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In vivo iontophoretic delivery of salmon calcitonin across microporated skin.

Journal of pharmaceutical sciences (2012-05-31)
Viswatej Vemulapalli, Yun Bai, Haripriya Kalluri, Anushree Herwadkar, Hyun Kim, Shawn P Davis, Phil M Friden, Ajay K Banga
RESUMEN

The purpose of this study was to determine the effect of microneedle (MN) technology and its combination with iontophoresis (ITP) on the in vivo transdermal delivery of salmon calcitonin (sCT). Maltose MNs (500 µm) were used to porate skin prior to application of the drug, with or without ITP. Micropores created by maltose MNs were characterized by histological sectioning and calcein imaging studies, which indicated uniformity of the created micropores. In vivo studies were performed in hairless rats to assess the degree of enhancement achieved by ITP (0.2 mA/cm² for 1 h), MNs (81 MNs), and their combination. In vivo studies indicate a serum maximal concentration of 0.61 ± 0.42 ng/mL, 1.79 ± 0.72 ng/mL, and 5.51 ± 0.32 ng/mL for ITP, MNs, and combination treatment, respectively. MN treatment alone increased serum concentration 2.5-fold and the combination treatment increased the concentration ninefold as compared with iontophoretic treatment alone. Combination treatment of ITP and MNs resulted in the highest delivery of sCT and therapeutic levels were achieved within 5 min of administration.

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Sigma-Aldrich
Calcitonin salmon, ≥97% (HPLC), powder
Calcitonin salmon, European Pharmacopoeia (EP) Reference Standard