Preparation and anti-MDR tumors study of folate and TPGS dual-modified DSPE-PEG micelles loaded with docetaxel

doi:10.5246/jcps.2015.07.054

Abstract

Abstract:

Multidrug resistance (MDR) operated by P-glycoprotein (P-gp) is one of the major causes in the treatment failure of cancers. In this work,docetaxel-loaded mixed micelles comprised of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy(polyethylene-glycol)₂₀₀₀ (DSPE-PEG₂₀₀₀),D-α-Tocopherylpolyethylene glycol 1000 succinate (TPGS₁₀₀₀) and DSPE-PEG₂₀₀₀-folate were developed to overcome MDR and reduce the side effect of docetaxel in cancer therapy. The diameters of micelles ranged from 13 to 26 nm and the encapsulation efficiencies were all above 85%. The influences of DSPE-PEG₂₀₀₀ and TPGS₁₀₀₀ ratios on the micellar characteristics and anti-resistant tumors effects were evaluated. Micelles with high TPGS₁₀₀₀ amount showed an increased cellular uptake and stronger cytotoxicity against MDR KBv cells. Moreover, the micelles modified by targeting ligand of folic acid exhibited better antitumor effect on folate receptor over-expressing KBv cells.The study provides a method for overcoming MDR in cancer therapy.

Key words: Micelles, Multidrug resistance, Preparation, DSPE-PEG, TPGS, Folate

CLC Number:

R944

Supporting:

Aiting Wang, Shuwen Tong, Xin Hu, Xianrong Qi. Preparation and anti-MDR tumors study of folate and TPGS dual-modified DSPE-PEG micelles loaded with docetaxel[J]. Journal of Chinese Pharmaceutical Sciences, 2015, 24(7): 419-426.

References

[1] Ganguly, A.; Banerjee, K.; Chakraborty, P.; Das, S.; Sarkar, A.; Hazra, A.; Banerjee, M.; Maity, A. Chatterjee, M.; Mondal, N.B.; Choudhuri, S.K. Biomed. Pharmacother. 2011, 65, 387-394.

[2] Batrakova, E.V.; Li, S.; Brynskikh, A.M.; Sharma, A.K.; Li, Y.L.; Boska, M.; Gong, N.; Mosley, R.L.; Alakhov, V.Y.; Gendelman, H.E.; Kabanov, A.V. J. Control. Release. 2010, 143, 290-301.

[3] Krishna, R.; Mayer, L.D. Eur. J. Pharm. Sci. 2000, 11, 265-283.

[4] Li-Blatter, X.C.; Nervi, P.; Seelig, A. BBA-Biomembranes. 2009, 1788, 2335-2344.

[5] Nervi, P.; Li-Blatter, X.C.; Aanismaa, P.; Seelig, A. BBA-Biomembranes. 2010, 1798, 515-525.

[6] Sikic, B.I.; Fisher, G.A.; Lum, B.L.; Halsey, J.; Beketic-Oreskovic, L.; Chen, G. Cancer Chemother. Pharm. 1997, 40, S13-S19.

[7] Coley, H.M. Multi-Drug Resistance in Cancer, Methods in Molecular Biology. 2010, 596, 341-358.

[8] Jakate, A.S.; Einhaus, C.M.; DeAnglis, A.P.; Retzinger, G.S.; Desai, P.B. Cancer Res. 2003, 63, 7314-7320.

[9] Bissery, M.C. Eur. J. Cancer. 1995, 31A, S1-S6.

[10] Izquierdo, M.A.; Garcia, M.; Ponton, J.L.; Martinez, M.; Valenti, V.; Navarro, M.; Gil, M.; Gardenal, F.; Mesia, R.; Perez, X.; Salazar, R.; Germa-Lluch, J.R. Eur. J. Cancer. 2006, 42, 1789-1796.

[11] Elsabahy, M.; Perron, M.E.; Bertrand, N.; Yu, G.; Leroux, J.C. Biomacromolecules. 2007, 8, 2250-2257.

[12] Liu, J.B.; Zahedi, P.; Zeng, F.Q.; Allen, C. J. Pharm. Sci. 2008, 97, 3274-3290.

[13] Cesur, H.; Rubinstein, I.; Pai, A.; Onyuksel, H. Nanomed-Nanotechnol. 2009, 5, 178-183.

[14] Tong, S.W.; Xiang, B.; Dong, D.W.; Qi, X.R. Int. J. Pharm. 2012, 434, 413-419.

[15] Cao, N.; Feng, S.S. Biomaterials. 2008, 29, 3856-3865.

[16] Collnot, E.M.; Baldes, C.; Wempe, M.F.; Hyatt, J.; Navarro, L.; Edgar, K.J.; Schaefer, U.F.; Lehr, C.M. J. Control. Release. 2006, 111, 35-40.

[17] Park, E.K.; Kim, S.Y.; Lee, S.B.; Lee, Y.M. J. Control. Release. 2005, 109, 158-168.

