Abstract
Two vesicular colloidal carriers, ethosomes® and transfersomes® were proposed for the topical delivery of linoleic acid, an active compound used in the therapeutic treatment of hyperpigmentation disorders, i.e. melasma, which is characterized by an increase of the melanin production in the epidermis. Dynamic light scattering was used for the physicochemical characterization of vesicles and mean size, size distribution and zeta potential were evaluated. The stability of formulations was also evaluated using the Turbiscan Lab® Expert based on the analysis of sample transmittance and photon backscattering. Ethosomes® and transfersomes® were prepared using Phospholipon 100 G®, as the lecithin component, and ethanol and sodium cholate, as edge activator agents, respectively. Linoleic acid at 0.05% and 0.1% (w/v) was used as the active ingredient and entrapped in colloidal vesicles. Technological parameters, i.e. entrapment efficacy, drug release and permeation profiles, were also investigated. Experimental findings showed that physicochemical and technological features of ethosomes® and transfersomes® were influenced by the lipid composition of the carriers. The percutaneous permeation experiments of linoleic acid-loaded ethosomes® and transfersomes® through human stratum corneum-epidermidis membranes showed that both carriers are accumulated in the skin membrane model as a function of their lipid compositions. The findings reported in this investigation showed that both vesicular carriers could represent a potential system for the topical treatment of hyperpigmentation disorders.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
D. Ainbinder, E. Touitou, Drug Deliv 12, 297 (2005)
H. Ando, Y. Funasaka, M. Oka, A. Ohashi, M. Furumura, J. Matsunaga, N. Matsunaga, V.J. Hearing, M. Ichihashi, J Lipid Res 40, 1312 (1999)
E.R. Bendas, M.I. Tadros, AAPS PharmSciTech 8, E107 (2007)
H.A. Benson, Expert Opin. Drug Deliv 3, 727 (2006)
C. Celia, E. Trapasso, D. Cosco, D. Paolino, M. Fresta, Colloids Surf B Biointerfaces 72, 155 (2009)
C. Celia, M.G. Calvagno, D. Paolino, S. Bulotta, C.A. Ventura, D. Russo, M. Fresta, J Nanosci Nanotechnol 8, 2102 (2008)
G. Cevc, Adv Drug Deliv Rev 56, 675 (2004)
G. Cevc, Clin Pharmacokinet 42, 461 (2003)
G. Cevc, D. Gebauer, Biophys J 84, 1010 (2003)
G. Cevc, G. Blume, Biochim Biophys Acta 1514, 191 (2001)
G. Cevc. Patent WO 00/38653; A61K 9/127 (2000)
R. Charlín, C.B. Barcaui, B.K. Kac, D.B. Soares, R. Rabello-Fonseca, L. Azulay-Abulafia, Int J Dermatol 47, 19 (2008)
Y.A. Cho, H.S. Gwak, Drug Dev Ind Pharm 30, 557 (2004)
N. Dayan, E. Touitou, Biomaterials 21, 1879 (2000)
V. Dubey, D. Mishra, N.K. Jain, Eur J Pharm Biopharm 67, 398 (2007)
G.M. El Maghraby, A.C. Williams, B.W. Barry, J Parm Pharmacol 58, 415 (2006)
M.M. Elsayed, G. Cevc, Biochim Biophys Acta 1808, 140 (2011)
G.M. El Zaafarany, G.A. Awad, S.M. Holayel, N.D. Mortada, Int J Pharm 397, 164 (2010)
M. Fresta, G. Puglisi, J Control Release 44, 141 (1997)
M. Fresta, G. Puglisi, J Drug Target 4, 95 (1996)
B. Godin, E. Touitou, J Control Release 94, 365 (2004)
B. Godin, E. Touitou, Curr Drug Deliv 2, 269 (2005)
B. Godin, E. Touitou, Crit Rev Ther Drug Carrier Syst 20, 63 (2003)
A. González-Paredes, M. Manconi, C. Caddeo, A. Ramos-Cormenzana, M. Monteoliva-Sánchez, A.M. Fadda, J Liposome Res 20, 269 (2010)
P.E. Grimes, Arch Dermatol 131, 1453 (1995)
