壳聚糖基阳离子胶束用于共负载两种不同性质药物的研究

以季胺化壳聚糖-O-聚己内酯(TMC-PCL)胶束为载体,用于共负载2种不同亲疏水性质的抗肿瘤物质,阿霉素和吲哚菁绿；并研究了胶束包埋对吲哚菁绿的稳定性和光热效应的影响,以及阿霉素从胶束中的释放行为.结果表明,2种抗肿瘤物质在TMC-PCL胶束中的实际载药量均可达20％,且包封率超过85％.进一步还用MTT法评价了不同载药胶束体系对肿瘤细胞的杀灭作用,发现共负载胶束经近红外激光辐照后,对肿瘤细胞的毒性远高于单载药体系.

CHITOSAN-BASED CATIONIC MICELLES FOR CO-INCORPORATION OF TWO TYPES OF DRUGS WITH DISTINCT HYDROPHILICITY

Trimethylated chitosan-O-poly(ε-caprolactone)(TMC-PCL) micelles were used as nanocarriers for co-loading of two types of drugs with distinct hydrophilicity,including FDA-approved near-infrared(NIR) photosensitizer,indocyanine green(ICG) and a first-line anti-cancer drug,doxorubicin(DOX).Both two agents could be incorporated within the micelles with entrapment efficiency of more than 85% and loading content of up to 20%.The loading content could be adjusted by varying feed ratio of the agents to the micelles.A red-shift in absorption peak of ICG from 780 nm to 800 nm was observed upon incorporation in to the micelles.The competitive binding of the micelles to ICG molecules also increased the momoner/dimer ratio of ICG.TMC-PCL micelles showed an excellent ICG retention ability,and only 18.18% of ICG was leaked from micelles after 48 hours incubation in physiological media.In addition,the incorporation of ICG within the micelles enhanced its thermal and optical stability.ICG-loaded micelles(ICG-micelles) exhibited higher heating capacity than free ICG.DOX release behavior was affected by the temperature,while the presence of ICG within the micelles had little effect on DOX release.The cytotoxicity of the dual-agent-loaded micelles towards HepG2 cells was found to be higher than that of single-agent-loaded counterparts.