Formulation and Pharmacokinetic Evaluation of Tetracycline-Loaded Solid Lipid Nanoparticles for Subcutaneous Injection in Mice

  • Xu Xi-ming
    Department of Pharmaceutics, School of Pharmacy, Jiangsu University
  • Wang Yan-song
    Department of Pharmaceutics, School of Pharmacy, Jiangsu University
  • Chen Rong-ying
    Department of Pharmaceutics, School of Pharmacy, Jiangsu University
  • Feng Chun-lai
    Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University
  • Yao Feng
    Department of Surgery, Harvard Medical School, Brigham and Women's Hospital
  • Tong Shan-shan
    Department of Pharmaceutics, School of Pharmacy, Jiangsu University
  • Wang Li
    Department of Pharmaceutics, School of Pharmacy, Jiangsu University
  • Yamashita Fumiyoshi
    Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University
  • Yu Jiang-nan
    Department of Pharmaceutics, School of Pharmacy, Jiangsu University

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抄録

The aim of this work was to prepare tetracycline-loaded solid lipid nanoparticles (Tet-SLN), and to evaluate the potential of these colloidal carriers for subcutaneous injection. Tet-SLN was prepared by microemulsion method and the preparation conditions were optimized by ternary phase diagram. At optimized process conditions, lyophilized Tet-SLN showed spherical particles with a mean diameter of 87.2±46.9 nm and a negative zeta potential of −6.69 mV, up to 1.7% tetracycline drug content was achieved after loading. In vitro release test showed a biphasic release profile for Tet-SLN and more than 80% of the drug was liberated from Tet-SLN in 48 h. After subcutaneous injection of Tet-SLN to mice, a considerable sustained release was observed; tetracycline in blood could be detected lasting 36 h, and lower concentrations of tetracycline in all tissues tested compared to the free tetracycline solution were observed. In conclusion, Tet-SLN can be prepared well by microemulsion method and subcutaneous injection of SLN provide a new perspective for drug sustained release.

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