Hamdi G, Ponchel G
Laboratoire de Pharmacotechnie et Biopharmacie, URA CNRS 1218, Faculté de Pharmacie, Université de Paris-Sud, Châtenay-Malabry, France.
Pharm Res. 1999 Jun;16(6):867-75. doi: 10.1023/a:1018878120100.
The influence of chemical parameters on the sensitivity to enzymatic degradation by alpha-amylase of starch microspheres cross-linked by epichlorohydrin was studied.
Starch microspheres were prepared using epichlorohydrin as a crosslinking agent. Their swelling degree, reflecting the number of glycerol diether bridges in the polymeric network, and the number of non-crosslinking monoglycerol ether groups corresponding to a side-reaction of epichlorohydrin with starch were determined. Degradation rates of the microspheres in presence of porcine alpha-amylase were determined by a microvolumetric method.
Degradation by alpha-amylase was surface-controlled and could be modulated by the introduction in the polymeric network of: (i) non-hydrolysable alpha-1,6 bonds related to the presence of amylopectin in the raw starch, (ii) glycerol diether and, (iii) monoether groups, all of these being likely to block the activity of alpha-amylase. In the case of highly cross-linked microspheres, the number of glycerol monoether pendent chains had a predominant effect on the degradation rate which ranged between 10(-2) and 10(-5) min(-1).
It was possible to modulate simultaneously the swelling degree and the enzymatic degradability of starch microspheres by adjusting the chemical parameters during the crosslinking reaction.
研究化学参数对环氧氯丙烷交联淀粉微球α-淀粉酶酶解敏感性的影响。
以环氧氯丙烷为交联剂制备淀粉微球。测定其溶胀度(反映聚合物网络中甘油二醚桥的数量)以及与环氧氯丙烷和淀粉副反应对应的非交联单甘油醚基团的数量。采用微量体积法测定猪α-淀粉酶存在下微球的降解速率。
α-淀粉酶的降解受表面控制,可通过在聚合物网络中引入以下物质进行调节:(i)与原淀粉中支链淀粉存在相关的不可水解α-1,6键;(ii)甘油二醚;(iii)单醚基团,所有这些都可能阻碍α-淀粉酶的活性。对于高度交联的微球,甘油单醚侧链的数量对降解速率起主要作用,降解速率在10⁻²至10⁻⁵ min⁻¹之间。
通过在交联反应过程中调整化学参数,可以同时调节淀粉微球的溶胀度和酶降解性。