Suitable carriers for encapsulation and distribution of endostar: comparison of endostar-loaded particulate carriers.
BACKGROUND
Particulate carriers are necessary to control the release of endostar and prolong its circulation in vivo. The purpose of this study was to identify a suitable carrier for the capsulation and delivery of endostar.


METHODS
We prepared a series of poly (DL-lactide-co-glycolide) (PLGA) and poly (ethylene glycol) (PEG)-modified PLGA (PEG-PLGA) particulate carriers, and then characterized them according to their ability to prolong the circulation of endostar, their physicochemical properties, endostar-loading content, and in vitro and in vivo particulate carrier release profiles.


RESULTS
All the particulate carriers had spherical core shell structures. The PEG-PLGA material and nanosize range appeared to enable the carriers to encapsulate more endostar, release endostar faster in vitro, and accumulate more endostar in vivo. The drug loading capacity of PEG-PLGA and PLGA nanoparticles was 8.03% ± 3.41% and 3.27% ± 5.26%, respectively, and for PEG-PLGA and PLGA microspheres was 15.32% ± 5.61% and 9.21% ± 4.73%. The cumulative amount of endostar released from the carriers in phosphate-buffered saline over 21 days was 23.79%, 20.45%, 15.13%, and 10.41%, respectively. Moreover, the terminal elimination half-life of endostar in the rabbit was 26.91 ± 7.93 hours and 9.32 ± 5.53 hours in the PEG-PLGA group and the PLGA nanoparticle group. Peak endostar concentration was reached at day 7 in the group treated with subcutaneous injection of PEG-PLGA microspheres and at day 14 in the group receiving subcutaneous injection of PLGA microspheres. Endostar was detectable in vivo in both groups after injection of the particulate carriers.


CONCLUSION
PEG-PLGA nanoparticles might be better than other nanoparticulate carriers for encapsulation and distribution of endostar.
['Chen|Weijie|W|', 'Hu|Sanyuan|S|']
D000818:Animals D004337:Drug Carriers D043169:Endostatins D019344:Lactic Acid D008297:Male D008863:Microspheres D053758:Nanoparticles D011092:Polyethylene Glycols D011100:Polyglycolic Acid D000077182:Polylactic Acid-Polyglycolic Acid Copolymer D011817:Rabbits D011994:Recombinant Proteins
endostar nanoparticle microsphere peptide delivery poly(DL-lactide-co-glycolide)