Novel pluronic-chitosan micelle as an ocular delivery system.
Pluronic micelles were prepared for ophthalmic delivery by incorporation of ethyl acetate as a dispersion agent and their surfaces were modified by chitosan to improve their bioavailability. The micelles disperse well in the solution and have a core-shell like structure with a particle size ranging from 93 to 181 nm for drug unloaded, 123-232 nm for drug-loaded, and a zeta potential between 6.1 and 9.2 mV, indicating very suitable use as ophthalmic carrier. The in vitro serum stability tests indicate the particle size of the micelles was very stable during the serum absorption. The turbidity test reveals that the prepared micelles were very stable under phosphate buffered saline environment, which can prevent the blurred vision. The loading efficiency of metipranolol in micelles can be as high as 83%. Finally, the in vitro and in vivo studies indicate the pluronic micelles modified by chitosan have sustained release behavior and good pharmacological response. As the results, the pluroic-chitosan micelles system provides a potential opportunity in decreasing frequency of administration and improving patient compliance for ocular drug delivery.
Department of Chemical and Materials Engineering, Southern Taiwan University of Science and Technology, Tainan 710, Taiwan. hrlin@mail.stust.edu.tw
Hong-Ru
HR
Lin
Pei-Csang
PC
Chang
D060433:Administration, Ophthalmic; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage; D000818:Animals; D048271:Chitosan; D020099:Coated Materials, Biocompatible / Q000737:chemistry; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D007429:Intraocular Pressure / Q000187:drug effects; D008422:Materials Testing; D014290:Metipranolol / Q000008:administration & dosage; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures / Q000737:chemistry / Q000648:ultrastructure; D009391:Nephelometry and Turbidimetry; D009883:Ophthalmic Solutions; D010316:Particle Size; D020442:Poloxamer; D011817:Rabbits; D017550:Spectroscopy, Fourier Transform Infrared
D000319:Adrenergic beta-Antagonists; D020099:Coated Materials, Biocompatible; D003692:Delayed-Action Preparations; D008823:Micelles; D009883:Ophthalmic Solutions; D020442:Poloxamer; D048271:Chitosan; D014290:Metipranolol