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Abstract

Phospholipids type, specific molecules and production processes increase the elastic properties of the membrane, making liposomes useful for the percutaneous transport of drugs and cosmetics. Herein we describe the elastic liposomes state-of-the-art technologies, the main elastic liposome systems, the parameters that quantify the membrane elasticity, the rheology of liposomes flowing down narrow capillaries and the possible mechanisms by which the elastic liposomes transport drugs to the deeper layers of the skin. Future perspectives of the conscientious development of elastic liposomes are envisaged.

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References

  1. Dayan, N. (ed.): Skin aging handbook: an integrated approach to biochemistry and product development. William Andrew Inc., Norwich (2008)

    Google Scholar 

  2. American Academy of Pediatrics, committee on drugs 1995 to 1997: Alternative routes of drug administration-advantages and disadvantages (subject review). Pediatrics 100 , 143–152 (1997)

    Google Scholar 

  3. Scheuplein, R.J.: Mechanism of percutaneous absorption. II. Transient diffusion and the relative importance of various routes of skin penetration. Journal of Investigative Dermatology 48, 79–88 (1967)

    CAS  Google Scholar 

  4. Szabó, G.: The number of eccrine sweat glands in human skin. In: Montagna, W., Silver, R.E.A. (eds.) Advances in Biology of Skin. Pergamon Press Inc., New York (1962)

    Google Scholar 

  5. Baroli, B.: Penetration of nanoparticles and nanomaterials in the skin: Fiction or reality? Journal of Pharmaceutical Sciences 99, 21–50 (2010), doi:10.1002/jps.21817

    Article  CAS  Google Scholar 

  6. Lasic, D.D.: Lipossomes: from physics to applications. Elsevier Science Publishers B.V., Amsterdan (1993)

    Google Scholar 

  7. Cevc, G., Gebauer, D.: Hydration-Driven Transport of Deformable Lipid Vesicles through Fine Pores and the Skin Barrier. Biophys. J. 84, 1010–1024 (2003)

    Article  CAS  Google Scholar 

  8. Cevc, G.: Lipid vesicles and other colloids as drug carriers on the skin. Advanced Drug Delivery Reviews 56, 675–711 (2004)

    Article  CAS  Google Scholar 

  9. Cevc, G., Blume, G.: Lipid vesicles penetrate into intact skin owing to the transdermal osmotic gradients and hydration force. Biochimica et Biophysica Acta (BBA) - Biomembranes 1104, 226–232 (1992)

    Article  CAS  Google Scholar 

  10. Cevc, G., Gebauer, D., Stieber, J., Schätzlein, A., Blume, G.: Ultraflexible vesicles, Transfersomes, have an extremely low pore penetration resistance and transport therapeutic amounts of insulin across the intact mammalian skin. Biochimica et Biophysica Acta (BBA) - Biomembranes 1368, 201–215 (1998)

    Article  CAS  Google Scholar 

  11. Cevc, G., Schätzlein, A., Richardsen, H.: Ultradeformable lipid vesicles can penetrate the skin and other semi-permeable barriers unfragmented. Evidence from double label CLSM experiments and direct size measurements. Biochimica et Biophysica Acta (BBA) - Biomembranes 1564, 21–30 (2002)

    Article  CAS  Google Scholar 

  12. Honeywell-Nguyen, P.L., Arenja, S., Bouwstra, J.A.: Skin Penetration and Mechanisms of Action in the Delivery of the D2-Agonist Rotigotine from Surfactant-Based Elastic Vesicle Formulations. Pharmaceutical Research 20, 1619–1625 (2003)

    Article  CAS  Google Scholar 

  13. Honeywell-Nguyen, P.L., Bouwstra, J.A.: Vesicles as a tool for transdermal and dermal delivery. Drug Discovery Today: Technologies 2, 67–74 (2005)

    Article  CAS  Google Scholar 

  14. Honeywell-Nguyen, P.L., Groenink, H.W.W., Bouwstra, J.A.: Elastic Vesicles as a Tool for Dermal and Transdermal Delivery. Journal of Liposome Research 16, 273–280 (2006)

