基于聚消旋乳酸的生物可降解性聚合物纳米胶囊用于金雀异黄素局部给药︰制备、表征及皮肤渗透研究_安娜

针对病种：皮肤癌

发表时间：2013年3月

发表国家：美国

登载刊物：生物医学纳米技术杂志

研究单位：巴西戈亚斯州联邦大学制药技术和药物释放系统实验室

研究人员：安娜露西亚特谢拉德卡瓦略赞皮耶里，法布里西亚萨巴费雷拉，艾丽卡克里斯皮姆雷森迪，等

主要结论：异黄酮金雀异黄素 (GEN) 是一种天然产物，对于皮肤癌症的治疗及化学预防具有潜在应用价值；然而其高脂溶性和化学不稳定性限制了它的临床使用。因此，防止GEN退化并增加其在皮肤中的渗透可能是一个有效的尝试方法。在这项工作中，通过预制聚合物（沉淀）的界面沉积制备了负载GEN-聚乳酸PLA纳米胶囊 (GEN-NC)；进行了为期 90 天的理化特性和稳定性研究.

Journal of Biomedical Nanotechnology, 2013, 9(3):527-34.

Biodegradable Polymeric Nanocapsules Based on Poly(DL-lactide) for Genistein Topical Delivery: Obtention, Characterization and Skin Permeation Studies

Ana Lúcia Teixeira de Carvalho Zampieri, Fabrícia Saba Ferreira, Erica Crispim Resende, et al

Faculdade de Farmácia, Lab. Tecnologia Farmacêutica e Sistemas de Liberação de Fármacos, Universidade Federal de Goiás, Goiânia, GO, 74.605-220, Brasil

The isoflavone genistein (GEN) is a natural product with potential applications for skin cancer treatment and chemoprevention; however its high lipophilicity and chemical instability limits its clinical use. Therefore, attempts towards protecting GEN against degradation and increasing its penetration in the skin might be a valid approach. In this work, GEN loaded-PLA nanocapsules (GEN-NC) were prepared by interfacial deposition of preformed polymer (nanoprecipitation); physicochemical characterization and stability studies for 90 days were conducted. GEN-NC were incorporated into semi-solid formulations and permeation experiments were carried out using porcine ear skin. GEN-NC optimized formulation presented a mean diameter of 139 +/- 7.31 nm, polydispersity index of 0.128 +/- 0.08, encapsulation efficiency of 89.63 +/- 2.27% and drug loading from 0.6 to 1.4 w/w%. Stability studies demonstrated that nanocapsules did not exhibit aggregation during the 90 days of the assay, however, a drop in encapsulation efficiency was observed in the first 10 days. Permeation experiments demonstrated that a higher amount of GEN reaches deeper layers of the skin and increased penetration was achieved when GEN-NC were incorporated in a semi-solid gel formulation, indicating that GEN-NC might be a promising nanocarrier system for skin delivery of GEN.

美国《生物医学纳米技术杂志》，2013年3月

基于聚消旋乳酸的生物可降解性聚合物纳米胶囊用于金雀异黄素局部给药︰制备、表征及皮肤渗透研究

安娜露西亚特谢拉德卡瓦略赞皮耶里，法布里西亚萨巴费雷拉，艾丽卡克里斯皮姆雷森迪，等

巴西戈亚斯州联邦大学制药技术和药物释放系统实验室

异黄酮金雀异黄素 (GEN) 是一种天然产物，对于皮肤癌症的治疗及化学预防具有潜在应用价值；然而其高脂溶性和化学不稳定性限制了它的临床使用。因此，防止GEN退化并增加其在皮肤中的渗透可能是一个有效的尝试方法。在这项工作中，通过预制聚合物（沉淀）的界面沉积制备了负载GEN-聚乳酸PLA纳米胶囊 (GEN-NC)；进行了为期 90 天的理化特性和稳定性研究。GEN-NC被加入到半固体制剂中和使用猪耳皮肤进行了渗透实验。GEN-NC优化配方提出平均直径为139 + /-7.31nm，分子量分布指数的为0.128+ /-0.08，封装效率为89.63 + /-2.27%和药物载量从 0.6到 1.4 w/w%。稳定性研究表明在 90 天的检测中纳米胶囊并没有表现出聚集，然而，在头 10 天观察到封装效率的下降。渗透实验表明更多数量的GEN达到更深层的皮肤，并且当GEN-NC被纳入到一种半固体凝胶配方时增加了渗透量，表明GEN-NC可能是一种有前途的药物纳米载体系统，用于皮肤输送GEN。