Deformable (Transfersome®) vesicles for improved drug delivery into and through the skin

Percutaneous Penetration Enhancers Chemical Methods in Penetration Enhancement: Nanocarriers

Volumn , Issue , 2016, Pages 39-59

  Cevc, Gregor ^a   Chopra, Amla ^b  

^a The Advanced Treatments Institute   (Germany)

^b DAYALBAGH EDUCATIONAL INSTITUTE   (India)

Author keywords

[No Author keywords available]

Indexed keywords

AGGREGATES; CONTROLLED DRUG DELIVERY; DEFORMATION; HYDROPHILICITY; MOLECULES; PHOSPHOLIPIDS; SURFACE ACTIVE AGENTS;

AGGREGATE STABILITY; BIOLOGICAL VALUES; COMPOSITION CHANGES; ELASTIC LIPOSOMES; SECONDARY BARRIERS; SURFACE HYDROPHILICITY; THERAPEUTIC AGENTS; TRANSCUTANEOUS DELIVERY;

TARGETED DRUG DELIVERY;

EID: 84960310244     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1007/978-3-662-47862-2_3     Document Type: Chapter

References (78)

1. Aguilella V, Kontturi K, Murtomäki L, Ramirez P (1994) Estimation of the pore size and charge density in human cadaver skin. J Contr Rel 32: 249-257.
2. Bal V, McIndoe A, Denton G, Hudson D, Lombardi G, Lamb J, Lechler R (1990) Antigen presentation by keratinocytes induces tolerance in human T cells. Eur J Immunol 20(9): 1893-1897.
3. Bouwstra JA, Honeywell-Nguyen PL (2002) Skin structure and mode of action of vesicles. Adv Drug Deliv Rev 54(Suppl 1): 41-55.
4. Bouwstra JA, Honeywell-Nguyen PL, Gooris GS, Ponec M (2003) Structure of the skin barrier and its modulation by vesicular formulations. Progr Lipid Res 42(1): 1-36.
5. Brewer J, Bloksgaard M, Kubiak J, Sorensen J, Bagatolli LA (2013) Spatially resolved two-color diffusion measurements in human skin applied to transdermal liposome penetration. J Invest Dermatol 133(5): 1260-1268.
6. Cevc G (1992) Preparation for drug application in minute droplet form. PCT/EP91/01596.
7. Cevc G (1996) Transfersomes®, liposomes and other lipid dispersions on the skin: permeation enhancement, vesicle penetration and transdermal drug delivery. Crit Rev Ther Drug Carrier Syst 13: 257-388.
8. Cevc G (1997) Drug delivery across the skin. Exp Opin Invest Drugs 6: 1887-1937.
9. Cevc G (2003) Transdermal drug delivery of insulin with deformable carriers, Transfersomes®. Clin Pharmacokin 42: 461-474.
10. Cevc G (2004) Lipid vesicles and other colloids as drug carriers on the skin. Adv Drug Del Rev 56: 675-711.
11. Cevc G (2012a) Rational design of new product candidates: the next generation of highly deformable bilayer vesicles for noninvasive, targeted therapy. J Contr Rel 160: 135-146.
12. Cevc G (2012b) Optimised preparations of highly adaptable aggregates. PCT/EP2012/055040.
13. Cevc G (2012c) Drug-free compositions and methods for diminishing peripheral inflammation and pain. PCT/EP2012/055039.
14. Cevc G, Blume G (2001) New, highly efficient formulation of diclofenac for the topical, transdermal administration in deformable drug carriers, Transfersomes. Biochim Biophys Acta 1514: 191-205.
15. Cevc G, Blume G (2003) Biological activity and characteristics of triamcinolone-acetonide formulated with the self-regulating drug carriers, Transfersomes®. Biochim Biophys Acta 1614: 156-164.
16. Cevc G, Blume G (2004) Hydrocortisone and dexamethasone in ultra-deformable drug carriers, Transfersomes®, have an increased biological potency and reduced therapeutic dosages. Biochim Biophys Acta 1663: 61-73.
17. Cevc G, Gebauer D (2003) Hydration driven transport of deformable lipid vesicles through fine pores and the skin barrier. Biophys J 84: 1010-1024.
18. Cevc G, Vierl U (2003) Aggregates with increased deformability, comprising at least three amphipats for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin. PCT/EP03/11202.
19. Cevc G, Vierl U (2004) NSAID formulations, based on highly adaptable aggregates, for improved transport through barriers and topical drug delivery. US 2004/0071767.