    Article  CAS  Google Scholar 

  15. Lasic, D., Martin, F.: Stealth Liposomes. CRC Press, London (1995)

    Google Scholar 

  16. Lasic, D.D.: The mechanism of vesicle formation. Journal Biochemistry 256, 1–11 (1988)

    CAS  Google Scholar 

  17. Mezei, M., Gulasekharam, V.: Liposomes - a selective drug delivery system for the topical route of administration I. Lotion dosage form. Life Sciences 26, 1473–1477 (1980)

    Article  CAS  Google Scholar 

  18. Elsayed, M., Abdallah, O., Naggar, V., Khalafallah, N.: Lipid vesicles for skin delivery of drugs: Reviewing three decades of research. International Journal of Pharmaceutics 332, 1–16 (2007)

    Article  CAS  Google Scholar 

  19. Elsayed, M.M.A., Abdallah, O.Y., Naggar, V.F., Khalafallah, N.M.: Lipid vesicles for skin delivery of drugs: Reviewing three decades of research. International Journal of Pharmaceutics 332, 1–16 (2007)

    Article  CAS  Google Scholar 

  20. Benson, H.A.E.: Elastic Liposomes for Topical and Transdermal Drug Delivery. Current Drug Delivery 6, 217–226 (2009)

    CAS  Google Scholar 

  21. Cevc, G., Blume, G.: New, highly efficient formulation of diclofenac for the topical, transdermal administration in ultradeformable drug carriers, Transfersomes. Biochimica et Biophysica Acta (BBA) - Biomembranes 1514, 191–205 (2001)

    Article  CAS  Google Scholar 

  22. Cevc, G., Blume, G.: Biological activity and characteristics of triamcinolone-acetonide formulated with the self-regulating drug carriers, Transfersomes®. Biochimica et Biophysica Acta (BBA) - Biomembranes 1614, 156–164 (2003)

    Article  CAS  Google Scholar 

  23. Cevc, G., Schätzlein, A., Blume, G.: Transdermal drug carriers: Basic properties, optimization and transfer efficiency in the case of epicutaneously applied peptides. Journal of Controlled Release 36, 3–16 (1995)

    Article  CAS  Google Scholar 

  24. Cevc, G.: Transdermal Drug Delivery of Insulin with Ultradeformable Carriers. Clinical Pharmacokinetics 42, 461–474 (2003)

    Article  CAS  Google Scholar 

  25. Paul, A., Cevc, G., Bachhawat, B.K.: Transdermal immunization with large proteins by means of ultradeformable drug carriers. European Journal of Immunology 25, 3521–3524 (1995)

    Article  CAS  Google Scholar 

  26. El Maghraby, G.M.M., Williams, A.C., Barry, B.W.: Oestradiol skin delivery from ultradeformable liposomes: refinement of surfactant concentration. International Journal of Pharmaceutics 196, 63–74 (2000)

    Article  Google Scholar 

  27. El Maghraby, G.M.M., Williams, A.C., Barry, B.W.: Skin delivery of 5-fluorouracil from ultradeformable and standard liposomes in-vitro. Journal of Pharmacy and Pharmacology 53, 1069–1077 (2001)

    Article  Google Scholar 

  28. El Maghraby, G.M.M., Williams, A.C., Barry, B.W.: Skin hydration and possible shunt route penetration in controlled estradiol delivery from ultradeformable and standard liposomes. Journal of Pharmacy and Pharmacology 53, 1311–1322 (2001)

    Article  Google Scholar 

  29. Jain, S., Sapre, R., Tiwary, A., Jain, N.: Proultraflexible Lipid Vesicles for Effective Transdermal Delivery of Levonorgestrel: Development, Characterization, and Performance Evaluation. AAPS Pharm. Sci. Tech. 6, E513–E522 (2005)

    Article  Google Scholar 

  30. Trotta, M., Gallarate, M., Carlotti, M.E., Morel, S.: Preparation of griseofulvin nanoparticles from water-dilutable microemulsions. International Journal of Pharmaceutics 254, 235–242 (2003)

