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