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The Preparation of Folate-targeted Carboxymethyl-β-cyclodextrin Nanocomposites Loaded with Cisplatin and Its Evaluation of Inhibitory Effect on Nasopharyngeal Carcinoma in vitro
Liu Tao1, Ma Dong2, Ke Bo3, Xie Minqiang1*
1Department of Otolaryngology, Zhujiang Hospital, Southern Medical University, Guangzhou 510282, China; 2Department of Medical Engineering, Jinan University, Guangzhou 510630, China; 3Jiangxi Key Laboratory of Hematological Oncology
Abstract: In order to achieve targeted chemotherapy for NPC， FA-CM-β-CD-CDDP nanocomposites
was prepared by amidation reaction and ligand coupling technology in this research. The concentration of CDDP，
concentration of FA， morphology and particle size of nanocomposites were detected by OPDA colourimetry， UV
spectroscopy， transmission electron microscopy and laser particle detector， respectively. The phagocytic effects
of NPC FR expressing positive HNE-1 cells and FR expressing negative CNE-2 cells on FA-CM-β-CD-CDDP
coupling with FITC were observed using fluorescence microscope and the concentration of CDDP in cells was
detected by OPDA colourimetry. The effects of nanocomposites on HNE-1 cells proliferation and apoptosis were
measured with MTT， colony forming experiment and flow cytometry. Results showed that concentration of FA and
CDDP coupled with nanocomposites were 340 μg/mL and 2 mg/mL， respectively， and the encapsulation efficiency
of CDDP was 20.00%. FA-CM-β-CD-CDDP nanocomposites was in uniform dispersion， and its average particle
size was 157.8 nm. More FITC was seen in HNE-1 cells， concentration of CDDP in cells was 6.24 ng/mL， but less
FITC was seen in CNE-2 cells， and concentration of CDDP in cells was only 2.01 ng/mL. The growth inhibiting ratio
of HNE-1 cells in FA-CM-β-CD-CDDP group was significantly increased compared to control group (CM-β-CDCDDP)
after cells were treated for 24 h. IC50 (4.80 μg/mL) of CDDP in FA-CM-β-CD-CDDP group was significantly
decreased compared to control group (6.97 μg/mL). Cell growth inhibition rate of the two groups all were above
80% when the final concentration of CDDP of the two kinds of nanocomposites reached 16.00 μg/mL， and cell growth inhibition rate of the two groups had no significant difference after 48 h. Colony forming rate (33.21%) of HNE-1 cells in FA-CM-β-CD-CDDP group was significantly lower than that of control group (52.27%) when the final concentration of CDDP in two groups were 1.00 μg/mL， and apoptosis rates of HNE-1 cells in FA-CM-β-CDCDDP group (12.65% and 22.35%， respectively) were significantly higher than that of control group (6.91% and 14.21%， respectively) when the final concentration of CDDP both were 0.25 μg/mL and 1.00 μg/mL respectively after cells were treated for 24 h. The results showed that constructed FA-CM-β-CD-CDDP nanocomposites can targeted to inhibit FR expressing positive NPC cells proliferation and promote their apoptosis.
was prepared by amidation reaction and ligand coupling technology in this research. The concentration of CDDP，
concentration of FA， morphology and particle size of nanocomposites were detected by OPDA colourimetry， UV
spectroscopy， transmission electron microscopy and laser particle detector， respectively. The phagocytic effects
of NPC FR expressing positive HNE-1 cells and FR expressing negative CNE-2 cells on FA-CM-β-CD-CDDP
coupling with FITC were observed using fluorescence microscope and the concentration of CDDP in cells was
detected by OPDA colourimetry. The effects of nanocomposites on HNE-1 cells proliferation and apoptosis were
measured with MTT， colony forming experiment and flow cytometry. Results showed that concentration of FA and
CDDP coupled with nanocomposites were 340 μg/mL and 2 mg/mL， respectively， and the encapsulation efficiency
of CDDP was 20.00%. FA-CM-β-CD-CDDP nanocomposites was in uniform dispersion， and its average particle
size was 157.8 nm. More FITC was seen in HNE-1 cells， concentration of CDDP in cells was 6.24 ng/mL， but less
FITC was seen in CNE-2 cells， and concentration of CDDP in cells was only 2.01 ng/mL. The growth inhibiting ratio
of HNE-1 cells in FA-CM-β-CD-CDDP group was significantly increased compared to control group (CM-β-CDCDDP)
after cells were treated for 24 h. IC50 (4.80 μg/mL) of CDDP in FA-CM-β-CD-CDDP group was significantly
decreased compared to control group (6.97 μg/mL). Cell growth inhibition rate of the two groups all were above
80% when the final concentration of CDDP of the two kinds of nanocomposites reached 16.00 μg/mL， and cell growth inhibition rate of the two groups had no significant difference after 48 h. Colony forming rate (33.21%) of HNE-1 cells in FA-CM-β-CD-CDDP group was significantly lower than that of control group (52.27%) when the final concentration of CDDP in two groups were 1.00 μg/mL， and apoptosis rates of HNE-1 cells in FA-CM-β-CDCDDP group (12.65% and 22.35%， respectively) were significantly higher than that of control group (6.91% and 14.21%， respectively) when the final concentration of CDDP both were 0.25 μg/mL and 1.00 μg/mL respectively after cells were treated for 24 h. The results showed that constructed FA-CM-β-CD-CDDP nanocomposites can targeted to inhibit FR expressing positive NPC cells proliferation and promote their apoptosis.
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