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Thawatchai Phaechamud - One of the best experts on this subject based on the ideXlab platform.

  • Doxycycline Hyclate loaded in situ forming gels composed from bleached shellac ethocel and eudragit rs for periodontal pocket delivery
    Journal of The Saudi Pharmaceutical Society, 2021
    Co-Authors: Setthapong Senarat, Wai Wai Lwin, Jongjan Mahadlek, Thawatchai Phaechamud
    Abstract:

    Abstract Polymeric material plays an important role as a matrix former in the modulation of drug release of antimicrobial-loaded in situ forming gel (ISG) for efficient periodontitis treatment. This study was conducted to compare three polymers, namely bleached shellac (BS), Ethocel (EC) and Eudragit RS (ERS), as matrix formers of Doxycycline Hyclate (DH)-loaded solvent exchange-induced ISG. All prepared ISGs, except 25% EC ISG, exhibited the Newtonian flow behaviour. Transformation from solution into matrix-like was achieved rapidly within 5 min. Increasing the amount of these polymers extended the release of DH. DH-loaded EC and ERS ISG systems exhibited high antimicrobial activity, and all ISGs were effective in inhibiting the growth of Staphylococcus aureus, Escherichia coli, Streptococcus mutans, Porphyromonas gingivalis and Candida albicans. By comparison, the DH-loaded ERS ISG, through the solvent exchange mechanism, was found to be ease in injection with low viscosity and sustained the release with higher concentration, meanwhile, it also exhibited interesting in vitro degradability and antimicrobial activities. Therefore, the DH-loaded ERS ISG exhibited a potential use for localized periodontal drug delivery system for the treatment periodontitis.

  • emerging role of polyethylene glycol on Doxycycline Hyclate incorporated eudragit rs in situ forming gel for periodontitis treatment
    Journal of Pharmaceutical Investigation, 2020
    Co-Authors: Wai Wai Lwin, Jongjan Mahadlek, Napaphol Puyathorn, Setthapong Senarat, Thawatchai Phaechamud
    Abstract:

    Phase separation with solvent exchange induced-in situ forming gel (ISG) is an attractive delivery system for periodontitis treatment. Eudragit® RS-PO (ERS) in N-methyl pyrrolidone (NMP) was used as polymer matrix for Doxycycline Hyclate (DH)-loaded solvent-exchanged ISG; however, a high burst drug release was evident. The present study revealed the role of PEG 1500 on physicochemical properties and modification of a burst release for DH-loaded ISG. DH-loaded ISG system comprising PEG 1500 exhibited the Newtonian flow with acceptable injectability with PEG 1500 concentration dependence and high in vitro degradation owing to NMP and PEG 1500 liberation. Solvent exchange between NMP with PBS pH 6.8 conveyed the rapid phase separation of ERS/PEG 1500 as a matrix which the entrapped DH diffused out gradually. Both dialysis membrane and membrane-less methods proved the slower drug release of DH-loaded ERS ISG comprising PEG than PEG 1500-free ISG. SEM revealed the porous matrix topography from polymeric phase separation especially for higher PEG 1500 loading. PEG 1500 incorporation significantly decreased the inhibition diameter against S. aureus, E. coli and S. mutans (P < 0.05) indicating the retardation of drug release owing to the high viscosity of the PEG 1500. PEG 1500-incorporated DH-loaded ERS ISG exhibited the potential use for periodontitis treatment. PEG loading into solvent induced ERS in situ forming gel for Doxycycline Hyclate periodontal pocket delivery.

