J. Matsumoto et al., Preparation of nanoparticles consisted of poly(L-lactide)-poly(ethylene glycol)-poly(L-lactide) and their evaluation in vitro, INT J PHARM, 185(1), 1999, pp. 93-101
This study describes the preparation and the evaluation of biodegradable po
ly(L-lactide)-poly(ethylene glycol)poly(L-lactide) copolymer (PLA-PEG-PLA)
nanoparticles containing progesterone as a model drug. PLA and PLA-PEG-PLA
copolymers, whose PEG content ranged from 5.2 to 25.8% (w/w), were polymeri
zed in our laboratory. PEG with weight-average molecular weight (Mw) 6600 o
r 20 000 was introduced as a hydrophilic segment into a hydrophobic PLA hom
opolymer. A solvent evaporation method was used to prepare the nanoparticle
s, The drug trapping efficiencies were around 70% and the weight-averaged m
ean diameters of the nanoparticles were less than 335 nm. The amount of dru
g released increased as the PEG content and Mw of PLA-PEG-PLA copolymers in
creased and the total Mw of copolymers of nanoparticles decreased. The init
ial burst of drug release was reduced by removing the low Mw fraction from
the polymer. During the release test, both the extent to which the copolyme
rs were degraded and the size of the nanoparticles were increased slightly
by increasing the content of PEG in the polymers. Drug release from the nan
oparticles could potentially be controlled by changing the PEG content, PEG
Mw and total Mw of the copolymer. The molecular weight distribution (Mw/Mn
, Mn: number-average molecular weight) of copolymers was also an important
factor for controlled release. (C) 1999 Elsevier Science B.V. All rights re
served.