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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: 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.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

Mean quercetin plasma concentration.
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Fig8: Mean quercetin plasma concentration.

Mentions: It has been reported that quercetin is found in plasma as conjugates of glucuronic acid and sulfate groups [40]. Quercetin is released from the binding complex by acid hydrolysis method, and total content of quercetin in plasma was determined by HPLC [41]. Calibration samples were obtained by joining proper volumes of denominator Qu solution in methanol into blank plasma, gaining a calibration curve over the detected level range of 0.10 to 8.00 μg · mL-1 (R2 > 0.99). The results of the method validation ascertained by assessing the precision, accuracy, recovery, and limit of quantification and proved that the method was reliable. The bioavailability of Qu-PMs was looked into by investigating beagle dogs and comparing with that of pure Qu. After oral administration of a single dose equivalent to 16 mg · kg-1 of pure Qu or Qu-PMs, the mean quercetin concentrations in dog serum at different time intervals are plotted in Figure 8 and the calculated key pharmacokinetic parameters are summarized in Table 4. The plasma level of quercetin was detected only up to 24 h after administration of free drug, with the Cmax of 5.24 μg · mL-1. The drugs released from PMs were still detected in plasma 48 h after oral administration, with the Cmax of 7.56 μg · mL-1. As shown in Figure 8, after oral administration, Qu-PMs were absorbed much slower than pure quercetin with Tmax of 7.02 ± 2.02 h and 5.31 ± 1.08 h (p < 0.05), respectively.Figure 8


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)

Mean quercetin plasma concentration.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Fig8: Mean quercetin plasma concentration.
Mentions: It has been reported that quercetin is found in plasma as conjugates of glucuronic acid and sulfate groups [40]. Quercetin is released from the binding complex by acid hydrolysis method, and total content of quercetin in plasma was determined by HPLC [41]. Calibration samples were obtained by joining proper volumes of denominator Qu solution in methanol into blank plasma, gaining a calibration curve over the detected level range of 0.10 to 8.00 μg · mL-1 (R2 > 0.99). The results of the method validation ascertained by assessing the precision, accuracy, recovery, and limit of quantification and proved that the method was reliable. The bioavailability of Qu-PMs was looked into by investigating beagle dogs and comparing with that of pure Qu. After oral administration of a single dose equivalent to 16 mg · kg-1 of pure Qu or Qu-PMs, the mean quercetin concentrations in dog serum at different time intervals are plotted in Figure 8 and the calculated key pharmacokinetic parameters are summarized in Table 4. The plasma level of quercetin was detected only up to 24 h after administration of free drug, with the Cmax of 5.24 μg · mL-1. The drugs released from PMs were still detected in plasma 48 h after oral administration, with the Cmax of 7.56 μg · mL-1. As shown in Figure 8, after oral administration, Qu-PMs were absorbed much slower than pure quercetin with Tmax of 7.02 ± 2.02 h and 5.31 ± 1.08 h (p < 0.05), respectively.Figure 8

Bottom Line: 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.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