脂质体用于眼部后房的有效药物递送。
Liposomes for effective drug delivery to the ocular posterior chamber.
机构信息
School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou, 510006, Guangdong, China.
The First Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou, 510006, Guangdong, China.
出版信息
J Nanobiotechnology. 2019 May 13;17(1):64. doi: 10.1186/s12951-019-0498-7.
BACKGROUND
Age-related macular degeneration (AMD) is a leading cause of severe visual deficits and blindness. Meanwhile, there is convincing evidence implicating oxidative stress, inflammation, and neovascularization in the onset and progression of AMD. Several studies have identified berberine hydrochloride and chrysophanol as potential treatments for ocular diseases based on their antioxidative, antiangiogenic, and anti-inflammatory effects. Unfortunately, their poor stability and bioavailability have limited their application. In order to overcome these disadvantages, we prepared a compound liposome system that can entrap these drugs simultaneously using the third polyamidoamine dendrimer (PAMAM G3.0) as a carrier.
RESULTS
PAMAM G3.0-coated compound liposomes exhibited appreciable cellular permeability in human corneal epithelial cells and enhanced bio-adhesion on rabbit corneal epithelium. Moreover, coated liposomes greatly improved BBH bioavailability. Further, coated liposomes exhibited obviously protective effects in human retinal pigment epithelial cells and rat retinas after photooxidative retinal injury. Finally, administration of P-CBLs showed no sign of side effects on ocular surface structure in rabbits model.
CONCLUSIONS
The PAMAM G3.0-liposome system thus displayed a potential use for treating various ocular diseases.
背景
年龄相关性黄斑变性(AMD)是导致严重视力损害和失明的主要原因。同时,有令人信服的证据表明氧化应激、炎症和新生血管形成与 AMD 的发生和进展有关。几项研究已经发现盐酸小檗碱和大黄素具有抗氧化、抗血管生成和抗炎作用,可能是治疗眼部疾病的潜在药物。不幸的是,它们较差的稳定性和生物利用度限制了它们的应用。为了克服这些缺点,我们使用第三代聚酰胺-胺树状大分子(PAMAM G3.0)作为载体,制备了一种可以同时包封这些药物的复合脂质体系统。
结果
PAMAM G3.0 包裹的复合脂质体在人角膜上皮细胞中表现出相当大的细胞通透性,并增强了在兔角膜上皮上的生物黏附性。此外,包封脂质体大大提高了 BBH 的生物利用度。进一步的,包封脂质体在光氧化视网膜损伤后对人视网膜色素上皮细胞和大鼠视网膜显示出明显的保护作用。最后,在兔模型中,P-CBLs 的给药对眼部表面结构没有显示出副作用的迹象。
结论
因此,PAMAM G3.0-脂质体系统显示出了用于治疗各种眼部疾病的潜力。