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

Volumn 1368, Issue 2, 1998, Pages 201-215

  Cevc, Gregor ^a   Gebauer, Dieter ^a   Stieber, Juliane ^a   Schätzlein, Andreas ^b   Blume, Gabriele ^b  

^a Medical Biophysics   (Germany)

^b IDEA   (Germany)

Author keywords

Insulin; Transfersome; Vesicles

Indexed keywords

DRUG CARRIER; DRUG VEHICLE; INSULIN; LIPOSOME; TRANSFERSOME; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG DELIVERY SYSTEM; DRUG TRANSPORT; FEMALE; MAMMAL; NONHUMAN; PERMEABILITY BARRIER; PRIORITY JOURNAL; SKIN; SUBCUTANEOUS DRUG ADMINISTRATION;

ADMINISTRATION, 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;

ANIMALIA; MAMMALIA;

EID: 0032545780     PISSN: 00052736     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0005-2736(97)00177-6     Document Type: Article

References (38)

1. Buysschaert M. Optimized insulin delivery: achievements and limitations. Diabete Metabol. 15:1989;188-203.
2. Lassmann-Vague V. Unusual ways for administration of insulin. Diabete Metabol. 14:1989;728-731.
3. Saffran M., Sudesh G.K., Savariar C., Burnham J.C., Williams F., Neckers D.C. Science. 233:1986;1081-1084.
4. Das N., Basu M.K., Das M.K. Oral application of insulin encapsulated liposomes. Biochem. Int. 16:1988;983-989.
5. Cho Y.W., Flynn M. Oral delivery of insulin [letter]. Lancet. 23-30:1989;1518-1519.
6. Liedtke R.K., Suwelack K., Karzel K. Wirkung peroraler und transdermaler Insulin-Praparationen auf die Blutglukose-Konzentration bei Mausen. Arzneim.-Forsch. Drug Res. 40:1990;880-883.
7. Wang P.Y. Implantable reservoir for supplemental insulin delivery on demand by external compression. Biomaterials. 10:1989;197-201.
8. Walter H., Gunther A., Kronski D., Flaschentrager I., Mehnert H. Implantation of programmable infusion pumps for insulin delivery in type I diabetic patients. Klin. Wochenschr. 67:1989;583-587.
9. Aungst B.J., Rogers N.J., Shefter E. Comparison of nasal, rectal, buccal, sublingual and intramuscular insulin efficacy and the effects of a bile salt absorption promoter. J. Pharmacol. Exp. Ther. 244:1988;23-27.
10. Chiou G.C.Y., Chuang C.Y., Chang M.A. Systemic delivery of insulin through eyes to lower the glucose concentration. J. Ocul. Pharmacol. 5:1989;81-91.
11. Mishima M., Okada S., Wakita Y., Nakano M. Promotion of nasal absorption of insulin by glycyrrhetinic acid derivatives. I. J. Pharmacobio.-Dynam. 12:1989;31-36.
12. G. Cevc, Lipid properties as a basis for the modelling and design of liposome membranes, in: G. Gregoriadis (Ed.), Liposome Technology, 2nd ed., CRC-Press, Boca Raton, FL, 1992, pp. 1-36.
13. G. Cevc, Material transport across permeability barriers by means of lipid vesicles, in: R. Lipowsky (Ed.), Handbook of Physics of Biological Systems, vol. I, Elsevier Science, Chap. 9, 1995, pp. 441-466.
14. Cevc G., Blume G. Lipid vesicles penetrate into intact skin owing to the transdermal osmotic gradients and hydration force. Biochim. Biophys. Acta. 1104:1992;226-232.
15. Gompper G., Kroll D.M. Driven transport of fluid vesicles through narrow pores. Phys. Rev. E 52:1995;4198-4208.
16. Helfrich W. Elastic properties of lipid bilayers Theory and possible experiments. Z. Naturforsch. 28:1973;693-703.
17. Leibler S. Curvature instability in membranes. J. Physique (France). 47:1986;507-516.
18. Needham D., Evans E. Structure and mechanical properties of giant lipid (DMPC) vesicle bilayers from 20 Celsius below to 10 Celsius above the liquid - crystaline phase transition at 24 degree Celsius. Biochemistry. 27:1988;8261-8269.
