School of Pharmacy, Queen's University Belfast, Medical Biology Centre, Belfast, UK; Department of Pharmacognosy, College of Pharmacy, Najran University, Najran, Saudi Arabia.
School of Pharmacy, Queen's University Belfast, Medical Biology Centre, Belfast, UK.
Drug Discov Today. 2024 Aug;29(8):104098. doi: 10.1016/j.drudis.2024.104098. Epub 2024 Jul 10.
Block copolymer micelles, formed by the self-assembly of amphiphilic polymers, address formulation challenges, such as poor drug solubility and permeability. These micelles offer advantages including a smaller size, easier preparation, sterilization, and superior solubilization, compared with other nanocarriers. Preclinical studies have shown promising results, advancing them toward clinical trials. Their mucoadhesive properties enhance and prolong contact with the ocular surface, and their small size allows deeper penetration through tissues, such as the cornea. Additionally, copolymeric micelles improve the solubility and stability of hydrophobic drugs, sustain drug release, and allow for surface modifications to enhance biocompatibility. Despite these benefits, long-term stability remains a challenge. In this review, we highlight the preclinical performance, structural frameworks, preparation techniques, physicochemical properties, current developments, and prospects of block copolymer micelles as ocular drug delivery systems.
嵌段共聚物胶束由两亲聚合物自组装形成,可解决制剂挑战,如药物溶解度和渗透性差。与其他纳米载体相比,这些胶束具有更小的尺寸、更容易制备、更容易灭菌和更好的增溶等优势。临床前研究显示出有希望的结果,使它们能够推进到临床试验阶段。其黏膜黏附特性增强并延长了与眼表面的接触,其较小的尺寸允许更深地穿透组织,如角膜。此外,共聚物胶束提高了疏水性药物的溶解度和稳定性,维持药物释放,并允许进行表面修饰以提高生物相容性。尽管有这些好处,但长期稳定性仍然是一个挑战。在这篇综述中,我们重点介绍了作为眼部药物传递系统的嵌段共聚物胶束的临床前性能、结构框架、制备技术、物理化学性质、当前进展和前景。