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The enhancement of intracellular delivery of anti-cancer
drugs by the Tat peptide
Jin-Feng Zhao, Jing Wang, Ji-Yao Chen
Introduction
So far, the studies on intracellular delivery of CPPs for macromolecules with the noncovalent manner mainly
concentrated on the transportation of DNA, RNA and proteins, far few works
can be found on drug delivery particularly for the anti-cancer drugs. The aim of this work is to expand the
noncovalent linkage of CPPs with anticancer drugs to enhance the intracellular delivery, because the intracellular
delivery is the key step of the drug to kill the cancer cells. The Tat peptide, a frequently used CPP derived from the
HIV-1 Tat protein, was used in this
work. The doxorubicin (DOX), the sulfonated aluminum phthalocyanine (AlPcS) and the quantum
dots (QDs) were selected as the anti-cancer drugs to be delivered.
Experimental
Results
1. The enhancement of intracellular delivery of anti-cancer drugs
3. The statistical data of
enhancements of
drugs-Tat
Figure 1. (a) AlPcS,
(b)AlPcS+tat, FL images of Pcs in
KB cells. Pcs’s concentration:
6uM/ml, drug-culture time: 1 h.
Figure 2. (a) QDs, (b)QDs+tat,
FL images of Pcs in KB cells.
QDs’s concentration: 0.2uM/ml,
drug-culture time:0.5 h.
2. The
mechanism of
transport
enhancement
Figure 5. The statistical data of enhancements of drugs-Tat
on cellular uptakes in KB and Hela cells concluded from a
series of imaging measurements.
Figure 3. (a) AlPcS+tat, 40C, (b)AlPcS+tat, 370C in KB cells.
Figure 4. (a) QDs+tat, 40C,
(b)QDs+tat, 370C in KB cells
References
[1] Lee HJ. Pharmaceuticals. 2010; 1-16.
[2] Thoren EG, Persson D, Isakson P, Goksor M, Onfelt A and
Norden B. Biochem. Biophys. Res. Commun. 2003;307:100–
107.
Conclusion
1. The enhancement of intracellular
delivery of anti-cancer drugs by the Tat
peptide.
2. The transport enhancement of these
anticancer drugs by the Tat is
whether going through an enhanced
endocytotic process.