Enhancing the oral bioavailability of baicalein via Solutol® HS15 and Poloxamer 188 mixed micelles system

• Published in: Journal of pharmacy and pharmacology 2019-05, Vol.71 (5), p.765-773
• Main Authors: Shen, Hongxue, Liu, Yi, Zhang, Huanhuan, Ding, Pinggang, Zhang, Lan, Zhang, Liefeng, Ju, Jianming
• Format: Article
• Language: English
• Subjects: baicalein; Bioavailability; Controlled release; Drug delivery; Entrapment; Micelles; oral bioavailability; Permeability; Pharmacokinetics; Poloxamer 188; Solubility; Solutol HS15; Sustained release
• ISSN: 0022-3573; 2042-7158
• DOI: 10.1111/jphp.13058

Objectives 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. Methods 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. Key findings 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. Conclusions 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.