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Transdermal drug delivery is characterized by a controlled continuous delivery of drug molecules from skin surfaces, through its
layers, and into the systemic circulation. It bypasses enzymatic digestion in gastrointestinal tract and hepatic portal system which
can lead to excessive drug degradation and therapeutic ineffectiveness. Nevertheless, the skin permeation propensity of most drugs is
practically low due to the impermeable nature of stratum corneum, the uppermost layer of epidermis. A wide range of innovation has
been created to enhance the skin permeability to drugs. The current advances include micro-needles, iontophoresis, sonophoresis,
photomechanical waves, electroporation and pressurized air techniques. Starting from the year of 2008, Non-Destructive Biomedical
and Pharmaceutical Research Centre investigates microwave of specific characteristics for its potential as transdermal permeation
enhancer. The idea of involving microwave to modify the microstructure of skin stems from the fact that microwave is able to
amorphize drug crystals and exert macromolecular rearrangement in pharmaceutical matrices via hydrogen bonding, electrostatic
interaction and/or hydrophobic interaction in the past dosage form design studies. It implies that the microwave can possibly disturb
the lipid and protein regimes of epidermis or dermis to facilitate drug diffusion or partition across the skin barrier. This presentation
aims to provide the skin permeation enhancement mechanism of microwave for transdermal drug delivery and its relations with
chemical permeation enhancer, physical states of dosage form applied on skin and nanotechnology. In addition, issues related to
safety, in vivo drug pharmacokinetics and pharmacodynamics profiles, transdermal delivery combination techniques, integrated drug
administration and analytical microwave device, clinical trial and commercialization will be addressed.