Journal
PHARMACEUTICAL RESEARCH
Volume 28, Issue 1, Pages 7-21Publisher
SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-010-0097-7
Keywords
bioavailability; desmopressin (DDAVP); dissolving microneedles; recombinant human growth hormone (rhGH); transdermal delivery
Funding
- MEXT (Ministry of Education, Culture, Sports, Science and Technology, MEXT)
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Purpose Feasibility study of two-layered dissolving microneedles for percutaneous delivery of peptide/proteins using recombinant human growth hormone (rhGH) and desmopressin (DDAVP). Methods Two-layered dissolving microneedles were administered percutaneously to the rat skin. Plasma rhGH and DDAVP concentrations were measured by EIA and LC/MS/MS. In vivo dissolution and diffusion rates of drugs in the skin were studied using tracer dyes, lissamine green B (LG) for rhGH and evans blue (EB) for DDAVP. Diffusion of drugs vertically into the skin was studied using FITC-dextran (MW=20 kDa)-loaded dissolving microneedles. Stability experiments were performed at -80 degrees C and 4 degrees C. Results The absorption half-lives, t(1/2a), of rhGH and DDAVP from dissolving microneedles were 23.7 +/- 4.3-28.9 +/- 5.2 and 14.4 +/- 2.9-14.1 +/- 1.1 min; the extents of bioavailability were 72.8 +/- 4.2-89.9 +/- 10.0% and 90.0 +/- 15.4-93.1 +/- 10.3%, respectively. LG and EB disappeared from the administered site within 2 h and 3 h after administration. Five green fluorescein spots were detected at 15 s and enlarged transversally at 30 s. FITC-dextran was delivered into the microcapillaries at 5 min and 10 min. The rhGH and DDAVP were stable in dissolving microneedles for one month at -80 degrees C and 4 degrees C. Conclusions Results suggest that the two-layered dissolving microneedles are useful as an immediate-release transdermal DDS for peptide/protein drugs.
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