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载秋水仙碱壳聚糖纳米凝胶对尿酸诱导痛风动物模型的抗痛风作用评价。

Appraisal of anti-gout potential of colchicine-loaded chitosan nanoparticle gel in uric acid-induced gout animal model.

机构信息

Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University, Lucknow, India.

出版信息

Arch Physiol Biochem. 2022 Apr;128(2):547-557. doi: 10.1080/13813455.2019.1702702. Epub 2019 Dec 18.

Abstract

Present study is aimed at transdermal delivery of colchicine-loaded chitosan nanoparticles. The nanoformulations were prepared utilising spontaneous emulsification method and optimised through 2 factorial designs. The optimised formulation (CHNP-OPT) displayed an average particle size of 294 ± 3.75 nm, entrapment efficiency 92.89 ± 1.1% and drug content 83.45 ± 2.5%, respectively. release study demonstrated 89.34 ± 2.90% release over a period of 24 h. Further, CHNP-OPT incorporated into HPMC-E4M (hydroxypropyl methylcellulose) to form transdermal gel. CHNP displayed 74.65 ± 1.90% permeation and stability over a period of 90 days. The anti-gout potential of CHNP formulation was evaluated against monosodium urate (MSU) crystal-induced gout in animal model. There was significant reduction in uric acid level, during MSU administration, when compared with the conventional gel of colchicine. The enhanced therapeutic potential was witnessed through X-ray. The study revealed that colchicine-loaded CHNP proved their supremacy over plain colchicine and can be an efficient delivery system for gout treatment.

摘要

本研究旨在实现秋水仙碱载药壳聚糖纳米粒的经皮给药。利用自发乳化法制备纳米制剂,并通过 2 因素设计进行优化。优化后的制剂(CHNP-OPT)的平均粒径为 294±3.75nm,包封效率为 92.89±1.1%,载药量为 83.45±2.5%。释放研究表明,在 24 小时内释放了 89.34±2.90%的药物。进一步将 CHNP-OPT 掺入 HPMC-E4M(羟丙基甲基纤维素)中形成经皮凝胶。CHNP 在 90 天内显示出 74.65±1.90%的透皮率和稳定性。通过动物模型评估 CHNP 制剂对单钠尿酸盐(MSU)晶体诱导痛风的抗痛风作用。与秋水仙碱的常规凝胶相比,在给予 MSU 时尿酸水平显著降低。X 射线证实了增强的治疗潜力。研究表明,载秋水仙碱的 CHNP 优于普通秋水仙碱,可作为治疗痛风的有效给药系统。

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