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American Society for Experimental Neurotherapeutics Abstracts
August 2000

Transdermal Delivery of Interferon beta-1a by Transfersomes and Its Effects on Surrogate Markers

Arch Neurol. 2000;57(8):1239. doi:

Noninvasive delivery of interferon-beta (IFN-β) may reduce adverse events at the injection site, including necrosis, reduce systemic adverse effects potentially linked to the pharmacokinetics after injection, be less immunogenic (less neutralizing antibodies), and increase patient acceptance. Transfersomes (Tfs) were used to deliver IFN-β transdermally. Transfersomes are novel self-regulating drug carriers that can deliver macromolecules across the intact skin (Cevc, et al. J Controlled Release. 1995;36:3-16). The main objective of this pilot study was to investigate if IFN-β associated with Tfs produces systemic levels of IFN-β. The second aim was to study surrogate markers for drug effects (serum β2-microglobulin and urine neopterin) and adverse effects (body temperature). Normal pigs were treated with a single epicutaneous dose of 4.6 × 106 U/kg body weight IFN-β in Tfs, or with 3.8 × 105 U/kg body weight IFN-β solution subcutaneously. This was compared to empty vehicles epicutaneously and subcutaneously. Interferon-β Tfs produced plasma levels with a Cmax (peak arterial plasma concentrations)of 6 hours as compared with 2 hours for subcutaneous injection. The area under the curve (AUC) was lower for epicutaneous application by a factor of about 3. Interferon-β Tfs produced comparably higher amounts of neopterin and β2-microglobulin, indicating a better biopotency; in contrast, IFN-β Tfs were less pyrogenic. The results of this study indicate that Tf-mediated transdermal IFN-β delivery could become a valuable alternative to subcutaneous injection. More recent work using IFN-α Tfs showed that the bioavailability could be substantially increased by an improved formulation.

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