20. Cevc G, Vierl U (2007) Spatial distribution of cutaneous microvasculature and local drug clearance after drug application on the skin. J Contr Rel 118: 18-26.
21. Cevc G, Vierl U (2010) Nanotechnology and the transdermal route. A state of the art review and critical appraisal. J Contr Rel 141: 277-299.
22. Cevc G, Blume G, Schätzlein A (1997) Transfersomes mediated transepidermal delivery improves the regio-specificity and biological activity of corticosteroids in vivo. J Contr Rel 45: 211-226.
23. Cevc G, Gebauer D, Stieber J, Schätzlein A, Blume G (1998) Ultraflexible vesicles, Transfersomes®, have an extremely low pore penetration resistance and transport therapeutic amounts of insulin across the intact mammalian skin. Biochim Biophys Acta 1368: 201-215.
24. Cevc G, Schätzlein A, Richardsen H (2002) Ultradeformable lipid vesicles can penetrate the skin and other semi-permeable barriers intact. Evidence from double label CLSM experiments and direct size measurements. Biochim Biophys Acta 1564: 21-30.
25. Cevc G, Schätzlein A, Richardsen H, Vierl U (2003) Overcoming semi-permeable barriers, such as the skin, with deformable mixed lipid vesicles, Transfersomes®, liposomes or mixed lipid micelles. Langmuir 19: 10753-10763.
26. Cevc G, Mazgareanu S, Rother M (2008a) Preclinical characterisation of NSAIDs in ultradeformable carriers or conventional topical gels. Int J Pharm 360: 29-39.
27. Cevc G, Mazgareanu S, Rother M, Vierl U (2008b) Occlusion effect on transcutaneous NSAID delivery from conventional and carrier-based formulations. Int J Pharm 359: 190-197.
28. Chopra A, Cevc G (2014) Non-invasive, epicutaneous immunisation with toxoid in deformable vesicles protects mice against tetanus, chiefly owing to a Th2 response. Eur J Pharm Sci 56: 55-64.
29. Cleary GW (2011) Microneedles for drug delivery. Pharm Res 28(1): 1-6.
30. Conaghan PG, Dickson J, Bolten W, Cevc G, Rother M (2013) A multicentre, randomised, placebo-and active-controlled trial comparing the efficacy and safety of topical ketoprofen in Transfersome gel (IDEA-033) with ketoprofen-free vehicle (TDT 064) and oral celecoxib for knee pain associated with osteoarthritis. Rheum Res 52(7): 1303-1312.
31. du Plessis WN, Müller JDG (1994) The influence of in vivo treatment of skin with liposomes on the topical absorption of a hydrophilic and a hydrophobic drug in vitro. Int J Pharm 103: R1-R5.
32. Dubey V, Mishra D, Dutta T, Nahar M, Saraf DK, Jain NK (2007) Dermal and transdermal delivery of an anti-psoriatic agent via ethanolic liposomes. J Contr Rel 123(2): 148-154.
33. Elsayed MMA, Cevc G (2011a) Turbidity spectroscopy for characterization of submicroscopic drug carriers, such as nanoparticles and lipid vesicles: size determination. Pharm Res 28: 2204-2222.
34. Elsayed MMA, Cevc G (2011b) The vesicle-to-micelle transformation of phospholipid-cholate mixed aggregates: a state of the art analysis including membrane curvature effects. Biochim Biophys Acta 1808: 140-153.
35. Escobar-Chávez JJ, Bonilla-Martínez D, Villegas-González MA, Molina-Trinidad E, Casas-Alancaster N, Revilla-Vázquez AL (2011) Microneedles: a valuable physical enhancer to increase transdermal drug delivery. J Clin Pharmacol 51(7): 964-977.
36. Fesq H, Gloeckner A, Abeck D, Ring J, Lehmann J, Rother M, Cevc G (2003) Improved risk-benefit ratio for a triamcinolone acetonide Transfersome® formulation in comparison to a commercial triamcinolone acetonide formulation. Br J Dermatol 149: 611-619.
37. Glenn GM, Scharton-Kersten T, Vassell R, Mallet CP, Hale TL, Alving CR (1998) Transcutaneous immunisation with Cholera toxoid protects mice against lethal mucosal toxoid challenge. J Immunol 161: 3211-3214.
38. Godin B, Touitou E (2003) Ethosomes: new prospects in transdermal delivery. Crit Rev Ther Drug Carrier Syst 20: 63-102.
