> Publications > Topical Administration of Mucoadhesive Liposomes-Epoetin-β for Targeting the Ocular Posterior Segment

OptoDrum

Publication

March 26, 2026 • ✎ STRIA TECH

Topical Administration of Mucoadhesive Liposomes-Epoetin-β for Targeting the Ocular Posterior Segment

Topics:

Ocular and CNS Toxicity Models

Retinal Degeneration

Retinal Degeneration and Inherited Retinal Disease

Publication

Molecular Pharmaceutics Journal (Apr 07, 2025) Topical Administration of Mucoadhesive Liposomes-Epoetin-β for Targeting the Ocular Posterior Segment

Pakian S, Nabid MR, Satarian L, Abandansari HS, Mirkani A

DOI: 10.1021/acs.molpharmaceut.5c00079 >>

This preclinical study developed topical mucoadhesive thiolated hyaluronic acid–modified cationic liposomes to deliver the neuroprotective agent Epoetin-β to the retinal posterior segment. The nanoformulation showed uniform size, good biocompatibility in RGC-5 cells, and achieved about 1.9-fold higher retinal penetration versus free Epoetin-β in mice, with a trend toward better visual acuity after optic nerve injury. Behavioral assessment using optomotor response relied on Striatech’s OptoDrum system, supporting sensitive detection of functional recovery.

Delivering drugs to the posterior eye segment is a complex task, particularly for treating retinal diseases. Neuroprotective approaches to maintain neuronal integrity have garnered significant attention in recent research. Here, we developed a mucoadhesive nanoparticulate system based on thiolated hyaluronic acid-modified cationic liposomes (HA-SH@liposomes) for topical administration. To fabricate these liposomes, we utilized microfluidic technology with a toroidal mixer to ensure consistent size and stability. Cationic liposomes were prepared by using the microfluidic method, and Epoetin-β (EPOβ), a neuroprotective agent, was loaded into the liposomes. Following this, HA-SH was conjugated to the EPOβ/HA-SH@liposomes using a postmicrofluidics conjugation method, wherein HA-SH was added dropwise to facilitate electrostatic interactions between the cationic liposomes and the anionic polymer. The resulting liposomes exhibited a mean size of 144 ± 1.3 nm and a polydispersity index (PDI) of 0.09 ± 0.01, indicating their uniformity. We evaluated the biocompatibility of the EPOβ/HA-SH@liposomes in vitro using live/dead and MTS assays on the RGC-5 cell line, demonstrating no notable cytotoxicity compared to the controls. To assess the in vivo performance, we conducted extensive ophthalmological examinations in C57/BL6 mice, including immunofluorescence staining to track the distribution of EPOβ and EPOβ/HA-SH@liposomes within the eyeball. Additionally, we quantified EPOβ levels in the retina using an enzyme-linked immunosorbent assay (ELISA) kit after the topical application of free EPOβ and the EPOβ/HA-SH@liposome formulation. The immunofluorescence staining revealed efficient delivery of EPOβ into the retina and choroid via the transcorneal route when administered as EPOβ/HA-SH@liposomes. ELISA results showed that the liposomal formulation achieved approximately 1.9× greater penetration efficiency than free EPOβ. Furthermore, optokinetic response (OKR) assays indicated that animals treated with EPOβ/HA-SH@liposomes exhibited slightly improved visual acuity compared with those treated with free EPOβ, though the difference was not statistically significant. In conclusion, the topical ocular administration of EPOβ/HA-SH@liposomes facilitated the efficient delivery of EPOβ to the retina, promoting retinal recovery and confirming its neuroprotective properties. This preclinical study provides a foundation for innovative strategies in the topical delivery of neuroprotective agents in ocular therapy.