Home Preparation and Characterization of Genipin-Crosslinked Chitosan Microspheres for the Sustained Release of Salidroside
Article
Licensed
Unlicensed Requires Authentication

Preparation and Characterization of Genipin-Crosslinked Chitosan Microspheres for the Sustained Release of Salidroside

  • Mei Luo , Hailong Peng , Zhonghua Deng , Zhonghua Yin , Qiang Zhao and Hua Xiong EMAIL logo
Published/Copyright: May 14, 2015

Abstract

Chitosan microspheres (CsMs) that encapsulate salidroside (Sal) were prepared by the emulsion crosslinking method with naturally occurring genipin (Gp) and then examined for their in vitro release. Sal-loaded CsMs (Sal-CsMs) showed nearly spherical and smooth surfaces with internal voids. The particle size of Sal-CsMs ranged within 0.56–5.01 μm, and their encapsulation efficiency and loading capacity were beyond 77.58% and 23.29%, respectively. The stability of Sal improved after entrapment into the CsMs. The release rate of Sal from CsMs was initially rapid, followed by sustained release. The release behavior depended on the pH of the release medium. The main release mechanisms underlying the release procedure were anomalous behavior and Fickian diffusion. These results indicated that CsMs with a novel crosslinker of Gp was a potential carrier system for producing functional foods containing Sal.

Funding statement: Funding: This work was supported by the Planning Subject of “the Twelfth Five–Year–Plan” National Science and Technology for the Rural development of China (No. 2013AA102203–05), the National Natural Science Foundation of China (No. 21266020), the Natural Science Foundation of Jiangxi Province (20142BAB213003), and Jiangxi Department of Education Fund (GJJ13039).

References

1. MaoG, DengH, YuanL, LiD, WangZ. Protective role of salidroside against aging in a mouse model induced by D-galactose. Biomed Environ Sci2010;23:1616.10.1016/S0895-3988(10)60047-5Search in Google Scholar

2. MaL, CaiD, LiH, TongB, SongL, WangY. Anti-fatigue effects of salidroside in mice. J Med C PLA2008;23:8893.10.1016/S1000-1948(08)60028-3Search in Google Scholar

3. WangH, DingY, ZhouJ, SunX, WangS. The in vitro and in vivo antiviral effects of salidroside from Rhodiola rosea L. Against coxsackievirus B3. Phytomedicine2009;16:14655.10.1016/j.phymed.2008.07.013Search in Google Scholar PubMed

4. LiQY, WangHM, WangZQ, MaJF, DingJQ, ChenSD. Salidroside attenuates hypoxia-induced abnormal processing of amyloid precursor protein by decreasing BACE1 expression in SH-SY5Y cells. Neurosci Lett2010;481:1548.10.1016/j.neulet.2010.06.076Search in Google Scholar PubMed

5. SunC, WangZ, ZhengQ, ZhangH. Salidroside inhibits migration and invasion of human fibrosarcoma HT1080 cells. Phytomedicine2012;19:35563.10.1016/j.phymed.2011.09.070Search in Google Scholar PubMed

6. ZhangJ, LiuA, HouR, ZhangJ, JiaX, JiangW, et al. Salidroside protects cardiomyocyte against hypoxia-induced death: a HIF-1α-activated and VEGF-mediated pathway. Eur J Pharmacol2009;607:614.10.1016/j.ejphar.2009.01.046Search in Google Scholar PubMed

7. GuptaV, LahiriSS, SultanaS, TulsawaniRK, KumarR. Anti-oxidative effect of Rhodiola imbricata root extract in rats during cold, hypoxia and restraint (C-H-R) exposure and post-stress recovery. Food Chem Toxicol2010;48:101925.10.1016/j.fct.2010.01.012Search in Google Scholar PubMed

8. YuS, LiuL, WenT, LiuY, WangD, HeY, et al. Development and validation of a liquid chromatographic/electrospray ionization mass spectrometric method for the determination of salidroside in rat plasma: application to the pharmacokinetics study. J Chromatogr B2008;861:1015.10.1016/j.jchromb.2007.11.035Search in Google Scholar PubMed

