Park, Jae Hyung Cho, Yong Woo Son, Yoen Ju Kim, Kwangmeyung Chung, Hesson Jeong, Seo Young Choi, Kuiwon Park, Chong Rae Park, Rang-Woon Kim, In-San Kwon, Ick Chan 2024-01-21T03:31:40Z 2024-01-21T03:31:40Z 2021-09-01 2006-04 0303-402X https://pubs.kist.re.kr/handle/201004/135637 An anthracycline drug, adriamycin, was chemically conjugated onto the backbone of glycol chitosan via an acid-labile cis-aconityl linkage. The physicochemical characteristics of the glycol chitosan-adriamycin (GC-ADR) conjugates were investigated by dynamic light scattering, atomic force microscopy, and fluorescence spectroscopy. The GC-ADR conjugates were capable of fort-ning nano-sized self-aggregates in an aqueous medium, when the adriamycin content in the conjugate was in the range of 2.0-5.0 wt.%. The self-aggregates were spherical in shape, and had mean diameters of 238-304 nm, depending on the adriamycin content. The critical aggregation concentrations of the conjugates, estimated by the fluorescence quenching method, were as low as 1.0-2.5 x 10(-2) mg/ml. The size of self-aggregates was not affected by the polymer concentration m the range from 50 to 2,000 mu g/ml, and was maintained up to 8 days in phosphate-buffered saline (pH 7.4), indicating high colloidal stability. The release of adriamycin from self-aggregates was significantly dependent on the pH of the medium due to the cis-aconityl linkage; e.g., the amount of adriamycin released for 4 days was 7.3 +/- 0.3% at pH 7, whereas it was 29.3 +/- 1.9% at pH 4. The cell viability results demonstrated that free adriamycin shows more potent cytotoxicity than the conjugates, primarily attributed to the sustained release of adriamycin from self-aggregates. In conclusion, the self-aggregates, formed by GC-ADR conjugates, might be useful for the site-specific delivery of adriamycin in a sustained manner. English SPRINGER POLYION COMPLEX MICELLES PH-SENSITIVE LINKAGE POLYMERIC MICELLES IN-VITRO PHYSICOCHEMICAL CHARACTERISTICS MACROMOLECULAR THERAPEUTICS HYDROGEL NANOPARTICLES ANTITUMOR EFFICACY BLOCK-COPOLYMERS DOXORUBICIN Preparation and characterization of self-assembled nanoparticles based on glycol chitosan bearing adriamycin Article 10.1007/s00396-005-1438-7 1 COLLOID AND POLYMER SCIENCE, v.284, no.7, pp.763 - 770 COLLOID AND POLYMER SCIENCE 284 7 763 770 scie scopus 000237946100008 2-s2.0-33745183292 Chemistry, Physical Polymer Science Chemistry Polymer Science Article POLYION COMPLEX MICELLES PH-SENSITIVE LINKAGE POLYMERIC MICELLES IN-VITRO PHYSICOCHEMICAL CHARACTERISTICS MACROMOLECULAR THERAPEUTICS HYDROGEL NANOPARTICLES ANTITUMOR EFFICACY BLOCK-COPOLYMERS DOXORUBICIN glycol chitosan adriamycin self-aggregates sustained release cytotoxicity