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新型基于壳聚糖的水性分散体作为用于局部应用的高效药物传递系统。流变学、质构和释放研究。

Novel aqueous chitosan-based dispersions as efficient drug delivery systems for topical use. Rheological, textural and release studies.

机构信息

Dpto. de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, Prof. García González no. 2, 41012 Sevilla, Spain.

Dpto. Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, Prof. García González no. 2, 41012 Sevilla, Spain.

出版信息

Carbohydr Polym. 2016 Oct 20;151:692-699. doi: 10.1016/j.carbpol.2016.06.006. Epub 2016 Jun 3.

Abstract

The use of a novel cross-linked thiolated chitosan (CTS) was investigated as the main component of aqueous dispersions (at 1% and 3% w/v) for topical drug delivery systems. The nonionic theophiline (Th) and the cationic diltiazem(.)HCl (Dt) (at 0.5% w/v concentration) were used as model drugs. All aqueous dispersions behaved as viscoelastic fluids. The CTS 1% dispersions showed predominance of viscous component and low viscosity. However, in the CTS 3% dispersions, both the elastic component and high viscosities prevailed. So, texture parameters improved from CTS 1% to 3% dispersions and CTS 3%-Dt showed greater cohesion and adhesion than CTS 3%-Th, but always below CTS alone. All dispersions showed a Fickian diffusion mechanism. Despite release profiles of both drugs almost fully overlapped at 1% CTS, diffusion coefficients confirmed Dt released faster than Th at 3% CTS. The rheological behavior and the chemical nature of the drugs explained these results.

摘要

研究了一种新型的交联巯基化壳聚糖(CTS)作为水基分散体(1%和 3%w/v)的主要成分,用于局部药物传递系统。非离子茶碱(Th)和阳离子地尔硫卓(.HCl)(0.5%w/v 浓度)被用作模型药物。所有水基分散体均表现为粘弹性流体。CTS 1%分散体表现出粘性成分占主导地位和低粘度。然而,在 CTS 3%分散体中,弹性成分和高粘度都占主导地位。因此,从 CTS 1%分散体到 CTS 3%分散体,纹理参数得到改善,CTS 3%-Dt 显示出比 CTS 3%-Th 更大的内聚性和附着力,但始终低于单独的 CTS。所有分散体都表现出菲克扩散机制。尽管在 1% CTS 下,两种药物的释放曲线几乎完全重叠,但扩散系数证实 Dt 在 3% CTS 下比 Th 释放得更快。流变行为和药物的化学性质解释了这些结果。

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