Enhancing oral bioavailability of quercetin using novel soluplus polymeric micelles View Full Text


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Article Info

DATE

2014-12

AUTHORS

Linghui Dian, Enjiang Yu, Xiaona Chen, Xinguo Wen, Zhengzan Zhang, Lingzhen Qin, Qingqing Wang, Ge Li, Chuanbin Wu

ABSTRACT

To improve its poor aqueous solubility and stability, the potential chemotherapeutic drug quercetin was encapsulated in soluplus polymeric micelles by a modified film dispersion method. With the encapsulation efficiency over 90%, the quercetin-loaded polymeric micelles (Qu-PMs) with drug loading of 6.7% had a narrow size distribution around mean size of 79.00 ± 2.24 nm, suggesting the complete dispersibility of quercetin in water. X-ray diffraction (XRD) patterns illustrated that quercetin was in amorphous or molecular form within PMs. Fourier transform infrared spectroscopy (FTIR) indicated that quercetin formed intermolecular hydrogen bonding with carriers. An in vitro dialysis test showed the Qu-PMs possessed significant sustained-release property, and the formulation was stable for at least 6 months under accelerated conditions. The pharmacokinetic study in beagle dogs showed that absorption of quercetin after oral administration of Qu-PMs was improved significantly, with a half-life 2.19-fold longer and a relative oral bioavailability of 286% as compared to free quercetin. Therefore, these novel soluplus polymeric micelles can be applied to encapsulate various poorly water-soluble drugs towards a development of more applicable therapeutic formulations. More... »

PAGES

684

References to SciGraph publications

Identifiers

URI

http://scigraph.springernature.com/pub.10.1186/1556-276x-9-684

DOI

http://dx.doi.org/10.1186/1556-276x-9-684

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1017037099

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/26088982


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