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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

FTIR of Qu (a), physical mixture (b), void PMs (c), and Qu-PMs (d).
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Fig6: FTIR of Qu (a), physical mixture (b), void PMs (c), and Qu-PMs (d).

Mentions: The molecular interactions within the solid matrix of the PMs were examined by FTIR method. On the basis of their structure, the possible interaction between quercetin and soluplus is hydrogen bonding, which may result in the shifting and peak broadening of the absorption bands at the interacting functional groups on the FTIR. The aromatic -OH group in quercetin might come into a hydrogen bond. FTIR of pure quercetin, void PMs, physical mixture of void PMs and quercetin, and Qu-PMs are presented in Figure 6. Pure quercetin showed a number of characteristic bands representing O-H stretching (3,700 to 3,300 cm-1), C = O absorption (1,670 cm-1), C-C stretching (1,612 cm-1), C-H bending (1,456, 1,383 and 866 cm-1), C-O stretching in the ring structure (1,272 cm-1), and C-O stretching (1,070 to 1,150 cm-1). The existence of these bands is consistent with the report of past studies [36]. Void PMs also show a number of bands, including OH stretch (3,500 to 3,250 cm-1), sp3CH stretching (2,932 cm-1), ester carbonyl stretching (1,742 cm-1), and C = O stretching for tertiary amide (1,641 cm-1). On the spectra of Qu-PMs, the position of carbonyl absorption peaks in Qu-PMs was shifted to 1737.93 cm-1 and 1636.80 cm-1, respectively. However, no similar peak shifting was observed in the physical mixture. These results illustrate that there might be some interactions between quercetin and soluplus in Qu-PMs.Figure 6


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)

FTIR of Qu (a), physical mixture (b), void PMs (c), and Qu-PMs (d).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Fig6: FTIR of Qu (a), physical mixture (b), void PMs (c), and Qu-PMs (d).
Mentions: The molecular interactions within the solid matrix of the PMs were examined by FTIR method. On the basis of their structure, the possible interaction between quercetin and soluplus is hydrogen bonding, which may result in the shifting and peak broadening of the absorption bands at the interacting functional groups on the FTIR. The aromatic -OH group in quercetin might come into a hydrogen bond. FTIR of pure quercetin, void PMs, physical mixture of void PMs and quercetin, and Qu-PMs are presented in Figure 6. Pure quercetin showed a number of characteristic bands representing O-H stretching (3,700 to 3,300 cm-1), C = O absorption (1,670 cm-1), C-C stretching (1,612 cm-1), C-H bending (1,456, 1,383 and 866 cm-1), C-O stretching in the ring structure (1,272 cm-1), and C-O stretching (1,070 to 1,150 cm-1). The existence of these bands is consistent with the report of past studies [36]. Void PMs also show a number of bands, including OH stretch (3,500 to 3,250 cm-1), sp3CH stretching (2,932 cm-1), ester carbonyl stretching (1,742 cm-1), and C = O stretching for tertiary amide (1,641 cm-1). On the spectra of Qu-PMs, the position of carbonyl absorption peaks in Qu-PMs was shifted to 1737.93 cm-1 and 1636.80 cm-1, respectively. However, no similar peak shifting was observed in the physical mixture. These results illustrate that there might be some interactions between quercetin and soluplus in Qu-PMs.Figure 6

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