A controlled-release ocular delivery system for ibuprofen based on nanostructured lipid carriers.
The objective of this study was to develop an ocular drug delivery system based on nanostructured lipid carrier and investigate its in vitro and in vivo characteristics. Ibuprofen was chosen as the model drug. Four different formulations of ibuprofen nanostructured lipid carriers were prepared by melted-ultrasonic methods; gelucire 44/14 was screened as one of the solid lipid matrix materials due to the good particle size dispersion and excellent contribution to the corneal permeability of the model drug. The modified Franz-type diffusion cells and isolated corneas were used in the test of drug corneal permeability and the in vivo releasing tests were carried out using microdialysis method. gelucire 44/14 and transcutol P could enhance the corneal permeability by different mechanisms. The corresponding apparent permeability coefficients (P(app)) were 1.28 and 1.36 times more than that of the control preparation. Stearylamine could prolong the pre-cornea retention time of the model drug to some extent. Ibuprofen nanostructured lipid carriers displayed controlled-release property. The AUC of the optimized formulation of ibuprofen nanostuctured lipid carriers was 3.99 times more than that of ibuprofen eye drops).
Li
Xiang
X
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China. lixiangdoudou@163.com
Nie
Shu-fang
SF
Kong
Jun
J
Li
Ning
N
Ju
Cheng-yi
CY
Pan
Wei-san
WS
D000287:Administration, Topical; D000588:Amines / Q000737:chemistry; D000818:Animals; D001767:Blinking / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003315:Cornea / Q000187:drug effects / Q000378:metabolism*; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D005026:Ethylene Glycols / Q000737:chemistry; D005079:Excipients / Q000737:chemistry* / Q000633:toxicity; D007052:Ibuprofen / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D008055:Lipids / Q000737:chemistry*; D008297:Male; D017551:Microdialysis; D049329:Nanostructures; D009883:Ophthalmic Solutions; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry; D011817:Rabbits; D013678:Technology, Pharmaceutical / Q000379:methods
D000588:Amines; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005026:Ethylene Glycols; D005079:Excipients; D008055:Lipids; D009883:Ophthalmic Solutions; C104509:gelucire 44-14; D011092:Polyethylene Glycols; C010111:carbitol; C009317:stearylamine; D007052:Ibuprofen