, Nashiru Billa, Clive J. Roberts, David J. ScurrAbstract:An amphotericin B-containing (AmB) solid lipid nanoparticulate drug delivery system intended for oral administration, comprised of bee's wax and Theobroma Oil as lipid components was formulated with the aim to ascertain the location of AmB within the lipid matrix: (a) a homogenous matrix; (b) a drug-enriched shell; or (c) a drug enriched core. Both the drug-loaded and drug-free nanoparticles were spherical with AmB contributing to an increase in both the z-average diameter (169 ± 1 to 222 ± 2 nm) and zeta potential (40.8 ± 0.9 to 50.3 ± 1.0 mV) of the nanoparticles. A maximum encapsulation efficiency of 21.4% ± 3.0%, corresponding to 10.7 ± 0.4 mg encapsulated AmB within the lipid matrix was observed. Surface analysis and electron microscopic imaging indicated that AmB was dispersed uniformly within the lipid matrix (option (a) above) and, therefore, this is the most suitable of the three models with regard to modeling the propensity for uptake by epithelia and release of AmB in lymph.
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properties of an oral nanoformulation of a molecularly dispersed amphotericin b comprising a composite matrix of Theobroma Oil and bee s wax
Nanomaterials, 2014Co-Authors: Chloe See Wei Tan, Nashiru Billa, Clive J. Roberts, David J. ScurrAbstract:An amphotericin B-containing (AmB) solid lipid nanoparticulate drug delivery system intended for oral administration, comprised of bee's wax and Theobroma Oil as lipid components was formulated with the aim to ascertain the location of AmB within the lipid matrix: (a) a homogenous matrix; (b) a drug-enriched shell; or (c) a drug enriched core. Both the drug-loaded and drug-free nanoparticles were spherical with AmB contributing to an increase in both the z-average diameter (169 ± 1 to 222 ± 2 nm) and zeta potential (40.8 ± 0.9 to 50.3 ± 1.0 mV) of the nanoparticles. A maximum encapsulation efficiency of 21.4% ± 3.0%, corresponding to 10.7 ± 0.4 mg encapsulated AmB within the lipid matrix was observed. Surface analysis and electron microscopic imaging indicated that AmB was dispersed uniformly within the lipid matrix (option (a) above) and, therefore, this is the most suitable of the three models with regard to modeling the propensity for uptake by epithelia and release of AmB in lymph.
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Lipid Effects on Expulsion Rate of Amphotericin B from Solid Lipid Nanoparticles
AAPS PharmSciTech, 2014Co-Authors: See Wei Tan, Nashiru BillaAbstract:We aimed to investigate the effects that natural lipids, Theobroma Oil (TO) and beeswax (BW), might have on the physical properties of formulated nanoparticles and also the degree of expulsion of encapsulated amphotericin B (AmB) from the nanoparticles during storage. Lecithin and sodium cholate were used as emulsifiers whilst oleic acid (OA) was used to study the influence of the state of orderliness/disorderliness within the matrices of the nanoparticles on the degree of AmB expulsion during storage. BW was found to effect larger z-average diameter compared with TO. Lecithin was found to augment the stability of the nanoparticles imparted by BW and TO during storage. An encapsulation efficiency (%EE) of 59% was recorded when TO was the sole lipid as against 42% from BW. In combination however, the %EE dropped to 39%. When used as sole lipid, TO or BW formed nanoparticles with comparatively higher enthalpies, 21.1 and 23.3 J/g respectively, which subsequently caused significantly higher degree of AmB expulsion, 81 and 83% respectively, whilst only 11.8% was expelled from a binary TO/BW mixture. A tertiary TO/BW/OA mixture registered the lowest enthalpy at 8.07 J/g and expelled 12.6% of AmB but encapsulated only 22% of AmB. In conclusion, nanoparticles made from equal concentrations of TO and BW produced the most desirable properties and worthy of further investigations.
Ali Babar - One of the best experts on this subject based on the ideXlab platform.