    Article  CAS  Google Scholar 

  31. Trotta, M., Peira, E., Carlotti, M.E., Gallarate, M.: Deformable liposomes for dermal administration of methotrexate. International Journal of Pharmaceutics 270, 119–125 (2004)

    Article  CAS  Google Scholar 

  32. Trotta, M., Peira, E., Debernardi, F., Gallarate, M.: Elastic liposomes for skin delivery of dipotassium glycyrrhizinate. International Journal of Pharmaceutics 241, 319–327 (2002)

    Article  CAS  Google Scholar 

  33. Song, Y.-K., Kim, C.-K.: Topical delivery of low-molecular-weight heparin with surface-charged flexible liposomes. Biomaterials 27, 271–280 (2006)

    Article  CAS  Google Scholar 

  34. Kirjavainen, M., Urtti, A., Jääskeläinen, I., Suhonen, T.M., Paronen, P., Valjakka-Koskela, R., Kiesvaara, J., Mönkkönen, J.: Interaction of liposomes with human skin in vitro – the influence of lipid composition and structure. Biochimica et Biophysica Acta (BBA) - Lipids and Lipid Metabolism 1304, 179–189 (1996)

    Article  CAS  Google Scholar 

  35. van den Bergh, B.A.I., Bouwstra, J.A., Junginger, H.E., Wertz, P.W.: Elasticity of vesicles affects hairless mouse skin structure and permeability. Journal of Controlled Release 62, 367–379 (1999)

    Article  Google Scholar 

  36. van den Bergh, B.A.I., Salomons-de Vries, I., Bouwstra, J.A.: Interactions between liposomes and human stratum corneum studied by freeze-substitution electron microscopy. International Journal of Pharmaceutics 167, 57–67 (1998)

    Article  Google Scholar 

  37. van den Bergh, B.A.I., Vroom, J., Gerritsen, H., Junginger, H.E., Bouwstra, J.A.: Interactions of elastic and rigid vesicles with human skin in vitro: electron microscopy and two-photon excitation microscopy. Biochimica et Biophysica Acta (BBA) - Biomembranes 1461, 155–173 (1999)

    Article  Google Scholar 

  38. van den Bergh, B.A.I., Wertz, P.W., Junginger, H.E., Bouwstra, J.A.: Elasticity of vesicles assessed by electron spin resonance, electron microscopy and extrusion measurements. International Journal of Pharmaceutics 217, 13–24 (2001)

    Article  Google Scholar 

  39. El Maghraby, G.M.M., Williams, A.C., Barry, B.W.: Interactions of surfactants (edge activators) and skin penetration enhancers with liposomes. International Journal of Pharmaceutics 276, 143–161 (2004)

    Article  Google Scholar 

  40. Honeywell-Nguyen, P.L., Frederik, P.M., Bomans, P.H.H., Junginger, H.E., Bouwstra, J.A.: Transdermal Delivery of Pergolide from Surfactant-Based Elastic and Rigid Vesicles: Characterization and in Vitro Transport Studies. Pharmaceutical Research 19, 991–997 (2002)

    Article  CAS  Google Scholar 

  41. van Hal, D.A., Jeremiasse, E., de Vringer, T., Junginger, H.E., Bouwstra, J.A.: Encapsulation of lidocaine base and hydrochloride into non-ionic surfactant vesicles (NSVs) and diffusion through human stratum corneum in vitro. European Journal of Pharmaceutical Sciences 4, 147–157 (1996)

    Article  Google Scholar 

  42. Nugroho, A.K., Li, G., Grossklaus, A., Danhof, M., Bouwstra, J.A.: Transdermal iontophoresis of rotigotine: influence of concentration, temperature and current density in human skin in vitro. Journal of Controlled Release 96, 159–167 (2004)

    Article  CAS  Google Scholar 

  43. Touitou, E., Alkabes, M., Dayan, N.: Ethosomes: novel lipid vesicular system for enhanced delivery. Pharmaceutics Research, 305–306 (1997)

    Google Scholar 

  44. Touitou, E., Dayan, N., Bergelson, L., Godin, B., Eliaz, M.: Ethosomes - novel vesicular carriers for enhanced delivery: characterization and skin penetration properties. Journal of Controlled Release 65, 403–418 (2000)

