Summary
The skin is an evolutionary masterpiece of living tissue which is the final control unit for determining the local and systemic availability of any drug which must pass into and through it. In vivo in humans, many factors will affect the absorption of drugs. These include individual biological variation and may be influenced by race. The skin site of the body will also influence percutaneous absorption. Generally, those body parts exposed to the open environment (and to cosmetics, drugs and hazardous toxic substances) are most affected. Treating patients may involve single daily drug treatment or multiple daily administration. Finally, the body will be washed (normal daily process or when there is concern about skin decontamination) and this will influence percutaneous absorption.
The vehicle of a drug will affect release of drug to skin. On skin, the interrelationships of this form of administration involve drug concentration, surface area exposed, frequency and time of exposure. These interrelationships determine percutaneous absorption. Accounting for all the drug administered is desirable in controlled studies. The bioavailability of the drug then is assessed in relationship to its efficacy and toxicity in drug development.
There are methods, both quantitative and qualitative, in vitro and in vivo, for studying percutaneous absorption of drugs. Animal models are substituted for humans to determine percutaneous absorption. Each of these methods thus becomes a factor in determining percutaneous absorption because they predict absorption in humans. The relevance of these predictions to humans in vivo is of intense research interest.
The most relevant determination of percutaneous absorption of a drug in humans is when the drug in its approved formulation is applied in vivo to humans in the intended clinical situation. Deviation from this scenario involves the introduction of variables which may alter percutaneous absorption.
Similar content being viewed by others
Explore related subjects
Discover the latest articles and news from researchers in related subjects, suggested using machine learning.References
Berardesca E, de Rigol J, Leveque JL, Maibach HI. In vivo biophysical characterization of skin physiological differences in races. Dermatologica 182: 89–93, 1991
Berardesca E, Maibach HI. Racial differences in sodium lauryl sulphate induced cutaneous irritation: Black and White. Contact Dermatitis 17: 12–17, 1987
Bronaugh RL, Stewart RF, Simon M. Methods for in vitro percutaneous absorption studies: use of excised human skin. Journal of Pharmaceutical Sciences 75: 1094–1097, 1986
Bucks DAW, Maibach HI, Guy RH. Percutaneous absorption of steroids: effect of repeated application. Journal of Pharmaceutical Sciences 74: 1337–1339, 1985a
Bucks DAW, Wester RC, Mobayen MM, Yang D, Maibach HI, et al. In vitro percutaneous absorption and stratum corneum binding of alachlor: effect of formulation dilution with water. Toxicology and Applied Pharmacology 100: 417–423, 1985b
Feldman RJ, Maibach HI. Regional variation in percutaneous penetration of 14C cortisone in man. Journal of Investigative Dermatology 48: 181–183, 1967
Gean CJ, Tur E, Maibach HI, Guy RH. Cutaneous responses to topical methyl nicotinate in Black, Oriental and Caucasian subjects. Archives of Dermatology Research 281: 95–98, 1989
Guy RH, Tur E, Bjerke S, Maibach HI. Are there age and racial differences to methyl nicotinate-induced vasodilation in human skin? Journal of the American Academy of Dermatology 12: 1001–1006, 1985
Johnson LC, Corah NL. Racial differences in skin resistance. Science 139: 766–767, 1960
McKenzie AW, Stoughton RB. Method for comparing percutaneous absorption of steroids. Archives of Dermatology 86: 608–610, 1962
Melendres JL, Bucks DAW, Camel E, Wester RC, Maibach HI. In vivo percutaneous absorption of hydrocortisone multiple application dosing in man. Pharmaceutical Research 6: S–248, 1990
Pershing LK, Krueger GG. Human skin sandwich flap model for percutaneous absorption. In Bronaugh & Maibach (Eds) Percutaneous Absorption, 2nd ed., pp. 397–414, Marcel Dekker, Inc., New York, 1989
Reinertson RP, Wheatley VR. Studies on the chemical composition of human epidermal lipids. Journal of Investigative Dermatology 32: 49–59, 1959
Riviere JE, Bowman KF, Monteiro-Riviere NA, Dix LP, Carver MP. The isolated perfused porcine skin flap (IPPSF). Fundamentals of Applied Toxicology 7: 444–453, 1986
Riviere JE, Bowman KF, Monteiro-Riviere NA. On the definition of viability on isolated perfused skin preparations. British Journal of Dermatology 116: 739–741, 1987
Rougier A, Dupuis D, Lotte C, Roguet R, Schaefer H. Correlation between stratum corneum reservoir function and percutaneous absorption. Journal of Investigative Dermatology 81: 275, 1983
