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. 2014 Dec;9(1):2406.
doi: 10.1186/1556-276X-9-684. Epub 2014 Dec 18.

Enhancing oral bioavailability of quercetin using novel soluplus polymeric micelles

Linghui Dian  1 , Enjiang Yu, Xiaona Chen, Xinguo Wen, Zhengzan Zhang, Lingzhen Qin, Qingqing Wang, Ge Li, Chuanbin Wu
Affiliations

Enhancing oral bioavailability of quercetin using novel soluplus polymeric micelles

Linghui Dian et al. Nanoscale Res Lett. 2014 Dec.

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.

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Figures

Figure 1
Figure 1
The structure of quercetin (A), soluplus (B) and formation of PMs (C).
Figure 2
Figure 2
Effects of stabilizer F 127 concentration on size and EE of Qu-PMs ( n = 3).
Figure 3
Figure 3
Effect of magnetic stirring time on size and encapsulation efficiency ( n = 3).
Figure 4
Figure 4
Size (A), zeta potential (B), TEM (C), and colloidal solution (D) of Qu-PMs.
Figure 5
Figure 5
XRD of Qu (a), physical mixture (b), Qu-PMs (c), and void PMs (d).
Figure 6
Figure 6
FTIR of Qu (a), physical mixture (b), void PMs (c), and Qu-PMs (d).
Figure 7
Figure 7
Release of quercetin from propylene glycol solution and Qu-PMs suspension.
Figure 8
Figure 8
Mean quercetin plasma concentration.
See this image and copyright information in PMC

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