9. WeiQ, GeT, KongS. Salidroside promotes erythropoiesis and protects erythroblasts against oxidative stress by up-regulating glutathione peroxidase and thioredoxin. J Ethnopharmacol2011;133:30814.10.1016/j.jep.2010.09.025Search in Google Scholar PubMed

10. FanM, XuS, XiaS, ZhangX. Effect of different preparation methods on physicochemical properties of salidroside liposomes. J Agr Food Chem2007;55:308995.10.1021/jf062935qSearch in Google Scholar PubMed

11. PengH, LiW, NingF, YaoL, LuoM, ZhuX, et al. Amphiphilic chitosan derivatives-based liposomes: synthesis, development, and properties as a carrier for sustained release of salidroside. J Agr Food Chem2014;62:62633.10.1021/jf4039925Search in Google Scholar

12. PengH, DongR, WangS, ZhangZ, LuoM, BaiC, et al. A pH-responsive nano-carrier with mesoporous silica nanoparticles cores and poly(acrylic acid) shell-layers: fabrication, characterization and properties for controlled release of salidroside. Int J Pharm2013;446:1539.10.1016/j.ijpharm.2013.01.071Search in Google Scholar

13. Tuan HiepT, RamasamyT, PoudelBK, MarasiniN, Bo KyungM, Hyuk JunC, et al. Preparation and characterization of spray-dried gelatin microspheres encapsulating ganciclovir. Macromol Res2014;22:12430.10.1007/s13233-014-2018-9Search in Google Scholar

14. JinYC, KimIY, KimID, LeeHK, ParkJY, HanPL, et al. Biodegradable gelatin microspheres enhance the neuroprotective potency of osteopontin via quick and sustained release in the post-ischemic brain. Acta Biomater2014;10:312635.10.1016/j.actbio.2014.02.045Search in Google Scholar

15. LanY, LiWC, GuoR, ZhangY, XueW, ZhangYM. Preparation and characterisation of vancomycin-impregnated gelatin microspheres/silk fibroin scaffold. J Biomater Sci-Polym Ed2014;25:7587.10.1080/09205063.2013.836951Search in Google Scholar

16. RishiS, ZeinMC. The industrial protein from corn. Ind Crop Prod2001;13:17192.10.1016/S0926-6690(00)00064-9Search in Google Scholar

17. LiuX, SunQ, WangH, ZhangL, WangJY. Microspheres of corn protein, zein, for an ivermectin drug delivery system. Biomaterials2005;26:10915.10.1016/j.biomaterials.2004.02.013Search in Google Scholar

18. JameelaSR, KumaryTV, LalAV, JayakrishnanA. Progesterone-loaded chitosan microspheres: a long acting biodegradable controlled delivery system. J Control Release1998;52:1724.10.1016/S0168-3659(97)00187-9Search in Google Scholar

19. KawadkarJ, ChauhanMK. Intra-articular delivery of genipin cross-linked chitosan microspheres of flurbiprofen: preparation, characterization, in vitro and in vivo studies. Eur J Pharm Biopharm2012;81:56372.10.1016/j.ejpb.2012.04.018Search in Google Scholar PubMed

20. AgnihotriSA, AminabhaviTM. Novel interpenetrating network chitosan-poly(ethylene oxide-g-acrylamide) hydrogel microspheres for the controlled release of capecitabine. Int J Pharm2006;324:10315.10.1016/j.ijpharm.2006.05.061Search in Google Scholar PubMed

21. CasettariL, VllasaliuD, LamJKW, SolimanM, IllumL. Biomedical applications of amino acid-modified chitosans: a review. Biomaterials2012;33:756583.10.1016/j.biomaterials.2012.06.104Search in Google Scholar

22. Belscak-CvitanovicA, StojanovicR, ManojlovicV, KomesD, CindricIJ, NedovicV, et al. Encapsulation of polyphenolic antioxidants from medicinal plant extracts in alginate-chitosan system enhanced with ascorbic acid by electrostatic extrusion. Food Res Int2011;44:1094101.10.1016/j.foodres.2011.03.030Search in Google Scholar

