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用于高脂血症治疗的普伐他汀载药纳米凝胶的制剂开发与评价

Formulation Development and Evaluation of Pravastatin-Loaded Nanogel for Hyperlipidemia Management.

作者信息

Saraogi Gaurav Kant, Tholiya Siddharth, Mishra Yachana, Mishra Vijay, Albutti Aqel, Nayak Pallavi, Tambuwala Murtaza M

机构信息

Sri Aurobindo Institute of Pharmacy, Indore 453111, Madhya Pradesh, India.

SVKM's NMIMS School of Pharmacy & Technology Management, Shirpur 425405, Maharashtra, India.

出版信息

Gels. 2022 Jan 28;8(2):81. doi: 10.3390/gels8020081.

DOI:10.3390/gels8020081
PMID:35200462
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8871575/
Abstract

Hyperlipidemia is a crucial risk factor for the initiation and progression of atherosclerosis, ultimately leading to cardiovascular disease. The nanogel-based nanoplatform has emerged as an extremely promising drug delivery technology. Pravastatin Sodium (PS) is a cholesterol-lowering drug used to treat hyperlipidemia. This study aimed to fabricate Pravastatin-loaded nanogel for evaluation of its effect in hyperlipidemia treatment. Pravastatin-loaded chitosan nanoparticles (PS-CS-NPs) were prepared by the ionic gelation method; then, these prepared NPs were converted to nanogel by adding a specified amount of 5% poloxamer solution. Various parameters, including drug entrapment efficacy, in vitro drug release, and hemolytic activity of the developed and optimized formulation, were evaluated. The in vitro drug release of the nanogel formulation revealed the sustained release (59.63% in 24 h) of the drug. The drug excipients compatibility studies revealed no interaction between the drug and the screened excipients. Higher drug entrapment efficacy was observed. The hemolytic activity showed lesser toxicity in nanoformulation than the pure drug solution. These findings support the prospective use of orally administered pravastatin-loaded nanogel as an effective and safe nano delivery system in hyperlipidemia treatment.

摘要

高脂血症是动脉粥样硬化发生和发展的关键危险因素,最终可导致心血管疾病。基于纳米凝胶的纳米平台已成为一种极具前景的药物递送技术。普伐他汀钠(PS)是一种用于治疗高脂血症的降胆固醇药物。本研究旨在制备载普伐他汀的纳米凝胶,以评估其在高脂血症治疗中的效果。采用离子凝胶法制备了载普伐他汀的壳聚糖纳米粒(PS-CS-NPs);然后,通过加入特定量的5%泊洛沙姆溶液将这些制备的纳米粒转化为纳米凝胶。对所开发和优化制剂的各种参数进行了评估,包括药物包封率、体外药物释放和溶血活性。纳米凝胶制剂的体外药物释放显示药物具有缓释特性(24小时内释放59.63%)。药物辅料相容性研究表明药物与筛选出的辅料之间无相互作用。观察到较高的药物包封率。溶血活性表明纳米制剂的毒性低于纯药物溶液。这些研究结果支持口服载普伐他汀纳米凝胶作为高脂血症治疗中一种有效且安全的纳米递送系统的潜在应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/908d2cba0413/gels-08-00081-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/48bacb1bb02a/gels-08-00081-g001a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/131d565eb6cd/gels-08-00081-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/f35ece8ef8f4/gels-08-00081-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/b3ae05e8ab7c/gels-08-00081-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/15b657e67a9c/gels-08-00081-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/908d2cba0413/gels-08-00081-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/48bacb1bb02a/gels-08-00081-g001a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/131d565eb6cd/gels-08-00081-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/f35ece8ef8f4/gels-08-00081-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/b3ae05e8ab7c/gels-08-00081-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/15b657e67a9c/gels-08-00081-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b51/8871575/908d2cba0413/gels-08-00081-g006.jpg

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