Pharmacokinetic study of furosemide incorporated PLGA microspheres after oral administration to rat

Publish Year: 1395
نوع سند: مقاله ژورنالی
زبان: English
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شناسه ملی سند علمی:

JR_IJBMS-19-10_003

تاریخ نمایه سازی: 30 مهر 1400

Abstract:

Objective(s): The purpose of the current study was to assess the feasibility of microspheres from biocompatible polymer for oral bioavailability (BA) enhancement of potent sulfonamide- type loop diuretic- Furosemide - which used in the treatment of congestive heart failure, caused edema, cirrhosis, renal disease and as an adjunct in acute pulmonary edema. The comparatively poor and inconstant BA of furosemide, which occurs site-specifically in the stomach and upper small intestine, has been ascribed to the poor dissolution of furosemide. Materials and Methods: In attempt to enhance the drug BA, poly (dl-lactic-co-glycolic acid) (PLGA) microspheres of furosemide were obtained using solvent-evaporation method and the carrier characteristics were investigated subsequently. Results: The in vivo performance of optimum formulation was assessed by pharmacokinetic evaluation of drug after orally administration of free and loaded in microspheres to rats (۴ mg/Kg). For this reason, the concentration of drug in plasma was measured by a new developed and sensitive method of HPLC. Acceptable drug loading and encapsulation efficiency of microspheres were obtained to be ۷۰.۴۳ and ۸۵.۲۱ %, respectively. Microspheres provided improved pharmacokinetic parameters (Cmax = ۱۴۷.۹۴ ng/ml, Tmax = ۱.۹۲ hr) in rats as compared with pure drug (Cmax = ۷۵.۶۹ ng/ml, Tmax = ۱.۵ hr). The obtained AUC of drug in microsphere was ۱۰ fold higher than of the free drug. Conclusion: The results showed that the prepared microspheres successfully improved BA of the poorly water-soluble drug effectively.

Authors

Katayoun Derakhshandeh

Nano Drug Delivery Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran

Moin Karimi

Department of Pharmaceutics, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran

Abbas Hemati Azandaryani

Department of Pharmaceutics, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran

Gholamreza Bahrami

Department of Pharmacology and Toxicology, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah

Kiumras Ghanbari

Department of Pharmacology and Toxicology, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah

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