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通过负载帕利哌酮棕榈酸酯的纳米结构脂质载体经皮给药提高生物利用度。

Enhancement of bioavailability through transdermal drug delivery of paliperidone palmitate-loaded nanostructured lipid carriers.

机构信息

Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat, 390001, India.

出版信息

Ther Deliv. 2021 Aug;12(8):583-596. doi: 10.4155/tde-2021-0036. Epub 2021 Jul 21.

Abstract

The work describes enhanced bioavailability of paliperidone palmitate through transdermal delivery using nanostructured lipid carriers (NLC). NLCs were formulated by nanoprecipitation method followed by incorporation in transdermal patch and physicochemical characterization. NLCs showed high percentage entrapment efficiency of 83.44 ± 0.8%, drug loading of 24.75 ± 1.10% (w/w), particle size of 173.8 ± 3.25 nm, polydispersity index of 0.143 ± 0.05 and zeta potential of -15.9 ± 0.75 mV. and studies indicated zero-order controlled drug release from NLCs and transdermal patch up to 48 h. Pharmacokinetic studies indicated 1.76-fold enhanced bioavailability by transdermal route as compared with oral drug delivery. From the results, it was concluded that drug-loaded NLCs-transdermal patch is promising drug delivery system for poorly bioavailable drugs.

摘要

该工作描述了通过使用纳米结构脂质载体(NLC)经皮递送来提高棕榈酸帕利哌酮的生物利用度。NLC 通过纳米沉淀法制备,然后掺入透皮贴剂中,并进行理化特性表征。NLC 表现出 83.44±0.8%的高包封效率、24.75±1.10%(w/w)的载药量、173.8±3.25nm 的粒径、0.143±0.05 的多分散指数和-15.9±0.75mV 的zeta 电位。研究表明,NLC 和透皮贴剂中的药物呈零级控制释放,达 48 小时。药代动力学研究表明,与口服给药相比,经皮给药可使生物利用度提高 1.76 倍。结果表明,载药 NLC 透皮贴剂是一种有前途的生物利用度差的药物的药物传递系统。

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