39. Gompper G, Kroll DM (1995) Driven transport of fluid vesicles through narrow pores. Phys Rev E Stat Phys Plasmas Fluids Relat Interdiscip Topics 52: 4198-4208.
40. Guo J, Ping Q, Zhang L (2000) Transdermal delivery of insulin in mice by using lecithin vesicles as a carrier. Drug Deliv 7: 113-116.
41. Hadgraft J, Lane ME (2006) Passive transdermal drug delivery systems: recent considerations and advances. Am J Drug Del 4: 153-160.
42. Handjani RM, Ribier A, Vanlerberghe G, Zabotto A, Griat J (1989) Cosmetic and pharmaceutical compositions containing niosomes and a water soluble polyamide, and a process for preparing these compositions. USP 4830857.
43. Hofland HFJ, Bouwstra JA, Bodde HE, Spies S, Junginger HE (1989) Non-ionic surfactant vesicles in transdermal formulation: controlled release and in vitro effect on human skin. Pharm Res 6: S178.
44. Hofland HFJ, Vander Geest R, Bouwstra JA, Bodde HE, Junginger HE (1994) Estradiol permeation from non-ionic surfactant vesicles through human stratum corneum in vitro. Pharm Res 11: 659-664.
45. Honeywell-Nguyen PL, de Graaff AM, Wouter Groenink HW, Bouwstra JA (2002) The in vivo and in vitro interactions of elastic and rigid vesicles with human skin. Biochim Biophys Acta 1573: 130-140.
46. Honeywell-Nguyen PL, Groenink HW, Bouwstra J (2006) Elastic vesicles as a tool for dermal and transdermal delivery. J Liposome Res 16: 273-280.
47. Kneer W, Rother I, Rother M, Seidel E (2009) A multiple-dose, open-label, safety, compliance, and usage evaluation study of epicutaneously applied Diractin® (ketoprofen in Transfersome®) in joint/musculoskeletal pain or soft tissue inflammation. Curr Drug Saf 4: 5-10.
48. Levin G (2008) Advances in radio-frequency transdermal drug delivery. Pharmaceutic Technol 32(4): s12-s19.
49. Mezei ML (1985) Liposomes as a skin drug delivery system. In: Breimer DD, Speiser P (eds) Topics in pharmaceutical sciences. Elsevier, Amsterdam, pp 345-358.
50. Mezei M, Gulasekharam V (1980) Liposomes: a selective drug delivery system for the topical route of administration. 1. Lotion dosage form. Life Sci 26: 1473-1477.
51. Mezei M, Gulasekharam V (1982) Liposomes: a selective drug delivery system for the topical route of administration: gel dosage form. J Pharm Pharmacol 34: 473-474.
52. Mikszta JA, Laurent PE (2008) Cutaneous delivery of prophylactic and therapeutic vaccines: historical perspective and future outlook. Expert Rev Vaccines 7(9): 1329-1339.
53. Mohammed J, Gunderson AJ, Khong H-H, Koubek RD, Udey MC, Glick AB (2013) TGFb1 overexpression by keratinocytes alters skin dendritic cell homeostasis and enhances contact hypersensitivity. J Invest Dermatol 133: 135-143.
54. Paul A, Cevc G (1995) Non-invasive administration of protein antigens. Epicutaneous immunization with the bovine serum albumin. Vaccine Res 4: 145-164.
55. Paul A, Cevc G, Bachhawat BK (1995) Transdermal immunization with large proteins by means of ultradeformable drug carriers. Eur J Immunol 25: 3521-3524.
56. Prausnitz MR (2004) Microneedles for transdermal drug delivery. Adv Drug Del Rev 56: 581-587.
57. Prausnitz MR, Langer R (2008) Transdermal drug delivery. Nat Biotechnol 26(11): 1261-1268.
58. Randolph GJ, Angeli V, Swartz MA (2005) Dendritic-cell trafficking to lymph nodes through lymphatic vessels. Nature Rev Immunol 5: 617-628.
59. Reddy ST, van der Vlies AJ, Simeoni E, Angeli V, Randolph GJ, O'Neil CP, Lee LK, Swartz MA (2007) Exploiting lymphatic transport and complement activation in nanoparticle vaccines. Nature Biotechnol 25: 1159-1164.
60. Rother M, Lavins BJ, Kneer W, Lehnhardt K, Seidel EJ, Mazgareanu S (2007) Efficacy and safety of epicutaneous ketoprofen in Transfersome (IDEA-033) versus oral celecoxib and placebo in osteoarthritis of the knee: multicentre randomised controlled trial. Ann Rheum Dis 66: 1178-1183.