    Article  CAS  Google Scholar 

  45. Touitou, E., Godin, B., Dayan, N., Weiss, C., Piliponsky, A., Levi-Schaffer, F.: Intracellular delivery mediated by an ethosomal carrier. Biomaterials 22, 3053–3059 (2001)

    Article  CAS  Google Scholar 

  46. Touitou, E., Godin, B., Weiss, C.: Enhanced delivery of drugs into and across the skin by ethosomal carriers. Drug Development Research 50, 406–415 (2000)

    Article  CAS  Google Scholar 

  47. Elsayed, M.M.A., Abdallah, O.Y., Naggar, V.F., Khalafallah, N.M.: Deformable liposomes and ethosomes: Mechanism of enhanced skin delivery. International Journal of Pharmaceutics 322, 60–66 (2006)

    Article  CAS  Google Scholar 

  48. Helfrich, W.: Elastic properties of lipid bilayers: theory and possible experiments. Z. Naturforsch. 28c, 693–703 (1973)

    Google Scholar 

  49. Jones, D.A.: The important of surface area/volume ratio to the rate of oxygen uptake by red cells. Journal of General Physiology 74, 643–646 (1979)

    Article  CAS  Google Scholar 

  50. Noguchi, H., Gompper, G.: Shape transitions of fluid vesicles and red blood cells in capillary flows. Proceedings of the National Academy of Sciences of the United States of America 102, 14159–14164 (2005), doi:10.1073/pnas.0504243102

    Article  CAS  Google Scholar 

  51. Parker, K., Winlove, C.: The deformation of spherical vesicles with permeable, constant-area membranes: application to the red blood cell. Biophysical Journal 77, 3096–3107 (1999)

    Article  CAS  Google Scholar 

  52. Pamplona, D., Calladine, C.: The mechanics of axially symmetric liposomes. Journal of Biomechanical Engineering 115, 149–159 (1993)

    Article  CAS  Google Scholar 

  53. Egbaria, K., Ramachandran, C., Weiner, N.: Topical Delivery of Ciclosporin: Evaluation of Various Formulations Using in vitro Diffusion Studies in Hairless Mouse Skin. Skin Pharmacology and Physiology 3, 21–28 (1990)

    Article  CAS  Google Scholar 

  54. Schreier, H., Bouwstra, J.: Liposomes and niosomes as topical drug carriers: dermal and transdermal drug delivery. Journal of Controlled Release 30, 1–15 (1994)

    Article  CAS  Google Scholar 

  55. Egbaria, K., Ramachandran, C., Kittayanond, D., Weiner, N.: Topical delivery of liposomally encapsulated interferon evaluated by in vitro diffusion studies. Antimicrob. Agents Chemother. 34, 107–110 (1990), doi:10.1128/aac

    CAS  Google Scholar 

  56. Marsh, D.: Elastic curvature constants of lipid monolayers and bilayers. Chemistry and Physics of Lipids 144, 146–159 (2006)

    Article  CAS  Google Scholar 

  57. Rawicz, W., Olbrich, K.C., McIntosh, T., Needham, D., Evans, E.: Effect of Chain Length and Unsaturation on Elasticity of Lipid Bilayers  79, 328–339 (2000)

    Google Scholar 

  58. Hristova, K., Needham, D.: Phase behavior of a lipid/polymerlipid mixture in aqueous medium. Macromolecules 28, 991–1002 (1995)

    Article  CAS  Google Scholar 

  59. Marsh, D.: Elastic Constants of Polymer-Grafted Lipid Membranes  81, 2154–2162 (2001)

    Google Scholar 

  60. Bouwstra, J.A., Honeywell-Nguyen, P.L.: Skin structure and mode of action of vesicles. Advanced Drug Delivery Reviews 54, S41–S55 (2002)

    Article  Google Scholar 

  61. Williams, A.C.: Transdermal and Topical Drug Delivery, 1st edn., London (2003)

    Google Scholar 

  62. El Maghraby, G.M.M., Williams, A.C., Barry, B.W.: Can drug-bearing liposomes penetrate intact skin? Journal of Pharmacy and Pharmacology 58, 415–429 (2006)

