Formulation and Characterization of Eplerenone Nanoemulsion Liquisolids, An Oral Delivery System with Higher Release Rate and Improved Bioavailability

被引:33
|
作者
Khames, Ahmed [1 ,2 ]
机构
[1] Beni Suef Univ, Dept Pharmaceut & Ind Pharm, Bani Suwayf 62514, Egypt
[2] Taif Univ, Dept Pharmaceut & Ind Pharm, At Taif 21944, Saudi Arabia
关键词
eplerenone; nanoemulsion; liquisolids; Triacetin; bioavailability; DRUG; DISSOLUTION; MICROEMULSION; PERMEABILITY; SOLUBILITY; BLOCKADE; EFFICACY;
D O I
10.3390/pharmaceutics11010040
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Because Eplerenone (EPL) is a Biopharmaceutical Classification System (BCS) class-II drug and is prone to extensive liver degradation, it suffers from poor bioavailability after oral administration. This work aimed to prepare liquisolids loaded with EPL-nanoemulsions (EPL-NEs) that have a higher drug release rate and improved bioavailability by the oral route. Based on solubility studies, mixtures of Triacetin (oil) and Kolliphor EL/PEG 400 surfactant/co-surfactant (S-mix) in different ratios were used to prepare EPL-NE systems, which were characterized and optimized for droplet size, zeta potential, polydispersity index (PDI), and drug content. Systems were then loaded onto liquisolid formulations and fully evaluated. A liquisolid formulation with better drug release and tableting properties was selected and compared to EPL-NEs and conventional EPL oral tablets in solid-state characterization studies and bioavailability studies in rabbits. Only five NEs prepared at 1:3, 1:2, and 3:1 S-mix met the specified optimization criteria. The drug release rate from liquisolids was significantly increased (90% within 45 minutes). EPL-NE also showed significantly improved drug release but with a sustained pattern for four hours. Liquisolid bioavailability reached 2.1 and 1.2 relative to conventional tablets and EPL-NE. This suggests that the EPL-NE liquisolid is a promising oral delivery system with a higher drug release rate, enhanced absorption, decreased liver degradation, and improved bioavailability.
引用
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页数:18
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