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Combination Therapy Research of Curcumin Micellar Prodrug Encapsulated with Paclitaxel
Name : Qi Zhang
No. : 2011213027
Tutor : Zheng Wang
Contents
Introduction
Proposals
Current experiment
Schedules for the next stage
References
Introduction
O O
OH
OO
HO
Curcumin
Advantages: antioxidant \ antitumor activity low toxicity \ less adverse reactions
Disadvantages: unstable \ low water solubility low bioavailability
NH
O
O
O
HOO
O
OO
O
O
OH
O
O
OH
Paclitaxel
Advantages: high antitumor activities
Disadvantages: severe side effect low water solubility
Proposal
Micelle formation
Characterization
Drug loading and releasing
Investigation on stability
In vitro antitumor activity
Current experiment
H3CO
OHnMPEG2000
H3CO
n O
O
oHm
H3CO
n O
Oo
m
O
OOH
H3CO
n O
Oo
m
O
ONH OH
OH
OH
O OO
OOHO
OO
OHH3C
On O
O
om
O
ONH
OO
O Cur
CurCur
1H-NMR
• MPEG-PLA-Tris-Cur 图
接枝率 : 1.95 左右
Micelle formation
dialysis
Self-assemble Paclitaxel(different ratio)
MPEG-PLA-Tris-curcumin micelle
MPEG-PLA-Tris-curcumin/pax micelle
15 : 1 10 : 1.510 : 210 : 3
TEM
Void micelle
Size
Sample Size
空白胶束 98.6
载体 /胶束( 15/1) 107.4
载体 /胶束( 10/1.5) 108.7
载体 /胶束( 10/2) 116.8
载体 /胶束( 10/3) 124.9
Schedules for the next stage
Drug loading and releasing
Investigation on stability
In vitro antitumor activity
References
• Y. Q. Shen, E. Jin, et al., Prodrugs forming high drug-loading multifunctional nanocapsules for cancer intracellular drug delivery , J. Am. Chem. Soc. 2010, 132: 4259–4265.
• H. D. Tang, C. J. Murphy, B. Zhang, et al., Amphiphilic curcumin conjugate-forming nanoparticles as anticancer prodrug and drug carriers: in vitro and in vivo effects, Nanomedicine 2010, 5(6): 855-865.
• Y. Qiao, P. S. Rong, D. Zhuo, Preparation and properties of self-assemble paclitaxel-loaded core-shell type nano-micelles, Acta Pharmaceutica Sinica 2008, 43(4): 408-414.
• X. F. Zhang, Y. X. Li, X. S. Chen, et al., Synthesis and characterization of the paclitaxel/MPEG-PLA block copolymer conjugate, Biomaterials 2005, 26: 2121-2128
• Z. Ma, A. Haddadi, et al., Micelles of poly(ethylene oxide)-b-poly(e-caprolactone) as vehicles for the solubilization, stabilization,and controlled delivery of curcumin, Journal of Biomedical Materials 2007, 10: 301-310.