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Ketoprofen Suppository Dosage Forms: In Vitro Release and in Vivo Absorption Studies in Rabbits
Drug Development and Industrial Pharmacy, 1999Co-Authors: Ali Babar, T. Bellete, Fotios M. PlakogiannisAbstract:In vitro release of ketoprofen from suppository bases and in vivo absorption in rabbits were studied. Suppositories containing 50 mg of ketoprofen were prepared using Theobroma Oil, esterified (c10–c18) fatty acids, and polyethylene glycol 1000 bases. The displacement values of the drug were determined and found to be of the order of Theobroma Oil > esterified (c10–c18) fatty acids and polyethylene glycol 1000 bases. The suppository hardness data revealed that the Theobroma Oil base produced relatively brittle suppositories. Using the USP dissolution method, the release of ketoprofen was observed to be greatest from polyethylene glycol 1000 suppositories. With the dialysis technique, the maximum release of drug was obtained from Theobroma Oil suppository containing polysorbate 40 at a 6% level. Selected suppository formulations were evaluated for rectal absorption studies in rabbits. The in vivo data showed that the optimum drug absorption took place from the polyethylene glycol 1000 base and Theobroma oi...
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In Vitro Release of Testosterone from Suppository Bases and In Vivo Absorption Studies in Human Males
Journal of pharmaceutical sciences, 1993Co-Authors: Ali Babar, Hani M. Fares, Fotios M. PlakogiannisAbstract:Diffusion rates of testosterone from various suppository bases with and without surfactants were determined. In a limited study, selected suppository formulations were evaluated for efficiency of rectal absorption of testosterone in three male volunteers ranging in age from 25 to 30 years. Significant reductions in the ratios of urinary metabolites to free testosterone were observed with polyethylene glycol 1000, esterified (C10-C18) fatty acids, and Theobroma Oil-based samples.
Mohamed Ibrahim Noordin - One of the best experts on this subject based on the ideXlab platform.
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thermostability and polymorphism of Theobroma Oil and palm kernel Oil as suppository bases
Journal of Thermal Analysis and Calorimetry, 2009Co-Authors: Mohamed Ibrahim Noordin, Lip Yong ChungAbstract:Thermal stability of pharmaceutical ingredients is an important aspect. In this study, we adopted differential scanning calorimetry (DSC) to investigate thermal stability of suppository bases, Theobroma Oil (cocoa butter) and a palm kernel Oil (PKO) blend. The study shows Theobroma Oil possesses six polymorphic forms whilst the palm kernel Oil blend has three. Upon rescanning, the PKO blend does not show changes in the enthalpy of fusion and the melting point with time, whilst the Theobroma Oil shows significant reduction, and only regained its thermal stable state after 10 days. This indicates that PKO blend possesses better thermal stability.
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Robustness of Palm Kernel Oil Blend in Suppository Preparation Using Acetaminophen as a Model Drug
Journal of Pharmacy Technology, 2007Co-Authors: Mohamed Ibrahim Noordin, Lip Yong ChungAbstract:Background: Theobroma Oil suppository base has good characteristics for the delivery of most drugs, but its polymorphism renders it a difficult medium with which to work. Preparation of suppositories using Theobroma Oil must be carried out at a temperature below 36 °C to avoid formation of metastable polymorphs. Substitutes for Theobroma Oil are therefore desirable. Objective: To compare the characteristics of Theobroma Oil- and palm kernel Oil blend (PKOB)-based suppositories, each produced by 2 different techniques of preparation. Methods: Theobroma Oil and PKOB (consisting of hydrogenated palm kernel Oil and hydrogenated palm kernel stearin in an 8:2 ratio, with 5 stearic acid and 5 glyceryl monostearate) were used as a base. Suppositories were prepared by 2 different techniques, with acetaminophen used as the model drug. The standard technique used a water bath to melt the base preparation at 36 °C before incorporation of acetaminophen, while the second technique involved melting the base in an oven at 60 °C. The 2 types of suppositories produced by these techniques were then tested physically for appearance, hardness, liquefaction time, and melting characteristics using differential scanning calorimetry. Results: Satisfactory Theobroma Oil-based suppositories were produced by the water bath technique at 36 °C, but the oven technique at 60 °C failed to produce a good product. On the other hand, both techniques produced satisfactory PKOB-based suppositories that were similar in both physical and thermal characteristics. Conclusions: PKOB constituted with the above-mentioned ingredients can be exposed to a wider range of temperatures without risk of polymorphism.