Title: Preparation, optimization, and characterization of chitosan-coated solid lipid nanoparticles for ocular drug delivery


Authors: Fengzhen Wang1, , Mingwan Zhang2,3, , Dongsheng Zhang4, Yuan Huang5, Li Chen6, Sunmin Jiang7, Kun Shi8, Rui Li2


Institutions: 1Department of Pharmacy, the Affiliated Hospital of Xuzhou Medical University, Xuzhou, Jiangsu 221002, China; 2School of Pharmacy, Nanjing Medical University, Nanjing, Jiangsu 211166, China; 3Department of Pharmacy, Tongde Hospital of Zhejiang Province, Hangzhou, Zhejiang 310000, China; 4Department of Colorectal Surgery, the First Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu 210029, China; 5Department of Pharmacy, the Affiliated Wuxi People's Hospital of Nanjing Medical University, Hospital, Wuxi, Jiangsu 214023, China; 6Department of Pharmacy, Jiangsu University, the Affiliated Zhenjiang First Peoples Hospital, Zhenjiang, Jiangsu 212002, China; 7Department of Pharmacy, the Affiliated Wuxi Maternity and Child Health Care Hospital of Nanjing Medical University, Wuxi, Jiangsu 214000, China; 8Department of Orthopedichitosan, Xuzhou Central Hospital, Xuzhou, Jiangsu 221009, China.


Abstract: 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 chitosan-SLNs is a potential carrier for ophthalmic administration.


Keywords: solid lipid nanoparticle, orthogonal design, Box-Behnken design, ophthalmic administration, chitosan


Full Text: JBR-2016-0170.pdf


J Biomed Res published on 14 March 2018, https://doi.org/10.7555/JBR.32.20160170