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Enhancing oral bioavailability of quercetin using novel soluplus polymeric micelles.

Dian L, Yu E, Chen X, Wen X, Zhang Z, Qin L, Wang Q, Li G, Wu C - Nanoscale Res Lett (2014)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, Guangdong Medical College, Xincheng Road 1, Dongguan, 523808, Guangdong, People's Republic of China, 605911308@qq.com.

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.

No MeSH data available.


Related in: MedlinePlus

The structure of quercetin (A), soluplus (B) and formation of PMs (C).
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Fig1: The structure of quercetin (A), soluplus (B) and formation of PMs (C).

Mentions: Quercetin (3, 3′, 4′, 5, 7-pentahydroxy flavones, Figure 1A) is a flavonoid compound widely present in flower, leaf, and fruit of plants such as Sophora japonica L., Dendranthema morifolium (Ramat.) Tzvel, and Crataegus pinnatifida bunge, with a variety of biological activity and high medical value [12]. Literature indicates that quercetin can inhibit the growth and proliferation of a variety of cancer cell lines (human ovarian cancer, breast cancer, lung cancer, human colon cancer, etc.) [13–16]. Quercetin can also lower the multidrug-resistance in cancer cells [17, 18] and enhance the antitumor effects of drugs [19, 20].Figure 1


Enhancing oral bioavailability of quercetin using novel soluplus polymeric micelles.

Dian L, Yu E, Chen X, Wen X, Zhang Z, Qin L, Wang Q, Li G, Wu C - Nanoscale Res Lett (2014)

The structure of quercetin (A), soluplus (B) and formation of PMs (C).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4493852&req=5

Fig1: The structure of quercetin (A), soluplus (B) and formation of PMs (C).
Mentions: Quercetin (3, 3′, 4′, 5, 7-pentahydroxy flavones, Figure 1A) is a flavonoid compound widely present in flower, leaf, and fruit of plants such as Sophora japonica L., Dendranthema morifolium (Ramat.) Tzvel, and Crataegus pinnatifida bunge, with a variety of biological activity and high medical value [12]. Literature indicates that quercetin can inhibit the growth and proliferation of a variety of cancer cell lines (human ovarian cancer, breast cancer, lung cancer, human colon cancer, etc.) [13–16]. Quercetin can also lower the multidrug-resistance in cancer cells [17, 18] and enhance the antitumor effects of drugs [19, 20].Figure 1

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, Guangdong Medical College, Xincheng Road 1, Dongguan, 523808, Guangdong, People's Republic of China, 605911308@qq.com.

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.

No MeSH data available.


Related in: MedlinePlus