Skip to main content

Advertisement

Log in

Percutaneous Absorption of Drugs

  • Review Article
  • Drug Disposition
  • Published:
Clinical Pharmacokinetics Aims and scope Submit manuscript

An Erratum to this article was published on 01 January 1993

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Subscribe and save

Springer+ Basic
$34.99 /Month
  • Get 10 units per month
  • Download Article/Chapter or eBook
  • 1 Unit = 1 Article or 1 Chapter
  • Cancel anytime
Subscribe now

Buy Now

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

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

    Article  PubMed  CAS  Google Scholar 

  • Berardesca E, Maibach HI. Racial differences in sodium lauryl sulphate induced cutaneous irritation: Black and White. Contact Dermatitis 17: 12–17, 1987

    Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • Bucks DAW, Maibach HI, Guy RH. Percutaneous absorption of steroids: effect of repeated application. Journal of Pharmaceutical Sciences 74: 1337–1339, 1985a

    Article  PubMed  CAS  Google Scholar 

  • 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

    Article  Google Scholar 

  • Feldman RJ, Maibach HI. Regional variation in percutaneous penetration of 14C cortisone in man. Journal of Investigative Dermatology 48: 181–183, 1967

    Google Scholar 

  • 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

    Article  CAS  Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • Johnson LC, Corah NL. Racial differences in skin resistance. Science 139: 766–767, 1960

    Article  Google Scholar 

  • McKenzie AW, Stoughton RB. Method for comparing percutaneous absorption of steroids. Archives of Dermatology 86: 608–610, 1962

    Article  Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

  • Reinertson RP, Wheatley VR. Studies on the chemical composition of human epidermal lipids. Journal of Investigative Dermatology 32: 49–59, 1959

    PubMed  CAS  Google Scholar 

  • 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

    Article  CAS  Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • 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

    Article  CAS  Google Scholar 

  • 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

    Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • Weigan DA, Gaylor JR. Irritant reaction in Negro and Caucasian skin. Southern Medical Journal 67: 548–551, 1974

    Article  Google Scholar 

  • Wester RC, Maibach HI. Cutaneous pharmacokinetics: 10 steps to percutaneous absorption. Drug Metabolism Reviews 14: 169–205, 1983

    Article  PubMed  CAS  Google Scholar 

  • 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

    Google Scholar 

  • Wester RC, Maibach HI. Animal models for percutaneous absorption. In Maibach & Lowe (Eds) Models in dermatology, Vol. 2, pp. 159–169, Karger, Basel, 1985

    Google Scholar 

  • Wester RC, Noonan PK, Maibach HI. Frequency of application of percutaneous absorption of hydrocortisone. Archives of Dermatology 13: 620–622, 1977

    Article  Google Scholar 

  • 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

    Article  CAS  Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • 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

    Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • 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

    Google Scholar 

  • Wester R, Rougier A, Lotte C, Maibach H. Influence of race on percutaneous absorption in human subjects. Pharmaceutical Research 7: S–211, 1990

    Google Scholar 

  • Wester RC, Maibach HI. Percutaneous absorption in diseased skin. In Surber & Maibach (Eds) Topical corticosteroids, pp. 128–141, Karger, Basel, 1992

    Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • 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

    Google Scholar 

  • 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

    Article  Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

  • 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

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Additional information

An erratum to this article is available at http://dx.doi.org/10.1007/BF03259380.

Rights and permissions

Reprints 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

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003088-199223040-00002

Keywords