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通过引入酰化壳聚糖改善自纳米乳化药物递送系统(SNEDDS)的粘膜粘附性能。

Improved mucoadhesive properties of self-nanoemulsifying drug delivery systems (SNEDDS) by introducing acyl chitosan.

作者信息

Efiana Nuri Ari, Mahmood Arshad, Lam Hung Thanh, Zupančič Ožbej, Leonaviciute Gintare, Bernkop-Schnürch Andreas

机构信息

Department of Pharmaceutical Technology, Institute of Pharmacy, Leopold-Franzens- University of Innsbruck, Innrain 80/82, A-6020 Innsbruck, Austria; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ahmad Dahlan, Jl. Prof. Dr. Soepomo, S.H., Janturan, Warungboto, Umbulharjo, Yogyakarta, Indonesia.

Department of Pharmaceutical Technology, Institute of Pharmacy, Leopold-Franzens- University of Innsbruck, Innrain 80/82, A-6020 Innsbruck, Austria.

出版信息

Int J Pharm. 2017 Mar 15;519(1-2):206-212. doi: 10.1016/j.ijpharm.2017.01.012. Epub 2017 Jan 8.

Abstract

This study was aimed to improve the mucoadhesive properties of SNEDDS by the incorporation of acyl chitosan including octanoyl chitosan (OC), lauroyl chitosan (LC) and palmitoyl chitosan (PC). SNEDDS and acyl chitosan SNEDDS were characterized regarding droplet size and zeta potential. Their mucoadhesivity on porcine intestinal mucosa was evaluated by falling liquid film technique using Sudan Red G as marker. Degree of substitution of chitosan was determined to be 52.8%, 64.8 and 48.5% for OC, LC and PC, respectively. SNEDDS and acyl chitosan SNEDDS displayed a droplet size less than 50nm and 80-300nm as well as a zeta potential of -0.2 to -1.6 and 0.05 to 0.99mV, respectively. Introducing 2% acyl chitosan into SNEDDS increased the residence time of SNEDDS on intestinal mucosa 2-fold. It is concluded that due to the incorporation of acyl chitosan into SNEDDS, their mucoadhesive properties can be increased.

摘要

本研究旨在通过加入酰化壳聚糖(包括辛酰壳聚糖(OC)、月桂酰壳聚糖(LC)和棕榈酰壳聚糖(PC))来改善自乳化药物传递系统(SNEDDS)的粘膜粘附特性。对SNEDDS和酰化壳聚糖SNEDDS的粒径和zeta电位进行了表征。以苏丹红G为标记物,采用落液膜技术评价了它们在猪肠粘膜上的粘膜粘附性。壳聚糖的取代度分别为:OC为52.8%,LC为64.8%,PC为48.5%。SNEDDS和酰化壳聚糖SNEDDS的粒径分别小于50nm和80 - 300nm,zeta电位分别为-0.2至-1.6mV和0.05至0.99mV。向SNEDDS中加入2%的酰化壳聚糖可使SNEDDS在肠粘膜上的停留时间增加两倍。得出的结论是,由于在SNEDDS中加入了酰化壳聚糖,它们的粘膜粘附特性得以提高。

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