Univ. Lille, CNRS, Centrale Lille, Univ. Polytechnique Hauts-de-France, UMR 8520 - IEMN, F-59000 Lille, France.
Laboratory of General Biochemistry and Physical Pharmacy, Faculty of Pharmaceutical Sciences, Ghent University, 9000 Ghent, Belgium.
ACS Appl Mater Interfaces. 2023 Jan 25;15(3):3760-3771. doi: 10.1021/acsami.2c18598. Epub 2023 Jan 16.
Reaching the corneal endothelium through the topical administration of therapeutic drugs remains a challenge in ophthalmology. Besides, endothelial cells are not able to regenerate, and diseases at this site can lead to corneal blindness. Targeting the corneal endothelium implies efficient penetration through the three corneal layers, which still remains difficult for small molecules. Carbon quantum dots (CQDs) have demonstrated great potential for ocular nanomedicine. This study focuses on the corneal penetration abilities of differently charged CQDs and their use as permeation enhancers for drugs. Excised whole bovine eyes were used as an model to investigate corneal penetration of CQDs derived from glucosamine using β-alanine, ethylenediamine, or spermidine as a passivation agent. It was found that negatively charged CQDs have limited corneal penetration ability, while positively charged CQDs derived from glucosamine hydrochloride and spermidine (CQD-S) penetrate the entire corneal epithelium all the way down to the endothelium. CQD-S were shown to enhance the penetration of FITC-dextran 150 kDa, suggesting that they could be used as efficient penetration enhancers for therapeutic delivery to the corneal endothelium.
通过局部给药将治疗药物递送到角膜内皮仍然是眼科领域的一个挑战。此外，内皮细胞不能再生，而该部位的疾病会导致角膜失明。靶向角膜内皮意味着需要有效地穿透三层角膜，这对于小分子来说仍然很困难。碳量子点 (CQD) 在眼科纳米医学中显示出巨大的潜力。本研究专注于不同带电 CQD 的角膜穿透能力及其作为药物渗透增强剂的用途。使用来源于葡糖胺的 β-丙氨酸、乙二胺或亚精胺作为钝化剂的离体全牛眼被用作模型来研究 CQD 的角膜穿透能力。结果发现，带负电荷的 CQD 穿透角膜的能力有限，而带正电荷的来源于葡糖胺盐酸盐和亚精胺的 CQD (CQD-S) 则可以穿透整个角膜上皮直至内皮。结果表明 CQD-S 可以增强 FITC-葡聚糖 150 kDa 的穿透，这表明它们可以用作将治疗药物递送到角膜内皮的有效渗透增强剂。
