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PEO-PCL-PEO 三嵌段共聚物共稳定的视黄醇乳液的经皮给药:PCL 嵌段长度的影响。

Topical delivery of retinol emulsions co-stabilised by PEO-PCL-PEO triblock copolymers: effect of PCL block length.

机构信息

Department of Applied Chemistry, Kyungpook National University, Buk-gu, Daegu, South Korea.

出版信息

J Microencapsul. 2012;29(8):739-46. doi: 10.3109/02652048.2012.686528. Epub 2012 May 14.

Abstract

This article describes enhanced skin permeation and UV/thermal stability of retinol emulsions by the co-stabilisation of Tween20 and biodegradable poly(ethylene oxide)-block-poly(ε-caprolactone)-block-poly(ethylene oxide) (PEO-PCL-PEO) triblock copolymers having different lengths of hydrophobic PCL block. A triblock copolymer with a longer PCL block has a lower hydrophile-lipophile balance (HLB) value. Commercial Retinol 50C® (BASF Co., Ludwigshafen, Germany) was used as the source of retinol. Ultrasonication of the Retinol 50C® emulsion with the triblock copolymers led to an increase in retinol solubilisation and a decrease in average particle size of the resulting retinol emulsion. These characteristics improved skin permeation of retinol through the stratum corneum of artificial skin and subsequent proliferation of viable epidermis cell. Employment of the triblock copolymer with a longer PCL block increased both UV and thermal stabilization of the retinol. These results suggest that HLB and PCL block length are important factors to enhance the topical delivery of retinol into the skin.

摘要

本文通过将吐温 20 和可生物降解的聚(氧化乙烯)-嵌段-聚(ε-己内酯)-嵌段-聚(氧化乙烯)(PEO-PCL-PEO)两亲三嵌段共聚物共同稳定化,描述了视黄醇乳剂的皮肤渗透增强和 UV/热稳定性,其中两亲三嵌段共聚物具有不同长度的疏水性 PCL 嵌段。具有较长 PCL 嵌段的两亲三嵌段共聚物具有较低的亲水亲油平衡(HLB)值。商业视黄醇 50C®(巴斯夫公司,路德维希港,德国)用作视黄醇的来源。用两亲三嵌段共聚物超声处理视黄醇 50C®乳剂会导致视黄醇增溶,并降低所得视黄醇乳剂的平均粒径。这些特性改善了视黄醇通过人工皮肤角质层的渗透,随后增加了表皮细胞的存活增殖。使用具有较长 PCL 嵌段的两亲三嵌段共聚物增加了视黄醇的 UV 和热稳定性。这些结果表明,HLB 和 PCL 嵌段长度是增强视黄醇向皮肤局部递送的重要因素。

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