公开(公告)号：KR1020080095130A

公开(公告)日：2008-10-28

申请号：KR1020070039524

申请日：2007-04-23

Applicant: 한국과학기술연구원

Inventor： 권익찬 ,  이두성 ,  김광명 ,  김봉섭 ,  박경순 ,  김민상 ,  한종권 ,  고진영

IPC: A61K9/52 ,  A61P35/00

CPC classification number: A61K9/5089 ,  A61K9/5031

Abstract: A drug delivery system is provided to be easily disintegrated at low pH of a topical portion of various cancers or inflammatory diseases due to high sensitivity on the pH and decrease toxicity of a drug itself, thereby releasing a large amount of a drug into the diseased portion selectively to enhance therapeutic effect of the drug and being useful for treating various cancers or inflammatory diseases. A drug delivery system consists of a pH-sensitive block copolymer encapsulating a hydrophobic drug therein and having a hydrophilic moiety and a hydrophobic moiety, wherein the hydrophilic moiety is polyethylene glycol, poly(N-2-(hydroxypropyl)methacrylamide), poly(divinyl ether-co-maleic anhydride) or poly(styreneco-maleic anhydride), the hydrophobic moiety is poly(beta-amino ester)(PAE), poly(amido amine)(PAA) or a copolymer thereof(PAEA), and the drug is an anti-cancer agent selected from the group consisting of paclitaxel, doxorubicin, retinoic acid, cis-platin, camptothecin, 5-FU, docetaxel, tamoxifen, anasterozole, carboplatin, topotecan, belotecan, irinotecan, gleevec and vincristine or an anti-inflammatory agent selected from the group consisting of aspirin, salicylates, ibuprofen, naproxen, fenoprofen, indomethacin, phenyltazone, methotrexate, cyclophosphamide, mechlorethamine, dexamethasone, prednisolone, celecoxib, valdecoxib, nimesulide, cortisone and corticosteroid.

Abstract translation: 提供了药物递送系统，由于对pH高的敏感性和药物本身的毒性降低，因此容易在各种癌症或炎性疾病的局部部分的低pH下崩解，从而将大量药物释放到患病部位 选择性地增强药物的治疗效果并且可用于治疗各种癌症或炎性疾病。 药物递送系统由在其中封装疏水性药物并具有亲水部分和疏水部分的pH敏感性嵌段共聚物组成，其中亲水部分是聚乙二醇，聚（N-2-（羟丙基）甲基丙烯酰胺），聚（二乙烯基 醚 - 共 - 马来酸酐）或聚（苯乙烯 - 顺丁烯二酸酐），疏水部分是聚（β-氨基酯）（PAE），聚（酰氨基胺）（PAA）或其共聚物（PAEA） 是选自紫杉醇，多柔比星，视黄酸，顺铂，喜树碱，5-FU，多西紫杉醇，他莫昔芬，西曲唑，卡铂，托泊替康，美沙替丹，伊立替康，格列卫和长春新碱或抗生素的抗癌剂， 选自阿司匹林，水杨酸酯，布洛芬，萘普生，非诺洛芬，吲哚美辛，苯那唑，甲氨蝶呤，环磷酰胺，氮芥，地塞米松，泼尼松龙，塞来考昔，伐地考昔，尼美舒利，可的松和皮质类固醇的炎症剂。