关键词: anterior segment block copolymer micelles characterization ocular barriers ocular drug delivery posterior segment

Mesh : Micelles Humans Drug Delivery Systems / methods Polymers / chemistry Animals Administration, Ophthalmic Drug Carriers / chemistry Solubility

来  源:   DOI:10.1016/j.drudis.2024.104098

Abstract:
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.
摘要:
嵌段共聚物胶束,由两亲性聚合物的自组装形成,解决配方挑战,如药物溶解性和渗透性差。这些胶束提供的优点包括较小的尺寸,更容易准备,灭菌,和优越的溶解,与其他纳米载体相比。临床前研究显示了有希望的结果,推进临床试验。它们的粘膜粘附特性增强并延长与眼表的接触,它们的小尺寸允许更深的穿透组织,如角膜。此外,共聚胶束提高了疏水性药物的溶解性和稳定性,持续药物释放,并允许表面修饰以增强生物相容性。尽管有这些好处,长期稳定仍然是一个挑战。在这次审查中,我们强调了它们的临床前表现,结构框架,制备技术,物理化学性质,目前的发展,以及作为眼部药物递送系统的前景。
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