Ultraflexible vesicles, Transfersomes, have an extremely low pore penetration resistance and transport therapeutic amounts of insulin across the intact mammalian skin.

TitleUltraflexible vesicles, Transfersomes, have an extremely low pore penetration resistance and transport therapeutic amounts of insulin across the intact mammalian skin.
Publication TypeJournal Article
Year of Publication1998
AuthorsCevc G, Gebauer D, Stieber J, Schatzlein A, Blume G
JournalBiochim Biophys Acta
Volume1368
Issue2
Pagination201-15
Date Published1998 Jan 19
ISSN0006-3002
KeywordsAdministration, Cutaneous, Adult, Animals, Blood Glucose, C-Peptide, Cholic Acid, Cholic Acids, Drug Carriers, Female, Humans, Insulin, Liposomes, Mice, Mice, Inbred Strains, Micelles, Permeability, Phosphatidylcholines, Rats, Recombinant Proteins, Skin
Abstract

New vehicles for the non-invasive delivery of agents are introduced. These carriers can transport pharmacological agents, including large polypeptides, 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 as standard liposomes or mixed lipid micelles, do not mediate a systemic biological effect upon epicutaneous applications. In contrast to this, the properly devised adaptable carriers, when administered on the intact skin, transport therapeutic amounts of biogenic molecules into the body. This process can be nearly as efficient as an injection needle, as seen from the results of experiments in mice and humans with the insulin-carrying vesicles. The carrier-mediated transcutaneous insulin delivery is unlikely to involve shunts, lesions or other types of skin damage. Rather than this, insulin is inferred to be transported into the body between the intact skin cells with a bio-efficiency of at least 50% of the s.c. dose action.

Alternate JournalBiochim. Biophys. Acta
PubMed ID9459598