5-FLUORORACIL LOADING AND RELEASING BEHAVIOR FROM ALKYLATED POLYAMIDOAMINE G3.0 DENDRIMER-FOLATE
In recent years, many researches have been developing towards biocompatible improvement and cellular penetrating ability of dendrimers in order to use in diagnosis and treatment therapy for several type of cancer. In this study, to enhance biocompatibility, drug loading efficiency and cellular uptake of the polyamidoamine dendrimer, the dendrimer generation 3.0 (G 3.0) was conjugated with hexanoyl chloride and targeted with acid folic (G3.0-C6-FA). The structure of the G3.0-C6-FA was determined by 1H-NMR. According to 1H-NMR spectra, 9 hexanoyl groups and 2 folate groups were attached to the G3.0 dendrimer. TEM image of G3.0-C6 dendrimer exhibited spherical shape and nano sizes ranging from 3 to 4 nm and TEM image of the G3.0-C6-FA indicated a size distribution ranging from 5 to 7 nm. In addition, Fluorouracil (5-FU)-loaded G3.0 and 5-FU-loaded G3.0-C6-FA were also prepared to evaluate drug loading efficiency was using High-performance liquid chromatography (HPLC). The obtained results indicated that drug loading efficiency of G3.0-C6-FA (13,8% of 5-FU) is higher than G3.0 (11% of 5-FU). 5- G3.0-C6-FA also showed a slow release profile of the drug. These positive results show a potential of the drug-nanocarrier system in practical application.
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