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Background: <p>Strontium ranelate (SR) is an effective bone regeneration drug; however, its low bioavailability and strong hydrophilicity cause a strong cytotoxicity, venous thrombosis, and allergic reactions when administered in its free form. This study aims to enhance the SR bioavailability by utilizing nanostructured lipid carriers (NLC) as a drug delivery system (DDS).</p> Methods: <p>To improve the drug delivery efficiency and sustained release of the NLC, their surfaces were coated with chitosan oligosaccharide (COS), a natural polymer. The synthesis of COS-NLC was confirmed by measuring particle size and zeta potential, while surface morphology was evaluated using atomic force microscopy (AFM). SR loading efficiencies and release profiles were analyzed via reversed-phase high-performance liquid chromatography (RP-HPLC), and cytotoxicity was evaluated in mouse fibroblast L929 cells.</p> Results: <p>Particle characterization indicated that the COS coating slightly increased the particle size (i.e., from 128.99 ± 2.77 to 131.46 ± 2.13&#xa0;nm) and zeta potential (i.e., from − 13.94 ± 0.49 to − 6.58 ± 0.32&#xa0;mV) of the NLC. The COS-NLC exhibited a high SR-loading efficiency of ~ 86.31 ± 3.28%. An <i>in vitro</i> release test demonstrated an improved sustained release tendency of SR from the COS-NLC compared to that from the uncoated NLC. In cytotoxicity assays using L929 cells, the COS coating reduced the cytotoxicity of the formulated DDS, and the SR-COS-NLC exhibited a 1.4-fold higher cell regeneration effect than SR alone.</p> Conclusion: <p>These findings suggest that the developed COS-NLC serve as an effective and biocompatible DDS platform for the delivery of poorly bioavailable drugs.</p>

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Construction of Chitosan Oligosaccharide-Coated Nanostructured Lipid Carriers for the Sustained Release of Strontium Ranelate

  • 期刊论文

  • 发表日期：

    2025年3月12日

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  • Hayeon Lim,
  • Yoseph Seo,
  • Sung Jun Min,
  • Daehyeon Yoo,
  • Dong Nyoung Heo,
  • Il Keun Kwon,
  • Taek Lee

摘要

Background:

Strontium ranelate (SR) is an effective bone regeneration drug; however, its low bioavailability and strong hydrophilicity cause a strong cytotoxicity, venous thrombosis, and allergic reactions when administered in its free form. This study aims to enhance the SR bioavailability by utilizing nanostructured lipid carriers (NLC) as a drug delivery system (DDS).

Methods:

To improve the drug delivery efficiency and sustained release of the NLC, their surfaces were coated with chitosan oligosaccharide (COS), a natural polymer. The synthesis of COS-NLC was confirmed by measuring particle size and zeta potential, while surface morphology was evaluated using atomic force microscopy (AFM). SR loading efficiencies and release profiles were analyzed via reversed-phase high-performance liquid chromatography (RP-HPLC), and cytotoxicity was evaluated in mouse fibroblast L929 cells.

Results:

Particle characterization indicated that the COS coating slightly increased the particle size (i.e., from 128.99 ± 2.77 to 131.46 ± 2.13 nm) and zeta potential (i.e., from − 13.94 ± 0.49 to − 6.58 ± 0.32 mV) of the NLC. The COS-NLC exhibited a high SR-loading efficiency of ~ 86.31 ± 3.28%. An in vitro release test demonstrated an improved sustained release tendency of SR from the COS-NLC compared to that from the uncoated NLC. In cytotoxicity assays using L929 cells, the COS coating reduced the cytotoxicity of the formulated DDS, and the SR-COS-NLC exhibited a 1.4-fold higher cell regeneration effect than SR alone.

Conclusion:

These findings suggest that the developed COS-NLC serve as an effective and biocompatible DDS platform for the delivery of poorly bioavailable drugs.