G. Weiss et al., SIMPLE COACERVATION OF HYDROXYPROPYL METHYLCELLULOSE PHTHALATE (HPMCP) .2. MICROENCAPSULATION OF IBUPROFEN, International journal of pharmaceutics, 124(1), 1995, pp. 97-105
Microencapsulation with hydroxypropyl methylcellulose phthalate (HPMCP
) through simple coacervation by the addition of 20% (w/w) sodium sulp
hate solution was investigated on the basis of the temperature-depende
nt coacervate formation of the polymer. The nonsteroidal antirheumatic
drug ibuprofen was used as model substance. This paper describes the
microencapsulation process and the resulting microcapsules. Furthermor
e, the influence of docusate sodium present during encapsulation was i
nvestigated with respect to the phase separation behaviour of HPMCP an
d the wall characteristics of the microcapsules. Simple coacervation o
f HPMCP is a suitable method for the microencapsulation of ibuprofen.
The coacervate enveloped the suspended drug which had no effect upon t
he phase separation of the polymer owing to the low solubility of ibup
rofen in the HPMCP solution, The microencapsulation process was contro
lled by temperature increase: additional coacervate for the coating of
the drug crystals was formed and the resulting coacervate shells were
subsequently prehardened by jelling. This enabled the recovery and is
olation of the microcapsules to be performed. The coating of the drug
crystals occurred as twins and multiples when microencapsulation was p
erformed without surfactant; SEM micrographs demonstrated the high she
ll quality of the microcapsules and polymer yield calculations showed
the almost complete utilization of the coacervate for enveloping the d
rug crystals in surfactant-free systems. Small amounts of docusate sod
ium present during microencapsulation resulted in a more individual en
capsulation of the ibuprofen crystals; however, coating by the coacerv
ate was incomplete and the microcapsules showed clod-like polymer shel
l deficiencies. As a consequence, an increased release rate of ibuprof
en at pH 4.0 was observed compared to microcapsules prepared without u
sing surfactant. Since docusate sodium had no effect upon the phase se
paration behaviour of HPMCP under the conditions used for microencapsu
lation, the incomplete polymer coating was attributed to competition b
etween surfactant and coacervate for the solid/liquid interface.