A.K. Gupta, M.D. Gover, K. Nouri, S. Taylor, J Am Acad Dermatol 55, 1048 (2006)
K. Hac-Wydro, K. Jedrzejek, P. Dynarowicz-Łatka, Colloids Surf B Biointerfaces 72, 101 (2009)
C.C. Hedli, N.R. Rao, K.R. Reuhl, C.M. Witmer, R. Snyder, Arch Toxicol 70, 135 (1996)
P.L. Honeywell-Nguyen, S. Arenja, J.A. Bouwstra, Pharm Res 20, 1619 (2003)
P.L. Honeywell-Nguyen, J.A. Bouwstra, J Control Release 86, 145 (2003)
K. Ishiguro, H. Oku, A. Suitani, Y. Yamamoto, Biol Pharm Bull 25, 1655 (2002)
C. Jewell, S. Cusack, K.D. Cashman, Prostaglandins Leukot Essent Fatty Acids 72, 163 (2005)
M.H. Lee, H.J. Kim, D.J. Ha, J.H. Paik, H.Y. Kim, J Korean Med Sci 17, 518 (2002)
S. Leekumjorn, H.J. Cho, Y. Wu, N.T. Wright, A.K. Sum, C. Chan, Biochim Biophys Acta 1788, 1508 (2009)
M. Manconi, C. Sinico, D. Valenti, G. Loy, A.M. Fadda, Int J Pharm 234, 237 (2002)
V. Nikolaou, A.J. Stratigos, A.D. Katsambas, J Cosmet Dermatol 5, 303 (2006)
J.L. O’Donoghue, J Cosmet Dermatol 5, 196 (2006)
D. Paolino, G. Lucania, D. Mardente, F. Alhaique, M. Fresta, J Control Release 106, 99 (2005)
L. Pratsch, A. Herrmann, K. Arnold, Biomed Biochim Acta 43, S85 (1984)
Y. Rao, F. Zheng, X. Zhang, J. Gao, W. Liang, AAPS PharmSciTech 9, 860 (2008)
M.I. Rendon, J Drugs Dermatol 3, S27 (2004)
D. Rigopoulos, S. Gregoriou, A. Katsambas, J Cosmet Dermatol 6, 195 (2007)
M.L. Rogerson, B.H. Robinson, S. Bucak, P. Walde, Colloids Surf B Biointerfaces 48, 24 (2006)
A.C. Rowat, N. Kitson, J.L. Thewalt, Int J Pharm 307, 225 (2006)
P. Santos, A.C. Watkinson, J. Hadgraft, M.E. Lane, Skin Pharmacol Physiol 21, 246 (2008)
A. Schätzlein, G. Cevc, Br J Dermatol 138, 583 (1998)
Y. Shigeta, H. Imanaka, H. Ando, A. Ryu, N. Oku, N. Baba, T. Makino, Skin whitening effect of linoleic acid is enhanced by liposomal formulations. Biol Pharm Bull 27, 591 (2004a)
Y. Shigeta, H. Imanaka, S. Yonezawa, N. Oku, N. Baba, T. Makino, Biol Pharm Bull 27, 879 (2004b)
S.I. Simões, C.M. Marques, M.E. Cruz, G. Cevc, M.B. Martins, Eur J Pharm Biopharm 58, 509 (2004)
C. Sinico, C. Caddeo, D. Valenti, A.M. Fadda, A.R. Bilia, F.F. Vincieri, J Liposome Res 18, 83 (2008)
S.P. Soni, J.A. Ward, S.E. Sen, S.E. Feller, S.R. Wassall, Biochemistry 48, 11097 (2009)
E. Touitou, B. Godin, N. Dayan, C. Weiss, A. Piliponsky, F. Levi-Schaffer, Biomaterials 22, 3053 (2001)
E. Touitou, N. Dayan, L. Bergelson, B. Godin, M. Eliaz, J Control Release 65, 403 (2000)
E. Touitou, Patent WO 95/35095; A61K9/127, 7/00 (1995)
D.D. Verma, S. Verma, G. Blume, A. Fahr, Eur J Pharm Biopharm 55, 271 (2003)
L. Yang, L.K. Leung, Y. Huang, Z.Y. Chen, J Agric Food Chem 48, 3072 (2000)
Acknowledgements
This work was partially supported by XXV M.I.U.R. Ph.D. program financial support in Pharmaceutical Science. The authors are very grateful to Dr. Lynn Whitted for her revision of the language of this paper.
Conflict of interest
The authors declare that they have no conflict of interest. The authors alone are responsible for the content and writing of the paper.
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Celia, C., Cilurzo, F., Trapasso, E. et al. Ethosomes® and transfersomes® containing linoleic acid: physicochemical and technological features of topical drug delivery carriers for the potential treatment of melasma disorders. Biomed Microdevices 14, 119–130 (2012). https://doi.org/10.1007/s10544-011-9590-y
Published:
Issue Date:
DOI: https://doi.org/10.1007/s10544-011-9590-y