Preparation, characterization and pharmacokinetics of thiolated-chitosan microspheres loading quercetin in rats

XIA Xiaojing; XU Beihua; ZHANG Tingqin; HU Ying

doi:10.11665/j.issn.1000-5048.20140210

Journal of China Pharmaceutical University > 2014 > 45(2): 185-191. > DOI: 10.11665/j.issn.1000-5048.20140210

XIA Xiaojing, XU Beihua, ZHANG Tingqin, HU Ying. Preparation, characterization and pharmacokinetics of thiolated-chitosan microspheres loading quercetin in rats[J]. Journal of China Pharmaceutical University, 2014, 45(2): 185-191. DOI: 10.11665/j.issn.1000-5048.20140210

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Preparation, characterization and pharmacokinetics of thiolated-chitosan microspheres loading quercetin in rats

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Thiolated-chitosan microspheres(Thio-Cs-Ms)loading quercetin(QT)as model drug were prepared. The thiol group content, drug-loading capability, morphology in SEM and in microscope before and after hydration, release in vitro and pharmacokinetics in rats were evaluated. The thiol group content was(147. 0±8. 2)μmol/g, the drug-loading capability was(5. 33±0. 12)%. There were several pores on the surface of microspheres observed in SEM images. The microspheres expanded to be sphericity immediately after hydrating, and their morphology were intact after release in microscope. The behavior of release in vitro were no significant difference in water, simulated gastric fluid and simulated intestinal fluid evaluated by dissolution curve similarity factor. The release of Thio-Cs-Ms was fit for Higuchi equation Q=0. 161t1/2. Thio-Cs-Ms exhibited enhancing muco-adhesive ability in excised stomach and intestinal experiments. The bioavailability of Thio-Cs-Ms was obviously higher than that of suspension and Cs-Ms loading quercetin after oral administration in rats. Thio-Cs-Ms loading quercetin might to be one of the most promising preparations of quercetin.
- quercetin,
- thiol,
- chitosan microspheres,
- pharmacokinetics

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[1]	Bischoff SC.Quercetin:potentials in the prevention and therapy of disease[J].Micronutrients,2008,11(6):733-740.
[2]	Bernkop-Schnürch A,Hornof M,Guggi D.Thiolated chitosans[J].Eur J Pharm Biopharm,2004,57(1):9-17.
[3]	Makhlof A,Werle M,Tozuka Y,et al.Nanoparticles of glycol chitosan and its thiolated derivative significantly improved the pulmonary delivery of calcitonin[J].Int J Pharm,2010,397(1/2):92-95.
[4]	Iqbal J,Shahnaz G,Perera G,et al.Thiolated chitosan:development and in vivo evaluation of an oral delivery system for leuprolide[J].Eur J Pharm Biopharm,2012,80(1):95-102.
[5]	Dubey RR,Parikh RH Two-stage optimization process for formulation of chitosan microspheres[J].AAPS PharmSciTech,2004,5(1):E5.
[6]	Sakloetsakun D,Hombach JM,Bernkop-Schnürch A.In situ gelling properties of chitosan-thioglycolic acid conjugate in the presence of oxidizing agents[J].Biomaterials,2009,30(31):6 151-6 157.
[7]	Rahmat D,Sakloetsakun D,Shahnaz G,et al.Design and synthesis of a novel cationic thiolated polymer[J].Int J Pharm,2011,411(1/2):10-17.
[8]	Akiyama YN,Nagahara T,Kashihara S,et al.In vitro and in vivo evaluation of mucoadhesive microspheres prepared for the gastrointestinal tract using polyglycerol esters of fatty acids and a poly(acrylic acid)derivative[J].Pharm Res,1995,12(3):397-405.
[9]	Hollman PC,van Trijp JM,Buysman MN,et al.Relative bioavailability of the antioxidant flavonoid quercetin from various foods in man[J].FEBS Lett,1997,418(1/2):152-156.

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Preparation, characterization and pharmacokinetics of thiolated-chitosan microspheres loading quercetin in rats

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