Regio-selective therapeutics
- Delivery to deep skin and underlying muscles/joints
Drugs can be delivered with Transfersomes®
in a fashion that avoids, to a great extent, the clearance through the
skin capillary bed (peripheral blood-capillary plexus). This permits the
drugs to penetrate the skin and reach the underlying tissue in amounts
substantially higher than those achieved with conventional topical formulations.
Compared to oral preparations, the regional delivery by Transfersome®
formulation can provide a faster onset and a longer duration of action.
IDEA's drug delivery approach also substantially lowers systemic drug
concentration, and thus diminishes the danger of systemic adverse effects.
Diclofenac applied on the skin in Transfersomes® is delivered
site-specifically into deep muscular tissue. In contrast, a much higher
drug dose administered epicutaneously in a hydrogel is poorly targeted
and does not reach therapeutic local drug concentrations, except through
the blood.
An example for the successful regional delivery of a small
drug by Transfersomes® are formulations of nonsteroidal anti-inflammatory
drugs (NSAIDs). A comparison with the performance of the traditional topical
hydrogel formulation is made for the popular drug diclofenac in the illustration
above.
A therapeutically meaningful diclofenac concentration in
the target muscle tissue is reached even when the locally administered
drug dose in Transfersomes® is much lower than the amount typically
used with a commercial hydrogel.
In pigs, for example, it is sufficient to use merely 0.3
mg diclofenac in highly deformable Transfersomes® per kg body weight,
spread over an area of 25 cm², to ensure therapeutic drug concentration
in a 5 cm thick muscle specimen, collected under the agent application
site. The concurrently measured systemic drug level is nearly an order
of magnitude lower. In contrast, if the drug is used in a hydrogel at
an 8 times higher dose, the average intramuscular concentration is three
times below the therapeutic level. and comparable to that measured in the
serum.
NSAID formulations with Transfersomes® were also shown already
to be clinically effective. This is illustrated in the following
figure for a different NSAID.
An NSAID applied on the skin in Transfersomes®
ensures good local therapeutic effect, comparable to that of an equally dosed
oral product. The result obtained with a conventional
commercial topical product is much worse and does not differ from placebo.
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