Tabata Y, Ikada Y
Research Center for Medical Polymers and Biomaterials, Kyoto University, Japan.
J Pharm Pharmacol. 1987 Sep;39(9):698-704. doi: 10.1111/j.2042-7158.1987.tb06972.x.
Gelatin microspheres containing muramyl dipeptide (MDP) were prepared by crosslinking with glutaraldehyde. They were added to mouse peritoneal macrophages (PMs) to potentiate the tumour growth inhibitory activity. The PMs which had internalized the microspheres exhibited growth inhibitory activity to syngeneic, allogeneic, and xenogeneic tumour cells. A similar effect was observed for PMs incubated with free MDP, but the MDP encapsulated in the microspheres was more efficient in enhancing the PM activity than the free MDP. In addition, PMs were activated in much shorter periods upon incubation with the microsphere-encapsulated MDP. The duration of activity could be controlled for up to 7 days by changing the extent of crosslinking of microspheres. Dose-response experiments established that microsphere-encapsulated MDP is able to activate PMs to inhibit growth of tumour cells at concentrations approximately 2000 times lower than the free MDP present in media. The activity of PMs was also acquired on intraperitoneal injection of the microspheres, in contrast to PMs with the free MDP.
通过与戊二醛交联制备了含有胞壁酰二肽（MDP）的明胶微球。将它们添加到小鼠腹腔巨噬细胞（PMs）中以增强肿瘤生长抑制活性。摄取了微球的PMs对同基因、异基因和异种肿瘤细胞均表现出生长抑制活性。用游离MDP孵育的PMs也观察到类似效果，但包裹在微球中的MDP在增强PM活性方面比游离MDP更有效。此外，与包裹微球的MDP孵育后，PMs在更短的时间内被激活。通过改变微球的交联程度，活性持续时间可控制长达7天。剂量反应实验表明，包裹微球的MDP能够激活PMs以抑制肿瘤细胞生长，其浓度比培养基中存在的游离MDP低约2000倍。与注射游离MDP的PMs相反，腹腔注射微球后PMs也获得了活性。
