Abstract: Microneedles is a novel type of transdermal drug delivery technology based on macromolecule polymers. The research of dissolving microneedles has aroused enormous attention, recently. The optimum preparation conditions of dissolving microneedles were optimized through lite-rature review and experiments. Several common polymer materials including hyaluronic acid (HA), chondroitin sulfate (CS), polyvinyl pyrrolidone (PVP), polyvinyl alcohol (PVA), carboxymethyl cellulose (CMC), poly(methylvinylether-co-maleic anhydride) (Gantrez) and hydroxypropyl methyl cellulose (HPMC) were selected to synthesize the dissolving microneedles in a single or composite manner, in which model drug lidocaine hydrochloride was loaded. Specifically, the female mold was made from metal microneedles by reverse mould method, and the dissolving microneedles were prepared by casting method. According to the solubility of the polymer materials and the model drug, the suitable solvent for preparing microneedles was screened out. Dissolving microneedles prepared with distilled water presented favorable needle shape and less bubbles. Bubbles in matrix solution could be eliminated by centrifugation in a fast and efficient way. Taking the morphology, mechanical pro-perty and hygroscopicity as the evaluation indicators, the feasibility of preparing drug-loaded dissolving microneedles from various polymer materials was studied. The proportions of the various components were adjusted and optimized to find out the polymer materials with excellent mechanical properties, moisture resistance and high drug loading amount. Dissolving microneedles prepared by optimal parameters were characterized by SEM and skin puncture experiment. The results indicated that the microneedles prepared by macromolecule polymers of Gantrez S-97 and HPMC at a mass ratio of 4∶1 were able to load with 70wt% lidocaine hydrochloride. It possessed excellent mechanical properties and slight hygroscopicity, which could easily penetrate into the skin and realize the smooth delivery of large dosage of drugs.
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