Membranas no Estudo de Permeação Cutânea
publicado em 01/04/2000
Patrícia Santos Lopes
Faculdade de Ciências Farmacêuticas e Bioquímicas Oswaldo Cruz, São Paulo SP
Profª Dra. Telma Mary Kaneko
Departamento de Farmácia, Faculdade de Ciências Farmacêuticas da Universidade de São Paulo, São Paulo SP
Vários estudos têm sido realizados para determinar a melhor alternativa para simular o comportamento da pele humana quanto à permeação. Neste artigo, as autoras revisam os principais experimentos realizados.
Many studies has being perfomed to determine the best alternative to simulate the human skin behavior before the permeation. In this paper, the authors review the principal experiments already performed.
Vários estudios tienen sido realizados para determinación de la mejor alternativa de simulacción del comportaminelo de la piel humana con respecto a la permeacción. En ese articulo, los autores revisan los principales experimentos realizados.
A pele é o mais pesado dos órgãos do corpo humano, Interage com as mucosas do trato respiratório, digestivo e urogenital, formando uma cápsula, que separa a parte interna do corpo do ambiente externo. Esta estrutura flexível e auto regenerativa defende os fluidos internos e os tecidos vivos contra as variações de temperatura, umidade radiação e poluição. Este tegumento não apenas protege fisicamente os órgãos internos e limita a passagem de substâncias, mas também regula a temperatura e pressão sanguínea, agindo nos sistemas circulatório e na evaporação. A pele media as sensações do tato, dor, calor e frio, expressa a vermelhidão da raiva e embaraço, o suor da ansiedade e a palidez do medo, além de identificar as características de cabelo, textura, odor e cor particulares de cada indivíduo.1,2 Este órgão ainda sintetiza e metaboliza substâncias, tendo como uma das suas funções secretar compostos.3
Como a pele é o mais acessível dos tecidos humanos, é facilmente danificada, tanto física, química ou biologicamente. Frequentemente é exposta a abrasões, solventes orgânicos, detergentes, resíduos químicos, poluentes e produtos que podem ser alergênicos, produzidos por bactérias, fungos, leveduras e plantas.
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1. Barry BW. Dermatological formulations: percutaneous absorption. New York: Marcel Dekker. 1983. v. 18, cap. 1. p. 1-48.
2. Shah VP, Maibach Hl. Topical drug bioavailability, bioequivalence and penetration. New York: Plenum Press, 1993. 453p.
3. Bentley MVLB. Desenvolvimento de produtos dermatológicos contendo corticosteroides: avaliação da liberação e penetração transcutânea por metodologia in vitro. São Paulo, 1994. 155p. (Tese de Doutorado - Faculdade de Ciências Farmacêuticas - USP).
4. Martin A. Bustamante P. Physical pharmacy: physical chemical principles in the pharmaceutical sciences. 4ed., Philadelphia: Lea & Febiger, 1993. cap.13. p. 324-349.
5. Block LH. Medicated Applications. In Gennaro AR, ed. Remington's pharmaceutical sciences. 18ed., Easton: Mack 1990. cap 84. p 1596-1602.
6. Huang Y, Wu S, Wang C. Responses Surface Method: A Novel Strategy to Optimize Iontophoretic Transdermal Delivery of Thyrotropin-realasing Hormone, Pharm. Res. 13 547-552, 1996.
7. Santi P, Guy RH. Reverse iontophoresis - parameters determining electro-osmotic flow. II Electrode chamber formulation, J Controlled Release 42 29-36, 1996.
8. Vanbever R, Boulengé E, Préat, V. Transdermal Delivery of Fentanyl by Electroporation 1. Influence of Electrical Factors, Pharm Res. 13 559-565, 1996.
9. Zhang I, Shung, KK, Edwards DA. Hydrogels with Enhanced Mass Transfer for Transdermal Drug Delivery. J. Pharm. Sci. 85 1312-1316, 1996.
10. Henry S, McAllister DV, Allari MG, Prausnitz MR. Microfabricated Microneedles: A Novel Approach to Transdermal Drug Delivery. J Pharsi Sci 87 922 925, 1998.
11. Godwin DA, Michniak BB, Creek KE. Evaluation of transdermal Penetration Enhancers Using A Novel Skin Alternative. J Pharm Sci 86 1001-05, 1997.
12. Skelly JP, Shah VP, Maibach Hl. Guy RH, Wester RC, Flynn G, Yacobi A. FDA and AAPS Report of the Workshop on Principles and Practices of In Vitro Percutaneous Penetration Studies: Relevance to Bioavailability and Bioequivalence, Pharma Res 4 265-267, 1987.
13. Shah VP, Flynn GL, Guy RH, Maibach HL, Schaefer H, Skelly JP, Wester RC, Yacobi A. In Vivo Percutaneous Penetration / Absorption, Washington DC, May 1989, Pharm Res 8 1071-1075, 1991.
14. Regnier M, Caron D. Reichert U, Schaefer H. Barrier function of human skin and human reconstructed epidermis, J Pharm Sci 82 404-407, 1993.
