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Formulation, characterization and ex-vivo permeation studies on gentamicin-loaded transdermal patches based on PURASORB polymers

机译:基于PURASORB聚合物的庆大霉素负载透皮贴剂的配制,表征和离体渗透研究

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Topical administration of gentamicin, an aminoglycoside antibiotic commonly used for treatment of bacterial infections, is limited by toxicity and membrane impermeability. The purpose of this study was to develop an alternative non-invasive, convenient and cost-effective drug delivery system for enhanced skin delivery of gentamicin. Thepatcheswereformulated by solvent evaporation technique using PURASORB®polymersand evaluated for drug content, thermal properties, physicochemical performance, stability, skin irritability andex-vivodrug permeation through rat skin using a modified Franz diffusion cell. The DSC results indicate absence of strong interaction between gentamicin and the polymers. Theformulationsshowedgooddrug encapsulation,stability, physicochemical properties, tolerability on rat skin andex-vivodrug permeation through rat skin.Compared with a commercially available gentamicin sulphate cream the transdermal patches gave higherex-vivoskin permeation through rat skinwith patches of PURASORB®PL 32 showinghighestpermeationflux(5.161 µg/cm2.h) and permeation coefficient (1.032× 10-6cm/h). The results of this study indicates that patches of PURASORB®PL 32 represent a new delivery system for enhnaced skin delivery of gentamicin.
机译:庆大霉素(一种通常用于治疗细菌感染的氨基糖苷类抗生素)的局部给药受到毒性和膜不透性的限制。这项研究的目的是开发一种替代的非侵入性,方便且具有成本效益的药物递送系统,以增强庆大霉素的皮肤递送。使用PURASORB®聚合物通过溶剂蒸发技术对贴剂进行重新配制,并使用改良的Franz扩散池评估药物含量,热性能,理化性能,稳定性,皮肤过敏性和离体药物透过大鼠皮肤的渗透性。 DSC结果表明庆大霉素与聚合物之间不存在强相互作用。制剂显示出良好的药物包封性,稳定性,理化性质,在大鼠皮肤上的耐受性以及通过大鼠皮肤的体外释药的渗透性。与市售硫酸庆大霉素乳膏相比,透皮贴剂通过PURASORB® PL 32表现出最高的通量(x = 5.161)的贴剂在大鼠皮肤中的离体渗透率更高。 g / cm2.h)和渗透系数(1.032×10-6cm / h)。这项研究的结果表明,PURASORB® PL 32的贴剂代表了一种增强的庆大霉素皮肤递送的新递送系统。

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