The aim of the present investigation is to encapsulate rofecoxib in niosomes and incorporate the prepared niosomes into dermal gel base for sustained therapeutic action. Niosomes were prepared by lipid film hydration technique and were analyzed for size, entrapment efficiency and drug retention capacity. Niosomal vesicles were then incorporated into blank carbopol gel to form niosomal gel. The in vitro permeation study across pig skin was performed using Keshary-Chien glass diffusion cell. The size and entrapment efficiency of the niosomal vesicles increased with gradual increase in HLB value of nonionic surfactants used. Maximum drug entrapment was observed with Span 20 with HLB value of 8.6 and drug leakage from vesicles was less at refrigerated condition than at the room temperature. Higher proportion of cholesterol made the niosomal formulation more stable with high drug retention properties. The niosomal gel showed a prolong drug release behavior compared to plain drug gel. Differential scanning calorimetric study of drug loaded gel and pig skin after permeation study confirmed inertness of carbopol gel base toward rofecoxib and absence of drug metabolism in the skin during permeation study, respectively. The niosomal formulations were successfully prepared by lipid film hydration technique using cholesterol and Span as nonionic surfactant. Presence of cholesterol made niosomes more stable with high drug entrapment efficiency and retention properties. The lower flux value of niosomal gel as compared to plain drug gel across pig skin assured the prolong drug release behavior with sustained action.
机构:
Univ Calif San Francisco, Sch Med, Dept Dermatol, San Francisco, CA 94143 USAUniv Calif San Francisco, Sch Med, Dept Dermatol, San Francisco, CA 94143 USA
Choi, MJ
Maibach, HI
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Univ Calif San Francisco, Sch Med, Dept Dermatol, San Francisco, CA 94143 USAUniv Calif San Francisco, Sch Med, Dept Dermatol, San Francisco, CA 94143 USA
机构:
Tabriz Univ Med Sci, Drug Appl Res Ctr, Pharmaceut Technol Lab, Tabriz, IranTabriz Univ Med Sci, Drug Appl Res Ctr, Pharmaceut Technol Lab, Tabriz, Iran
Hamishehkar, Hamed
Rahimpour, Yahya
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Tabriz Univ Med Sci, Biotechnol Res Ctr, Tabriz, Iran
Tabriz Univ Med Sci, Student Res Comm, Tabriz, IranTabriz Univ Med Sci, Drug Appl Res Ctr, Pharmaceut Technol Lab, Tabriz, Iran
Rahimpour, Yahya
Kouhsoltani, Maryam
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Tabriz Univ Med Sci, Drug Appl Res Ctr, Pharmaceut Technol Lab, Tabriz, IranTabriz Univ Med Sci, Drug Appl Res Ctr, Pharmaceut Technol Lab, Tabriz, Iran
机构:
Univ Santiago de Compostela, RIADT, Nucl Magnet Resonance Unit, Campus Vida, Santiago De Compostela 15706, SpainUniv Valladolid, Inst Appl Ophthalmobiol IOBA, E-47011 Valladolid, Spain