Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, China.
Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China.
J Pharm Pharmacol. 2019 May;71(5):765-773. doi: 10.1111/jphp.13058. Epub 2018 Dec 14.
To increase the solubility of baicalein (BAI) by preparing BAI-micelles (BAI-M) with Solutol HS15 (HS15) and Poloxamer 188 (F68), thereby improving its oral bioavailability.
Baicalein micelles were prepared with HS15 and F68 by thin-film dispersion method and optimized by central composite design (CCD) approach. Physicochemical, in vitro release, Caco-2 cell transport and pharmacokinetic studies of BAI-M were performed.
The optimal formulation showed spherical shape by characterization of the transmission electron microscope with average small size (23.14 ± 1.46 nm) and high entrapment efficiency (92.78±0.98%) and drug loading (6.45±1.54%). The in vitro release study of BAI-M showed a significantly sustained release pattern compared with free BAI. Caco-2 cell transport study demonstrated that high permeability of BAI was achieved after loading it into micelles. Meanwhile, pharmacokinetics study of BAI-M showed a 3.02-fold increase in relative oral bioavailability compared with free BAI.
Based on our findings, we concluded that HS15 can be used as a carrier in this drug delivery system that includes F68, and BAI-M has great potential in improving solubility and oral bioavailability.
通过用 Solutol HS15（HS15）和聚氧乙烯醚 188（F68）制备黄芩素（BAI）胶束（BAI-M）来提高 BAI 的溶解度，从而提高其口服生物利用度。
采用薄膜分散法制备黄芩素胶束，并用中心复合设计（CCD）方法进行优化。对 BAI-M 的理化性质、体外释放、Caco-2 细胞转运和药代动力学进行了研究。
通过透射电子显微镜的表征，最佳配方显示出球形形状，平均粒径较小（23.14±1.46nm），包封效率（92.78±0.98%）和载药量（6.45±1.54%）均较高。BAI-M 的体外释放研究表明，与游离 BAI 相比，其具有明显的持续释放模式。Caco-2 细胞转运研究表明，BAI 载入微胶束后，其通透性大大提高。同时，BAI-M 的药代动力学研究表明，与游离 BAI 相比，其相对口服生物利用度提高了 3.02 倍。
根据我们的研究结果，我们得出结论，HS15 可以作为该药物传递系统中 F68 的载体，BAI-M 在提高溶解度和口服生物利用度方面具有很大的潜力。
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