NOVEL PROSTAGLANDIN E1 DERIVATIVE, AND NANOPARTICLE HAVING SAME ENCAPSULATED THEREIN
申请人:LTT Bio-Pharma Co., Ltd.
公开号:EP2361918A1
公开(公告)日:2011-08-31
A PGE1 derivative is provided which has an excellent sustained, slow-release PGE1 action. In addition, a PGE1-derivative-containing nanoparticle produced using this PGE1 derivative is provided, which effectively targets an affected site, has excellent drug slow-release properties, and has reduced side effects. This PGE1-derivative-containing nanoparticle is a nanoparticle containing a prostaglandin E1 derivative represented by the following formula (1)
(wherein n denotes an integer of 1 to 12),
obtained by hydrophobicizing the prostaglandin E1 derivative with a metal ion, and reacting tne hydrophobicized prostaglandin E1 derivative with poly L-lactic acid or a poly(L-lactic acid/glycolic acid) copolymer and a poly DL- or L-lactic acid-polyethylene glycol block copolymer or a poly(DL- or L-lactic acid/glycolic acid)-polyethylene glycol block copolymer.
提供了一种PGE1衍生物,具有出色的持续缓释PGE1作用。此外,提供了一种含有该PGE1衍生物的纳米颗粒,它能有效地靶向受影响的部位,具有优异的药物缓释性能,并减少了副作用。该PGE1衍生物含有纳米颗粒,该纳米颗粒含有以下公式(1)所代表的前列腺素E1衍生物(其中n表示1到12的整数),通过用金属离子使前列腺素E1衍生物疏水化,并将疏水化的前列腺素E1衍生物与聚L-乳酸或聚(L-乳酸/聚乙二醇酸)共聚物和聚DL-或L-乳酸-聚乙二醇嵌段共聚物或聚(DL-或L-乳酸/乙二醇酸)-聚乙二醇嵌段共聚物反应而得到。