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Chitosan-genipin microspheres for the controlled release of drugs: clarithromycin, tramadol and heparin.
Mar Drugs 2010; 8(6):1750-62MD

Abstract

The aim of this study was to first evaluate whether the chitosan hydrochloride-genipin crosslinking reaction is influenced by factors such as time, and polymer/genipin concentration, and second, to develop crosslinked drug loaded microspheres to improve the control over drug release. Once the crosslinking process was characterized as a function of the factors mentioned above, drug loaded hydrochloride chitosan microspheres with different degrees of crosslinking were obtained. Microspheres were characterized in terms of size, morphology, drug content, surface charge and capacity to control in vitro drug release. Clarithromycin, tramadol hydrochloride, and low molecular weight heparin (LMWH) were used as model drugs. The obtained particles were spherical, positively charged, with a diameter of 1-10 microm. X-Ray diffraction showed that there was an interaction of genipin and each drug with chitosan in the microspheres. In relation to the release profiles, a higher degree of crosslinking led to more control of drug release in the case of clarithromycin and tramadol. For these drugs, optimal release profiles were obtained for microspheres crosslinked with 1 mM genipin at 50 °C for 5 h and with 5 mM genipin at 50 °C for 5 h, respectively. In LMWH microspheres, the best release profile corresponded to 0.5 mM genipin, 50 °C, 5 h. In conclusion, genipin showed to be eligible as a chemical-crosslinking agent delaying the outflow of drugs from the microspheres. However, more studies in vitro and in vivo must be carried out to determine adequate crosslinking conditions for different drugs.

Authors+Show Affiliations

Instituto de Estudios Biofuncionales, Departamento Química-Física II, Universidad Complutense Paseo Juan XXIII, Madrid, Spain. ruthharris@ieb.ucm.esNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20631867

Citation

Harris, Ruth, et al. "Chitosan-genipin Microspheres for the Controlled Release of Drugs: Clarithromycin, Tramadol and Heparin." Marine Drugs, vol. 8, no. 6, 2010, pp. 1750-62.
Harris R, Lecumberri E, Heras A. Chitosan-genipin microspheres for the controlled release of drugs: clarithromycin, tramadol and heparin. Mar Drugs. 2010;8(6):1750-62.
Harris, R., Lecumberri, E., & Heras, A. (2010). Chitosan-genipin microspheres for the controlled release of drugs: clarithromycin, tramadol and heparin. Marine Drugs, 8(6), pp. 1750-62. doi:10.3390/md8061750.
Harris R, Lecumberri E, Heras A. Chitosan-genipin Microspheres for the Controlled Release of Drugs: Clarithromycin, Tramadol and Heparin. Mar Drugs. 2010 May 26;8(6):1750-62. PubMed PMID: 20631867.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Chitosan-genipin microspheres for the controlled release of drugs: clarithromycin, tramadol and heparin. AU - Harris,Ruth, AU - Lecumberri,Elena, AU - Heras,Angeles, Y1 - 2010/05/26/ PY - 2010/03/10/received PY - 2010/04/23/revised PY - 2010/05/17/accepted PY - 2010/7/16/entrez PY - 2010/7/16/pubmed PY - 2011/2/18/medline KW - chitosan KW - clarithromycin KW - controlled release KW - genipin KW - heparin KW - microspheres KW - tramadol SP - 1750 EP - 62 JF - Marine drugs JO - Mar Drugs VL - 8 IS - 6 N2 - The aim of this study was to first evaluate whether the chitosan hydrochloride-genipin crosslinking reaction is influenced by factors such as time, and polymer/genipin concentration, and second, to develop crosslinked drug loaded microspheres to improve the control over drug release. Once the crosslinking process was characterized as a function of the factors mentioned above, drug loaded hydrochloride chitosan microspheres with different degrees of crosslinking were obtained. Microspheres were characterized in terms of size, morphology, drug content, surface charge and capacity to control in vitro drug release. Clarithromycin, tramadol hydrochloride, and low molecular weight heparin (LMWH) were used as model drugs. The obtained particles were spherical, positively charged, with a diameter of 1-10 microm. X-Ray diffraction showed that there was an interaction of genipin and each drug with chitosan in the microspheres. In relation to the release profiles, a higher degree of crosslinking led to more control of drug release in the case of clarithromycin and tramadol. For these drugs, optimal release profiles were obtained for microspheres crosslinked with 1 mM genipin at 50 °C for 5 h and with 5 mM genipin at 50 °C for 5 h, respectively. In LMWH microspheres, the best release profile corresponded to 0.5 mM genipin, 50 °C, 5 h. In conclusion, genipin showed to be eligible as a chemical-crosslinking agent delaying the outflow of drugs from the microspheres. However, more studies in vitro and in vivo must be carried out to determine adequate crosslinking conditions for different drugs. SN - 1660-3397 UR - https://www.unboundmedicine.com/medline/citation/20631867/Chitosan_genipin_microspheres_for_the_controlled_release_of_drugs:_clarithromycin_tramadol_and_heparin_ L2 - https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/20631867/ DB - PRIME DP - Unbound Medicine ER -