Rougier A, Dupuis D, Lotte C, Roguet R, Wester RC, et al. Regional variation of percutaneous absorption in man: measurement by the stripping method. Archives of Dermatologic Research 278: 465, 1986
Stoughton RB. Bioassay methods for measuring percutaneous absorption. In Montagna et al. (Eds) Pharmacology of the skin, p. 542, Appleton-Century-Crofts, New York, 1969
Wedig JH, Maibach HI. Percutaneous penetration of dipyrithrone in man: effect of skin color (race). Journal of the American Academy of Dermatology 5: 433–437, 1981
Weigan DA, Gaylor JR. Irritant reaction in Negro and Caucasian skin. Southern Medical Journal 67: 548–551, 1974
Wester RC, Maibach HI. Cutaneous pharmacokinetics: 10 steps to percutaneous absorption. Drug Metabolism Reviews 14: 169–205, 1983
Wester RC, Maibach HI. Individual and regional variation with in vitro percutaneous absorption. In Bronaugh & Maibach (Eds) In vitro percutaneous absorption, pp. 25–30, CRC Press, Boca Raton, 1991
Wester RC, Maibach HI. Animal models for percutaneous absorption. In Maibach & Lowe (Eds) Models in dermatology, Vol. 2, pp. 159–169, Karger, Basel, 1985
Wester RC, Noonan PK, Maibach HI. Frequency of application of percutaneous absorption of hydrocortisone. Archives of Dermatology 13: 620–622, 1977
Wester RC, Noonan PK, Maibach HI. Variation on percutaneous absorption of testosterone in the Rhesus monkey due to anatomic site of application and frequency of applications. Archives of Dermatology Research 267: 229, 1980a
Wester RC, Noonan PK, Maibach HI. Percutaneous absorption of hydrocortisone increases significantly with long term administration: in vivo studies in the Rhesus monkey. Archives of Dermatology 116: 186–188, 1980b
Wester RC, Noonan PK, Smeach S, Kosobud L. Pharmacokinetics and bioavailability of intravenous and topical nitroglycerin in the Rhesus monkey: estimate of percutaneous first-pass metabolism. Journal of Pharmaceutical Sciences 72: 745–748, 1983
Wester RC, Maibach HI, Surinchak J, Bucks DAW. Predictability of in vitro diffusion systems: effect of skin types and ages on percutaneous absorption of triclocarban. In Bronaugh & Maibach (Eds) Percutaneous penetration, pp. 223–226, Marcel Dekker, New York, 1985
Wester RC, Mobayen M, Maibach HI. In vivo and in vitro absorption and binding to powdered human stratum corneum as methods to evaluate skin absorption of environmental chemical contaminants from ground and surface water. Journal of Toxicology and Environmental Health 21: 367–374, 1987
Wester RC, McMaster J, Bucks DAW, Bellet EM, Maibach HI. Percutaneous absorption in Rhesus monkeys and estimation of human chemical exposure. In Wang et al. (Eds) Biological monitoring for pesticide exposure: measurement, estimation, and risk reduction, pp. 152–157, ACS Press, Washington, DC, 1989
Wester R, Rougier A, Lotte C, Maibach H. Influence of race on percutaneous absorption in human subjects. Pharmaceutical Research 7: S–211, 1990
Wester RC, Maibach HI. Percutaneous absorption in diseased skin. In Surber & Maibach (Eds) Topical corticosteroids, pp. 128–141, Karger, Basel, 1992
Wester RC, Patel R, Nacht S, Leyden J, Melendres J, et al. Controlled release of benzyl peroxide from a porous microsphere polymeric system can reduce topical irritancy. Journal of the American Academy of Dermatology 24: 720–726, 1991a
Wester RC, Melendres J, Sarasen R, McMaster J, Maibach HI. Glyphosate skin binding, absorption, residual tissue distribution and skin decontamination. Fundamental and Applied Toxicology 16: 725–732, 1991b
Wester RC, Maibach HI, Melendres J, Sedik L, Knaak J, et al. In vivo and in vitro percutaneous absorption and skin evaporation of isofenphos in man. Fundamentals of Applied Toxicology, in press, 1992
Wickrema SAJ, Shaw SR, Weber DJ. Percutaneous absorption and excretion of tritium-labeled diflorasone diacetate, a new topical corticosteroid in the rat, monkey and man. Journal of Investigative Dermatology 71: 372–377, 1978
Williams RL, Thakker KM, John V, Lin ET, Gee WL, et al. Nitroglycerin absorption from transdermal systems: formulation effects and metabolite concentrations. Pharmaceutical Research 8: 744–749, 1991
Wilson D, Berardesca E, Maibach HI. In vitro transepidermal water loss: differences between black and white human. British Journal of Dermatology 119: 647–651, 1988
Author information
Authors and Affiliations
Additional information
An erratum to this article is available at http://dx.doi.org/10.1007/BF03259380.
Rights and permissions
About this article
Cite this article
Wester, R.C., Maibach, H.I. Percutaneous Absorption of Drugs. Clin. Pharmacokinet. 23, 253–266 (1992). https://doi.org/10.2165/00003088-199223040-00002
Published:
Issue Date:
DOI: https://doi.org/10.2165/00003088-199223040-00002