Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 423, Issue 2, Pages 257-263Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2011.11.046
Keywords
Microneedle; Peptide delivery; Salmon calcitonin; Transdermal drug delivery
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Funding
- U.S. National Institutes of Health
- Gulhane Military Medical Academy, Turkey
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Peptides and polypeptides have important pharmacological properties but only a limited number have been exploited as therapeutics because of problems related to their delivery. Most of these drugs require a parenteral delivery system which introduces the problems of pain, possible infection, and expertise required to carry out an injection. The aim of this study was to develop a transdermal patch containing microneedles (MNs) coated with a peptide drug, salmon calcitonin (sCT), as an alternative to traditional subcutaneous and nasal delivery routes. Quantitative analysis of sCT after coating and drying onto microneedles was performed with a validated HPLC method. In vivo studies were carried out on hairless rats and serum levels of sCT were determined by ELISA. The AUC value of MNs coated with a trehalose-containing formulation (250 +/- 83 ng/mL min) was not significantly different as compared to subcutaneous injections (403 +/- 53 ng/mL min), but approximately 13 times higher than nasal administration (18.4 +/- 14.5 ng/mL min). T-max (5 +/- 5 min) values for MN mediated administration were 50% shorter than subcutaneous injections (15 min), possibly due to rapid sCT dissolution and absorption by dermal capillaries. These results suggest that with further optimization of coating formulations, microneedles may enable administration of sCT and other peptides without the need for hypodermic injections. (C) 2011 Elsevier B.V. All rights reserved.
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