title: Novel surface-modified nanostructured lipid carriers with partially deacetylated water-soluble chitosan for efficient ocular delivery.
abstract: The objective of this study was to propose novel surface-modified nanostructured lipid carriers with partially deacetylated water-soluble chitosan (NLC-PDSC) as an efficient ocular delivery system to improve its transcorneal penetration and precorneal retention. PDSC with a deacetylation degree of around 50% was synthesized using an improved method. NLC loaded with flurbiprofen (FB) were prepared by melt emulsification method. They presented spherical morphology under both transmission electron microscope and scanning electron microscope. After coating with 0.15% (w/v) PDSC solution, the NLC showed a core-shell structure and a reversed zeta potential. The enhanced transcorneal penetration of the coated NLC was evaluated using isolated rabbit corneas, with significantly increased apparent permeability coefficient being 1.40- and 1.75-fold of the NLC and FB phosphate solution (FB-sol; p < 0.05), respectively. Precorneal retention assessed by gamma scintigraphy in vivo showed that the area under the remaining activity-time curve of the PDSC-coated formulation was 1.3-fold of the NLC and 2.4-fold of FB-sol. Moreover, in vivo ocular tolerance study indicated that there was no difference in irritation between the coated and noncoated NLC. In conclusion, novel NLC demonstrate high potential for ocular drug delivery.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University Shenyang, Liaoning Province 110016, People's Republic of China.
authors.forename: Baocheng
authors.initials: B
authors.lastname: Tian
authors.forename: Qiuhua
authors.initials: Q
authors.lastname: Luo
authors.forename: Shuangshuang
authors.initials: S
authors.lastname: Song
authors.forename: Dandan
authors.initials: D
authors.lastname: Liu
authors.forename: Hao
authors.initials: H
authors.lastname: Pan
authors.forename: Wenji
authors.initials: W
authors.lastname: Zhang
authors.forename: Ling
authors.initials: L
authors.lastname: He
authors.forename: Shilin
authors.initials: S
authors.lastname: Ma
authors.forename: Xinggang
authors.initials: X
authors.lastname: Yang
authors.forename: Weisan
authors.initials: W
authors.lastname: Pan
mesh_terms: D060433:Administration, Ophthalmic; D000818:Animals; D048271:Chitosan / Q000737:chemistry*; D003315:Cornea / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D008297:Male; D049329:Nanostructures / Q000737:chemistry*; D010539:Permeability; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D011817:Rabbits; D013499:Surface Properties; D014867:Water / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D008055:Lipids; D004364:Pharmaceutical Preparations; D014867:Water; D048271:Chitosan