Sy. Lin et al., In vitro degradation and dissolution behaviours of microspheres prepared by three low molecular weight polyesters, J MICROENC, 17(5), 2000, pp. 577-586
Three low-molecular weight polyesters, poly( L-lactic acid) (PLA), copoly(
lactic acid/glycolic acid) (PLGA) and poly(delta-valerolactone) (PV), were
used to prepare water-soluble sodium diclofenac-loaded microspheres by usin
g the oil-in-oil (o/o) emulsircation-solvent evaporation method. Their micr
omeritic and physicochemical properties, and degradation and dissolution be
haviours were determined in vitro. The results indicate that high encapsula
tion efficiency and better monodispersity might be achieved by the o/o emul
sification-solvent evaporation method, depending on the amount of drug load
ing used. The slower evaporation of organic solvent from the system during
microencapsulation seemed to modify the crystallinity of drug and polyester
in the microspheres, determined by powder x-ray diffractometry and differe
ntial scanning calorimetry. The in vitro degradation rate of all the micros
pheres in pH 7.4 phosphate buffer solution showed first-order kinetics and
ranked in the order of PLGA> PLA> PV microspheres. Furthermore, the first-o
rder release rate was also found in all the microspheres after an initial d
rug burst and ranked in the order of PLGA> PLA> PV microspheres, too. The r
elationship between degradation and dissolution behaviours of these microsp
heres is discussed.