Adoption of polymeric micelles to enhance the oral bioavailability of dexibuprofen: formulation, in-vitro evaluation and in-vivo pharmacokinetic study in healthy human volunteers

被引:32
作者
Abdelbary, Ghada [1 ]
Makhlouf, Amal [1 ]
机构
[1] Cairo Univ, Dept Pharmaceut & Ind Pharm, Fac Pharm, Cairo 11562, Egypt
关键词
Dexibuprofen; healthy human volunteers; pharmacokinetic study; pluronics; polymeric micelles; DRUG; NANOPARTICLES; STABILIZATION; DESIGN; OPTIMIZATION; SOLUBILITY; COMPLEXES; IBUPROFEN; EMULSION; STORAGE;
D O I
10.3109/10837450.2013.823994
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
This work aimed to incorporate Dexibuprofen (DXI), the pharmacologically active and more potent form of ibuprofen, into polymeric micelles based tablets with enhanced oral bioavailability. Thin film hydration technique was employed to prepare DXI polymeric micelles using Pluronic (R) F127 and/or P123 solutions in different ratios (ranging from 1: 1 up to 1: 10). Prepared micelles were characterized regarding particle size, drug loading and entrapment efficiency. Selected formulae were lyophilized in presence of cryoprotectants and subjected to solid-state characterization as well as scanning and transmission electron microscopy. Subsequently, tablets were prepared and evaluated in-vitro regarding physical properties and drug release. An in-vivo pharmacokinetic study was performed in six healthy human volunteers in comparison to the commercially available tablet of DXI. Solid-state characterization proved that DXI was homogenously dispersed in Pluronic micelles' matrices. Formula TF5 tablets comprising lyophilized micelles (F5; DXI: Pluronic F127 in 1: 1 ratio and 0.25% mannitol) showed higher C-max and earlier t(max) values than those of the commercial formula, where the relative bioavailability was calculated to be 160.15%. The experimental evidence in this research leads to the conclusion that polymeric micelles present enabling properties for oral delivery of drugs with low solubility.
引用
收藏
页码:717 / 727
页数:11
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