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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

Release of quercetin from propylene glycol solution and Qu-PMs suspension.
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Fig7: Release of quercetin from propylene glycol solution and Qu-PMs suspension.

Mentions: As quercetin is insoluble in water, it simulated gastric fluid and intestinal fluid at room temperature (7.7, 5.4, and 28.87 μg · mL-1, respectively) [37]. Ethanol (35% (v/v)) was used as a receptor medium to obtain a sink condition in the dynamic dialysis study [33]. Drug release from quercetin contained propylene glycol solution and Qu-PMs suspension through the dialysis membrane at 37°C was shown in Figure 7. The pure quercetin from the solution showed about 96.13% release for a period of 24 h, during which no more than 26.22% of quercetin was released from Qu-PMs. Qu-PMs suspension exhibited sustained-release property and the accumulated release at 240 h is only 57.78%. The sustained release may be attributed to the diffusion of quercetin entrapped within the core of PMs.Figure 7


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)

Release of quercetin from propylene glycol solution and Qu-PMs suspension.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Fig7: Release of quercetin from propylene glycol solution and Qu-PMs suspension.
Mentions: As quercetin is insoluble in water, it simulated gastric fluid and intestinal fluid at room temperature (7.7, 5.4, and 28.87 μg · mL-1, respectively) [37]. Ethanol (35% (v/v)) was used as a receptor medium to obtain a sink condition in the dynamic dialysis study [33]. Drug release from quercetin contained propylene glycol solution and Qu-PMs suspension through the dialysis membrane at 37°C was shown in Figure 7. The pure quercetin from the solution showed about 96.13% release for a period of 24 h, during which no more than 26.22% of quercetin was released from Qu-PMs. Qu-PMs suspension exhibited sustained-release property and the accumulated release at 240 h is only 57.78%. The sustained release may be attributed to the diffusion of quercetin entrapped within the core of PMs.Figure 7

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