Fernandes Ana R, Sanchez-Lopez Elena, Santini Antonello, Santos Tiago Dos, Garcia Maria L, Silva Amélia M, Souto Eliana B
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
i3s-Instituto de Investigação e Inovação em Saúde, Universidade do Porto, R. Alfredo Allen 208, 4200-135 Porto, Portugal.
Nanomaterials (Basel). 2021 Oct 18;11(10):2758. doi: 10.3390/nano11102758.
Oil-in-water nanoemulsions (NEs) are considered a suitable nanotechnological approach to improve the eye-related bioavailability of lipophilic drugs. The potential of cationic NEs is prominent due to the electrostatic interaction that occurs between the positively charged droplets with the negatively charged mucins present in the tear film. This interaction offers prolonged NEs residence at the ocular surface, increasing the drug absorption. Triamcinolone acetonide (TA) is one of the first pharmacologic strategies applied as an intravitreal injection in the treatment of age-related macular degeneration (AMD). Newly synthesized quaternary derivatives of 1,4-diazabicyclo[2.2.2]octane (DABCO) and quinuclidine surfactants have been screened with the purpose to select the best compound to formulate long-term stable NEs that combine the best physicochemical properties for the loading of TA intended for ocular administration.
水包油纳米乳剂(NEs)被认为是一种合适的纳米技术方法,可提高亲脂性药物的眼部生物利用度。由于带正电荷的液滴与泪膜中带负电荷的粘蛋白之间发生静电相互作用,阳离子纳米乳剂的潜力尤为突出。这种相互作用使纳米乳剂在眼表的停留时间延长,增加了药物吸收。曲安奈德(TA)是最早用于玻璃体内注射治疗年龄相关性黄斑变性(AMD)的药物策略之一。已筛选了新合成的1,4-二氮杂双环[2.2.2]辛烷(DABCO)和奎宁环表面活性剂的季铵衍生物,目的是选择最佳化合物来制备长期稳定的纳米乳剂,这些纳米乳剂结合了用于眼部给药的TA负载的最佳物理化学性质。