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Modulation of serratiopeptidase transdermal patch by lipid-based transfersomes

机译:脂质基转移体对serratiopeptidease透皮贴剂的调节

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摘要

Serratiopeptidase is a proteolytic enzyme obtained from serratia marcescens strain E-15 and used as anti-inflammatory and analgesic drug. Serratiopeptidase undergoes first pass metabolism, causes the gastrointestinal disturbance and systemic toxicity after oral administration. To overcome the limitations of serratiopeptidase, transdermal drug delivery system is an alternative method. So, the aim of present work was to modulate serratiopeptidase transdermal patch by lipid-based transfersomes. Particle size of drug was the major concern to cross stratum corneum which acts as a barrier. This difficulty was surmounted by modulating the vesicles such as transfersomes which carries the drug into the skin by passing the barrier of stratum corneum. Serratiopeptidase was encapsulated in transfersomes in different ratios of lecithin and cholesterol. Particle size of transfersomes, folding endurance, thickness, tensile strength, adhesion test, encapsulation efficiency, in vitro and in vivo release, Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimeter (DSC) studies of patch were used as characterization parameters. Serratiopeptidase transfersomes size was found to be 50 mu m with smooth surface. The promising entrapment efficiencies of transfersomes and formulation were found to be 96.76 and 98.7%, respectively. In vitro and in vivo release studies showed controlled and steady release of serratiopeptidase for 24h. FTIR and DSC confirmed the encapsulation of drug in patch without interaction. It is concluded that transfersomes are interesting carriers for enzymatic drugs for topical application.
机译:Serratiopeptidase是从粘质沙雷氏菌E-15菌株获得的蛋白水解酶,用作抗炎和止痛药。血清肽酶首先经过代谢,口服后引起胃肠道不适和全身毒性。为了克服serratiopeptidase的局限性,透皮给药系统是一种替代方法。因此,当前工作的目的是通过基于脂质的传递体调节Serratiopeptidase透皮贴剂。药物的粒径是跨角质层的主要考虑因素,而角质层是一种屏障。通过调节诸如传递体之类的囊泡克服了这一困难,该囊泡通过角质层的屏障将药物带入皮肤。 Serratio肽肽酶以不同比例的卵磷脂和胆固醇被包裹在转移体中。传递体的粒径,耐折强度,厚度,抗张强度,附着力测试,包封效率,体内外释放,傅里叶变换红外光谱(FTIR)和差示扫描量热仪(DSC)研究了贴剂。发现SERA比肽酶转移体的大小为50μm,表面光滑。发现转移体和制剂的有前途的包封效率分别为96.76和98.7%。体外和体内释放研究表明,serratiopeptidase的控制和稳定释放24小时。 FTIR和DSC证实药物在贴剂中的包封没有相互作用。结论是,传递体是用于局部应用的酶促药物的有趣载体。

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