Peptide transdermal

While chemical enhancers can be a successful tool for the improvement of small dmg permeabihty through skin, for big molecules other strategies have to be undertaken. Indeed, proteins and peptides transdermal administration requires the use of... 

While uncontrolled topical delivery of proteins and peptides for local application such as open wound healing is easily achieved, it is much more challenging to use transdermal delivery systems to deliver protein across intact skin. In theory, transdermal delivery could provide constant drug release for days, avoids first-pass metabolism, and could allow drug effects to be rapidly terminated by simply removing... 

PUlai, O., V. Nair, R. Podnri, and R. Panchagnnla, Transdermal iontophoresis. Part IT. Peptide and protein delivery. Methods Find Exp Chn Pharmacol, 1999. 21(3) 229-40. 

While opioid peptides have been very useful for investigating the pharmacology of different opioid receptor subtypes, pharmacological investigations have established that no pharmacodynamic advantage is to be expected from opioid peptides with respect to analgesic activity or side-effects. Furthermore, they have their own shortcomings with respect to potential clinical applications. Most importantly their peptidic structure usually prohibits administration by the oral or transdermal route, which are the routes of choice for pain treatment. 

Hoogstraate, A.J., et al. 1991. Kinetics, ultrastructural aspects and molecular modelling of transdermal peptide flux enhancement by V-alkylazacycloheptanones. Int J Pharm 76 37. 

Cevc, G., A. Schatzein, and G. Blume. 1995. Transdermal drug carriers Basic properties, optimization and transfer efficiency in the case of epicutaneously applied peptides. J Control Release 36 3. 

Green, P.G., et al. 1992. Transdermal iontophoresis of amino acids and peptides in vitro. J Control Release 21 187. 

Banga, A.K., and Y.W. Chien. 1993. Hydrogel-based iontotherapeutic delivery devices for transdermal delivery of peptides/protein drugs. Pharm Res 10 697. 

Although, as described above, the vagina is permeable to many peptides and proteins, in most cases the bioavailability is insufficient for systemic therapy and is also highly variable. Penetration enhancers may be used to promote peptide absorption across the vaginal epithelium. However, less extensive investigations on the use of penetration enhancers for the vaginal route have been carried out in comparison to other routes, such as intranasal and transdermal (see Sections 9.7.1 and 8.6.1). 

As discussed in Chapter 1 (Section 1.1) certain drugs (including peptides, proteins and nucleic acid therapeutics) are unsuitable for oral delivery and must be given intravenously. Research has recently been directed towards the development of alternatives to the parenteral route, such as the transdermal, nasal and other routes thus far discussed in this book, for the systemic delivery of such drugs. 

Figure 9 Soup spoon confonnation with van der Waals contours of N-dodecylaza-cycloheptan-2-one, obtained through torsion of the peptide bond over 10", with tpci-C2-C3-C4 = 62 . Refer to original reference for computational details. (From Ref. 83. Reprinted from International Journal of Pharmaceutics, 76(1-2), Hoogsraate et al. Kinetics, ultrastructural aspects and molecular modelling of transdermal peptide flux enhancement by W-alkylazacycloheptanones, pp. 37-47, 1991, with kind permission from Elsevier Science, NL, Sara Burgerhartstraat 25, 1055 KV, Amsterdam, The Netherlands.)...

Craane-van Hinsberg. Transdermal peptide iontophoresis, Ph.D. Dissertation, Leiden University, The Netherlands, 1994. 

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