Biodegradable β-Cyclodextrin Conjugated Gelatin Methacryloyl Microneedle for Delivery of Water-Insoluble Drug

可生物降解的β-环糊精结合明胶甲基丙烯酰微针用于输送水不溶性药物

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作者:Xingwu Zhou, Zhimin Luo, Avijit Baidya, Han-Jun Kim, Canran Wang, Xing Jiang, Moyuan Qu, Jixiang Zhu, Li Ren, Fereshteh Vajhadin, Peyton Tebon, Niyuan Zhang, Yumeng Xue, Yudi Feng, Chengbin Xue, Yi Chen, KangJu Lee, Junmin Lee, Shiming Zhang, Chun Xu, Nureddin Ashammakhi, Samad Ahadian, Mehmet Remzi

Abstract

Transdermal delivery of water-insoluble drugs via hydrogel-based microneedle (MN) arrays is crucial for improving their therapeutic efficacies. However, direct loading of water-insoluble drug into hydrophilic matrices remains challenging. Here, a biodegradable MN array patch that is fabricated from naturally derived polymer conjugates of gelatin methacryloyl and β-cyclodextrin (GelMA-β-CD) is reported. When curcumin, an unstable and water-insoluble anticancer drug, is loaded as a model drug, its stability and solubility are improved due to the formation of an inclusion complex. The polymer-drug complex GelMA-β-CD/CUR can be formulated into MN arrays with sufficient mechanical strength for skin penetration and tunable drug release profile. Anticancer efficacy of released curcumin is observed in three-dimensional B16F10 melanoma models. The GelMA-β-CD/CUR MN exhibits relatively higher therapeutic efficacy through more localized and deeper penetrated manner compared with a control nontransdermal patch. In vivo studies also verify biocompatibility and degradability of the GelMA-β-CD MN arrays patch.

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