a National Organization of Drug Control and Research (NODCAR) , Cairo , Egypt .
b Department of Pharmaceutics, Faculty of Pharmacy , Cairo University .
Drug Deliv. 2015;22(6):731-9. doi: 10.3109/10717544.2014.896428. Epub 2014 Mar 27.
Tretinoin (TRT) is a widely used retinoid for the topical treatment of acne, photo-aged skin, psoriasis and skin cancer which makes it a good candidate for topical formulation. Yet side effects, like redness, swelling, peeling, blistering and, erythema, in addition to its high lipophilicity make this challenging. Therefore, the aim of this study was the development of TRT-loaded proniosomes to improve the drug efficacy and to increase user acceptability and compliance by reducing its side effects. Nine formulae were prepared according to 3(2) factorial design and were evaluated for their morphology, vesicle size, entrapment efficiency (EE %), and% of drug released after 5 h. Hydrogel of the candidate formula, N8G (proniosomes prepared with 0.025% TRT, and Span60: cholesterol molar ratio of 3:1 and incorporated in 1% carbopol gel) was developed and evaluated for skin irritation test and clinical study in acne patients compared to marketed product. Candidate formula showed higher efficacy and very low irritation potential when compared to marketed product in human volunteers.
维 A 酸（TRT）是一种广泛用于治疗痤疮、光老化皮肤、银屑病和皮肤癌的外用维甲酸，这使其成为外用制剂的良好候选药物。然而，其副作用，如发红、肿胀、脱皮、起泡和红斑，以及高亲脂性，使得这具有挑战性。因此，本研究的目的是开发载维 A 酸前体脂质体，以提高药物疗效，并通过减少其副作用来提高使用者的接受度和依从性。根据 3(2) 因子设计，制备了九种配方，并对其形态、囊泡大小、包封效率（EE%）和 5 小时后药物释放的%进行了评价。候选配方 N8G（用 0.025% TRT、Span60:胆固醇摩尔比为 3:1 制备的前体脂质体，并掺入 1%卡波姆凝胶）的水凝胶被开发并用于痤疮患者的皮肤刺激性试验和临床研究，与市售产品进行比较。候选配方在志愿者中显示出比市售产品更高的疗效和极低的刺激性潜力。
