Beijing Laboratory of Biomedical Materials, College of Materials Science and Engineering, Beijing University of Chemical Technology, Beijing, 100029, P.R. China.
Beijing Laboratory of Biomedical Materials, College of Materials Science and Engineering, Beijing University of Chemical Technology, Beijing, 100029, P.R. China..
J Control Release. 2017 Nov 10;265:14-21. doi: 10.1016/j.jconrel.2017.03.383. Epub 2017 Mar 24.
As an alternative to hypodermic needles, coated polymer microneedles (MNs) are able to deliver drugs to subcutaneous tissues after being inserted into the skin. The dip-coating process is a versatile, rapid fabricating method that can form coated MNs in a short time. However, it is still a challenge to fabricate coated MNs with homogeneous and precise drug doses in the dip-coating process. In this study, to fabricate coated polymer microneedles with controlled drug loading, an adjustable apparatus that can be lifted and lowered was designed to immerse a polylactic acid (PLA) MN patch in the coating solutions. Using the coating solution containing 0.5% (w/w) sulforhodamine B, the drug loadings were up to 12ng, 14ng, and 18ng per needle for the MNs with heights of 550μm, 650μm, and 750μm, respectively. Moreover, for the MNs with a 650-μm height, when increasing the viscosity of the coating solutions from 150mPa·s to 1360mPa·s, 2850mPa·s, and 8200mPa·s, the drug loading increased from 2.5ng to 5ng, 14ng, and 22ng per needle, respectively. Meanwhile, the drug delivery efficiencies of these MNs were approximately 90%. In the insertion experiments, the MNs could successfully penetrate the skin and deliver the coated drug with approximately 90% efficiency when the MN tips were exposed to the outer environment. In vivo studies in mice indicated that the coated polymer MNs continuously delivered drugs, and the skin recovered without any injuries. These results demonstrated that the coated polymer MN was a safe and effective method for transdermal drug delivery.
作为皮下注射针的替代方法,涂覆聚合物微针(MN)在插入皮肤后能够将药物递送至皮下组织。浸涂工艺是一种通用的、快速的制造方法,可以在短时间内形成涂覆 MN。然而,在浸涂过程中制造具有均匀和精确药物剂量的涂覆 MN 仍然是一个挑战。在这项研究中,为了制造具有受控药物负载的涂覆聚合物微针,设计了一个可升降的可调装置,将聚乳酸(PLA)MN 贴片浸入涂层溶液中。使用含有 0.5%(w/w)磺基罗丹明 B 的涂层溶液,MN 高度分别为 550μm、650μm 和 750μm 的微针的药物负载量分别高达 12ng、14ng 和 18ng。此外,对于高度为 650μm 的 MN,当将涂层溶液的粘度从 150mPa·s 增加到 1360mPa·s、2850mPa·s 和 8200mPa·s 时,药物负载量分别从 2.5ng 增加到 5ng、14ng 和 22ng。同时,这些 MN 的药物递送效率约为 90%。在插入实验中,当 MN 针尖暴露在外部环境中时,MN 能够成功穿透皮肤并以约 90%的效率递涂层药物。在小鼠的体内研究中,涂覆聚合物 MN 持续递送药物,并且皮肤没有任何损伤地恢复。这些结果表明,涂覆聚合物 MN 是一种安全有效的经皮药物递送方法。