Fitaihi Rawan, Abukhamees Shorooq, Orlu Mine, Craig Duncan Q M
Research Department of Pharmaceutics, School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.
Pharmaceutics. 2023 May 30;15(6):1622. doi: 10.3390/pharmaceutics15061622.
Microneedles (MNs) have attracted considerable interest as a means of ocular drug delivery, a challenging delivery route due to the limitations imposed by the various biological barriers associated with this organ. In this study, a novel ocular drug delivery system was developed by formulating a dissolvable MN array containing dexamethasone-loaded PLGA microparticles for scleral drug deposition. The microparticles serve as a drug reservoir for controlled transscleral delivery. The MNs displayed sufficient mechanical strength to penetrate the porcine sclera. Dexamethasone (Dex) scleral permeation was significantly higher than in topically instilled dosage forms. The MN system was able to distribute the drug through the ocular globe, with 19.2% of the administered Dex detected in the vitreous humour. Additionally, images of the sectioned sclera confirmed the diffusion of fluorescent-labelled microparticles within the scleral matrix. The system therefore represents a potential approach for minimally invasive Dex delivery to the posterior of the eye, which lends itself to self-administration and hence high patient convenience.
微针作为一种眼部给药方式已引起了广泛关注,由于与该器官相关的各种生物屏障所带来的限制,眼部给药是一条具有挑战性的给药途径。在本研究中,通过制备一种含有载有地塞米松的聚乳酸-羟基乙酸共聚物(PLGA)微粒的可溶解微针阵列,用于巩膜药物沉积,从而开发出一种新型眼部给药系统。这些微粒作为药物储库,用于控制经巩膜给药。微针表现出足够的机械强度以穿透猪的巩膜。地塞米松(Dex)的巩膜渗透显著高于局部滴注剂型。微针系统能够使药物在眼球内分布,在玻璃体液中检测到19.2%的给药Dex。此外,切片巩膜的图像证实了荧光标记微粒在巩膜基质内的扩散。因此,该系统代表了一种将Dex微创递送至眼后部的潜在方法,这种方法便于自我给药,从而极大地方便了患者。