Enhancement of transdermal delivery of docetaxel by surfactant-ethanolic liposomes

doi:10.5246/jcps.2011.05.059

Abstract

Abstract: One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present study, we developed a surfactant-ethanolic liposomal system to improve the transdermal delivery of docetaxel (DTX), a model drug for high molecular weight and poorly water-soluble drugs. Surfactant-ethanolic liposomes (SEL) were composed of phospholipids, ethanol, sodium cholate, DTX and PBS which were prepared by thin film dispersion method. The developed formulations were characterized by determining the vesicle shape and surface morphology, size and size distribution, entrapment efficiency and drug loading capacity. The effects of the developed formulations on the permeation of DTX across rat skin in vitro were investigated using the modified Franz diffusion cell under both occlusive and non-occlusive application conditions. The DTX SELs with optimum composition (phospholipid–surfactant, 85:15, w/w) provided a significantly higher steady-state amount of flux and cumulative permeation, compared to the tranditional liposomes, surfactant liposomes and ethanolic liposomes. The optimal SELs exhibited stable vesicle size, morphology and drug loading capacity. Our results indicated that SELs were promising carriers to enhance the transdermal delivery of DTX.

Key words: Surfactant-ethanolic liposomes, Transdermal delivery, Docetaxel, Permeation study

CLC Number:

R943.43

Supporting:

Yu-Qin Qiu, Shuang Li, Fang Li, Suo-Hui Zhang, Yun-Hua Gao^*

. Enhancement of transdermal delivery of docetaxel by surfactant-ethanolic liposomes[J]. , DOI: 10.5246/jcps.2011.05.059.

References

[1] Guy, R.H.; Hadgraft, J. Transdermal drug delivery, in Drugs and the Pharmaceutical Sciences (Swarbrick, J. Ed.), Vol 123. New York: Marcel Dekker. 2003, 1-23.
[2] Bos, J.D.; Meinardi, M.M.H.M. Exp. Dermatol. 2000, 9, 165-169.
[3] Barry, B.W. Eur. J. Pharm. Sci. 2001, 14, 101-114.
[4] Elsayed, M.M.A.; Abdallah, O.Y.; Naggar, V.F.; Khalafallah, N.M. Int. J. Pharm. 2007, 332, 1-16.
[5] Touitou, E.; Dayan, N.; Bergelson, L.; Godin, B.; Eliaz, M. J. Control. Release. 2000, 65, 403-418.
[6] Suwakul, W.; Ongpipattanakul, B.; Vardhanabhuti, N. J. Liposome Res. 2006, 16, 391-401.
[7] Cevc, G.; Blume, G. Biochim. Biophys. Acta. 1992, 1104, 226-232.
[8] Cevc, G.; Schatzlein, A.; Blume, G. J. Control. Release. 1995, 36, 3-16.
[9] Cevc, G.; Blume, G.; Schatzlein, A. J. Control. Release. 1997, 45, 211-226.
[10] Dayan, N.; Touitou, E. Biomaterials. 2000, 21, 1879-1885.
[11] Bendas, E.R.; Tadros, M.I. AAPS PharmSciTech. 2007, 8, E1-E8.
[12] Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Guide for the Care and Use of Laboratory Animals (National Academy Press, Washington, D.C. 1996).
[13] Panchagnula, R.; Desu, H.; Jain, A.; Khandavilli, S. J. Pharm. Sci. 2004, 93, 2177-2183.
[14] Trotta, M.; Peira, E.; Debernardi, F.; Gallarate, M. Int. J. Pharm. 2002, 241, 319-327.
[15] Cevc, G. Adv. Drug Deliv. Rev. 2004, 56, 675-711.
[16] El Maghraby, G.M.M.; Williams, A.C.; Barry, B.W. Int. J. Pharm. 2000, 196, 63-74.
[17] Kirjavainen, M.; Urtti, A.; Jaaskelainen, I.; Suhonen, T.M.; Paronen, P.; Koskela, R.V.; Kiesvaara, J.; Monkkonen, J. Biochim. Biophys. Acta. 1996, 1304, 179-189.
[18] Williams, A.C.; Barry, B.W. Adv. Drug Deliv. Rev. 2004, 56, 603-618.
[19] Immordino, M.L.; Brusa, P.; Arpicco, S.; Stella, B.; Dosio, F.; Cattel, L. J. Control. Release. 2003, 91, 417-429.