title: The potential use of novel chitosan-coated deformable liposomes in an ocular drug delivery system.
abstract: In this study, novel chitosan-coated deformable liposomes (DL-CS) were proposed as an ocular drug delivery system to prolong pre-corneal retention, and improve transcorneal penetration and absorption. Flurbiprofen-loaded deformable liposomes (FP-DL) were prepared by a modified ethanol injection method and then coated with chitosan. Both DL and DL-CS exhibited a homogeneous particle size distribution, high encapsulation efficiency and good stability. After coating with 0.1% CS, the zeta potential was shifted from negative to positive. The apparent permeability coefficient of FP-DL-0.1% CS evaluated using isolated rabbit corneas was 1.29-, 1.95- and 4.59- fold greater than that of uncoated FP-DL, conventional liposomes and FP solution (P<0.01), respectively. The in vivo pre-corneal retention time and elimination dynamics were assessed using gamma scintigraphy technology. The area under the remaining activity-time of FP-DL-0.1% CS was prolonged 2.84- and 1.53-fold compared with that of the FP solution and FP-DL groups, respectively. Moreover, the ocular irritation test in vivo revealed that DL-0.1% CS produced no ocular damage or abnormal clinical signs. These results indicate that DL-CS appears to be a novel ophthalmic drug delivery strategy with the potential to overcome the limitations of conventional eye drops.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, PR China.
authors.forename: Hongdan
authors.initials: H
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, PR China; School of Pharmacy, Queen's University Belfast, Belfast BT7 1NN, UK.
authors.forename: Hao
authors.initials: H
authors.lastname: Pan
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, PR China.
authors.forename: Panpan
authors.initials: P
authors.lastname: Li
authors.affiliation: Department of Internal Medicine, Cardiovascular Research Center, University of Michigan, Ann Arbor, MI 48109, USA.
authors.forename: Hui
authors.initials: H
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, PR China.
authors.forename: Xin
authors.initials: X
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, PR China.
authors.forename: Weisan
authors.initials: W
authors.lastname: Pan
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, PR China. Electronic address: hiyueyuan@163.com.
authors.forename: Yue
authors.initials: Y
authors.lastname: Yuan
mesh_terms: D060433:Administration, Ophthalmic; D000818:Animals; D048271:Chitosan / Q000737:chemistry*; D003315:Cornea / Q000187:drug effects* / Q000378:metabolism; D004339:Drug Compounding; D016503:Drug Delivery Systems; D065546:Drug Liberation; D005480:Flurbiprofen / Q000378:metabolism / Q000493:pharmacokinetics*; D008081:Liposomes / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D008297:Male; D010316:Particle Size; D010539:Permeability; D011817:Rabbits; D046509:Tissue Culture Techniques
chemical_list: D008081:Liposomes; D005480:Flurbiprofen; D048271:Chitosan
keywords: Deformable liposomes; Edge activator; Gamma scintigraphy; Ocular tolerance; Penetration enhancement; Pre-corneal retention