Preparation and in vitro release of 5-fluorouracil-loaded poly (lactic-co-glycolic-acid)/ nano-hydroxyapatite microspheres / 中国组织工程研究

ABSTRACT

BACKGROUND: Poly (lactic-co-glycolic-acid) (PLGA)/nano-hydroxyapatite (nHA) composite microspheres may continuously release drug in phosphate buffer solution in vitro.OBJECTIVE: To prepare 5-fluorouracil (5-Fu)-loaded PLGA/nHA microspheres, and research the effect of nHA on drug loading,encapsulation efficiency and in vitro release.DESIGN, TIME AND SETTING: An in vitro materials observation was performed at Laboratory of College of Materials Science and Engineering, South China University of Technology between February and July 2009.MATERIALS PLGA was provided by Jinan Daigang Biomaterial Co., Ltd.; nHA by Key Lab for Special Functional Materials,Ministry of Education; 5-Fu by Shanghai Kaiyang Biomaterial Co., Ltd.METHODS: 5-Fu, a water-soluble anti-cancer drug, was used as model drug, and was firstly adsorbed by nHA and coated with biodegradable and blocompatible materials of PLGA so as to prepare PLGA/nHA-5-Fu composite microspheres by a single-emulsion solvent evaporation method (S/O/W). nHA and drug-loaded nHA were analyzed by transmission electron microscope (TEM), scanning electron microscope (SEM), and Fourier transform infrared spectroscopy (FTIR). Drug loading and encapsulation efficiency as well as in vitro release of microspheres were studied with SEM, laser particle size analyzer, and UV-spectrophotometer.MAIN OUTCOME MEASURES: Interaction between nHA and 5-Fu; drug loading, encapsulation efficiency, and in vitro release of Microspheres RESULTS: FTIR showed that nHA had a strong adsorption with 5-Fu. Drug loading and encapsulation efficiency of PLGA/nHA-5-Fu composite microspheres were 3.83% and 86.78%, respectively, which were significantly greater than PLGA-5-Fu microspheres. After initial burst, composite microspheres released more slowly than PLGA microspheres alone. At day 27, the cumulative release rate of composite microspheres and PLGA microspheres alone were 84.87% and 99.87%,respectively.CONCLUSION: Because nHA has a strong adsorption with 5-Fu, PLGA/nHA-5-Fu composite microspheres compared to PLGA-5-Fu microspheres alone enhances drug loading and encapsulation efficiency, and has a better drug delivery effect.