Transfersomes® - Innovative Transdermal Drug Carriers. In: Modified
Release Drug Delivery Systems. (M. Rathbone, M. Robert, J. Hadgraft, eds.)
M. Dekker, New York, pp 533-546 (2002).
G. Cevc*
*Medizinische Biophysik, Technische Universität München
Ismaningerstr. 22, D-81675 München, Deutschland, EU
Specialized intercellular lipidic seals and the tight packing
of cells in the skin prevent molecules greater than a few hundred Dalton
from crossing the organ. However, composite, 'intelligent' aggregates,
that exert directed pressure on the intercellular junctions in the skin,
can open numerous hydrophilic channels through the stratum corneum and
carry pharmacological agents, including polypeptides, across the intact
permeability barrier after non-occlusive administration. The distinct
characteristics of such aggregates, Transfersomes ('carrying bodies'),
are the non-uniform and high aggregate deformability (mechano-sensitivity)
and the high responsiveness to external transcutaneous gradient(s) (e.g.
hydro-sensitivity). Combination of both these properties enables Transfersomes
to move through the skin typically between the cell envelope and the skin
sealing lipid multilayers. Aggregates without the described characteristics,
such as conventional liposomes or mixed lipid micelles, remain confined
to the skin surface. The results of in vivo experiments with corticosteroids
(hydrocortisone, dexamethasone, triamcinolone), non-steroidal anti-inflammatory
agents (diclofenac), and proteins (calcitonin, insulin, serum albumin)
in Transfersomes illustrate the main advantages of 'smart carriers': the
drug targeting into the skin (> 99.9%), the improvement of regional/systemic
drug concentration ratio (10 x ), and the high efficiency of non-invasive
macromolecular delivery. In every case, the duration of biological action
is also prolonged.
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