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Fengzhen Wang,Mingwan Zhang,Dongsheng Zhang,Yuan Huang,Li Chen,Sunmin Jiang,Kun Shi,Rui Li.Journal of Biomedical Research,2018,32(6):411-423
Preparation, optimization, and characterization of chitosancoated solid lipid nanoparticles for ocular drug delivery
Received:December 20, 2016  Revised:January 22, 2018
Keywordssolid lipid nanoparticle, orthogonal design, Box-Behnken design, ophthalmic administration, chitosan
Grant Program
Fengzhen Wang Department of Pharmacy, the Affiliated Hospital of Xuzhou Medical University, Xuzhou, Jiangsu , China
Mingwan Zhang School of Pharmacy, Nanjing Medical University, Nanjing, Jiangsu , China;Department of Pharmacy, Tongde Hospital of Zhejiang Province, Hangzhou, Zhejiang , China
Dongsheng Zhang Department of Colorectal Surgery, the First Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu , China
Yuan Huang Department of Pharmacy, the Affiliated Wuxi People's Hospital of Nanjing Medical University, Hospital, Wuxi, Jiangsu , China
Li Chen Department of Pharmacy, Jiangsu University, the Affiliated Zhenjiang First People¨s Hospital, Zhenjiang, Jiangsu , China
Sunmin Jiang Department of Pharmacy, the Affiliated Wuxi Maternity and Child Health Care Hospital of Nanjing Medical University, Wuxi, Jiangsu , China
Kun Shi Department of Orthopedichitosan, Xuzhou Central Hospital, Xuzhou, Jiangsu , China
Rui Li School of Pharmacy, Nanjing Medical University, Nanjing, Jiangsu , China
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      The present study aimed to develop and optimize chitosan coated solid lipid nanoparticles (chitosan-SLNs) encapsulated with methazolamide. Chitosan-SLNs were successfully prepared by a modified oil-in-water emulsification-solvent evaporation method with glyceryl monostearate as the solid lipid and phospholipid as the surfactant. Systematic screening of formulation factors was carried out. The optimized formula for preparation was screened by orthogonal design as well as Box-Behnken design with entrapment efficiency, particle size and zeta potential as the indexes. The entrapment efficiency of the optimized formulation (methazolamide-chitosan-SLNs) prepared was (58.5 \ 4.5)%, particle size (247.7 \ 17.3) nm and zeta potential (33.5 \ 3.9) mV. Transmission electron microscopy showed homogeneous spherical particles in the nanometer range. A prolonged methazolamide in vitro release profile was obtained in the optimized chitosan-SLNs suspension compared with methazolamide solution. No ocular damages were observed in the susceptibility test on albino rabbits. The results suggest that the combination of orthogonal design and Box-Behnken design is efficient and reliable in the optimization of nanocarriers, and chitosanSLNs is a potential carrier for ophthalmic administration.