Study on the fabrication and characterization of tip-loaded dissolving microneedles for transdermal drug delivery.

In order to increase the utilization rate of drug carried by microneedles and reduce waste, a two-step casting method was proposed to fabricate tip-loaded dissolving microneedles in this paper. The tip-loaded dissolving microneedles, also named layered microneedles, was consisted of two layers. The tip layer of the microneedles carried model drug, while the backing layer was fabricated with pure dissolving material. Polyvinyl alcohol, polyvinylpyrrolidone and hyaluronic acid were used as the base materials to fabricate the dissolving layers of the microneedle patches. Rhodamine B was chosen as the model drug to show the layered structure of tip-loaded microneedles. The material formulation and fabricating conditions of the tip-loaded dissolving microneedles and their transdermal insulin delivery efficiency were systematically studied. Nanoindentation testing showed that the tips of all three kinds of dissolving microneedles can bear the maximum loading of 50 mN with no damages, indicated sufficient mechanical strength for smooth skin puncturing as the minimum pressure required was 10 mN only. Moreover, our fabricated tip-loaded dissolving microneedles can greatly reduce the drug waste cause by unused backing layer in normal microneedles and realize a 30% enhancement of drug delivery efficiency after puncture treatment.