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Objectives-The aim of the study was to investigate the effect of microneedle (MN) treatment on the transdermal delivery of a model drug (rhodamine B, Rh B) encapsulated in polylactic-coglycolic acid (PLGA) nanoparticles (NPs) focusing on the MN characteristics and application variables. Methods-Gantrez®MNs were fabricated using laser-engineered silicone micro-mould templates. PLGA NPs were prepared using a modified emulsion-diffusion-evaporation method * Corresponding author. Conflict of interest:The Author(s) declare(s) that they have no conflicts of interest to disclose. Conclusions-This dual MN/NPs mediated approach offers potential for both the dermal and transdermal delivery of therapeutic agents with poor passive diffusion. Europe PMC Funders Group

The aim of this study was to develop a dissolving microneedle (MN) patch for administration of inactivated polio vaccine (IPV) with improved thermal stability when compared with conventional liquid IPV. Excipient screening showed that a combination of maltodextrin and D-sorbitol in histidine buffer best preserved IPV activity during MN patch fabrication and storage. As determined by D-antigen ELISA, all three IPV serotypes maintained > 70% activity after 2 months and > 50% activity after 1-year storage at 5 °C or 25 °C with desiccant. Storage at 40 °C yielded > 40% activity after 2 months and > 20% activity after 1 year. In contrast, commercial liquid IPV types 1 and 2 lost essentially all activity within 1 month at 40 °C and IPV type 3 had < 40% activity. Residual moisture content in MN patches measured by thermogravimetric analysis was 1.2–6.5%, depending on storage conditions. Glass transition temperature measured by differential scanning calorimetry, structural changes measured by X-ray diffraction, and molecular interactions measured by Fourier transform infrared spectroscopy showed changes in MN matrix properties, but they did not correlate with IPV activity changes during storage. We conclude that appropriately formulated MN patches can exhibit thermostability that could enable distribution of IPV with less reliance on cold chain storage.Electronic supplementary materialThe online version of this article (10.1007/s13346-018-00608-9) contains supplementary material, which is available to authorized users.

There is an urgent need to replace the injection currently used for low molecular weight heparin (LMWH) multi-dose therapy with a non-invasive delivery device. In this study, laser-engineered dissolving microneedle (DMN) arrays fabricated from aqueous blends of 15% w/w poly (methylvinylether co maleic anhydride) have been fabricated as a potential device for the active transdermal delivery of nadroparin calcium (NC) as a model LMWH. An array loading of 630 IU of NC was achieved without compromising the array mechanical strength or the drug bioactivity. Application of NC-DMNs to dermatomed human skin (DHS) using the single step “poke and release” approach allowed permeation of approximately 10.6 % of the total NC load over a 48 h-study period. The cumulative amount of NC that permeated DHS at 24 h and 48 h attained 12.28 ± 4.23 IU/cm2 and 164.84 ± 8.47 IU/cm2, respectively. Skin permeation of NC could be modulated by controlling the DMN array variables, such as MN length and array density as well as application force to meet various clinical requirements including adjustment for body mass and renal function. NC-loaded DMN offer potentials as a relatively low cost functional delivery system for the transdermal delivery of LMWH and other macromolecules.