Macromolecular HPMA-based nanoparticles with cholesterol for solid-tumor targeting: detailed study of the inner structure of a highly efficient drug delivery system.

摘要: We report a rigorous investigation into the detailed structure of nanoparticles already shown to be successful drug delivery nanocarriers. The basic conjugates consists an N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer bearing anticancer doxorubicin (Dox) bound via pH-sensitive hydrazone bond and defined amount cholesterol moieties that vary in hydrophobicity. results show size, anisotropy, aggregation number Naggr grows with increasing content. From ab initio calculations, we conclude most probable HPMA copolymer–cholesterol is pearl necklace structure, where ellipsoidal pearls mainly composed are covered by shell; connected bridges hydrophilic chains. Using combination techniques, unambiguously Dox not impregnated inside core but instead uniformly distributed acr...