Chiappetta Diego A, Sosnik Alejandro
Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina.
Eur J Pharm Biopharm. 2007 Jun;66(3):303-17. doi: 10.1016/j.ejpb.2007.03.022. Epub 2007 Mar 31.
The low solubility in biological fluids displayed by about 50% of the drugs still remains the main limitation in oral, parenteral, and transdermal administration. Among the existing strategies to overcome these drawbacks, inclusion of hydrophobic drugs into polymeric micelles is one of the most attractive alternatives. Amphiphilic poly(ethylene oxide)-poly(propylene oxide) block copolymers are thermoresponsive materials that display unique aggregation properties in aqueous medium. Due to their ability to form stable micellar systems in water, these materials are broadly studied as hydrosolubilizers for poorly water-soluble drugs. The present review provides a concise description of the most important applications of PEO-PPO-based copolymers in the Pharmaceutical Technology field as means for attaining improved solubility, stability, release, and bioavailability of drugs.
约50%的药物在生物流体中溶解度较低,这仍然是口服、肠胃外和透皮给药的主要限制因素。在克服这些缺点的现有策略中,将疏水性药物包封到聚合物胶束中是最具吸引力的方法之一。两亲性聚(环氧乙烷)-聚(环氧丙烷)嵌段共聚物是热响应性材料,在水性介质中表现出独特的聚集特性。由于它们能够在水中形成稳定的胶束系统,这些材料作为难溶性药物的增溶剂被广泛研究。本综述简要描述了基于PEO-PPO的共聚物在制药技术领域的最重要应用,这些应用可提高药物的溶解度、稳定性、释放度和生物利用度。