1988
DOI: 10.1038/clpt.1988.201
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Successful transdermal administration of therapeutic doses of a polypeptide to normal human volunteers

Abstract: The human stratum corneum constitutes a relatively impermeable barrier to the transdermal absorption of most substances, including polypeptides and proteins. This double-blind, randomized, crossover study in 13 normal men evaluated whether a low level of electrical current could induce changes in cutaneous permeability sufficient to produce absorption of a polypeptide. We compared cutaneous absorption of 5 mg of leuprolide (a 9 amino acid luteinizing hormone releasing hormone analogue) in transdermal patches c… Show more

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Cited by 85 publications
(14 citation statements)
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“…In this respect the recently developed iontophoretic delivery devices appear to be very promising, particulary in pulsatile-controlled peptide drug delivery. By applying this new technique (poly) peptide penetration through the skin can be impressively enhanced, as has been reported for TRH, vasopressin and insulin in various animal models (89)(90)(91)(92) and for therapeutically relevant doses of the LHRH analogue leuprolide in human volunteers (93).…”
Section: '1 Vitro Percutaneous Transport Has Been Observedmentioning
confidence: 88%
“…In this respect the recently developed iontophoretic delivery devices appear to be very promising, particulary in pulsatile-controlled peptide drug delivery. By applying this new technique (poly) peptide penetration through the skin can be impressively enhanced, as has been reported for TRH, vasopressin and insulin in various animal models (89)(90)(91)(92) and for therapeutically relevant doses of the LHRH analogue leuprolide in human volunteers (93).…”
Section: '1 Vitro Percutaneous Transport Has Been Observedmentioning
confidence: 88%
“…For macromolecules and protein and peptide structures there have also been a number of encouraging published studies including: calcitonin (salmon) [29], corticotrophin-releasing hormone [30], delta sleep-inducing peptide [31], dextran sulphate [32], inulin [33], insulin [34][35][36][37][38], gonadotropinreleasing hormone [39], growth hormone-releasing factor [40], leuprolide acetate [23,41,43], leutenising hormonereleasing hormone [44][45][46], neutral thyrotrophin-releasing hormone [47], oligonucleotides [48,49], parathyroid hormone [50,51] and vasopressin [52,53]. To date, however, clinical studies have been limited to smaller molecules such as lidocaine [54][55][56], dexamethasone [57], etofenamate [58], naproxen [59], metoclopramide plus hydrocortisone [60], cortisone [61], vincristine [62] and fentanyl [63].…”
Section: Iontophoresismentioning
confidence: 99%
“…Iontophoretic transdermal delivery can offer the possibility for noninvasive and continuous steady-state delivery of the peptide into the systemic circulation. Although, successful iontophoretic delivery of leuprorelin across the skin in vivo has been demonstrated earlier [9,25], problems related to the poor transport efficiency and biological variation of the peptide transport still remain to be solved. Therefore, our study was aimed: (1) to test whether transdermal delivery of cationic peptide leuprorelin could be improved by pulsed current iontophoresis in comparison with the most common current profile À constant current, (2) to investigate and quantify the possible changes in iontophoretic transport mechanisms involved under these two current profiles, and (3) to study the potential of cation-exchange fibers as drug reservoirs for the transdermal delivery of this peptidic drug.…”
Section: Introductionmentioning
confidence: 98%