• ISSN 16748301
  • CN 32-1810/R
Volume 32 Issue 6
Jun.  2018
Article Contents

Citation:

Preparation, optimization, and characterization of chitosancoated solid lipid nanoparticles for ocular drug delivery

  • Received Date: 2016-12-20
    Accepted Date: 2018-01-22

    Fund Project: This work was supported by grants from the National Natural Science Foundation of China (81100977).

  • 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 electronmicroscopy 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.
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Preparation, optimization, and characterization of chitosancoated solid lipid nanoparticles for ocular drug delivery

  • 1. Department of Pharmacy, the Affiliated Hospital of Xuzhou Medical University, Xuzhou, Jiangsu 221002, China
  • 2. School of Pharmacy, Nanjing Medical University, Nanjing, Jiangsu 211166, China
  • 3. Department of Pharmacy, Tongde Hospital of Zhejiang Province, Hangzhou, Zhejiang 310000, China
  • 4. Department of Colorectal Surgery, the First Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu 210029, China
  • 5. Department of Pharmacy, the Affiliated Wuxi People's Hospital of Nanjing Medical University, Hospital, Wuxi, Jiangsu 214023, China
  • 6. Department of Pharmacy, Jiangsu University, the Affiliated Zhenjiang First People’s Hospital, Zhenjiang, Jiangsu 212002, China
  • 7. Department of Pharmacy, the Affiliated Wuxi Maternity and Child Health Care Hospital of Nanjing Medical University, Wuxi, Jiangsu 214000, China
  • 8. Department of Orthopedichitosan, Xuzhou Central Hospital, Xuzhou, Jiangsu 221009, China
Fund Project:  This work was supported by grants from the National Natural Science Foundation of China (81100977).

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 electronmicroscopy 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.

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