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基于纳米结构脂质载体的壳聚糖热敏水凝胶用于地塞米松递送的研发与表征

Development and characterization of nanostructured lipid carriers based chitosan thermosensitive hydrogel for delivery of dexamethasone.

作者信息

Tan Guoxin, Yu Shihui, Li Jinyu, Pan Weisan

机构信息

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.

出版信息

Int J Biol Macromol. 2017 Oct;103:941-947. doi: 10.1016/j.ijbiomac.2017.05.132. Epub 2017 May 22.

Abstract

This study aims to explore a novel composite thermosensitive in situ gelling formulation which the nanostructured lipid carriers (NLC) was incorporated into hydroxypropyltrimethyl ammonium chloride chitosan (HACC)-based hydrogels, and the resulting formulation investigated for its potential to act as a potential sustained ocular delivery system. NLC formulation loaded with dexamethasone (DXM) were prepared using the melt-emulsification method. The particle size, zeta potential, encapsulation efficiency, and morphological properties of the NLC were characterized. The HACC was synthesized and structure was analyzed by FT-IR and H NMR. A thermosensitive hydrogel was designed and prepared by simply mixing HACC and β-glycerophosphate (β-GP). The obtained formulation showed a rapid solution-to-gel transition at 35°C. The NLC were then incorporated in HACC/β-GP hydrogel to form a NLC-loaded hydrogel carrier. In vitro release studies, 88.65% of total DXM was released from the NLC-HACC/GP gel within 3days, indicating DXM-based NLC-gel could release drug sustainably. Taken together, DXM-based NLC-HACC/GP gel is a promising drug delivery system.

摘要

本研究旨在探索一种新型的复合热敏原位凝胶制剂,即将纳米结构脂质载体(NLC)掺入基于羟丙基三甲基氯化铵壳聚糖(HACC)的水凝胶中,并对所得制剂作为潜在的持续眼部给药系统的潜力进行研究。采用熔融乳化法制备了载有地塞米松(DXM)的NLC制剂。对NLC的粒径、zeta电位、包封率和形态学性质进行了表征。合成了HACC,并通过傅里叶变换红外光谱(FT-IR)和氢核磁共振(H NMR)对其结构进行了分析。通过简单混合HACC和β-甘油磷酸酯(β-GP)设计并制备了一种热敏水凝胶。所得制剂在35℃时显示出快速的溶液-凝胶转变。然后将NLC掺入HACC/β-GP水凝胶中,形成载有NLC的水凝胶载体。体外释放研究表明,3天内88.65%的总DXM从NLC-HACC/GP凝胶中释放出来,表明基于DXM的NLC-凝胶能够持续释放药物。综上所述,基于DXM的NLC-HACC/GP凝胶是一种很有前景的药物递送系统。

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