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壳聚糖-黄原胶(壳寡糖)包被的脂质体作为利福平肺部给药的潜在载体。

Liposomes coated with chitosan-xanthan gum (chitosomes) as potential carriers for pulmonary delivery of rifampicin.

机构信息

Department of Farmaco Chimico Tecnologico, University of Cagliari, 09124 Cagliari, Italy.

出版信息

J Pharm Sci. 2012 Feb;101(2):566-75. doi: 10.1002/jps.22775. Epub 2011 Oct 13.

Abstract

The aim of this work was to develop new microparticles for drug delivery to lungs by coating liposomes with chitosan (CH)-xanthan gum (XG) polyelectrolyte complexes to obtain chitosomes. To this purpose, two groups of liposomes were prepared using a mixture of soy phosphatidylcholine and hydrogenated soy phosphatidylcholine in two different concentrations to evaluate their capability to entrap appropriate amounts of the model drug rifampicin. The obtained vesicles were then coated with different CH-XG weight ratios and liposomes and chitosomes were characterized in terms of morphology, size, size distribution, zeta potential, drug entrapment, and rheological properties. The efficiency of chitosomes and liposomes during nebulization was also studied. Results of this study indicated that nebulization and rheological properties of chitosomes are affected by the CH-XG weight ratio. In particular, CH-XG 1:0.5 (w/w) coating was able to greatly improve drug total mass output and drug deposition in the lower stages of the impinger.

摘要

这项工作的目的是通过用壳聚糖(CH)-黄原胶(XG)聚电解质复合物包被脂质体来开发用于肺部药物输送的新微粒体,以获得壳质体。为此,使用两种不同浓度的大豆卵磷脂和氢化大豆卵磷脂混合物制备了两组脂质体,以评估它们包封模型药物利福平的适当量的能力。然后用不同的 CH-XG 重量比对获得的囊泡进行包被,并在形态、大小、大小分布、Zeta 电位、药物包封和流变性能方面对脂质体和壳质体进行了表征。还研究了雾化过程中壳质体和脂质体的效率。这项研究的结果表明,壳质体的雾化和流变性能受到 CH-XG 重量比的影响。特别是,CH-XG 1:0.5(w/w)包被能够大大提高药物总质量输出和冲击式沉淀器较低阶段的药物沉积。

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