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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.


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Effect of magnetic stirring time on size and encapsulation efficiency (n = 3).
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Fig3: Effect of magnetic stirring time on size and encapsulation efficiency (n = 3).

Mentions: Qu-PMs were prepared through magnetic stirring for particle size reduction. Figure 3 shows the decrease in particle size upon increasing the stirring time up to 2 h. Magnetic stirring of 2 h brought about the smaller particle size (59.32 ± 1.01 nm) and larger encapsulation efficiency (95.12% ± 3.54%) compared with shorter stirring time. So, magnetic stirring of 2 h was selected for further research.Figure 3


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)

Effect of magnetic stirring time on size and encapsulation efficiency (n = 3).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Fig3: Effect of magnetic stirring time on size and encapsulation efficiency (n = 3).
Mentions: Qu-PMs were prepared through magnetic stirring for particle size reduction. Figure 3 shows the decrease in particle size upon increasing the stirring time up to 2 h. Magnetic stirring of 2 h brought about the smaller particle size (59.32 ± 1.01 nm) and larger encapsulation efficiency (95.12% ± 3.54%) compared with shorter stirring time. So, magnetic stirring of 2 h was selected for further research.Figure 3

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