title: New heparin-indomethacin conjugate with an ester linkage: synthesis, self aggregation and drug delivery behavior.
abstract: New heparin-indomethacin conjugate with an ester linkage was prepared by the carbodiimide-mediated condensation reaction, and then characterized by FTIR and (1)HNMR analyses. Due to its amphiphilic character, such a conjugate could self-aggregate into spherical nanoparticles in aqueous system, as confirmed by fluorescence spectroscopy, dynamic light scattering and transmission electron microscopy. By the in vitro drug release tests, the resultant conjugate nanoparticles were found to have a sustained and esterase-sensitive release behavior for conjugated indomethacin. In addition, the uptake of these conjugate nanoparticles into human nasopharyngeal carcinoma CNE1 cells was confirmed by fluorescence microscopy.
authors.affiliation: DSAPM Lab and PCFM Lab, Institute of Polymer Science, School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China.
authors.forename: Nan-Nan
authors.initials: NN
authors.lastname: Li
authors.forename: Bing-Na
authors.initials: BN
authors.lastname: Zheng
authors.forename: Jian-Tao
authors.initials: JT
authors.lastname: Lin
authors.forename: Li-Ming
authors.initials: LM
authors.lastname: Zhang
mesh_terms: D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D004952:Esters / Q000737:chemistry*; D006493:Heparin / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D007213:Indomethacin / Q000138:chemical synthesis* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008856:Microscopy, Fluorescence; D053758:Nanoparticles / Q000648:ultrastructure; D010316:Particle Size; D013055:Spectrophotometry, Infrared
chemical_list: D004952:Esters; D006493:Heparin; D007213:Indomethacin
keywords: Cellular uptake; Drug delivery; Heparin–indomethacin conjugate; Prodrug nanoparticles; Self aggregation