Transdermal delivery, chemical structure

A new generation of transdermal drug delivery (TDD) system was developed to contain one or more skin permeation enhancers in the surface adhesive coating layers. This TDD system has been found, experimentally, to release the enhancers to the surface of stratum corneum to modify the skin s barrier properties, prior to the controlled delivery of the active drug. The extent of enhancement in skin permeability appears to be dependent upon the chemical structure of drug to be delivered transdermally as well as the type and the concentration of enhancer used. The mechanism of skin permeation enhancement have been explored and are analyzed in this report. 

The mechanisms of heat-assisted transdermal delivery include an increase in drug diffusion, increase in skin permeability, alteration of skin structure, increase in body circulation, and increase in the release rate of drug from local skin tissue into systemic circulation. Heat can also increase drug solubility. The advantage of heat control is that it does not involve chemical... 

Kanikkannan N, Kandimalla K, Lamba S, Singh M. Structure-activity relationship of chemical penetration enhancers in transdermal drug delivery. Curr Med Chem 2000 7 593-608. 

The remarkable resistance of the SC intercellular lipid network to the passive penetration of therapeutic agents has intensified the search for devices, chemical and physical, with the ability to perturb this lipid environment. Of the many physical techniques investigated, iontophoresis (or electrically enhanced transdermal transport) has become an important focal point [160-162]. Unparalleled in its ability to deliver (noninvasively) ionized drugs across the skin, its modus operandi appears to be largely dependent on transcutaneous ion-conducting pathways (which may be paracellular), rather than a function of direct interaction with the lipid infrastructure [163]. Nevertheless, the effect of the applied current on the lipid (and protein) domains is a matter of interest with respect to both safety considerations (i.e., does the applied current induce stmctural alterations ) and mechanistic insight. ATR-FTIR has been used in a number of studies to discern the effect of iontophoresis on SC lipid and protein structures, both in vivo and in vitro. In separate studies, human SC was examined in vivo following the delivery of current at 0.1-0.2 mA/cm for 30... 

The present summary will cover only those technologies where the drug formulation itself is used to penetrate the skin via its mechanical energy. It will not describe any technology where a needle is used to puncture the skin, even if the needle is not visible to the patient or only the epidermis is punctured, such as mini-needles, microneedles, pen injectors, or autoinjectors. Also excluded are systems that ablate the skin mechanically or otherwise disrupt its chemical or mechanical structure to increase its permeability, such as laser ablation, microdermal ablation, electroporation, or iontophoresis. These are usually referred to as transdermal drug delivery, but can also be described as needle free. 

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