ULTRAFLEXIBLE VESICLES, TRANSFERSOMES, HAVE AN EXTREMELY LOW PORE PENETRATION RESISTANCE AND TRANSPORT THERAPEUTIC AMOUNTS OF INSULIN ACROSS THE INTACT MAMMALIAN SKIN
G. Cevc et al., ULTRAFLEXIBLE VESICLES, TRANSFERSOMES, HAVE AN EXTREMELY LOW PORE PENETRATION RESISTANCE AND TRANSPORT THERAPEUTIC AMOUNTS OF INSULIN ACROSS THE INTACT MAMMALIAN SKIN, Biochimica et biophysica acta. Biomembranes, 1368(2), 1998, pp. 201-215
New vehicles for the non-invasive delivery of agents are introduced. T
hese carriers can transport pharmacological agents, including large po
lypeptides, through the permeability barriers: such as the intact skin
. This capability depends on the self-regulating carrier deformability
which exceeds that of the related but not optimized lipid aggregates
by several orders of magnitude. Conventional lipid suspensions, such a
s standard liposomes or mixed lipid micelles, do not mediate a systemi
c biological effect upon epicutaneous applications. In contrast to thi
s, the properly devised adaptable carriers, when administered on the i
ntact skin, transport therapeutic amounts of biogenic molecules into t
he body. This process can be nearly as efficient as an injection needl
e, as seen from the results of experiments in mice and humans with the
insulin-carrying vesicles. The carrier-mediated transcutaneous insuli
n delivery is unlikely to involve shunts, lesions or other types of sk
in damage. Rather than this, insulin is inferred to be transported int
o the body between the intact skin cells with a bio-efficiency of at l
east 50% of the s.c. dose action. (C) 1998 Elsevier Science B.V.