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速尿在长循环壳聚糖共轭聚乳酸-羟基乙酸共聚物纳米粒中的缓释增强

Enhanced sustained release of furosemide in long circulating chitosan-conjugated PLGA nanoparticles.

作者信息

Kashyap Sapna, Singh Amit, Mishra Abha, Singh Vikas

机构信息

Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi -221005, India.

School of Biochemical Engineering, Indian Institute of Technology, Banaras Hindu University, Varanasi -221005, India.

出版信息

Res Pharm Sci. 2019 Mar 8;14(2):93-106. doi: 10.4103/1735-5362.253356. eCollection 2019 Apr.

Abstract

Furosemide (FSM) is commonly used in the treatment of edema associated with congestive cardiac failure, cirrhosis of the liver, renal disease, including the nephrotic syndrome and hypertension. However, in ascites, it is clinically limited due to its frequent dosing and short biological half-life and its prolonged-release preparations are not available. Therefore, the main objective behind the present research work is to develop chitosan coated and conjugated poly (lactic-co-glycolic acid) (PLGA) nanocarriers, to sustain the delivery of FSM with improved systemic circulation. Emulsion-solvent evaporation technique was used for the preparation of nanoparticles. pharmacokinetic study showed 2.6, 3.10, and 4.30 folds enhancement in relative availability of FSM for FSM-PLGA, FSM-chitosan-coated-PLGA and FSM-chitosan-conjugated- PLGA nanoparticles, respectively than FSM. The present research work concluded that FSM loaded chitosan conjugated PLGA nanoparticles could enhance the systemic circulation of FSM with improved pharmacokinetics parameters.

摘要

呋塞米(FSM)常用于治疗与充血性心力衰竭、肝硬化、肾脏疾病(包括肾病综合征)和高血压相关的水肿。然而,在腹水治疗中,由于其给药频繁、生物半衰期短且没有缓释制剂,其临床应用受到限制。因此,本研究工作的主要目的是开发壳聚糖包衣和共轭聚乳酸-羟基乙酸共聚物(PLGA)纳米载体,以维持呋塞米的递送并改善其在体循环中的情况。采用乳液溶剂蒸发技术制备纳米颗粒。药代动力学研究表明,与呋塞米相比,FSM-PLGA、壳聚糖包衣FSM-PLGA和壳聚糖共轭FSM-PLGA纳米颗粒中呋塞米的相对生物利用度分别提高了2.6倍、3.10倍和4.30倍。本研究工作得出结论,负载呋塞米的壳聚糖共轭PLGA纳米颗粒可以改善呋塞米的药代动力学参数,增强其在体循环中的效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b4b6/6791168/aff2392b9a18/RPS-14-93-g001.jpg

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