In:
Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 71, No. 5 ( 2019-04-12), p. 765-773
Abstract:
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.
Type of Medium:
Online Resource
ISSN:
2042-7158
,
0022-3573
Language:
English
Publisher:
Oxford University Press (OUP)
Publication Date:
2019
detail.hit.zdb_id:
2041988-0
detail.hit.zdb_id:
2050532-2
SSG:
15,3
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