期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 378, 期 1-2, 页码 159-166出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2009.05.021
关键词
Insulin nanoparticle; S/O/O emulsion; Microsphere; Protein delivery
资金
- National Fund for Distinguished Young Scholar of China [50425309]
- National Natural Science Foundation of China-A3 Foresight Program [20621140369]
- Ministry of Science and Technology of China [20071314]
Insulin has been encapsulated in poly(lactic-co-glycolic acid) (PLGA) microspheres by solid-in-oil-in-oil (S/O/O) emulsion technique using DMF/corn oil as new solvent pairs. To get better encapsulation efficiency, insulin nanoparticles were prepared by the modified isoelectric point precipitation method so that it had good dispersion in the inner oil phase. The resulting microspheres had drug loading of 10% (w/w), while the encapsulation efficiency could be up to 90-100%. And the insulin release from the microspheres could last for 60 days. Microspheres encapsulated original insulin with the same method had lower encapsulation efficiency, and shorter release period. Laser scanning confocal microscopy indicated the insulin nanoparticle and original insulin had different distribution in microspheres. The results suggested that using insulin nanoparticle was better than original insulin for microsphere preparation by S/O/O method. Study about the secondary structure of insulin by Fourier transform infrared spectroscopy (FTIR) indicated high insulin structural integrity during the process. in vivo test showed insulin in microspheres retained its bioactivity. In addition, cytotoxicity evaluation by the MTT assay has proved that no extra toxicity was introduced into the microspheres during the emulsion process. (C) 2009 Elsevier B.V. All rights reserved.
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