Design And Development Of Drug-loaded Polymer Micelle For Ocular Drug Delivery

In this work,we designed a kind of amphipathy polymer nanomicelle carrier,which was made up of hydrophilic MPEG and hydrophobic PAE,and then modified by hyaluronic acid with mucous adhesion.The primary coverage of the research was to transport ophthalmic drugs to the posterior segment of the eye aiming to increase the bioavailability of drugs,and evaluate the therapeutic effect of drug-loaded micelles on ocular neovascularization diseases.The characterization of the prepared drug-loaded micelles included morphology,particle size,charge and drug loading of nanomicelles.And the performance testing included drug release,corneal penetration,and suppression of vascular.The results of the study were as follows:(1)The amphiphilic polymer carrier was obtained by three steps.The first step was to make terminal hydroxyl of MPEG acrylonylation.The second step was to prepare PAE by Michael addition reaction and get intermediate product MPEG-b-PAE,and the third step was to get the final product MPEG-b-PAE-g-HA by esterification.(2)Genistein-loaded micelles and blank micelles were prepared by dialysis.The dynamic light scattering method was used to detect the size of the drug-loaded micelles.The size and potential were 84.5 nm and-14.9 mV separately.Transmission electron microscopy showed that the micelles were spherical.The drug loading amount of the drug-loaded micelles was 0.56%by ultraviolet spectrum.(3)In vitro drug release tests with dialysis method showed that,drug-loaded micelles have controlled release effect compared with the pure drug solution;The corneal permeability tests with vertical diffusion cells demonstrated that the cumulative penetration of drug-loaded micelles was 1.5 times of the pure drug solution;Matrigei matrix gel was used to induce the formation of lumen structure of HUVEC cells.The results showed that the number of lumen of the drug-loaded micelle group decreas a lot compared with the control group.