15. Hadgraft J, Walters KA, Wotton PK. Facilitated percutaneous absorption: a comparison and evaluation of two in vitro models. Int J Pharm 32 257-263, 1986.
16. Maltani Y, Shimada K, Nagai T. Menthol, Oleic Acid and Lauricidin in Absorption Enhancement of Free and Sodium Salt of Diclofenac Using Ethanol Treated Silicone Membrane as Model for Skin. Chem Pharm Bull 44 403-408, 1996.
17. Kennedy AH, Golden GM, Gay CL, Guy RH, Francoeur ML, Mak VHW. Stratum Corneum Lipids of Human Epidermal Keratinocytes Air-Liquid Cultures: Implications for Barrier Function. Pharm Res 13 1162-1167. 1996.
18. Rolland A De Michelis G. Influence of Formulation, Receptor Fluid, and Occlusion, on In Vitro Drug Release from Topical Dosages Forms, Using an Automated Flow-Though Diffusion Cell. Pharm Res 9 82-86, 1992.
19. Yamaguchi Y, Usami T, Natsume H, Aoyagi T, Nagase Y, Sugibayashi K, Morimoto Y. Evaluation of Skin Permeability of Drugs by Newly Prepared Polymer Membranes. Chem Pharm Bull 45 537-541, 1997.
20. Priborsky J. Muhlbachová E. Evaluation of in vitro percutaneous absorption across human skin and in animal models. J Pharm Pharmacol 7 468-472, 1990.
21. Montagna W, Carlisle K. Structural Changes in Human Skin. Invest Dermatol 73 47-53, 1979.
22. Marzulli FN, Maibach Hl. Dermatotoxicology. In: Monteiro Riviere, NA Anatomical factors affecting barrier function, 5ed. Washington: Taylor & Francis, 1996. p.3-33.
23. Brounagh RL, Stewart RF, Congdon ER. Methods for in vitro percutaneous absorption studies II: Animal models for human skin. Toxicol Appl Pharmacol 62 481-488, 1982.
24. Kraelin MEK, Lipicky RJ, Bronaugh RL. Metabolism of Benzocaine during Percutaneous Absorption in the Hairless Guinea Pig: Acetylbenzocaine Formation and Activity. Skin Pharmacol 9 221-230, 1996.
25. Kitagawa S, Hosokai A, Kaseda Y, Yamamoto N, Karieku Y, Matsuoka E. Permeability of benzoic acid derivatives in excised guinea pig dorsal skin and effects of L-menthol, Int J Pharm 161 115-122, 1998.
26. Naito S, Tsai Y. Percutaneous absorption of indomethacin from ointment bases in rabbits. Int J Pharm 8 263-278, 1981.
27. Niazy EM. Influence of oleic acid and other permeation promoters on transdermal delivery of dihydroergotamine through rabbit skin. Int J Pharm 67 97-100, 1991.
28. Wu PC, Huang YB, Fang JY. Tsai YH. Percutaneous Absorption of Captopril from Hydrophilic Cellulose Derivatives through Excised Rabbit Skin and Human Skin. Drug Develop Ind Phari 24 179-182, 1998.
29. Porzio S, Caselli G, Pellegrini L, Pallottini V, Rosario M, Coppola A, Boltri L, Gentile M, Clavenna G, Melillo G. Efficacy of a new topical gel-spray formulation of ketoprofen Lysine salt in the rat: Percutaneous permeation in vitro and in vivo and pharmacological activity. Pharma Res 37 41-47. 1998.
30. Seki T, Kawaguchi T, Sugibayashi K, Juni K, Morimoto Y. Percutaneous absorption of azidothymidine in rats. Int J Pharm 57 73-75, 1989.
31. Bando H, Mohri S, Yamashita F, Takakura Y, Hashida M. Effects of Skin Metabolism on Percutaneous Penetration of Lipophilic Drugs. J Pharm Sci 8G 759-61, 1997.
32. Sazaki H, Kojima M, Mori Y, Nakamura J, Shibazaki J. Enhancing effect of pyrrolidone derivatives on transdermal drug delivery. II. Effect of application concentration and pretreatment of onhancer. Int J Pharm 60 177-183, 1990.
33. Sazaki H, Kojima M, Mori Y, Nakamura J, Shibazaki J. Enhancing effect of pyrrolidone darivatives on transdermal drug delivery. I. In J Pharm 44 15-24, 1988.
34. Roper CS, Howes D, Blain PG, Willians FM, Percutaneous Penetration of 2-Phenoxyethanol through Rat and Human Skin. Food Chem Toxic 35 1009-1016, 1997.
35. Ho HO, Huang FC, Sokoloski TD, Sheu MT. The Influence of Cosolvents on the In-vitro Percutaneous Penetration of Diclofenac Sodium from a Gel System. J Pharm Pharmacol 46 636-642, 1994.