19. G. Cevc, G. Schätzlein, D. Gebauer, G. Blume, Ultra-high efficiency of drug and peptide transfer through the intact skin by means of novel drug carriers, transfersomes, in: K.R. Brain, V.J. James, K.A. Walters, (Eds.), Prediction of Percutaneous Penetration, 3rd International Conference, 14-16 April, 1993, Vol. 3b, STS Publishing, Cardiff, pp. 226-236.
20. Mayer L.D., Hope M.J., Cullis P.R. Vesicles of variable sizes produced by a rapid extrusion procedure. Biochim. Biophys. Acta. 856:1986;161-168.
21. Gonzalez P., Planas M.E., Rodriguez L., Sanchez S., Cevc G. Noninvasive, percutaneous induction of topical analgesia by a new type of drug carriers and prolongation of the local pain-insensitivity by analgesic liposomes. Anesth. Analg. 75:1992;615-621.
22. J. Hadgraft, R.H. Guy (Eds.), Transdermal Drug Delivery, Developmental Issues and Research Initiatives, Marcel Dekker, New York, 1989.
23. Potts R.O., Guy R.H. Prediciting skin permeability. Pharm. Res. 9:1992;663-669.
24. Fartasch M., Bassukas I.D., Diepgen T.L. Structural relationship between epidermal lipid lamellae, lammelar bodies and desmosomes in human epidermis, an ultrastructural study. Br. J. Dermatol. 128:1993;1-9.
25. E. Christophers, M. Schubert, C. Goos, The epidermis, in: M.W. Greaves, S. Shuster (Eds.), Pharmacology of the Skin, Vol. 1, Springer, Berlin, 1989, pp. 3-30.
26. A. Schätzlein, G. Cevc, Skin penetration by phospholipid vesicles, transfersomes, as visualized by means of the confocal laser scanning microscopy, in: G. Cevc, F. Paltauf (Eds.), Phospholipids, Characterization, Metabolism and Novel Biological Applications, AOCS Press, 1995, pp. 191-209.
27. Aguiella V., Kontturi K., Murtomäki L., Ramírez P. Estimation of the pore size and charge density in human cadaver skin. J. Control. Release. 32:1994;249-257.
28. Paul A., Cevc G., Bachhawat B.K. Transdermal immunization with large proteins by means of ultradeformable drug carriers. Eur. J. Immunol. 25:1995;35221-35224.
29. G. Cevc, Dermal insulin, in: M. Berger, F.A. Gries (Eds.), Frontiers in Insulin Pharmacology, Georg Thieme Verlag, Stuttgart, 1993, pp. 161-169.
30. Starke A.A., Heinemann L., Hohmann A., Berger M. The action profiles of human NPH insulin preparations. Diabetic Med. 6:1989;239-244.
31. Schreier H., Bouwstra J. Liposomes and niosomes as topical drug carriers, dermal and transdermal drug delivery. J. Control. Release. 30:1994;1-15.
32. Lipowsky R. Vesicle thermodynamics. Nature. 349:1991;475-481.
33. O'Hagan D.T., Illum L. Absorption of peptides and proteins from the respiratory tract and the potential for development of locally administered vaccine. Crit. Rev. Ther. Drug Carrier Syst. 7:1990;35-97.
34. Meyer B.R., Katzeff H.L., Eschbach J., Trimmer J., Zacharias S.R., Rosen S., Sibalis D. Transdermal delivery of human insulin to albino rabbits using electrical current. Am. J. Med. Sci. 297:1989;321-325.
35. Kimmerle R., Friffing G., McCall A., Ruderman N.B., Stoltz E., Melby J.C. Could intranasal insulin be useful in the treatment of non-insulin dependent diabetes mellitus? Diabetes Res. Clin. Pract. 13:1991;69-76.
36. Wearley L.L. Recent progress in protein and peptide delivery by noninvasive routes. Crit. Rev. Ther. Drug Carrier Syst. 8:1991;331-394.
37. Cevc G., Schätzlein A., Blume G. Transdermal drug carriers, basic properties, optimization and transfer-efficiency in the case of epicutaneously applied peptides. J. Control. Release. 36:1995;3-16.
38. G. Cevc, 1991, Eur. pat. 91 114 163.8-2114.