DEVELOPMENT OF PH-RESPONSIVE NANOPARTICLES AND USE OF PH-RESPONSIVE NANOPARTICLES FOR PREPARING ENHANCED TUMOR PERMEATION AND UPTAKE OF ANTICANCER DRUGS
The present invention relates a pH-responsive nanoparticles which includes amphiphilic block copolymers and poly lactic-co-glycolic acid (PLGA). The amphiphilic block copolymers further includes polyethylene glycol (PEG) derivatives and Histidine derivatives. By the coating of the block amphiphilic copolymers on the surface of hydrophobic core composed of anti-cancer drugs or contrast agents or photothermal agents or metallic nanoparticles or a combination thereof, the pH-responsive nanoparticles for enhanced tumor penetration was attained. The physiochemical characterization of the pH-responsive nanoparticles demonstrates that the pH-responsive nanoparticles effectively promote cellar uptake in weak acidic environment and damage tumor cells.本發明是關於一種酸鹼應答型奈米微粒,由酸鹼應答型高分子材料以及聚乳酸烴基乙酸共聚物(PLGA)於水相中,透過疏水性作用力互相聚集而形成,其中該雙性高分子包含聚乙二醇(PEG)衍生物以及組胺酸(Histidine)衍生物。該酸鹼應答型奈米微粒之疏水核心區可包載化療藥物、光熱藥劑、顯影劑、奈米金屬粒子或其組合,而透過該酸鹼應答型奈米微粒本身特殊的物化特性,使其能在腫瘤組織微酸環境中大量累積並有效被癌細胞胞飲與滲透至腫瘤深層區域,進而顯著抑制腫瘤生長。
