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Transdermal Delivery of Heparin Using Pulsed Current Iontophoresis
Stefania Pacini, Tiziana Punzi, Massimo Gulisano, Fabiola Cecchi, Simonetta Vannucchi, and Marco Ruggiero
Pharmaceutical Research (2005)
Purpose. In clinical practice heparin has to be administered by injection with obvious disadvantages;
thus, transdermal delivery by electrically assisted methods have been studied. In this study we evaluated
the efficacy of a Food and Drug Administration-approved pulsed current iontophoresis system in
delivering heparin through living rat skin.
Methods. Fluorescent and radioactive heparin as well as a commercial heparin preparation were
delivered through rat skin via a pulsed current iontophoresis system.
Results. Pulsed current iontophoresis allowed fluorescent heparin to cross the stratum corneum
localizing in epidermis and dermis. Unfractionated, high-, and low molecular weight fraction pools,
obtained by fractionating [35S]-unfractionated heparin on a molecular weight sieve, were then separately
tested. Pulsed current iontophoresis elicited the transdermal delivery of low molecular weight heparin,
but not that of high molecular weight heparin. Finally, pulsed current iontophoresis of an unfractionated
pharmaceutical heparin preparation significantly decreased plasmatic factor Xa activity.
Conclusions. We hypothesize that this technique could be used to administer low molecular weight
heparin in a cost-efficient and safe manner without the need for syringes and needles.
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