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评价基于糠醛醇的凝胶作为萘普生局部应用的新型载体。

Evaluation of glycofurol-based gel as a new vehicle for topical application of naproxen.

机构信息

Department of Pharmaceutics, King Saud University, College of Pharmacy, PO Box 22452, Riyadh, 11495, Kingdom of Saudi Arabia.

出版信息

AAPS PharmSciTech. 2010 Sep;11(3):1138-46. doi: 10.1208/s12249-010-9485-x. Epub 2010 Jul 23.

Abstract

In view of the good skin tolerability, glycofurol was used as a vehicle-based gel, and its effect in the topical penetration of Naproxen (NAP) was investigated. The aims of this study were to develop a suitable gel with bioadhesive property, spreadability, and viscosity for topical anti-inflammatory effect. Three gelling and adhesive agents were examined: Carbopol 974P, Gantrez AN 119, and polyvinylpyrollidone K30. Skin permeation rates and lag times of NAP were evaluated using the Franz-type diffusion cell in order to optimize the gel formulation. The permeation rate of NAP-based gel across the excised rat skin was investigated. A significant increase in permeability parameters such as steady-state flux (J(ss)), permeability coefficient (K(p)), and penetration index (PI) was observed in optimized formulation containing 2% Transcutol as an permeation enhancer. From skin irritation test, it was concluded that the optimized novel glycofurol-based gel formulation was safe to be used for topical drug delivery. The developed glycofurol-based gel appeared promising for dermal and transdermal delivery of naproxen and could be applicable with water-insoluble drugs, which would circumvent most of the problems associated with drug therapy.

摘要

鉴于良好的皮肤耐受性,甘醇被用作基于载体的凝胶,并研究了其对萘普生(NAP)局部渗透的影响。本研究的目的是开发一种具有生物粘附性、铺展性和粘度的合适凝胶,以实现局部抗炎效果。研究考察了三种胶凝和粘性剂:卡波姆 974P、Gantrez AN 119 和聚乙烯吡咯烷酮 K30。为了优化凝胶配方,使用 Franz 型扩散池评估了 NAP 的皮肤渗透速率和滞后时间。研究了基于 NAP 的凝胶在离体大鼠皮肤上的渗透。结果表明,在含有 2% Transcutol 的优化配方中,渗透增强剂显著增加了渗透参数,如稳态通量(J(ss))、渗透系数(K(p))和渗透指数(PI)。从皮肤刺激性试验得出结论,优化的新型甘醇基凝胶制剂可安全用于局部药物递送。开发的甘醇基凝胶似乎有望用于萘普生的皮肤和经皮给药,并且可适用于水不溶性药物,这将避免与药物治疗相关的大多数问题。

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