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<p>In this research work methotrexate-loaded nanostructured lipid carriers (MNLCs) were taken for the development and further conjugated with folic acid using chitosan as a mediator to achieve site-specific activated macrophage targeting in RA. MNLCs were optimized by a 2<sup>3</sup>- full factorial design. MNLCs were developed by the homogenization technique. The effects of independent variables were checked on Y<sub>1</sub>-particle size, Y<sub>2</sub>- polydispersity index (PDI), and Y<sub>3</sub>-entrapment efficiency (EE). The optimized MNLCs showed particle size 122 ± 5.1&#xa0;nm, PDI 0.316 ± 0.20, Zeta potential − 45 ± 1.5 mV, and EE 94.98 ± 0.85%. FTIR and DSC results confirm that the drug gets incorporated into nanostructured lipid carriers. Surface-modified MNLCs were prepared by conjugation of the N-hydroxy succinimide folic acid ester with chitosan as a mediator. Surface modified MNLCs were confirmed by FTIR spectroscopy. The particle size, PDI and Zeta potential of FA-CS-MNLCs were found to be 130 ± 0.62&#xa0;nm, 0.323 ± 0.32 and − 33 ± 2 mV respectively. SEM analysis confirms the spherical morphology of FA-CS-MNLCs. The sustained release of the drug was observed in phosphate buffer pH 7.4. In vitro cellular uptake studies on macrophage RAW 264.7 cells indicate improved uptake of FA-CS-MNLCs than MNLCs it could be because of advanced recognition of folate receptors. The in vivo antiarthritis study confirms that FA-CS-MNLCs effectively treat arthritis compared to MNLCs and Methotrexate. The prepared FA-CS-MNLCs were found to stable after six months stability study. Thus developed FA-CS-NLCs could be a potential approach for targeted RA therapy.</p>

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Methotrexate-Loaded Nanostructured Lipid Carriers for Targeted Rheumatoid Arthritis Therapy: In Vitro and In Vivo Investigations

  • 期刊论文

  • 发表日期：

    2026年2月16日

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  • Prajakta Naiknaware,
  • Manoj B. Shinde,
  • Varsha Mane,
  • Avinash Bhosale,
  • Akash Narawade

摘要

In this research work methotrexate-loaded nanostructured lipid carriers (MNLCs) were taken for the development and further conjugated with folic acid using chitosan as a mediator to achieve site-specific activated macrophage targeting in RA. MNLCs were optimized by a 23- full factorial design. MNLCs were developed by the homogenization technique. The effects of independent variables were checked on Y1-particle size, Y2- polydispersity index (PDI), and Y3-entrapment efficiency (EE). The optimized MNLCs showed particle size 122 ± 5.1 nm, PDI 0.316 ± 0.20, Zeta potential − 45 ± 1.5 mV, and EE 94.98 ± 0.85%. FTIR and DSC results confirm that the drug gets incorporated into nanostructured lipid carriers. Surface-modified MNLCs were prepared by conjugation of the N-hydroxy succinimide folic acid ester with chitosan as a mediator. Surface modified MNLCs were confirmed by FTIR spectroscopy. The particle size, PDI and Zeta potential of FA-CS-MNLCs were found to be 130 ± 0.62 nm, 0.323 ± 0.32 and − 33 ± 2 mV respectively. SEM analysis confirms the spherical morphology of FA-CS-MNLCs. The sustained release of the drug was observed in phosphate buffer pH 7.4. In vitro cellular uptake studies on macrophage RAW 264.7 cells indicate improved uptake of FA-CS-MNLCs than MNLCs it could be because of advanced recognition of folate receptors. The in vivo antiarthritis study confirms that FA-CS-MNLCs effectively treat arthritis compared to MNLCs and Methotrexate. The prepared FA-CS-MNLCs were found to stable after six months stability study. Thus developed FA-CS-NLCs could be a potential approach for targeted RA therapy.