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 Influence of the pectin gels properties in vitro release from rutin calcium pectinate microparticles
Tác giả hoặc Nhóm tác giả: Uyen T. D. Huynh, Ali Assifaoui, Odile Chambin
Nơi đăng: 4th Conference on Innovation in Drug Delivery: Site-Specific Drug Delivery, Antibes – Juan-Les-Pins, France; Số: 25-28/09;Từ->đến trang: 25-28/09;Năm: 2016
Lĩnh vực: Y - Dược; Loại: Báo cáo; Thể loại: Quốc tế
TÓM TẮT
Pectins are widely used in food and pharmaceutical industry, as well as in numerous other biomedical applications, namely: drug delivery, gene delivery, tissue engineering and wound healing due to their thickening and gelling properties.The chemical structural basis of pectin is linear galacturonan, a polymer of 1,4-linked α-D-galacturonic acid units which could be partially methyl esterified. Low methoxyl (LM) pectins, with less than 50% of the carboxyl groups esterified, form gels in the presence of Ca2+ ions and can be used to encapsulate drug, particularly to target the colon. Generally, LM pectin is characterised by its degree of methylation (DM) and degree of amidation (DA).In this work, we have investigated the impact of the gel properties on the drug release of three types of calcium pectinate microparticles containing amidated low methoxyl pectin (ALMP-Ca), non-amidated low methoxyl pectin (LMP-Ca) and polygalacturonic acid (PGA-Ca). These microparticles which entrapped an antioxidant (rutin) were produced by ionotropic gelation. The viscoelastic properties of the three different gels were studied using a stress-controlled dynamic rheometer. The size, shape, encapsulation efficiency, water uptake and in-vitro release in simulated intestinal fluid (pH 7.4) of the different microparticles were assessed.Our results have shown that the rutin release from ALMP-Ca was higher than from the two others microparticles (LMP-Ca and PGA-Ca). The higher release for ALMP-Ca can be explained by the higher water uptake of these microparticles. The viscoelastic properties of the ALMP-Ca showed the lowest G’ (storage modulus), G’’ (loss modulus) and tand. The lowest G’ and G’’ may be due to the low amount of carboxylate groups in the ALMP in comparison with LMP and PGA, while the lowest tand indicated that the flexibility of the gel network is higher. Due to this flexibility, the gel network structure could be more sensitive to water uptake which enhanced the rutin release. For LMP-Ca and PGA-Ca microparticles, the water uptake and the drug release were similar. In conclusion, the pectin structural properties influence the rheological properties of gels which are directly linked to microparticles properties and rutin release behaviour. The properties of pectinate microparticles seem to be more sensitive to the presence of amidated groups than to the presence of ester groups.
ABSTRACT
Pectins are widely used in food and pharmaceutical industry, as well as in numerous other biomedical applications, namely: drug delivery, gene delivery, tissue engineering and wound healing due to their thickening and gelling properties. The chemical structural basis of pectin is linear galacturonan, a polymer of 1,4-linked α-D-galacturonic acid units which could be partially methyl esterified. Low methoxyl (LM) pectins, with less than 50% of the carboxyl groups esterified, form gels in the presence of Ca2+ ions and can be used to encapsulate drug, particularly to target the colon. Generally, LM pectin is characterised by its degree of methylation (DM) and degree of amidation (DA). In this work, we have investigated the impact of the gel properties on the drug release of three types of calcium pectinate microparticles containing amidated low methoxyl pectin (ALMP-Ca), non-amidated low methoxyl pectin (LMP-Ca) and polygalacturonic acid (PGA-Ca). These microparticles which entrapped an antioxidant (rutin) were produced by ionotropic gelation. The viscoelastic properties of the three different gels were studied using a stress-controlled dynamic rheometer. The size, shape, encapsulation efficiency, water uptake and in-vitro release in simulated intestinal fluid (pH 7.4) of the different microparticles were assessed. Our results have shown that the rutin release from ALMP-Ca was higher than from the two others microparticles (LMP-Ca and PGA-Ca). The higher release for ALMP-Ca can be explained by the higher water uptake of these microparticles. The viscoelastic properties of the ALMP-Ca showed the lowest G’ (storage modulus), G’’ (loss modulus) and tand. The lowest G’ and G’’ may be due to the low amount of carboxylate groups in the ALMP in comparison with LMP and PGA, while the lowest tand indicated that the flexibility of the gel network is higher. Due to this flexibility, the gel network structure could be more sensitive to water uptake which enhanced the rutin release. For LMP-Ca and PGA-Ca microparticles, the water uptake and the drug release were similar. In conclusion, the pectin structural properties influence the rheological properties of gels which are directly linked to microparticles properties and rutin release behaviour. The properties of pectinate microparticles seem to be more sensitive to the presence of amidated groups than to the presence of ester groups.
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