Department of Pharmaceutics, King Saud University, College of Pharmacy, PO Box 22452, Riyadh, 11495, Kingdom of Saudi Arabia.
AAPS PharmSciTech. 2010 Sep;11(3):1138-46. doi: 10.1208/s12249-010-9485-x. Epub 2010 Jul 23.
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.
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。