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Article Dans Une Revue International Journal of Pharmaceutics Année : 1998

Proanthocyanidin microcapsules: preparation, properties and free radical scavenging activity

Résumé

Microcapsules were prepared by interfacial cross-linking of grape proanthocyanidin (GPO) with terephthaloyl chloride (TC). Using 5% TC, 30-min reaction time and a stirring speed of 5000 rpm, batches were prepared from 10% GPO solutions in buffers pH 8, 9.8, and 11, respectively. Microcapsules were studied with respect to morphology (microscopy), size (laser diffraction technique), stability in water at 45°C and, for stable batches, IR spectroscopy, degradation in human plasma, and free radical scavenging activity studied by electron paramagnetic resonance (EPR) using both extinction of the stable radical DPPH (2,2-diphenyl-picryl-hydrazyl), and scavenging of OH° (evaluated using 5,5-dimethyl-pyrrolidine-N-oxide; DMPO). All particles had a mean size <10 μm. Microcapsules obtained at pH 8 were unstable (yellow supernatant after 8 days). Microcapsules obtained at pH 9.8 and 11 exhibited a high stability (>5 months). Using a stirring speed of 3000 rpm at pH 11 provided 15-μm particles which gave a yellow supernatant after 3 weeks. The IR spectra of the two stable batches (pH 9.8 and 11) showed bands at 1736 and 1267 cm−1 reflecting the formation of esters. They were slowly degraded in plasma, and although less active than the initial GPO, they exhibited a significant antioxidant activity. The method appears to be an efficient means of stabilizing the polyphenol without suppressing the free radical scavenging activity.

Dates et versions

hal-03423359 , version 1 (10-11-2021)

Identifiants

Citer

M.-C Andry, Herve Vezin, I Dumistracel, Jean-Luc Bernier, M.-C Lévy. Proanthocyanidin microcapsules: preparation, properties and free radical scavenging activity. International Journal of Pharmaceutics, 1998, International Journal of Pharmaceutics, 171 (2), pp.217-226. ⟨10.1016/s0378-5173(98)00183-5⟩. ⟨hal-03423359⟩

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