Alshehri Sultan M, Shakeel Faiyaz, Ibrahim Mohamed A, Elzayat Ehab M, Altamimi Mohammad, Mohsin Kazi, Almeanazel Osaid T, Alkholief Musaed, Alshetaili Abdullah, Alsulays Bader, Alanazi Fars K, Alsarra Ibrahim A
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, Prince Sattam bin Abdulaziz University, Al-Kharj, Saudi Arabia.
Saudi Pharm J. 2019 Feb;27(2):264-273. doi: 10.1016/j.jsps.2018.11.008. Epub 2018 Nov 14.
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.
芹菜素（APG）是一种难溶性生物活性化合物/营养保健品，口服时生物利用度较差。因此，本研究工作的目的是采用不同技术开发APG固体分散体（SDs），期望提高其口服给药后的体外溶出速率和体内生物利用度。以泊洛沙姆-F127（PL）为载体，通过微波、熔融和捏合技术制备了不同的APG固体分散体。使用“热重分析（TGA）、差示扫描量热法（DSC）、傅里叶变换红外（FTIR）光谱仪、粉末X射线衍射（PXRD）和扫描电子显微镜（SEM）”对制备的固体分散体进行表征。表征后，对制备的APG固体分散体进行体外药物释放/溶出曲线研究和体内药代动力学研究。TGA、DSC、FTIR、PXRD和SEM的结果表明成功形成了APG固体分散体。体外溶出实验表明，与对照组（32.74%）相比，所有固体分散体中APG的释放量均显著增加（67.39 - 84.13%）。对每种技术制备的APG优化固体分散体进行大鼠体内药代动力学研究。结果表明，与纯药物和市售胶囊相比，采用微波和熔融技术制备的固体分散体中APG的口服吸收有显著改善。与市售胶囊（100.00%）相比，微波固体分散体中APG的口服生物利用度提高了（从100.00%提高到319.19%），提高了3.19倍。APG从固体分散体中的溶出速率和口服吸收显著提高，表明所开发的固体分散体系统可成功用于APG的口服给药系统。
