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<p><b>Overcoming the skin barrier with artificial smart carriers of drugs </b> </p> <p align="left">G. Cevc</p> <p align="left">Medical Biophysics Klinikum r.d.I., Ismaningerstr. 22,<br> The Technical University of Munich, D-81675 Munich, E.U. </p> <p align="left"><b>In: <i>Intelligent Materials: Novel Concepts for Controlled Release Technologies.</i> (S. Dinh and J. DeNuzzio, eds.) ACS Books, Washington, DC, 1999.</b></p> <p align="left">Special intercellular lipidic seals and the tight packing of cells in the skin prevent molecules greater than a few hundred Dalton to cross the organ. Electrical (iontophoresis) or mechanical (ultrasonication) methods generate too few passages in the barrier to overcome the obstacle and to deliver large molecules across the skin. Such goal is achieved by suitable composite, 'intelligent' aggregates that exert directed pressure on the intercellular junctions in the skin; this opens numerous hydrophilic channels through the stratum corneum, typically between the cell envelope and the skin sealing lipid multi-layers. The common 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). Mechano-sensitivity is reflected in the strongly non-linear Transfersome reaction to ambient stress; hydrosensitivity is seen from the very strong Transfersome tendency to bind water. Combination of both properties enables Transfersomes to move through the skin and carry pharmacological agents, including polypeptides, across the intact permeability barrier after non-occlusive administration. 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 respective main achievements are 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 (> 50%). In every case, the duration of biological action is prolonged.</p> <p><a href="index.html"><----</a> | <a href="../.././index.html" target="_top" onmouseover="putstattext('What is special about IDEA?'); return true;">Home</a> | <a href="../../about-us/index.html" target="_top" onmouseover="putstattext('About IDEA history, people, external collaboratory and future plans.'); return true;">About us</a> | <a href="../../corporate_factsheet/index.html" target="_top" onmouseover="putstattext('Corporate Factsheet'); return true;">Corporate Factsheet</a> | <a href="../../science/index.html" target="_top" onmouseover="putstattext('Academic collaborations, publications, etc.'); return true;">Science</a> | Publications | <a href="../../product_opportunities/index.html" target="_top" onmouseover="putstattext('IDEA offers better compliance, local drug targeting and patent protection.'); return true;">Product opportunities</a> | <a href="../../financial/index.html" target="_top" onmouseover="putstattext('Investors and basic financial data.'); return true;">Finance</a> | <a href="../../press_releases/index.html" target="_top" onmouseover="putstattext('Original texts.'); return true;">Press releases</a> | <a href="../../latest_newsletter/index.html" target="_top" onmouseover="putstattext('IDEAS latest newsletter'); return true;">Latest newsletter</a> | <a href="../../press_clippings/index.html" target="_top" onmouseover="putstattext('IDEA in the press.'); return true;">Press clippings</a> | <a href="../../conferences/index.html" target="_top" onmouseover="putstattext('Here you will find many dates where you can meet us and where we can talk...'); return true;">Conferences</a> | <a href="../../career/index.html" target="_top" onmouseover="putstattext('We constantly seek best talents and dedication, offering much in return.'); return true;">Career</a> | <a href="../../contact/index.html" target="_top" onmouseover="putstattext('We would like to hear from you!'); return true;">Contact</a> | <a href="../../faq/index.html" target="_top" onmouseover="putstattext('Product bio/acceptability, liposome/Transfersome, ...'); return true;">Scientific FAQ</a> | <a href="../../glossary/index.html" target="_top" onmouseover="putstattext(''); return true;">Glossary</a> | <a href="../../sitemap/index.html" target="_top" onmouseover="putstattext('Get an impression on IDEA!'); return true;">Site Map</a> | <a href="../../search/index.html" target="_top" onmouseover="putstattext('Find documents based on keywords!'); return true;">Search</a> |  </p>