    Article  Google Scholar 

  63. Kirjavainen, M., Urtti, A., Jääskeläinen, I., Marjukka Suhonen, T., Paronen, P., Valjakka-Koskela, R., Kiesvaara, J., Mönkkönen, J.: Interaction of liposomes with human skin in vitro – The influence of lipid composition and structure. Biochimica et Biophysica Acta (BBA) - Lipids and Lipid Metabolism 1304, 179–189 (1996)

    Article  CAS  Google Scholar 

  64. Trotta, M.P.E., Debernardi, F., Gallarate, M.: Elastic liposomes for skin delivery of dipotassium glycyrrhizinate. International Journal of Pharmaceutics 241, 319–327 (2002)

    Article  CAS  Google Scholar 

  65. Honeywell-Nguyen, P.L., Bouwstra, J.A.: The in vitro transport of pergolide from surfactant-based elastic vesicles through human skin: a suggested mechanism of action. Journal of Controlled Release 86, 145–156 (2003)

    Article  CAS  Google Scholar 

  66. Yamashita, F., Hashida, M.: Mechanistic and empirical modeling of skin permeation of drugs. Advanced Drug Delivery Reviews 55, 1185–1199 (2003)

    Article  CAS  Google Scholar 

  67. Flynn, G.: Physicochemical determinants of skin absorption; in principles of route-to-route extrapolation in risk assessment. In: Henry, G.T.R.C.J. (ed.) Principles of Route to-route Extrapolation in Risk Assessment. Elsevier, New York (1990)

    Google Scholar 

  68. Potts, R.O., Guy, R.H.: Predicting Skin Permeability. Pharmaceutical Research 9, 663–669 (1992), doi:10.1023/a:1015810312465

    Article  CAS  Google Scholar 

  69. Abraham, M., Chadha, H., Mitchell, R.: The factors that influence skin penetration of solutes. Journal of Pharmaceutical Pharmacology 47, 8–16 (1995)

    CAS  Google Scholar 

  70. Roberts, M., Cross, S., Anissimov, Y.: Mathematical models in percutaneous absorption in Percutaneous Absorption drugs-cosmetics-mechanisms-methodology. In: Bronaugh, R.L., Maibach, H.I. (eds.) Percutaneous Absorption. Marcel Dekker, New York (2005)

    Google Scholar 

  71. Cevc, G., Blume, G., Schätzlein, A.: Transfersomes-mediated transepidermal delivery improves the regio-specificity and biological activity of corticosteroids in vivo. Journal of Controlled Release 45, 211–226 (1997)

    Article  CAS  Google Scholar 

  72. Cevc, G., Blume, G.: Hydrocortisone and dexamethasone in very deformable drug carriers have increased biological potency, prolonged effect, and reduced therapeutic dosage. Biochimica et Biophysica Acta (BBA) - Biomembranes 1663, 61–73 (2004)

    Article  CAS  Google Scholar 

  73. Cevc, G., Schatzlein, A.G., Richardsen, H., Vierl, U.: Overcoming Semipermeable Barriers, Such as the Skin, with Ultradeformable Mixed Lipid Vesicles, Transfersomes, Liposomes, or Mixed Lipid Micelles. Langmuir 19, 10753–10763 (2003)

    Article  CAS  Google Scholar 

  74. Bruinsma, R.: Rheology and shape transitions of vesicles under capillary flow. Physica A: Statistical and Theoretical Physics 234, 249–270 (1996)

    Article  Google Scholar 

  75. Frisken, B.J., Asman, C., Patty, P.J.: Studies of Vesicle Extrusion. Langmuir 16, 928–933 (2000), doi:10.1021/la9905113

    Article  CAS  Google Scholar 

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Santana, M.H.A., Zanchetta, B. (2011). Elastic Liposomes. In: Beck, R., Guterres, S., Pohlmann, A. (eds) Nanocosmetics and Nanomedicines. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-19792-5_7

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