  • solvent exchange and drug release characteristics of Doxycycline Hyclate loaded bleached shellac in situ forming gel and microparticle
    International Journal of Biological Macromolecules, 2019
    Co-Authors: Thawatchai Phaechamud, Napaphol Puyathorn, Setthapong Senarat, Pitsiree Praphanwittaya
    Abstract:

    Abstract Doxycycline Hyclate (DX)-loaded bleached shellac (BS) in situ forming gel (isg) and in situ microparticle (ism) were prepared using dimethyl sulfoxide (DMSO), N-methyl pyrrolidone (NMP) and 2-pyrrolidone (PYR) as solvents. Solvent and drug release characteristics of them were investigated. Diffusion rate of solvent applied in formulation was as following: DMSO > NMP > PYR. In situ forming systems comprising PYR had the slowest release rate of solvent and drug while water flowed into system in rank of solvent order as following: DMSO > NMP > PYR. Size and density of pores were increased by time similarly to release rate of solvent and drug. At steady state, total mass loss converted to PYR ≫ NMP > DMSO similarly to water content pattern. The solvent and DX release from ism were apparently slower than those from isg owing to barrier effect from oil component. The isg and ism prepared from DMSO exhibited the highly sponge-like structure than that using PYR which the later matrices eventually dissipated due to hydrolysis of BS which was accelerated by PYR-induced water accumulation. PYR was the most appropriated solvent for BS isg and ism because their formulations demonstrated the proper sustained drug release and preferable self-degradation.

  • peppermint oil Doxycycline Hyclate loaded eudragit rs in situ forming gel for periodontitis treatment
    Journal of Pharmaceutical Investigation, 2018
    Co-Authors: Thawatchai Phaechamud, Jongjan Mahadlek, Sarun Tuntarawongsa
    Abstract:

    Antibiotic-loaded in situ forming gels are particularly attractive for periodontitis treatment. They are in a sol form and gradually alter to a solid-like depot after administration into a periodontal pocket to deliver and maintain the effective high level of drug in the gingival crevicular fluid. Solvent-inducing in situ forming gel mostly exhibits the burst drug release owing to rapid diffusion of solvent. This study incorporated peppermint oil to modulate the drug release and the gel characteristics of Doxycycline Hyclate-loaded Eudragit RS in situ forming gel systems. Peppermint oil increased the viscosity and syringeability of the Eudragit RS solution comprising NMP as solvent and retarded the water penetration. Therefore the diminishment of burst liberation and the prolongation of drug release with an addition of peppermint oil were attained with concentration dependence mainly following Fickian diffusion mechanism. The drug release from the membrane-less diffusion method was apparently slower than that from the dialysis method because the rapid phase separation into solid-like matrix through a direct contact with dissolution medium generated a hard surrounding shell. These solvent exchange-inducing in situ forming gels comprising peppermint oil effectively inhibited Staphylococcus aureus, Escherichia coli, Streptococcus mutans and Porphyrommonas gingivalis; therefore, they exhibited the potential use as localized delivery systems for periodontitis treatment.

  • solvent effect on fluid characteristics of Doxycycline Hyclate loaded bleached shellac in situ forming gel and microparticle formulations
    Journal of Pharmaceutical Investigation, 2018
    Co-Authors: Thawatchai Phaechamud, Pitsiree Praphanwittaya, Kunchalee Laotaweesub
    Abstract:

    This research purposed to better comprehend the behavior of solvent including dimethyl sulfoxide (DMSO), N-methyl-2-pyrrolidone (NMP) and 2-pyrrolidone (PYR) in bleached shellac solution from preparation process of in situ forming gel (isg) and microparticle (ism). Doxycycline Hyclate-loaded bleached shellac isg was used as the internal phase of oil in oil emulsion of ism. Fluid characteristics including pH, density, relative viscosity and surface/interfacial tension, droplet size of emulsion, phase separation rate and apparent viscosity were determined. Bleached shellac dissolved in these solvents via strongly hydrogen bonding and van der Wall forces. In the case of ism systems, the trend of viscosity was similar with isg but their viscosity was lower because of the presence of oil in the external phase. PYR formula were the most viscous whereas those prepared with NMP were contrary therefore PYR could interact with bleached shellac molecule less than NMP. The solubility parameter, interfacial tension, apparent and relative viscosities confirmed that NMP was a good solvent for this resin. However, NMP exhibited a partial miscible with oil; thus, generated a rapid phase separation. Therefore DMSO and PYR could use as the solvents to fabricate into the o/o emulsion of ism with a suitable manner for local injection owing to their newtonian or pseudoplastic flows. These results will be useful for future investigation of physicochemical characteristics of obtained gel or microparticle and also their solvent exchange and drug release behavior.

