Aziz Zarith Asyikin Binti Abdul, Ahmad Akil, Mohd-Setapar Siti Hamidah, Hassan Hashim, Lokhat David, Kamal Mohammad Amjad, Ashraf Ghulam Md
Center of Lipids Engineering and Applied Research, Ibnu Sina Institute for Industrial and Scientific Research, Universiti Teknologi Malaysia, 81310 UTM Skudai, Johor, Malaysia.
King Fahd Medical Research Center, King Abdulaziz University, P.O. Box 80216, Jeddah 21589, Saudi Arabia.
Curr Drug Metab. 2017;18(1):16-29. doi: 10.2174/1389200217666160921143616.
In clinical studies, drugs with hydrophobic characteristic usually reflect low bioavailability, poor drug absorption, and inability to achieve the therapeutic concentration in blood. The production of poor solubility drugs, in abundance, by pharmaceutical industries calls for an urgent need to find the alternatives for resolving the above mentioned shortcomings. Poor water solubility drugs loaded with polymeric micelle seem to be the best alternative to enhance drugs solubility and bioavailability. Polymeric micelle, formed by self-assembled of amphiphilic block copolymers in aqueous environment, functioned as solubilizing agent for hydrophobic drug. This review discusses the fundamentals of polymeric micelle as drug carrier through representative literature, and demonstrates some applications in various clinical trials. The structure, characteristic, and formation of polymeric micelle have been discussed firstly. Next, this manuscript focuses on the potential of polymeric micelles as drug vehicle in oral, transdermal routes, and anti-cancer agent. Several results from previous studies have been reproduced in this review in order to prove the efficacy of the micelles in delivering hydrophobic drugs. Lastly, future strategies to broaden the application of polymeric micelles in pharmaceutical industries have been highlighted.
在临床研究中,具有疏水特性的药物通常表现出低生物利用度、药物吸收差以及无法在血液中达到治疗浓度。制药行业大量生产难溶性药物,迫切需要找到解决上述缺点的替代方法。负载于聚合物胶束中的难溶性药物似乎是提高药物溶解度和生物利用度的最佳替代方案。两亲性嵌段共聚物在水性环境中自组装形成的聚合物胶束,可作为疏水性药物的增溶剂。本综述通过代表性文献探讨了聚合物胶束作为药物载体的基本原理,并展示了其在各种临床试验中的一些应用。首先讨论了聚合物胶束的结构、特性和形成。接下来,本文重点关注聚合物胶束作为药物载体在口服、透皮给药途径以及抗癌药物方面的潜力。为了证明胶束在递送疏水性药物方面的功效,本综述重现了先前研究的若干结果。最后,强调了拓宽聚合物胶束在制药行业应用的未来策略。