61. Rother M, Seidel EJ, Clarkson PM, Mazgareanu S, Vierl U, Rother I (2009) Efficacy of epicutaneous Diractin® (ketoprofen in Transfersome® gel) for the treatment of pain related to eccentric muscle contractions. Drug Des Devel Ther 3: 143-149.
62. Schaefer P, Bewick-Sonntag C, Capri MG, Berardesca E (2002) Physiological changes in skin barrier function in relation to occlusion level, exposure time and climatic conditions. Skin Pharmacol Appl Skin Physiol 15: 7-19.
63. Schätzlein A, Cevc G (1998) Non-uniform cellular packing of the stratum corneum and permeability barrier function on intact skin: a high-resolution confocal laser microscopy study using highly deformable vesicles (Transfersomes®). Brit J Dermatol 138: 583-592.
64. Schreier H, Bouwstra J (1994) Liposomes and niosomes as topical drug carriers: dermal and transdermal drug delivery. J Contr Rel 30: 1-15.
65. Simões SI, Marques CM, Cruz MEM, Cevc G, Martins MBF (2004) Cholate effect on solubilisation and permeability of simple and protein loaded phosphatidylcholine/sodium cholate mixed aggregates designed to mediate macromolecules transdermal delivery. Eur J Pharm Biopharm 58: 509-519.
66. Simões SI, Delgado TC, Lopes RM, Jesus S, Ferreira AA, Morais JA, Cruz ME, Corvo ML, Martins MB (2005a) Developments in the rat adjuvant arthritis model and its use in therapeutic evaluation of novel non-invasive treatment by SOD in Transfersomes. J Contr Rel 103: 419-434.
67. Simões SI, Tapadas JM, Marques CM, Cruz MEM, Martins MBF, Cevc G (2005b) Permeabilisation and solubilisation of soybean phosphatidylcholine bilayer vesicles, as membrane models, by polysorbate, Tween 80. Eur J Pharm Sci 26: 307-317.
68. Simões S, Marques C, Cruz ME, Martins MB (2009) Anti-inflammatory effects of locally applied enzyme-loaded ultradeformable vesicles on an acute cutaneous model. J Microencapsul 26: 649-658.
69. Sugita K, Kabashima K, Atarashi K, Shimauchi T, Kobayashi M, Tokura Y (2006) Innate immunity mediated by epidermal keratinocytes promotes acquired immunity involving Langerhans cells and T cells in the skin. Clin Exp Immunol 147: 176-183.
70. Udey MC (2012) Epidermal Langerhans cells tune skin reactivity to contact allergens. J Clin Invest 122(5): 1602-1605.
71. van den Bergh BAI, Vroom J, Gerritsen H, Junginger HE, Bouwstra JA (1999) Interactions of elastic and rigid vesicles with human skin in vitro: electron microscopy. Biochim Biophys Acta 1461: 155-173.
72. van Kuijk-Meuwissen ME, Junginger HE, Bouwstra JA (1998) Interactions between liposomes and human skin in vitro, a confocal laser scanning microscopy study. Biochim Biophys Acta 1371: 31-39.
73. Verma DD, Verma S, Blume G, Fahr A (2003) Particle size of liposomes influences dermal delivery of substances into skin. Int J Pharm 258(1): 141-151.
74. Vierl U, Löbbecke L, Nagel N, Cevc G (1994) Solute effects on the colloidal and phase behavior of lipid bilayer membranes: ethanol-dipalmitoylphosphatidylcholine mixtures. Biophys J 67: 1067-1079.
75. Wachter C, Vierl U, Cevc G (2008) Adaptability and elasticity of the mixed lipid bilayer vesicles containing non-ionic surfactant designed for targeted drug delivery across the skin. J Drug Target 16: 611-625.
76. Warner RR, Lilly NA (1994) Correlation of water content with ultrastructure in the stratum corneum, Bioengineering of the skin. In: Water and the stratum corneum. CRC Press, Boca Raton, pp 3-12.
77. Warner RR, Boissy Y, Lilly N, Spears M, McKillop K, Marshall J, Stone K (1999) Water disrupts stratum corneum lipid lamellae: damage is similar to surfactants. J Invest Dermatol 113(6): 960-966.
78. Warner RR, Stone KJ, Boissy YL (2003) Hydration disrupts human stratum corneum ultrastructure. J Invest Dermatol 120: 275-284.