Lopez E Cabarcos - One of the best experts on this subject based on the ideXlab platform.

  • loading and release of Doxycycline Hyclate from strontium substituted calcium phosphate cement
    Acta Biomaterialia, 2010
    Co-Authors: Hamdan M Alkhraisat, Jatsue Cabrejosazama, Julia Lucasaparicio, Tamimi F Marino, Torres J Garciadenche, Blanco L Jerez, Carmen Rueda, Uwe Gbureck, Lopez E Cabarcos
    Abstract:

    Abstract Novel Sr-substituted calcium phosphate cement (CPC) loaded with Doxycycline Hyclate (DOXY-h) was employed to elucidate the effect of strontium substitution on antibiotic delivery. The cement was prepared using as reactants Sr-substituted β-tricalcium phosphate (Sr-β-TCP) and acidic monocalcium phosphate monohydrate. Two different methods were used to load DOXY-h: (i) the adsorption on CPC by incubating the set cement in drug-containing solutions; and (ii) the use of antibiotic solution as the cement liquid phase. The results revealed that the Sr-substituted cement efficiently adsorbs the antibiotic, which is attributed to an enhanced accessibility to the drug-binding sites within this CPC. DOXY-h desorption is influenced by the initial adsorbed amount and the cement matrix type. Furthermore, the fraction of drug released from CPCs set with DOXY-h solution was higher, and the release rate was faster for the CPC prepared with 26.7% Sr-β-TCP. The analysis of releasing profiles points to Fickian diffusion as the mechanism responsible for antibiotic delivery. We can conclude that Sr substitution in secondary calcium phosphate cements improves their efficiency for DOXY-h adsorption and release. The antibiotic loading method provides a way to switch from rapid and complete to slower and prolonged drug release.

  • loading and release of Doxycycline Hyclate from strontium substituted calcium phosphate cement
    Acta Biomaterialia, 2010
    Co-Authors: Hamdan M Alkhraisat, Jatsue Cabrejosazama, Julia Lucasaparicio, Tamimi F Marino, Torres J Garciadenche, Blanco L Jerez, Carmen Rueda, Uwe Gbureck, Lopez E Cabarcos
    Abstract:

    Novel Sr-substituted calcium phosphate cement (CPC) loaded with Doxycycline Hyclate (DOXY-h) was employed to elucidate the effect of strontium substitution on antibiotic delivery. The cement was prepared using as reactants Sr-substituted beta-tricalcium phosphate (Sr-beta-TCP) and acidic monocalcium phosphate monohydrate. Two different methods were used to load DOXY-h: (i) the adsorption on CPC by incubating the set cement in drug-containing solutions; and (ii) the use of antibiotic solution as the cement liquid phase. The results revealed that the Sr-substituted cement efficiently adsorbs the antibiotic, which is attributed to an enhanced accessibility to the drug-binding sites within this CPC. DOXY-h desorption is influenced by the initial adsorbed amount and the cement matrix type. Furthermore, the fraction of drug released from CPCs set with DOXY-h solution was higher, and the release rate was faster for the CPC prepared with 26.7% Sr-beta-TCP. The analysis of releasing profiles points to Fickian diffusion as the mechanism responsible for antibiotic delivery. We can conclude that Sr substitution in secondary calcium phosphate cements improves their efficiency for DOXY-h adsorption and release. The antibiotic loading method provides a way to switch from rapid and complete to slower and prolonged drug release.

Hamdan M Alkhraisat - One of the best experts on this subject based on the ideXlab platform.

