Biological Activity and Characteristics of Triamcinolone-Acetonide formulated with the self-regulating Drug Carriers, Transfersomes®
G. Cevc, G. Blume
Biochim. Biophys. Acta 1614:156-164 (2003).
Novel formulations of the halogenated corticosteroid, triamcinolone-acetonide,
based on ultradeformable mixed lipid vesicles, Transfersomes®, are described.
Their performance was tested in vivo using radioactive label measurements, to
study the drug biodistribution, and murine ear edema, to determine the drug
bioactivity. Sparse use of drug loaded Transfersomes® on the skin ensures
an almost exclusive delivery of triamcinolone-acetonide into the organ, thus
arguably increasing the treatment safety. Delivery of triamcinolone acetonide
in the skin with ultradeformable vesicles prolongs the anti-inflammatory drug
action several times compared to the drug usage in a conventional creme or an
ointment, the robustness of biological response for the former being at least
identical to the latter. The required dose of Transfersome® based
triamcinolone acetonide is also greatly reduced. The drug dose of 0.2 μg cm-2
suppresses 75% of arachidonic acid induced murine ear edema for at least 48 h.
In contrast, a conventional formulation of triamcinolone-acetonide requires a
10 fold higher drug dosage to achieve similar effect. In either case,
increasing the applied corticosteroid amount delays the onset of anti-oedema action.
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