Suppr超能文献

采用聚合物胶束纳米载体在有限剂量条件下对人毛囊进行阿达帕林的选择性传递。

Selective delivery of adapalene to the human hair follicle under finite dose conditions using polymeric micelle nanocarriers.

机构信息

School of Pharmaceutical Sciences, University of Geneva & University of Lausanne, 1 Rue Michel Servet, 1211 Geneva, Switzerland.

出版信息

Nanoscale. 2018 Jan 18;10(3):1099-1110. doi: 10.1039/c7nr07706h.

Abstract

Drug delivery systems that target the pilosebaceous unit (PSU) selectively could improve the clinical management of diseases that originate in the hair follicle. The aims of this study were (i) to prepare polymeric micelles using d-α-tocopheryl polyethylene glycol succinate diblock copolymer that incorporated adapalene (ADA), a retinoid indicated for Acne vulgaris, and (ii) to investigate the feasibility of delivering ADA preferentially to the PSU under finite dose conditions - thereby better approximating actual conditions of use by patients. Incorporation of ADA into spherical micelles (d <20 nm) increased aqueous solubility by ∼50 000-fold (from <4 ng mL to 0.2 mg mL). Optimized micelle solution and gel formulations (0.02% ADA) were stable after storage for 4 weeks at 4 °C. Finite dose experiments using full-thickness porcine and human skin revealed that ADA delivery efficiency from micelle solution and gel formulations was equivalent and was >2- and 10-fold higher than that from Differin® gel and Differin® cream (products containing ADA at 0.1% (w/w)). Follicular delivery studies in human skin, using a punch biopsy technique to extract the intact PSU, demonstrated that the micelle solution and gel formulations did indeed enable preferential delivery of ADA to the PSU (4.5- and 3.3-fold higher, respectively, than that to PSU-free skin biopsies). Confocal laser scanning microscopy provided visual corroboration that ADA was uniformly distributed in the hair follicles. In conclusion, the results confirmed that polymeric micelle nanocarriers enabled selective, targeted drug delivery to the PSU under finite dose conditions and so might improve therapy of follicular diseases and decrease off-site side-effects.

摘要

靶向皮脂腺单位(PSU)的药物递送系统可以改善源于毛囊的疾病的临床管理。本研究的目的是:(i)使用聚乙二醇琥珀酸二-α-生育酚酯嵌段共聚物制备包含阿达帕林(ADA)的聚合物胶束,ADA 是治疗寻常痤疮的维甲酸;(ii)研究在有限剂量条件下优先将 ADA 递送至 PSU 的可行性 - 从而更好地模拟患者实际使用情况。将 ADA 纳入球形胶束(d <20 nm)使水溶解度增加了约 50,000 倍(从 <4 ng mL 到 0.2 mg mL)。优化的胶束溶液和凝胶制剂(0.02% ADA)在 4°C 下储存 4 周后仍稳定。使用全厚猪皮和人皮进行有限剂量实验表明,从胶束溶液和凝胶制剂中递送 ADA 的效率与Differin®凝胶和 Differin®乳膏(含有 0.1%(w/w)ADA 的产品)相当,且分别高出 2 倍和 10 倍。在人皮肤上进行毛囊递送研究,使用打孔活检技术提取完整的 PSU,证明胶束溶液和凝胶制剂确实能够优先将 ADA 递送至 PSU(分别比无 PSU 皮肤活检高 4.5 倍和 3.3 倍)。共聚焦激光扫描显微镜提供了视觉证实,ADA 均匀分布在毛囊中。总之,结果证实了聚合物胶束纳米载体能够在有限剂量条件下选择性地靶向 PSU 递药,从而可能改善毛囊疾病的治疗并减少非靶部位的副作用。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验