| 초록 |
Much attention has been paid to pH-sensitive drug delivery systems such as tumor targeting anticancer drug delivery, because it was reported that the extracellular pH of tumors is approximately 6.5~7.0, which is lower than that of normal tissues (pH 7.4). The purpose of this research to prepare of novel pH-sensitive poly(amino acid) derivatives as a carrier for paclitaxel and to study their drug release behavior. Amphiphilic polyaspartamide derivatives were synthesized by a successive graft reaction of octaceylamine, O-(2-aminoethyl)-O’-methylpolyethylene glycol, and 1-(3-aminopropyl)imidazole on polysuccinimide, and then a paclitaxel, one of best anti-neoplastic drugs, was loaded into graft copolymers using simple method of controlling pH of polymer solution, and paclitaxel release profile was investigated at various pHs by HPLC method. They also showed high paclitaxel loading efficiency and triggered drug release behavior at acidic pH. Injection of PTX-loaded nano-aggregates into the tail vein of tumor-bearing mice showed superior anti-tumor effect than when formulated with Cremophor EL. These pH-sensitive polymers are a potential candidate for tumor targeting drug delivery carrier which require a triggered release system. |