[18] Han, X.; Liu, J.; Liu, M.; Xie, C.; Zhan, C.Y.; Gu, B.; Liu, Y. Int. J. Pharm. 2009, 372, 125-131.

[19] Wu, J.; Liu, Q.; Lee, R.J. Int. J. Pharm. 2006, 316, 148-153.

[20] Gao, W.; Xiang, B.; Meng, T.T.; Liu, F.; Qi, X.R. Biomaterials. 2013, 34, 4137-4149.

[21] Photos, P.J.; Bacakova, L.; Discher, B.; Bates, F.S.; Discher, D.E. J. Control. Release. 2003, 90, 323-334.

[22] Wang, A.T.; Liang, D.S.; Liu, Y.J.; Qi, X.R. Biomaterials. 2015, 53, 160-172.

[23] Liu, B.R.; Yang, M.; Li, R.T.; Ding, Y.T.; Qian, X.P.; Yu, L.X.; Jiang, X.Q. Eur. J. Pharm. Biopharm. 2008, 69, 527-534.

[24] Meaden, E.R.; Hoggard, P.G.; Khoo, S.H.; Back, D.J. J. Immunol. Methods. 2002, 262, 159-165.

[25] Fiskus, W.; Rao, R.; Fernandez, P.; Herger, B.; Yang, Y.H.; Chen, J.G.; Kolhe, R.; Mandawat, A.; Wang, Y.C.; Joshi, R.; Eaton, K.; Lee, P.; Atadja, P.; Peiper, S.; Bhalla, K. Blood. 2008, 112, 2896-2905.

[26] Mu, C.F.; Balakrishnan, P.; Cui, F.D.; Yin, Y.M.; Lee, Y.B.; Choi, H.G.; Yong, C.S.; Chung, S.J.; Shim, C.K.; Kim, D.D. Biomaterials. 2010, 31, 2371-2379.

[27] Wang, X.; Wang, Y.G.; Chen, X.M.; Wang, J.C.; Zhang, X.; Zhang, Q. J. Control. Release. 2009, 139, 56-62.

[28] Bae, Y.H.; Park, K. J. Control. Release. 2011, 153, 198-205.

[29] Gill, K.K.; Kaddoumi, A.; Nazzal, S. Eur. J. Pharm. Sci. 2012, 46, 64-71.

[30] Sawant, R.R.; Sawant, R.M.; Torchilin, V.P. Eur. J. Pharm. Biopharm. 2008, 70, 51-57.

[31] Mu, L.; Elbayoumi, T.A.; Torchilin, V.P. Int. J. Pharm. 2005, 306, 142-149.

[32] Wang, Y.Z.; Fan, W.; Dai, X.; Katragadda, U.; Mckinley, D.; Teng, Q.; Tan, C. Mol. Pharm. 2014, 11, 1140-1150.

[33] Minko, T.; Batrakova, E.V.; Li, S.; Li, Y.L.; Pakunlu, R.I.; Alakhov, V.Y.; Kabanov, A.V. J. Control. Release. 2005, 105, 269-278.

[34] Barz, M.; Arminan, A.; Canal, F.; Wolf, F.; Koynov, K.; Frey, H.; Zentel, R.; Vicent, M.J. J. Control. Release. 2012, 163, 63-74.

[35] Rege, B.D.; Kao, J.P.Y.; Polli, J.E. Eur. J. Pharm. Sci. 2002, 16, 237-246.

[36] Collnot, E.M.; Baldes, C.; Wempe, M.F.; Kappl, R.; Huttermann, J.; Hyatt, J.A.; Edgar, K.J.; Schaefer, U.F.; Lehr, C.M. Mol. Pharm.2007, 4, 465-474.

[37] Collnot, E.M.; Baldes, C.; Schaefer, U.F.; Edgar, K.J.; Wempe, M.F.; Lehr, C.M. Mol. Pharm. 2010, 7, 642-651.

[38] Li, H.Y.; Miao, X.P.; Hou, M. West China Med. J. 2008, 23, 1226-1227.

[39] Mi, Y.; Liu, Y.T.; Feng, S.S. Biomaterials. 2011, 32, 4058-4066.

[40] Neuzil, J.; Dyason, J.C.; Freeman, R.; Dong, L.F.; Prochazka, L.; Wang, X.F.; Scheffler, I.; Ralph, S.J. J. Bioenerg. Biomembr. 2007, 39, 65-72.

[41] Quin, J.; Engle, D.; Litwiller, A.; Peralta, E.; Grasch, A.; Boley, T.; Hazelrigg, S. J. Surg. Res. 2005, 127, 139-143.

[42] Zhao, S.; Tan, S.W.; Guo, Y.Y.; Huang, J.; Chu, M.; Liu, H.D.; Zhang, Z.P. Biomacromolecules. 2013, 14, 2636-2646.