Modulating surface charge of dexamethasone non-spherical microcrystals for improved inner ear delivery.

Mingyue Ai, Chuanjia Guo, Liwei Wang, Ming Hu, Kaixu Xu, Chen Li, Zhimin Zhou

Colloids and surfaces. B, Biointerfaces 2021 Aug

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It is important to achieve precise surface charge manipulation of non-spherical drug microcrystals using facile and time-efficient methods for local drug delivery. In this study, silk-coated dexamethasone (DEX) non-spherical microcrystals were synthesized by precipitation technique followed by alternate deposition of poly(allylamine hydrochloride) (PAH) (or PAH-coated Fe3O4) and silk fibroin (SF) via layer-by-layer assembly. EDC and glutaraldehyde were employed to manipulate positive or negative charge of particles by simple chemical cross-linking reactions, respectively. In vivo assessment was carried out by intratympanic (IT) injection of DEX non-spherical microcrystals in guinea pigs. In vivo pharmacokinetic results demonstrate that negatively charged DEX microcrystals appeared to improve outcomes of inner ear delivery in comparison to positively-charged counterparts. This is partly because of the adhesive features of the SF. The present study may provide new ideas to construct surface charge-tunable drug delivery vehicles that are capable of crossing biological barriers, especially for inner ear delivery due to the simple and practical strategy. Copyright © 2021 Elsevier B.V. All rights reserved.

Citation

Mingyue Ai, Chuanjia Guo, Liwei Wang, Ming Hu, Kaixu Xu, Chen Li, Zhimin Zhou. Modulating surface charge of dexamethasone non-spherical microcrystals for improved inner ear delivery. Colloids and surfaces. B, Biointerfaces. 2021 Aug;204:111806