Shinde Chetan, Venkatesh Madhugiri Prakash, Pramod Kumar Tegginmat, Pai Deeksha Ramananda
Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Mysuru, India.
Autoimmunity. 2021 Feb;54(1):35-44. doi: 10.1080/08916934.2020.1846184. Epub 2020 Nov 12.
The promising potential of nano-structured lipid carrier (NLC) polymeric gel of CUR as an effective treatment for rheumatoid arthritis by intra-articular route of administration was investigated. NLC composed of cetylpalmitate, Labrafac PG & Captex 200, Tween 80 and Labrasol. The hot homogenization method employed by melt ultrasonication was used. The formulated NLC dispersions were characterized and were suitably dispersed into the matrix of pluronic F-127(PLF-127) and pluronic F-68 (PLF-68). A two-factor three-level full factorial design was employed to deduce the optimal concentrations of PLF-127 and PLF-68. The optimized formulations were sterilized by gamma radiation. The formulated NLC smart gels were characterized and evaluated for various parameters. The efficacy evaluation by antigen-induced monoarthritis model and biocompatibility testing by histopathological studies was performed. Formulated NLCs exhibited an average particle size of 165.12 nm, entrapment efficiency of 72.15%, and zeta potential of -21.67 mV. The optimized CUR-NLC smart gel was demonstrated to have a sol-gel transformation at 33.21 °C and 94.32% drug release at 84 h. NLC's which were sterile and easily syringeable, continued to remain within the colloidal range. CUR-NLC smart gels were found to be biocompatible and showed a significant reduction in rat knee joint inflammation compared to free drug.
研究了姜黄素纳米结构脂质载体(NLC)聚合物凝胶通过关节内给药途径作为类风湿性关节炎有效治疗方法的潜在前景。NLC由十六烷基棕榈酸酯、Labrafac PG和Captex 200、吐温80和Labrasol组成。采用熔体超声的热均质化方法。对制备的NLC分散体进行表征,并将其适当地分散到普朗尼克F - 127(PLF - 127)和普朗尼克F - 68(PLF - 68)的基质中。采用二因素三水平全因子设计来推导PLF - 127和PLF - 68的最佳浓度。优化后的制剂通过伽马辐射进行灭菌。对制备的NLC智能凝胶进行表征,并对各种参数进行评估。通过抗原诱导的单关节炎模型进行疗效评估,并通过组织病理学研究进行生物相容性测试。制备的NLC平均粒径为165.12nm,包封率为72.15%,zeta电位为 - 21.67mV。优化后的姜黄素 - NLC智能凝胶在33.21°C时表现出溶胶 - 凝胶转变,在84小时时药物释放率为94.32%。无菌且易于注射的NLC在胶体范围内保持稳定。与游离药物相比,姜黄素 - NLC智能凝胶具有生物相容性,并且大鼠膝关节炎症明显减轻。