Biodegradable Beta-cyclodextrin Conjugated Gelatin Methacryloyl Microneedle for Delivery of Water-insoluble Drug

Transdermal delivery of water-insoluble drugs via hydrogel-based microneedle (MN) arrays is crucial for improving their therapeutic efficacies. However, direct loading water-insoluble drug into hydrophilic matrices remains challenging. Here we report a biodegradable MN arrays patch that is fabricated from naturally derived polymer conjugates of gelatin methacryloyl and (beta) b-cyclodextrin (GelMA-b-CD). 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 inclusion complex. The polymer-drug complex GelMA-b-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 (3D) B16F10 melanoma models. The GelMA-b-CD/CUR MN exhibits relatively higher therapeutic efficacy through more localized and deeper penetrated manner compared with a control non-transdermal patch. In vivo studies also verify biocompatibility and degradability of the GelMA-b-CD MN arrays patch.
Transdermal delivery of water-insoluble drugs via hydrogel-based microneedle (MN) arrays is crucial for improving their therapeutic efficacies. However, direct loading water-insoluble drug into hydrophilic matrices remains challenging. Here we report a biodegradable MN arrays patch that is fabricated from naturally derived polymer conjugates of gelatin methacryloyl and (beta) -cyclodextrin (GelMA- -CD). 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 inclusion complex. The polymer-drug complex GelMA- -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 (3D) B16F10 melanoma models. The GelMA- -CD/CUR MN exhibits relatively higher therapeutic efficacy through more localized and deeper penetrated manner compared with a control non-transdermal patch. In vivo studies also verify biocompatibility and degradability of the GelMA- -CD MN arrays patch.