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Skin Penetration Enhancers
Open the gate for transdermal drug penetration
A Breakthrough in NSAID Topical Formulations

When physicians prescribe a topical non-steroidal anti-inflammatory drug, they have to consider the impermeable nature of the horny layer of the skin. The difficulty which this integument offers to transdermal drug delivery is made more complex by the biological variability of human skin permeability, in addition to the polar physical and chemical properties of NSAIDs. Various tactics may be employed to surmount the skin barrier. At present a popular solution for overcoming the intrinsic resistance of the horny layer and its biological variability is to incorporate penetration enhancers (accelerants or absorption promoters) into skin products or transdermal devices. An ideal penetration enhancer is considered to be a chemical which exhibits the only property that it reversibly reduces the barrier nature of the stratum corneum without the accelerant damaging any viable cells. Terpenoid compounds represent an interesting class of enhancers showing a wide range of activity, for drugs over a wide range of varying polarity.

Terpenes as Skin Penetration Enhancers

Terpenoids are natural compounds, found in essential oils, such as oil of turpentine and are widely used in perfumes, flavourings and medicines. Simple cyclic terpenes are used to promote transdermal drug penetration in topical pharmaceutical preparations. Cineol, the terpenoid compound incorporated into Dispercam Gel, showed an enhancement ratio of 95 towards polar compounds such as piroxicam.
Enhancement ratio (ER) is a term used to describe the penetration enhancing activity and is defined as:

Permeability coefficient after terpene treatment
ER = ----------------------------------------------------------------
Permeability coefficient before terpene treatment

The incorporation of a skin penetration enhancer in Dispercam Gel, opens the gate for transdermal piroxicam penetration through reversible reduction of the barrier nature of the stratum corneum, and thus:
Enabling a higher rate and extent of piroxicam absorption with less chances of enzymatic degradation by intradermal enzymes, as enzymatic saturation is rapidly achieved.
Achieving higher local drug concentrations in the synovial fluid and targeted tissues
Offering more rapid onset, longer duration and more intense relief of pain and inflammation.

Despite the great improvement in relief of pain and inflammation, the excellent tolerability of topical NSAID preparations is maintained.
This is achieved as higher tissue to plasma concentration ratio is obtained, thereby achieving a high local concentration of piroxicam at the affected site without elevating the drug plasma concentration.