Singh Neelu, Parashar Poonam, Tripathi Chandra Bhushan, Kanoujia Jovita, Kaithwas Gaurav, Saraf Shubhini A
a Department of pharmaceutical sciences , Babasaheb Bhimrao Ambedkar University (Central University) , Lucknow , India.
J Liposome Res. 2017 Jun;27(2):130-138. doi: 10.1080/08982104.2016.1174943. Epub 2017 Feb 1.
Gout is a painful disorder which does not have an efficient delivery system for its treatment.
Development and in vitro, in vivo evaluation of allopurinol-loaded nonionic surfactant-based niosomes was envisaged.
Niosomes were prepared with Span 20 and Tween 20 (1:1 molar ratio) using ether injection method. The formulations were screened for entrapment efficiency, particle size analysis, zeta potential, release kinetics, in vivo activity, and stability studies.
Stable, spherical vesicles of average particle size 304 nm with zeta-potential and entrapment efficiency of 22.2 mV and 79.44 ± 0.02%, respectively, were produced. In vitro release study revealed 82.16 ± 0.04% release of allopurinol within 24 h. The niosomal formulation was further evaluated for its antigout potential in monosodium urate (MSU) crystal induced gout animal model. The formulation demonstrated significant uric acid level reduction and enhanced antigout activity when compared with the pure allopurinol.
The better antigout activity displayed by niosomal formulation could be attributed to sustained release of drug, higher drug solubility within biological fluids, better membrane interaction, smaller size, and presence of cholesterol and surfactant.
This study reveals that niosomes can be an efficient delivery system for the treatment of gout.
痛风是一种疼痛性疾病，其治疗缺乏有效的给药系统。
设想开发载有别嘌醇的非离子表面活性剂基脂质体并进行体外、体内评价。
采用乙醚注入法，用司盘20和吐温20（摩尔比1:1）制备脂质体。对制剂进行包封率、粒径分析、zeta电位、释放动力学、体内活性和稳定性研究。
制备出平均粒径为304nm的稳定球形囊泡，zeta电位为22.2mV，包封率为79.44±0.02%。体外释放研究表明，24小时内别嘌醇的释放率为82.16±0.04%。在尿酸钠（MSU）晶体诱导的痛风动物模型中，进一步评价了脂质体制剂的抗痛风潜力。与纯别嘌醇相比，该制剂显示出显著的尿酸水平降低和增强的抗痛风活性。
脂质体制剂表现出更好的抗痛风活性，可能归因于药物的持续释放、在生物流体中更高的药物溶解度、更好的膜相互作用、更小的尺寸以及胆固醇和表面活性剂的存在。
本研究表明，脂质体可成为治疗痛风的有效给药系统。
