Glatiramer acetate in situ forming gel, a new approach for multiple sclerosis treatment.

IF 2.5 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Anahita Shobeirean, Hossein Attar, Reyhaneh Varshochian, Mohammad Amin Rezvanfar
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Abstract

Background: Glatiramer acetate (GA), a commonly used treatment for multiple sclerosis (MS), requires long-term frequent injections to ensure its effectiveness. This often leads to adverse effects, patient noncompliance, and economic inefficiency.

Objectives: In this study, poloxamer, as a thermosensitive polymer modified by chitosan (CS) and hyaluronic acid (HA), was employed to prepare an in situ forming prolonged release formulation of GA to overcome the problems derived from frequent repeated injections and to enhance the patient compliance.

Methods: The sol-gel formulation was produced through a cold method and optimized using design of experiments. The final product was characterized in terms of gelation time (GT), rheological behaviors, morphological properties, assay, and drug release kinetics.

Results: The in vitro release rate of GA during the first 24 h was quite rapid, but then it continued at a slower rate of 0.05 mg ml-1h-1. The in vivo analysis after the subcutaneous injections showed lower levels of IL-5, IL-13, and uric acid (UA) in mice treated with the gel formulation compared with those receiving free GA in the first few days. However, after 10 days, significantly higher concentrations were detected, which continued to increase slowly.

Conclusion: It can be concluded that the designed thermosensitive sol-gel formula is capable of extending the effectiveness of GA and can be considered as a promising sustained release formulation for the treatment of MS.

Abstract Image

醋酸格拉替雷原位成形凝胶,治疗多发性硬化症的新方法。
背景:醋酸格拉替雷(GA)是治疗多发性硬化症(MS)的常用药物,需要长期频繁注射以确保疗效。这往往会导致不良反应、患者不依从以及经济效益低下:本研究采用壳聚糖(CS)和透明质酸(HA)改性的热敏聚合物聚氧乙烯(poloxamer)制备 GA 原位成型缓释制剂,以克服频繁重复注射带来的问题,提高患者的依从性:方法:溶胶凝胶制剂是通过冷制法生产的,并通过实验设计进行了优化。方法:通过冷制法制备出溶胶-凝胶配方,并利用实验设计对其进行了优化,从凝胶化时间(GT)、流变行为、形态特性、检测和药物释放动力学等方面对最终产品进行了表征:结果:在最初的 24 小时内,GA 的体外释放速度非常快,但随后以 0.05 mg ml-1h-1 的较慢速度持续释放。皮下注射后的体内分析表明,与接受游离 GA 的小鼠相比,接受凝胶制剂治疗的小鼠在最初几天的 IL-5、IL-13 和尿酸(UA)水平较低。然而,10 天后,检测到的浓度明显升高,并继续缓慢增加:可以得出结论:所设计的热敏性溶胶-凝胶配方能够延长 GA 的疗效,可被视为治疗多发性硬化症的一种前景广阔的缓释配方。
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来源期刊
DARU Journal of Pharmaceutical Sciences
DARU Journal of Pharmaceutical Sciences PHARMACOLOGY & PHARMACY-
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期刊介绍: DARU Journal of Pharmaceutical Sciences is a peer-reviewed journal published on behalf of Tehran University of Medical Sciences. The journal encompasses all fields of the pharmaceutical sciences and presents timely research on all areas of drug conception, design, manufacture, classification and assessment. The term DARU is derived from the Persian name meaning drug or medicine. This journal is a unique platform to improve the knowledge of researchers and scientists by publishing novel articles including basic and clinical investigations from members of the global scientific community in the forms of original articles, systematic or narrative reviews, meta-analyses, letters, and short communications.
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