Synergistic effect of anionic lipid enhancer and electroosmosis for transcutaneous delivery of insulin

A lipid formulation consisting of 1,2-dimyristoyl-sn3-phosphatidylserine (DMPS) in a 0.2% sodium dodecylsulfate (SDS) solution was tested as an in vivo enhancer for the transcutaneous delivery of insulin. The formulation when applied to for 15 min was found to permeabilize porcine epidermis and prol...

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Bibliographic Details
Published in:International journal of pharmaceutics 2006-12, Vol.326 (1), p.1-6
Main Authors: Narasimha Murthy, S., Zhao, Ya-Li, Hui, Sek-Wen, Sen, Arindam
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Animals
Anionic lipid
Biological and medical sciences
Buffers
Electroosmosis
Electrophysiology
Epidermis - metabolism
General pharmacology
Insulin
Insulin - administration & dosage
Insulin - blood
Insulin - metabolism
Iodine Radioisotopes - therapeutic use
Lipids - chemistry
Medical sciences
Osmosis
Pharmaceutical technology. Pharmaceutical industry
Pharmacokinetics
Pharmacology. Drug treatments
Porcine epidermis
Rat skin
Rats
Rats, Sprague-Dawley
Skin - pathology
Swine
Time Factors
Transcutaneous delivery
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Summary:A lipid formulation consisting of 1,2-dimyristoyl-sn3-phosphatidylserine (DMPS) in a 0.2% sodium dodecylsulfate (SDS) solution was tested as an in vivo enhancer for the transcutaneous delivery of insulin. The formulation when applied to for 15 min was found to permeabilize porcine epidermis and prolong the permeable state as evidenced by electric resistance measurement. The formulation enhanced the transport of insulin through the epidermis by 40- to 100-fold, as compared to epidermis that was treated with SDS or DMPS alone. Application of electroosmosis across the formulation-treated epidermis enhanced the transport of insulin by an additional 10-fold. Pharmacokinetic studies were carried out in Sprague-Dawley rats. Transcutaneous delivery of insulin with formulation treatment and electroosmosis increased the plasma level of insulin by ∼10-fold over delivery by formulation treatment alone. With the above protocol plasma insulin concentration remained relatively constant for up to 4 h. The synergistic application of anionic lipid formulation and electroosmosis offers a promising non-invasive technique to deliver insulin transcutaneously.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2006.06.039