In the current study, p-aminobenzoic acid-loaded ethylcellulose microspheres
were prepared under various conditions by solvent evaporation method (o/w).
This preparation was carried out with different p-aminobenzoic
acid:ethylcellulose (PABA:EC) ratios, stirring speed, surfactant nature and
concentration in order to investigate their effect on encapsulation
efficiency and drug release kinetics. Scanning Electron Microscopy (SEM)
studies showed spherical microspheres with a porous surface and different
structures. The mean diameter of Sauter (d32) of these microparticles is in
the range from 47 to 165 ?m with PVA and from 793 to 870 ?m with Tween 80 by
adjusting process parameters. However, the encapsulation efficiency varied
from 37.52 to 79.05 % suitable for the adjustment of a p-aminobenzoic acid
with pro-longed release. Microspheres were characterized by FTIR, DSC and
XRD. The release of cation of p-aminobenzoic acid was performed in simulated
gastric medium at pH 1.2 and 37?0.5?C by UV-VIS analysis to estimate its
content. The release data were best fitted to Higuchi model with high
correlation coefficient (r?) and the obtained values of n from
Korsmeyer-Peppas showed that the drug release follows the Fickian diffusion
mechanism.
Four secondary amides have been prepared by the Schotten-Baumann reaction between model anilines (Pa1-4: p-XC6H4NH2: X1: H; X2:CH3; X3:COCH3; X4: CN) and methacryloyl chloride using aqueous THF/NaOH mixture at 0°C. MS1, MS2 and MS4 liquid monomers are obtained whereas MS3 is a solid monomer. Mass radical copolymerization of the different monomers (MS1-4) with N-vinyl-2-pyrrolidone yields to the corresponding four copolymers. All the monomers have been characterized by IR, 1H and 13C NMR. The (CP1-4) have been characterized by IR spectra, microanalysis, Tg ° and Mv. The kinetics of aniline delivery to give anilinium cations (PaH+)1-4 from solid MS3 and CP1-4 dispersed in water (pH= 1.2, 37°C) showed that aniline delivery from the different supports is controlled by a diffusion process and not the rate of amide hydrolysis. The amount (%) of free anilinium cations is inversely proportional to the molecular weight of polymeric supports. Accordingly, the monomer MS3 gave the largest amount of free anilinium cations (PaH+) 1-4
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