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.