透明质酸包覆的固体脂质纳米粒增强甲氨蝶呤的抗风湿活性并降低其毒性。
Hyaluronic acid-coated solid lipid nanoparticles enhance antirheumatic activity and reduce toxicity of methotrexate.
机构信息
Department of Biological Sciences, Sunandan Divatia School of Science, NMIMS (Deemed-to-be) University, 7th Floor, Mithibai College Building, Vile Parle (W), Mumbai, 400056, India.
Pharmaceutical Science & Technology, Institute of Chemical Technology, Matunga, Mumbai, 400019, India.
出版信息
Nanomedicine (Lond). 2022 Jul;17(16):1099-1114. doi: 10.2217/nnm-2022-0009. Epub 2022 Sep 30.
Methotrexate (MTX) is used to treat rheumatoid arthritis (RA) but is associated with severe toxicity. To minimize these side effects of MTX, the study was undertaken to explore its delivery using solid lipid nanoparticles (SLNs). MTX-loaded SLNs were synthesized and coated with hyaluronic acid (HA) for targeted drug delivery and evaluated for their safety and efficacy in a complete Freund's adjuvant (CFA) model. HA-MTX-SLNs (230.0 ± 46.4 nm) with 78.75% entrapment were developed and showed sustained drug release with a significant reduction in toxicity and enhanced activity of the drug at the targeted site upon oral administration in CFA-induced rats. HA-MTX-SLNs can be considered as an efficient therapeutic agents for the treatment of RA.
甲氨蝶呤（MTX）用于治疗类风湿关节炎（RA），但与严重的毒性有关。为了最大程度地减少 MTX 的这些副作用，研究采用固体脂质纳米粒（SLN）来探索其传递方式。 合成了载有 MTX 的 SLN，并涂覆透明质酸（HA）以实现靶向药物传递，并在完全弗氏佐剂（CFA）模型中评估其安全性和疗效。 开发了具有 78.75％包封率的 HA-MTX-SLNs（230.0±46.4nm），并显示出药物的持续释放，毒性显著降低，并且在 CFA 诱导的大鼠口服后在靶向部位的药物活性增强。 HA-MTX-SLNs 可被视为治疗 RA 的有效治疗剂。
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