微粒子製剤設計とDDS

コアーシェル型高分子ミセルの構造設計とDDSへの応用

抄録

Recently, colloidal carrier systems have been receiving much attention in the field of drug targeting because of their high loading capacity for drugs as well as of their unique disposition characteristics in the body. This paper highlights the utility of polymeric micelles formed through the multimolecular assembly of block copolymers as novel core-shell typed particulates for drug and gene targeting. The process of micellization in aqueous milieu is described in detail based on the differences in the driving force of core segregation, including hydrophobic interaction, electrostatic interaction, metal complexation, and hydrogen bonding of constituent block copolymers. The segregated core embedded in the hydrophilic palisade is shown to function as a reservoir for genes, enzymes, and a variety of drugs with diverse characteristics. Further, the body distribution of polymeric micelles is described to demonstrate their long-circulating characteristics. Focus is placed on the role of the hydrophilic shell in preventing micelles from reticular endothelial recognition, Significant tumor accumulation of polymeric micelles entrapping cytotoxic agents in the core is shown to emphasize their promising utility in tumor-targeting therapy. As an important perspective on carrier systems based on polymeric micelles, their feasibility as non-viral gene vectors is also summarized in this review article.