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阴离子凝胶作为电调制药物递送的载体。I. 溶剂和药物传输现象。

Anionic gels as vehicles for electrically-modulated drug delivery. I. Solvent and drug transport phenomena.

作者信息

Hsu C S, Block L H

机构信息

Graduate School of Pharmaceutical Sciences, Duquesne University, Pittsburgh, Pennsylvania 15282, USA.

出版信息

Pharm Res. 1996 Dec;13(12):1865-70. doi: 10.1023/a:1016045427545.

Abstract

PURPOSE

The purpose of this study was to elucidate the in vitro behavior of anionic gels as formulation matrices for electrically-modulated drug delivery. Agarose and combinations of agarose with other anionic polymers (carbomer 934P; xanthan gum) were selected and tested to evaluate their potential for drug delivery.

METHODS

Electrical current was applied by an automatic crossover power supply to minimize the current fluctuation. Hydrocortisone was selected as the model drug in order to minimize electrostatic interference with drug transport. Syneresis and drug migration were evaluated as a function of current application time and the intensity of electrical current.

RESULTS

The data show that electrical current strength and gellant content can affect both the syneresis and drug migration. A linear correlation was found between hydrocortisone loss and mass loss via the exudate. Moreover, in agarose-carbomer 934P gel systems, cumulative gel mass loss is a linear function of time at low intensities of electrical current (e.g., 0.5 mA and 1 mA). However, hydrocortisone distribution, after electrical application, is relatively asymmetric in those agarose-carbomer 934P gels (and in agarose-xanthan gum gels) in contrast to gel matrices containing only agarose.

CONCLUSIONS

In this study, the use of carbomer 934P in conjunction with agarose enables the formulator to achieve zero-order release with electrical application. Increased anisotropicity of a gel system due to the application of electrical current could alter the effectiveness of a drug delivery system.

摘要

目的

本研究的目的是阐明阴离子凝胶作为电调制药物递送制剂基质的体外行为。选择并测试了琼脂糖以及琼脂糖与其他阴离子聚合物(卡波姆934P;黄原胶)的组合,以评估它们在药物递送方面的潜力。

方法

通过自动交叉电源施加电流,以尽量减少电流波动。选择氢化可的松作为模型药物,以尽量减少对药物转运的静电干扰。评估了脱水收缩和药物迁移与电流施加时间和电流强度的关系。

结果

数据表明,电流强度和胶凝剂含量会影响脱水收缩和药物迁移。发现氢化可的松损失与通过渗出液的质量损失之间存在线性相关性。此外,在琼脂糖-卡波姆934P凝胶体系中,在低电流强度(例如0.5 mA和1 mA)下,累积凝胶质量损失是时间的线性函数。然而,与仅含琼脂糖的凝胶基质相比,在施加电流后,氢化可的松在那些琼脂糖-卡波姆934P凝胶(以及琼脂糖-黄原胶凝胶)中的分布相对不对称。

结论

在本研究中,将卡波姆934P与琼脂糖结合使用可使配方设计师在施加电流时实现零级释放。由于施加电流导致凝胶体系各向异性增加,可能会改变药物递送系统的有效性。

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