PDF(Pubmed)
Abstract：
Skin penetration of an active pharmaceutical ingredient is key to developing topical drugs. This penetration can be adjusted for greater efficacy and/or safety through the selection of dosage form. Two emerging dosage forms, cream-gel and gel-in-oil emulsion, were tested for their ability to deliver diclofenac into the skin, with the target of maximising skin retention while limiting systemic exposure. Prototypes with varying amounts of solvents and emollients were formulated and evaluated by in vitro penetration testing on human skin. Cream-gel formulas showed better skin penetration than the emulgel benchmark drug even without added solvent, while gel-in-oil emulsions resulted in reduced diffusion of the active into the receptor fluid. Adding propylene glycol and diethylene glycol monoethyl ether as penetration enhancers resulted in different diclofenac penetration profiles depending on the dosage form and whether they were added to the disperse or continuous phase. Rheological characterisation of the prototypes revealed similar profiles of cream-gel and emulgel benchmark, whereas gel-in-oil emulsion demonstrated flow characteristics suitable for massaging product into the skin. This study underlined the potential of cream-gel and gel-in-oil emulsions for adjusting active penetration into the skin, broadening the range of choices available to topical formulation scientists.
摘要：
活性药物成分的皮肤渗透是开发局部药物的关键。可以通过选择剂型来调节这种渗透以获得更大的功效和/或安全性。两种新兴的剂型，奶油凝胶和油包胶乳液，测试了双氯芬酸进入皮肤的能力，目标是最大限度地保持皮肤，同时限制全身暴露。配制具有不同量的溶剂和润肤剂的原型，并通过在人体皮肤上进行体外渗透测试进行评估。即使不添加溶剂，乳霜凝胶配方也显示出比乳液凝胶基准药物更好的皮肤渗透性，而油包胶乳液导致活性物质向受体流体的扩散减少。添加丙二醇和二甘醇单乙醚作为渗透增强剂导致不同的双氯芬酸渗透曲线,这取决于剂型以及它们是添加到分散相还是连续相中。原型的流变学特征揭示了乳膏凝胶和乳液凝胶基准的相似轮廓，而油包胶乳液显示出适合将产品按摩到皮肤中的流动特性。这项研究强调了乳膏凝胶和油包胶乳液调节活性物质向皮肤渗透的潜力，拓宽了可用于局部配方科学家的选择范围。
