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

Transdermal drug delivery offers advantages over nonparenteral routes such as bypassing first-pass metabolism and facile administration. Mammalian skin, however, functions as a protective layer to the external environment and a fundamental barrier for transdermal delivery. Various strategies have been developed to overcome this barrier physically including transdermal microneedle (MN) array patches able to penetrate the stratum corneum that greatly enhances systemic drug delivery with minimal pain and improved patient compliance.

A biodegradable MN array patch was fabricated from naturally derived polymer conjugates of gelatin methacryloyl and 𝜷-cyclodextrin (GelMA-𝜷-CD). When curcumin, an unstable and water-insoluble anticancer drug, was 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 was formulated into MN arrays with sufficient mechanical strength for skin penetration and tunable drug release profile. Anticancer efficacy of released curcumin was observed in three-dimensional B16F10 melanoma models. The GelMA-𝜷-CD/CUR MN exhibited relatively higher therapeutic efficacy through more localized and deeper penetrated manner compared with a control nontransdermal patch. In vivo studies also verified biocompatibility and degradability of the GelMA-𝜷-CD MN arrays patch.

Fig. 1 Schematic for GelMA-𝛽-CD synthesis and GelMA-𝛽-CD based microneedle fabrication and application. A) Synthesis route of GelMA-𝛽-CD by conjugating GelMA with (I) CM-𝛽-CD conjugation via EDC/NHS coupling. (II) Curcumin was loaded within GelMA-𝛽-CD pre-gel solution to form curcumin inclusion complex. B) Schematic for fabrication of GelMA-𝛽-CD/curcumin by (III) centrifugation and UV crosslinking; GelMA-𝛽-CD/curcumin arrays were tested on 3D B16F10 skin cancer model (IV).

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Zhou, X., Luo, Z., Baidya, A., Kim, H., Wang, C., Jiang, X., … Khademhosseini, A. (2020). Biodegradable β ‐Cyclodextrin Conjugated Gelatin Methacryloyl Microneedle for Delivery of Water‐Insoluble Drug. Advanced Healthcare Materials, 2000527. doi:10.1002/adhm.202000527