Liposomes for effective drug delivery to the ocular posterior chamber

Sisi Lai,Yingfeng Zhang,Junjie Chen,Kang Zhou,Yang Yu,Tuo Liu,Yanyan Wei,Wen Xiao,Ning Jiang,Qiuhong Liu,Quanwu Wu

doi:10.1186/s12951-019-0498-7

Abstract

BackgroundAge-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.ResultsPAMAM 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.ConclusionsThe PAMAM G3.0-liposome system thus displayed a potential use for treating various ocular diseases.

Highlights

Age-related macular degeneration (AMD) is a leading cause of severe visual deficits and blindness
The comparative proton nuclear magnetic resonance (1H-NMR) results before and after the reaction illustrated that the H-signal for the chemical displacement of 2.3–3.3 disappeared (Fig. 2a), indicating that Fluorescein isothiocyanate (FITC) had occupied a C-atom of PAMAM G3.0 successfully
As shown in the result, shell with a fine dendritic structure was obviously observed on the surface of compound liposomes (CBLs) coated with FITC-PAMAM, indirectly proving that PMAMA could coat the CBLs successfully by this method (Fig. 2b)

Summary

Introduction

Age-related macular degeneration (AMD) is a leading cause of severe visual deficits and blindness. Several studies have identified berberine hydrochloride and chrysophanol as potential treatments for ocular diseases based on their antioxidative, antiangiogenic, and anti-inflammatory effects. 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. In. Lai et al J Nanobiotechnol (2019) 17:64 addition, their half-lives in vitreous bodies can be prolonged with low toxicity [13]. Lai et al J Nanobiotechnol (2019) 17:64 addition, their half-lives in vitreous bodies can be prolonged with low toxicity [13] Their entry into deeper tissues is limited because of their low bioadhesion. Its spherical shape and enormous internal hydrophobic cavities allow it to encapsulate drug molecules as micelles, which could modify the liposomal structure to facilitate targeting [19,20,21,22]

Methods

Results

Conclusion