  • loading and release of Doxycycline Hyclate from strontium substituted calcium phosphate cement
    Acta Biomaterialia, 2010
    Co-Authors: Hamdan M Alkhraisat, Jatsue Cabrejosazama, Julia Lucasaparicio, Tamimi F Marino, Torres J Garciadenche, Blanco L Jerez, Carmen Rueda, Uwe Gbureck, Lopez E Cabarcos
    Abstract:

    Abstract Novel Sr-substituted calcium phosphate cement (CPC) loaded with Doxycycline Hyclate (DOXY-h) was employed to elucidate the effect of strontium substitution on antibiotic delivery. The cement was prepared using as reactants Sr-substituted β-tricalcium phosphate (Sr-β-TCP) and acidic monocalcium phosphate monohydrate. Two different methods were used to load DOXY-h: (i) the adsorption on CPC by incubating the set cement in drug-containing solutions; and (ii) the use of antibiotic solution as the cement liquid phase. The results revealed that the Sr-substituted cement efficiently adsorbs the antibiotic, which is attributed to an enhanced accessibility to the drug-binding sites within this CPC. DOXY-h desorption is influenced by the initial adsorbed amount and the cement matrix type. Furthermore, the fraction of drug released from CPCs set with DOXY-h solution was higher, and the release rate was faster for the CPC prepared with 26.7% Sr-β-TCP. The analysis of releasing profiles points to Fickian diffusion as the mechanism responsible for antibiotic delivery. We can conclude that Sr substitution in secondary calcium phosphate cements improves their efficiency for DOXY-h adsorption and release. The antibiotic loading method provides a way to switch from rapid and complete to slower and prolonged drug release.

  • loading and release of Doxycycline Hyclate from strontium substituted calcium phosphate cement
    Acta Biomaterialia, 2010
    Co-Authors: Hamdan M Alkhraisat, Jatsue Cabrejosazama, Julia Lucasaparicio, Tamimi F Marino, Torres J Garciadenche, Blanco L Jerez, Carmen Rueda, Uwe Gbureck, Lopez E Cabarcos
    Abstract:

    Novel Sr-substituted calcium phosphate cement (CPC) loaded with Doxycycline Hyclate (DOXY-h) was employed to elucidate the effect of strontium substitution on antibiotic delivery. The cement was prepared using as reactants Sr-substituted beta-tricalcium phosphate (Sr-beta-TCP) and acidic monocalcium phosphate monohydrate. Two different methods were used to load DOXY-h: (i) the adsorption on CPC by incubating the set cement in drug-containing solutions; and (ii) the use of antibiotic solution as the cement liquid phase. The results revealed that the Sr-substituted cement efficiently adsorbs the antibiotic, which is attributed to an enhanced accessibility to the drug-binding sites within this CPC. DOXY-h desorption is influenced by the initial adsorbed amount and the cement matrix type. Furthermore, the fraction of drug released from CPCs set with DOXY-h solution was higher, and the release rate was faster for the CPC prepared with 26.7% Sr-beta-TCP. The analysis of releasing profiles points to Fickian diffusion as the mechanism responsible for antibiotic delivery. We can conclude that Sr substitution in secondary calcium phosphate cements improves their efficiency for DOXY-h adsorption and release. The antibiotic loading method provides a way to switch from rapid and complete to slower and prolonged drug release.

Hector Sumano - One of the best experts on this subject based on the ideXlab platform.

  • pharmacokinetics of an injectable long acting parenteral formulation of Doxycycline Hyclate in pigs
    Journal of Veterinary Pharmacology and Therapeutics, 2014
    Co-Authors: Lilia Gutierrez, Luis Ocampo, F Espinosa, Hector Sumano
    Abstract:

    Based on its ideal PK/PD ratios, Doxycycline Hyclate (DOX-h), a time-dependant antibacterial, is ideally expected to achieve sustained plasma drug concentrations at or slightly above the MIC level for as long as possible between dosing intervals. Pursuing this end, a poloxamer-based matrix was used to produce a 10% long-acting injectable preparation (DOX-h-LA) and its serum concentrations vs. time profile investigated after its injection to pigs in the pericaudal s.c. by parallel design. Results were compared with the forced oral bolus dose and i.v. pharmacokinetics of DOX-h. For this study, 12 recently weaned pigs per group were included in this trial, and a dose of 20 mg/kg was injected in all cases. DOX-h-LA showed the greatest values for bioavailability (115.38%); maximum serum concentration (Cmax) value was 1.5 ± 0.2 with a time to reach Cmax of 3.41 ± 0.04 h and an elimination rate constant of 70.93 ± 0.87( ) h. Considering minimum effective serum concentration of 0.5 μg/mL, a dose interval of at least 5 days can be achieved for DOX-h-LA, whereas p.o. and i.v. dosing of DOX-h may only last 11 and 15 h, respectively. Pigs were slaughtered on day 30 after this trial, and no visible remnants of the preparation were detected neither fibrosis was observed after a thorough macroscopic and histopathological analysis.

