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氯沙坦钾黏液纳米颗粒:表征与药效学评价

mucilage nanoparticles of losartan potassium: Characterization and pharmacodynamics evaluation.

作者信息

Ghumman Shazia Akram, Mahmood Arshad, Noreen Sobia, Hameed Huma, Kausar Rizwana, Rana Maria, Aslam Asma

机构信息

College of Pharmacy, University of Sargodha, Sargodha 40100, Pakistan.

College of Pharmacy, Al Ain University, Abu Dhabi Campus, Abu Dhabi, UAE.

出版信息

Saudi Pharm J. 2023 Aug;31(8):101695. doi: 10.1016/j.jsps.2023.101695. Epub 2023 Jul 6.

Abstract

The current research was to develop nanoparticles based on mucilage (MPM) that could encapsulate losartan potassium (LP). Nanoparticles (NPs) produced through ionic-gelation method; the polymerization of the mucilage carried out using calcium chloride as cross-linking agent. The MPMLP-NPs demonstrated vastly enhanced pharmaceutical characteristics, presented discrete surface with spherical shape of 198.4-264.6 nm with PDI ranging 0.326-0.461 and entrapment efficiency was in the range of 80.65 ± 0.82-90.79 ± 0.96%. FTIR and DSC indicated the stability of drug during the formulation of nanoparticles. An acute oral toxicity investigation found no significant alterations in behavior and histopathology criteria. The MPMLP-NPs formulation revealed the better rates and sustained effect as assessed with the commercial product. Moreover, low dose of MPMLP-NPs showed similar anti-hypertensive effect as assessed with the marketed tablet.

摘要

当前的研究旨在开发基于黏液(MPM)的纳米颗粒,其能够包封氯沙坦钾(LP)。通过离子凝胶法制备纳米颗粒;使用氯化钙作为交联剂进行黏液的聚合。MPMLP-NPs表现出大大增强的药学特性,呈现离散的表面,球形形状,粒径为198.4 - 264.6 nm,多分散指数(PDI)范围为0.326 - 0.461,包封率在80.65±0.82 - 90.79±0.96%范围内。傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)表明在纳米颗粒制剂过程中药物的稳定性。急性经口毒性研究发现行为和组织病理学标准没有显著改变。与市售产品相比,MPMLP-NPs制剂显示出更好的速率和持续效果。此外,低剂量的MPMLP-NPs与市售片剂相比显示出相似的抗高血压作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/256a/10372173/9a113a9b820c/gr1.jpg

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