Their History and Characteristics

Polymeric micelles that are prepared from amphiphilic block or graft copolymers with a spherical core and a shell with a carrier size of 10-100 nm have been undergoing investigation since 1984 and have been studied more actively since 1990.25-27 The term block refers to the linear architecture of the copolymer in which the end of one segment is covalently joined to the head of the other segment to give a diblock AB type (Figure 4.1) or multiple block (ABn) type copolymers. On the other hand, graft copolymers have a comb-like structure with hydrophilic segments attached on the side of the cationic segments. Although the influence of the copolymer architecture on biological activity has not yet been clarified, both block and graft copolymers can form polymeric micelles because of their amphiphilic character. Interactions between the polymer chains that serve as the driving force for micelle formation include hydrophobic, electrostatic, and p-p interactions and hydrogen bonding. Because hydrophobic drugs can be stably trapped in the hydrophobic core of the polymeric micelles and exhibit water-solubility, polymeric micelles are attractive carriers for hydrophobic drugs. Moreover, electrostatic (ionic) interactions involving the hydrophilic surface of polymeric micelles may also be applicable to macromolecules possessing many electrostatic (ionic) charges, e.g., DNA.28

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