  • Pharmacokinetics of an injectable long-acting formulation of Doxycycline Hyclate in dogs
    Acta Veterinaria Scandinavica, 2012
    Co-Authors: Lilia Gutierrez, Dinorah Vargas, Zazil-ha Velasco, Carlos Vázquez, Hector Sumano
    Abstract:

    Based on its PK/PD ratios, Doxycycline Hyclate (DOX-h), a time-dependant antibacterial, is ideally expected to achieve both sustained plasma drug concentrations at or slightly above the MIC level for as long as possible between dosing intervals. Pursuing this end, a poloxamer-based matrix was used to produce a long-acting injectable preparation (DOX-h-LA) and its serum concentrations vs. time profile investigated after its SC injection to dogs (≤ 0.3 mL per injection site), and results compared with the oral (PO) and IV pharmacokinetics of DOX-h, prepared as tablet or as freshly made solution. A crossover (4 x 4 x 4) study design was employed with 12 Mongrel dogs, with washout periods of 21 days, and at dose of 10 mg/kg in all cases. DOX-h-LA showed the greatest values for bioavailability (199.48%); maximum serum concentration (Cmax) value was 2.8 ± 0.3 with a time to reach Cmax (Tmax) of 2.11 ± 0.12 h and an elimination half-life of 133.61 ± 6.32 h. Considering minimum effective serum concentration of 0.5 μg/mL, a dose-interval of at least 1 week h can be achieved for DOX-h-LA, and only 48 h and 24 h after the IV or PO administration of DOX-h as a solution or as tablets, respectively. A non-painful small bulge, apparently non-inflammatory could be distinguished at injection sites. These lumps dissipated completely in 30 days in all cases.

  • pharmacokinetics after administration of an injectable experimental long acting parenteral formulation of Doxycycline Hyclate in goats
    American Journal of Veterinary Research, 2008
    Co-Authors: Dinorah Vargas, Lilia Gutierrez, Ivan Juarez, Francisco Javier Gonzalez, Hector Sumano
    Abstract:

    Objective—To determine the pharmacokinetics after SC administration of an experimental, long-acting parenteral formulation of Doxycycline Hyclate in a poloxamer-based matrix and after IV and IM administration of an aqueous formulation of Doxycycline Hyclate in goats. Animals—30 clinically normal adult goats. Procedures—Goats were allocated to 3 groups (10 goats/group). One group of goats received Doxycycline Hyclate (10 mg/kg) IM, a second group received the same dosage of Doxycycline Hyclate IV, and the third group received the long-acting parenteral formulation of Doxycycline Hyclate SC. Serum concentrations of Doxycycline were determined before and at various intervals after administration. Results—The long-acting parenteral formulation of Doxycycline Hyclate had the greatest bioavailability (545%); mean ± SD maximum serum concentration was 2.4 ± 0.95 μg/mL, peak time to maximum concentration was 19.23 ± 2.03 hours, and elimination half-life was 40.92 ± 4.25 hours. Conclusions and Clinical Relevance—Re...

