Molinaro Giuseppe, Leroux Jean-Christophe, Damas Jacques, Adam Albert
Faculté de Pharmacie, Université de Montréal, Qué., Canada.
Biomaterials. 2002 Jul;23(13):2717-22. doi: 10.1016/s0142-9612(02)00004-2.
Chitosan, an amino-polysaccharide obtained from the alkaline deacetylation of chitin, presents an interest as a drug vehicle. Indeed, chitosan solutions containing glycerol-2-phosphate (beta-GP) undergo sol-gel transition at a temperature close to 37 degrees C, which make them suitable for the parenteral administration of drugs. However, before using these chitosan derivatives for biomedical applications, it is important to evaluate their biocompatibility, and particularly to test their inflammatory effects. When injected in the hindpaw of the rat, we have shown that: (i) four chitosan/beta-GP solutions tested triggered a non-specific response, with solutions prepared with chitosans of higher deacetylation degrees yielding a lesser inflammatory reaction and (ii) systemic pretreatment of animals with icatibant, apafant and diphenhydramine did not significantly diminish this response; dexamethasone practically abolished it for all solutions and ketanserine only slightly decreased it in one preparation at two different times. In conclusion, it appears that a higher degree of deacetylation of the chitin chain is desirable for superior biocompatibility.
壳聚糖是一种由甲壳素经碱性脱乙酰作用得到的氨基多糖,作为药物载体具有一定的研究价值。实际上,含有甘油 - 2 - 磷酸(β - GP)的壳聚糖溶液在接近37摄氏度的温度下会发生溶胶 - 凝胶转变,这使其适用于药物的肠胃外给药。然而,在将这些壳聚糖衍生物用于生物医学应用之前,评估它们的生物相容性非常重要,特别是要测试它们的炎症效应。当注射到大鼠后爪时,我们发现:(i)所测试的四种壳聚糖/β - GP溶液引发了非特异性反应,脱乙酰度较高的壳聚糖制备的溶液产生的炎症反应较小;(ii)用依替巴肽、阿帕泛和苯海拉明对动物进行全身预处理并没有显著减轻这种反应;地塞米松实际上消除了所有溶液的这种反应,而酮色林仅在两种不同时间的一种制剂中使其略有降低。总之,对于更好的生物相容性而言,似乎甲壳素链的脱乙酰度越高越好。