Abstract
Drug loaded dissolving microneedles (DMNs) fabricated with water soluble polymers have received increasing attentions as a safe and efficient transdermal drug delivery system. Usually, to reach a high drug delivery efficiency, an ideal drug distribution is gathering more drugs in the tip or the top part of DMNs. In this work, we introduce an easy and new method to introduce a bubble with controlled size into the body of DMNs. The introduction of bubbles can prevent the drug diffusion into the whole body of the MNs. The heights of the bubbles are well controlled from 75 μm to 400 μm just by changing the mass concentrations of polymer casting solution from 30 wt% to 10 wt%. The drug-loaded bubble MNs show reliable mechanical properties and successful insertion into the skins. For the MNs prepared from 15 wt% PVA solution, bubble MNs achieve over 80% of drug delivery efficiency in 20 seconds, which is only 10% for the traditional solid MNs. Additionally, the bubble microstructures in the MNs are also demonstrated to be consistent and identical regardless the extension of MN arrays. These scalable bubble MNs may be a promising carrier for the transdermal delivery of various pharmaceuticals.
Highlights
Skin was considered as a potential site for systemic delivery of biopharmaceuticals with the route of transdermal delivery, which was defined as a continuous administration of pharmaceuticals across the skin[1]
In this work, the traditional microneedles (TMNs) was defined as a kind of dissolving microneedle with solid body, which was fabricated by casting sufficient matrix into the mold after drug loading process as the method shown in Fig. 1a and b
bubble microneedles (BMNs) was defined as the dissolving microneedle with a bubble-shaped structure in the base of MN, which was fabricated by the method shown in Fig. 1a and c
Summary
Skin was considered as a potential site for systemic delivery of biopharmaceuticals with the route of transdermal delivery, which was defined as a continuous administration of pharmaceuticals across the skin[1]. To achieve higher drug delivery into the skins, the ideal model of DMNs should encapsulate drug only in the tip of MNs and release the drug rapidly after insertion. In this work, using a new fabrication method with one-step coating process, we fabricated the BMNs with varying sized bubble structures and investigated the property of them for transdermal drug delivery. The size of bubbles in MNs could be well controlled by changing the concentrations of polymer solution layers during casting process, and the controlled bubble size was able to further accurately control the drug distributions in MNs. BMNs described in this work have unique advantages in improving the efficiency of drug delivery and decreasing the time of administration, which is significant for the delivery of various biopharmaceutical and rapid self-administration of MNs in future
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