Development, Optimization, and Evaluation of Rutin-Loaded Liposomes in the Management of Rheumatoid Arthritis.

Gunjan Nautiyal, Shiv Kant Sharma, Dhirender Kaushik, Parijat Pandey
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Abstract

Background: Rheumatoid arthritis is a chronic autoimmune disease, progressively distinctive via cartilage destruction, auto-antibody production, severe joint pain, and synovial inflammation. Nanotechnology represents one of the utmost promising scientific technologies of the 21st century. Nanocarriers could be the key to unlocking its potential by encapsulating Rutin in targeted drug delivery systems, potentially for targeted Rheumatoid arthritis therapy.

Objective: The rationale of current research is to prepare liposomes loaded with a bioflavonoid drug rutin for effective management of rheumatoid arthritis.

Materials and methods: This study investigated the formulation of rutin liposomes using the thinfilm hydration technique, also known as the Bangham method. A Box-Behnken design was employed to optimize the formulation parameters. The LP2 batch was then characterized for its mean particle size, zeta potential, shape, diffraction pattern, and thermal properties. Finally, the in-vitro anti-oxidant and anti-inflammatory potential of the rutin liposomes were evaluated using appropriate assays.

Results: Out of thirteen batches, LP2 was found to be an optimized batch with a mean particle size of 167.1 nm, zeta potential -13.50 mV, and entrapment efficiency of 61.22%. The above results showed higher stability of rutin liposomes. Further characterization of LP2 for morphological assessment, XRD analysis, and DSC revealed its spherical shape less than 1 μm, polycrystalline nature, and thermographic peak at 139°C, respectively. Evaluation of the antioxidant properties and antiinflammatory potential of LP2 revealed its maximum therapeutic potential in the reduction of inflammation and protein denaturation when evaluated via in-vitro assays.

Conclusion: Rutin liposomal formulation has tremendous potential for the management of Rheumatoid arthritis due to its enhanced bioavailability, anti-oxidant, and anti-inflammatory properties when compared to free rutin.

芦丁脂质体在类风湿关节炎治疗中的开发、优化和评价。
背景:类风湿关节炎是一种慢性自身免疫性疾病,表现为软骨破坏、自身抗体产生、严重关节疼痛和滑膜炎症。纳米技术是21世纪最有前途的科学技术之一。纳米载体可能是释放其潜力的关键,通过将芦丁封装在靶向药物输送系统中,可能用于靶向类风湿性关节炎治疗。目的:制备生物类黄酮类药物芦丁脂质体,有效治疗类风湿性关节炎。材料与方法:本研究采用薄膜水合技术(又称Bangham法)制备芦丁脂质体。采用Box-Behnken设计法对配方参数进行优化。然后对LP2批进行了平均粒径、zeta势、形状、衍射图案和热性能的表征。最后,采用适当的方法评价芦丁脂质体的体外抗氧化和抗炎潜能。结果:在13个批次中,LP2为最佳批次,平均粒径为167.1 nm, zeta电位为-13.50 mV,包封效率为61.22%。上述结果表明,芦丁脂质体具有较高的稳定性。对LP2进行了进一步的形态学表征、XRD分析和DSC分析,结果表明LP2的形貌小于1 μm,具有多晶性质,在139℃时具有热像峰。通过体外实验对LP2的抗氧化性能和抗炎潜力进行评估,发现其在减少炎症和蛋白质变性方面具有最大的治疗潜力。结论:与游离芦丁相比,芦丁脂质体制剂具有增强的生物利用度、抗氧化和抗炎特性,在类风湿关节炎的治疗中具有巨大的潜力。
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