单一或复合高分子材料用于载药可溶性聚合物微针的制备

doi:10.11896/cldb.18040131

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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.

Key words： dissolving microneedles lidocaine hydrochloride polymer materials mechanical properties high drug loading

Published: 16 May 2019

CLC number:

R944.9

Fund:This work was supported by the Key Science and Technology Innovation Team of Zhejiang Province (2013TD15).

About author:: Haohui Zhan received his B.S. degree in pharmaceutical preparation from Wuhan Institute of Technology in 2016. He is currently pursuing his M.S. at the College of Pharmaceutical Science, Zhejiang University of Technology under the supervision of Prof. Fengsen Ma. His research has focused on the transdermal delivery of biologics and bioactiveingredients based on dissolving microneedles.
Fengsen Ma obtained his M.E. degree from Zhejiang University. He is currently a professor and master student supervisor. As a senior expert in the pharmaceutical research of Zhejiang Province, he is the principal person in charge of the two professional committees including biopharmaceuticals and medical devices. His laboratory has been engaged in the research and development of novel transdermal preparations, biopharmaceuticals and biological materials for many years. The basis of related research work, team, common key technologies and the application of products have been accumulated, especially for the system of microneedles technology. The team already has a lot of national invention patents and papers.

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Cite this article:

ZHAN Haohui,HUANG Yingcong,MA Fengsen. Drug-loaded Dissolving Microneedles Prepared by Single or Composite Polymer Materials[J]. Materials Reports, 2019, 33(10): 1738-1744.

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http://www.mater-rep.com/EN/10.11896/cldb.18040131 OR http://www.mater-rep.com/EN/Y2019/V33/I10/1738

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