23. SrinivasaPC, BaskaranR, RameshMN, PrashanthKVH, TharanathanRN. Storage studies of mango packed using biodegradable chitosan film. Eur Food Res Technol2002;215:5048.10.1007/s00217-002-0591-1Search in Google Scholar

24. AgnihotriSA, MallikarjunaNN, AminabhaviTM. Recent advances on chitosan-based micro- and nanoparticles in drug delivery. J Control Release2004;100:528.10.1016/j.jconrel.2004.08.010Search in Google Scholar

25. SinhaVR, SinglaAK, WadhawanS, KaushikR, KumriaR, BansalK, et al. Chitosan microspheres as a potential carrier for drugs. Int J Pharm2004;274:133.10.1016/j.ijpharm.2003.12.026Search in Google Scholar

26. PengH, XiongH, LiJ, XieM, LiuY, BaiC, et al. Vanillin cross-linked chitosan microspheres for controlled release of resveratrol. Food Chem2010;121:238.10.1016/j.foodchem.2009.11.085Search in Google Scholar

27. ZhangY, YuY, ShiX, ZhaoS, ChenA, HuangD, et al. Study on the preparation of genipin crosslinked chitosan microspheres of resveratrol and in vitro release. J Polym Res2013;20:17584.10.1007/s10965-013-0175-8Search in Google Scholar

28. HuangLH, SungH, TsaiC, HuangD. Biocompatibility study of a biological tissue fixed with a naturally occurring crosslinking reagent. J Biomed Mater Res1998;42:56876.10.1002/(SICI)1097-4636(19981215)42:4<568::AID-JBM13>3.0.CO;2-7Search in Google Scholar

29. NickersonMT, PatelJ, HeydDV, RousseauD, PaulsonAT. Kinetic and mechanistic considerations in the gelation of genipin-crosslinked gelatin. Int J Biol Macromol2006;39:298302.10.1016/j.ijbiomac.2006.04.010Search in Google Scholar

30. ButlerMF, NGYF, PudneyPDA. Mechanism and kinetics of the crosslinking reaction between biopolymers containing primary amine groups and genipin. J Polym Sci A Polym Chem2003;41:394153.10.1002/pola.10960Search in Google Scholar

31. MiF, SungH, ShyuS. Release of indomethacin from a novel chitosan microsphere prepared by a naturally occurring crosslinker: examination of crosslinking and polycation-anionic drug interaction. J Appl Polym Sci2001;81:170011.10.1002/app.1602Search in Google Scholar

32. HeJ, LuYC, LuoGS. Ca(II) imprinted chitosan microspheres: an effective and green adsorbent for the removal of cu(II), cd(II) and pb(II) from aqueous solutions. Chem Eng J2014;244:2028.10.1016/j.cej.2014.01.096Search in Google Scholar

33. NietoJM, PenichecovasC, PadronG. Characterization of chitosan by pyrolysis-mass spectrometry, thermal analysis and differential scanning calorimetry. Thermochim Acta1991;176:638.10.1016/0040-6031(91)80260-PSearch in Google Scholar

34. UmadeviSK, ThiruganeshR, SureshS, ReddyKB. Formulation and evaluation of chitosan microspheres of aceclofenac for colon-targeted drug delivery. Biopharm Drug Dispos2010;31:40727.10.1002/bdd.722Search in Google Scholar

35. DhawanS, SinglaA. Nifedipine loaded chitosan microspheres prepared by emulsification phase-separation. Biotech Histochem2003;78:24354.10.1080/10520290310001602396Search in Google Scholar

36. RitgerPL, PeppasNA. A simple equation for the description of solute release II. Fickian and anomalous release from swellable devices. J Control Release1987;5:3742.10.1016/0168-3659(87)90035-6Search in Google Scholar


Supplemental Material

The online version of this article (DOI: 10.1515/ijfe-2014-0314) offers supplementary material, available to authorized users.


Published Online: 2015-5-14
Published in Print: 2015-6-1

©2015 by De Gruyter

Downloaded on 15.9.2025 from https://www.degruyterbrill.com/document/doi/10.1515/ijfe-2014-0314/html
Scroll to top button