Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

• Main Authors: Sultan M. Alshehri, Faiyaz Shakeel, Mohamed A. Ibrahim, Ehab M. Elzayat, Mohammad Altamimi, Kazi Mohsin, Osaid T. Almeanazel, Musaed Alkholief, Abdullah Alshetaili, Bader Alsulays, Fars K. Alanazi, Ibrahim A. Alsarra
• Format: Article
• Language: English
• Published: Elsevier 2019-02-01
• Series: Saudi Pharmaceutical Journal
• Online Access: http://www.sciencedirect.com/science/article/pii/S131901641830272X

Apigenin (APG) is a poorly soluble bioactive compound/nutraceutical which shows poor bioavailability upon oral administration. Hence, the objective of this research work was to develop APG solid dispersions (SDs) using different techniques with the expectation to obtain improvement in its in vitro dissolution rate and in vivo bioavailability upon oral administration. Different SDs of APG were prepared by microwave, melted and kneaded technology using pluronic-F127 (PL) as a carrier. Prepared SDs were characterized using “thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier transform infra-red (FTIR) spectrometer, powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM)”. After characterization, prepared SDs of APG were studied for in vitro drug release/dissolution profile and in vivo pharmacokinetic studies. The results of TGA, DSC, FTIR, PXRD and SEM indicated successful formation of APG SDs. In vitro dissolution experiments suggested significant release of APG from all SDs (67.39–84.13%) in comparison with control (32.74%). Optimized SD of APG from each technology was subjected to in vivo pharmacokinetic study in rats. The results indicated significant improvement in oral absorption of APG from SD prepared using microwave and melted technology in comparison with pure drug and commercial capsule. The enhancement in oral bioavailability of APG from microwave SD (319.19%) was 3.19 fold as compared with marketed capsule (100.00%). Significant enhancement in the dissolution rate and oral absorption of APG from SD suggested that developed SD systems can be successfully used for oral drug delivery system of APG. Keywords: Apigenin, Microwave technology, Pluronic-F127, Solid dispersion, Bioavailability