  • pharmacokinetic study of an injectable long acting parenteral formulation of Doxycycline Hyclate in calves
    Research in Veterinary Science, 2008
    Co-Authors: D Vargasestrada, Jesus Graciamora, Hector Sumano
    Abstract:

    Abstract Doxycycline Hyclate (DOX-h) can be regarded as a time-dependant antibacterial. Hence, a parenteral long-acting formulation may be regarded as more pharmacologically sound. A poloxamer-based matrix was used to produce a long-acting injectable preparation (DOX-h-LA) and its serum concentrations vs. time profile investigated after its s.c. injection to calves. Serum concentrations profiles for such a prepartion were compared to the corresponding profiles obtained with an aqueous formulation of DOX-h injected either i.m. or i.v. in 10 calves in a crossover study at dose of 10 mg/kg, with washout periods. DOX-h-LA showed the greatest values for bioavailability (602%); maximum serum concentration ( C max ) value was 1.99 μg/mL with a time to reach C max ( T max ) of 25 h and an elimination half-life of 40.81 h. Considering minimum effective serum concentration of 0.5 μg/mL a dose-interval of 80 h can be achieved for DOX-h-LA, and only 9.7 h and 17 h after the i.v. or i.m. administration of DOX-h, respectively.

Orn Setthajindalert - One of the best experts on this subject based on the ideXlab platform.

  • cholesterol in situ forming gel loaded with Doxycycline Hyclate for intra periodontal pocket delivery
    European Journal of Pharmaceutical Sciences, 2017
    Co-Authors: Thawatchai Phaechamud, Orn Setthajindalert
    Abstract:

    Cholesterol has been widely used in drug delivery systems including implant. Doxycycline Hyclate (DH)-loaded cholesterol in situ forming gels using N-methyl pyrrolidone as a solvent were prepared and investigated for their properties including viscosity, rheology, syringeability, gel formation, drug release, degradation and antimicrobial activities. The burst drug release of a DH-loaded in situ forming gel using cholesterol as the gelling agent was minimized when the amount of benzyl benzoate was increased. The viscosity of the system was increased as the amount of benzyl benzoate was increased with Newtonian flow. The systems were easy to inject into the target site because of their minimal force of syringeability. They could transform from solution into matrix-like structures, but formulations with higher concentrations of benzyl benzoate took a longer time. However, the degradability was decreased when the amount of benzyl benzoate was increased. These systems inhibited P. gingivalis, S. mutans and S. aureus effectively. DH-loaded cholesterol in situ forming gel system comprising 10% benzyl benzoate was the most suitable owing to its sustainable release manner for 10days and therefore was the proper formulation for periodontitis treatment.

  • Doxycycline Hyclate loaded bleached shellac in situ forming microparticle for intraperiodontal pocket local delivery
    European Journal of Pharmaceutical Sciences, 2016
    Co-Authors: Thawatchai Phaechamud, Nuttapong Chanyaboonsub, Orn Setthajindalert
    Abstract:

    Bleached shellac (BS) is a water-insoluble polyester resin made up of sesquiterpenoid acids esterified with hydroxy aliphatic acids. In this study, BS dissolved in N-methyl pyrrolidone (NMP), dimethyl sulfoxide (DMSO) and 2-pyrrolidone was used as the internal phase of oil in oil emulsion using olive oil emulsified with glyceryl monostearate (GMS) as the external phase of in situ forming microparticles (ISM). Doxycycline Hyclate (DH)-loaded BS ISMs were tested for emulsion stability, viscosity, rheology, transformation into microparticles, syringeability, drug release, surface topography, in vitro degradation and antimicrobial activities against Staphylococcus aureus, Streptococcus mutans and Porphyromonas gingivalis. All emulsions exhibited pseudoplastic flow and notably low syringeability force. Slower transformation from emulsion into microparticles of ISM prepared with 2-pyrrolidone was owing to slower solvent exchange of this solvent which promoted less porous structure of obtained BS matrix microparticles. The system containing 2-pyrrolidone exhibited a higher degradability than that prepared with DMSO. Developed DH-loaded BS ISMs exhibited a sustainable drug release for 47days with Fickian diffusion and effectively inhibited P. gingivalis, S. mutans and S. aureus. Therefore a DH-loaded BS ISM using olive oil containing GMS as the external phase and 2-pyrrolidone as a solvent was a suitable formulation for periodontitis treatment.