36. Cappel MJ, Kreuter J. Effect of nonionic surfactants on transdermal drugs delivery. I: Polysorbates. Int J Pharm 69 143-153, 1991.
37. Sarpotdar PP, Zatz JL. Evaluation of Penetration Enhancement of Lidocaine by Nonionic Surfactants Though Hairless Mouse Skin In Vitro. J Pharm Sci 75 176-181, 1986.
38. Elyan BM, Sidhom MB, Plakogiannis FM. Evaluation of the Effect of Different Fatty Acids on the Percutaneous Absorption of Metaproterenol Sulfate. J Pharm Sci 85 101-105, 1996.
39. Chow DSL, Kaka , Wang Ti. Concentration-dependent enhancement of 1-dodecylazacycloheptan-2-one, on the percutaneous penetration kinetics of triancinolone acetonide. J Pharn Sci 73 1794-1799, 1984.
40. Tsai JC, Guy RH, Thornfeld CR, Gao WN, Feingold KR, Elias PM. Metabolic Approaches to Enhance Transdermal Drug Delivery. 1. Effect of Lipid Synthesis Inhibitors. J Pharm Sci 85 643-648, 1996.
41. Okamoto H, Muta K, Hashida M, Sezaki H. Percutaneuos Penetration of Acyclovir through Excised Hairless Mouse and Rat Skin: Effect of Vehicle and Percutaneous Penetration Enhancer. Pharm Res 7 64-68, 1990.
42. Reifenrath WG, Hawkins GS, Kurtz MS. Percutaneous penetration and Skin Retention of Topically Applied Compounds: An In Vitro-In Vivo Study. J Pharm Sci 80 526-532. 1991.
43. Kuramoto M. Tanaka T, Makita H. Nakamura Y, Yata N. Characteristics of Shed Snake Skin Permeability to Indomethacin and Fatty Alcohol. J Pharm Pharmacol 48 680-684, 1996.
44. Lin SY, Hou SJ, Hsu THS, Yeh FL, Comparisons of Different Animal Sking with Human Skin in Drug Percutaneous Penetration Studies. Meth Find Exp Clin Pharmacol 14 645-654, 1992.
45. Fang JY, Wu PC, Huang YB, Tsai YH. In vitro permeation study of capsaicin and its synthetic derivatives from ointment bases using various skin types. Int J Pharm 126 119-128, 1995.
46. Bond JR, Barry BW. Limitations of Hairless Mouse Skin as a Model for In Vitro Permeation Studies through Human Skin: Hydration Damage. J Invast Dermatol 90 486-489, 1988.
47. Cooper ER. Increased Skin Permeability for Lipophilic Molecules. J Pharm Sci 73 7153-1156, 1984.
48. Williams AC, Barry BW. Urea analogues in propylene glycol as penetration enhancers in human skin. Int J Phara 36 43-60, 1989.
49. Roy SD, Roos E, Sharma K. Transdermal delivery of buprenorphine through cadaver skin. J Pharm Sci 83 176-181, 1986.
50. Hewitt PG, Poblete N, Wester CR, Maibach IH, Shainhouse JZ. In Vitro Cutaneous Disposition of a Topical Diclofenac Lotion in Human Skin: Effect of a Multi Dose Regiment. Pharm Res 15 988-992, 1998.
51. Walters KA, Brain KR, Dressler WE, Green DM, Howes D, James VJ, Kelling CK, Watkinson AC, Gettings SD. Percutaneous Penetration of N-Nitroso-N-Methyldodecylamine through Human Skin in Vitro: Application from Cosmetics Vehicles. Food Chem Toxic 35 705-712, 1997.
52. Wester RC, Christoffel J, Hartway T, Poblata N, Maibach HI, Forsell J. Human Cadaver Skin Viability for In Vitro Percutaneous Absorption: Storage and Detrimental Effects of Heat-Separation and Freezing. Pharm Res 15 82-84, 1998.
53. Di Colo G, Giannessi C, Nannipieri E, Serafini MF, Vitale D. Influence of drug-surfactant and skin surfactant interaction on percutaneous absorption of two model compounds from ointment bases in vitro. Int J Pharm 50 27-34. 1989.
54. Treffel P. Gabard B. Skin Penetration and Sun Protection Factor of Ultra-Violet Filters from Two Vehicles. Pharm Res 13 770-774, 1996.
55. Cordero JÁ, Alarcon L, Escribano E, Obach R, Domenech JA. Comparative Study of the Transdermal Penetration of a Series of Nonsteroidal Anti-inflammatory Drugs. J Pharm Sci 86 503-08, 1997.
56. Brounaugh RL, Stewart RF. Methods for in vitro percutaneous absorption studies VI: preparation of the barrier layer. J Pharm Sci 75 487-491. 1986.
57. Walker M, Hulme TA, Rippon MG, Walmsley RS, Gunnigle S, Lewin M, Winsey S. In Vitro Model(s) for the Percutaneous Delivery of Active Tissue Repair Agents. J Pharm Sci 86 1379 1384. 1997.
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