Tokuda K, Natsugoe S, Kumanohoso T, Shimada M, Yoshizawa H, Hatate Y, Nakamura K, Yamada K, Nedachi M, Aiko T
First Dept. of Surgery, Kagoshima University School of Medicine.
Gan To Kagaku Ryoho. 1995 Sep;22(11):1641-3.
Cisplatin incorporated into polylactic acid/polyethylene glycol acid blend polymeric microspheres was prepared as a dosage (CDDP-MS) by the solvent evaporation method in an oil-in-oil emulsion system. When CDDP-MS was preserved in phosphate-buffer saline, the dissolution rate of cisplatin from CDDP-MS was 14% after one day, 25% after 5 days, 33% after 7 days, 66% after 21 days and 85% after 30 days. CDDP-MS and CDDP aqueous solution (CDDP-SOL) were intraperitoneally administered to compare the tissue distribution of cisplatin in 42 rats each. On days 0.5, 1, 5, 7, 14 and 21, omentum, lung, liver and kidney were removed, and the CDDP concentration was measured. The CDDP concentration of the CDDP-MS group was maintained at a high level in the omentum for a long time. On the other hand, the CDDP level of CDDP-MS group was low in the lung, liver and kidney, compared with the CDDP-SOL group. Consequently, it was suggested that CDDP-MS is useful as a carrier in a drug delivery system, since it improves the burst effect and releases CDDP for a long time without serious side effects.
采用油包油乳液体系中的溶剂蒸发法，将顺铂载入聚乳酸/聚乙醇酸共混聚合物微球中制成一种剂型（顺铂微球，CDDP-MS）。当CDDP-MS保存在磷酸盐缓冲盐水中时，顺铂从CDDP-MS中的溶解率在1天后为14%，5天后为25%，7天后为33%，21天后为66%，30天后为85%。分别给42只大鼠腹腔注射CDDP-MS和顺铂水溶液（CDDP-SOL），以比较顺铂的组织分布。在第0.5、1、5、7、14和21天，取出大网膜、肺、肝和肾，并测定顺铂浓度。CDDP-MS组的顺铂浓度在大网膜中长时间维持在较高水平。另一方面，与CDDP-SOL组相比，CDDP-MS组在肺、肝和肾中的顺铂水平较低。因此，提示CDDP-MS作为药物递送系统中的载体是有用的，因为它改善了突释效应，能长时间释放顺铂且无严重副作用。
