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作为抗皱剂的液晶纳米结构化分散体 α-硫辛酸的化妆品应用的临床疗效。

The clinical efficacy of cosmeceutical application of liquid crystalline nanostructured dispersions of alpha lipoic acid as anti-wrinkle.

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Misr International University, Cairo, Egypt.

Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

出版信息

Eur J Pharm Biopharm. 2014 Feb;86(2):251-9. doi: 10.1016/j.ejpb.2013.09.008. Epub 2013 Sep 18.

Abstract

Topical 5% alpha lipoic acid (ALA) has shown efficacy in treatment of photo-damaged skin. The aim of this work was to evaluate the potential of poloxamer (P407) gel as a vehicle for the novel lipid base particulate system (cubosome dispersions) of ALA. Cubosome dispersions were formulated by two different approaches, emulsification of glyceryl monoolein (GMO) and poloxamer (P407) in water followed by ultrasonication, and the dilution method using a hydrotrope. Three different concentrations of GMO were used to formulate the cubosome dispersions using the first method, 5% (D1), 10% (D2) and 15% w/w (D3). In the second technique an isotropic liquid was produced by combining GMO with ethanol, and this isotropic liquid was then diluted with a P407 solution (D4). The dispersions were characterized by zeta potential, light scattering techniques, optical and transmission electron microscopy, encapsulation efficiency and in vitro drug release. Results showed that D4 was not a uniform dispersion and that D1, D2 and D3 were uniform dispersions, in which by increasing the GMO content in the dispersion, the size of the cubosomes decreased, zeta potential became more negative, encapsulation efficiency increased up to 86.48% and the drug release rate was slower. P407 gels were prepared using the cold method. Two concentrations of P407 gel were fabricated, 20 and 30% w/w. P407 gels were loaded with either ALA or dispersions containing ALA cubosomes. P407 gels were characterized by critical gelation temperature, rheological measurements and in vitro drug release studies. Results suggested that by increasing P407 concentration, the gelation temperature decreases and viscosity increases. Drug release in both cases was found to follow the Higuchi square root model. Gel loaded with ALA cubosomes provided a significantly lower release rate than the gel loaded with the un-encapsulated ALA. A double blinded placebo controlled clinical study was conducted, aiming to evaluate the efficacy as an anti-wrinkle agent and volunteer's satisfaction upon application of topical 30% P407 gel loaded with ALA cubosomes. Results indicated reduction in facial lines, almost complete resolution of fine lines in the periorbital region and upper lip area and overall improvement in skin color and texture in most volunteers. There were no instances of irritation, peeling or other apparent adverse side effects.

摘要

局部用 5%α-硫辛酸(ALA)已被证明对光损伤皮肤的治疗有效。本工作旨在评估泊洛沙姆(P407)凝胶作为新型脂质基颗粒系统( cubosome 分散体) ALA 的载体的潜力。 cubosome 分散体通过两种不同的方法来制备,即甘油单油酸酯(GMO)和泊洛沙姆(P407)在水中乳化,然后进行超声处理,以及使用增溶剂的稀释方法。使用第一种方法,使用三种不同浓度的 GMO 来制备 cubosome 分散体,分别为 5%(D1)、10%(D2)和 15%w/w(D3)。在第二种技术中,通过将 GMO 与乙醇结合来产生各向同性液体,然后将该各向同性液体用 P407 溶液稀释(D4)。通过测定 Zeta 电位、光散射技术、光学和透射电子显微镜、包封效率和体外药物释放对分散体进行了表征。结果表明,D4 不是均匀的分散体,而 D1、D2 和 D3 是均匀的分散体,随着分散体中 GMO 含量的增加, cubosomes 的尺寸减小,Zeta 电位变得更负,包封效率增加至 86.48%,药物释放速率变慢。通过冷法制备了 P407 凝胶。制备了两种浓度的 P407 凝胶,分别为 20%和 30%w/w。将 ALA 或含有 ALA cubosomes 的分散体载入 P407 凝胶中。通过临界胶凝温度、流变学测量和体外药物释放研究对 P407 凝胶进行了表征。结果表明,随着 P407 浓度的增加,胶凝温度降低,粘度增加。在这两种情况下,药物释放均遵循 Higuchi 平方根模型。载有 ALA cubosomes 的凝胶比载有未包封的 ALA 的凝胶释放速度显著降低。进行了一项双盲安慰剂对照临床试验,旨在评估作为抗皱剂的疗效以及志愿者在应用载有 ALA cubosomes 的 30%P407 凝胶时的满意度。结果表明,面部线条减少,眶周和上唇区域的细小皱纹几乎完全消失,大多数志愿者的皮肤颜色和质地得到整体改善。没有出现刺激、脱皮或其他明显的不良反应。

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