Abstract

Assessing the bioavailability of drug molecules at the site of action provides better insight into the efficiency of a dosage form. However, determining drug concentration in the skin layers following topical application of dermatological formulations is a great challenge. The protocols followed in oral formulations could not be applied for topical dosage forms. The regulatory agencies are considering several possible approaches such as tape stripping, microdialysis etc. On the other hand, the skin bioavailability assessment of xenobiotics is equally important for topical formulations in order to evaluate the toxicity. It is always possible that drug molecules applied on the skin surface may transport thorough the skin and reaches systemic circulation. Thus the real time measurement of molecules in the skin layer has become obligatory. In the last two decades, quite a few investigations have been carried out to assess the skin bioavailability and toxicity of topical/dermatological products. This review provides current understanding on the basics of dermatokinetics, drug depot formation, skin metabolism and clearance of drug molecules from the skin layers following application of topical formulations.

Highlights

  • Basic considerations in the dermatokinetics of topical formulationsAnroop Nair1,*, Shery Jacob, Bandar Al-Dhubiab, Mahesh Attimarad, Sree Harsha. Assessing the bioavailability of drug molecules at the site of action provides better insight into the efficiency of a dosage form

  • Topical dermatological formulations are primarily intended to deliver therapeutically effective concentration of drug in skin layers, which are the target site

  • This article provides a valuable insight into the basic considerations in the dermatokinetics of topical formulations

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Summary

Basic considerations in the dermatokinetics of topical formulations

Anroop Nair1,*, Shery Jacob, Bandar Al-Dhubiab, Mahesh Attimarad, Sree Harsha. Assessing the bioavailability of drug molecules at the site of action provides better insight into the efficiency of a dosage form. Determining drug concentration in the skin layers following topical application of dermatological formulations is a great challenge. This review provides current understanding on the basics of dermatokinetics, drug depot formation, skin metabolism and clearance of drug molecules from the skin layers following application of topical formulations. Entretanto, a determinação da concentração de fármaco nas camadas da pele em seguida à aplicação tópica de formulações dermatológicas é um grande desafio. A avaliação da biodisponibilidade de xenobióticos na pele é igualmente importante para as formulações tópicas para se avaliar a toxicidade. Esta revisão fornece a compreensão atual com base na dermatocinética, formação de fármaco de depósito, metabolismo da pele e o clearance das moléculas de fármaco das camadas da pele em seguida à aplicação de formulações tópicas.

INTRODUCTION
SKIN BARRIERS
DRUG ABSORPTION IN SKIN
Assessment of dermatokinetics
APPROACHES IN DERMATOKINETCIS STUDIES
Tape stripping technique
Vasoconstrictor assay
Confocal laser scanning microscopy
SKIN DRUG CLEARANCE
SKIN METABOLISM
DRUG DEPOT IN SKIN
Findings
CONCLUSION
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