School of Mathematics and Physics, Faculty of Engineering and Physical Sciences, University of Surrey, Guildford, GU2 7XH, UK.
Reading School of Pharmacy, University of Reading, Whiteknights, Reading, RG6 6DX, UK.
Soft Matter. 2023 Jul 26;19(29):5513-5526. doi: 10.1039/d3sm00495c.
Oil-in-water emulsions, stabilised with conventional surfactants, are commonly used in eye drops for ocular drug delivery. However, the presence of surfactants can sometimes irritate tissues. Furthermore, conventional emulsions often have poor retention on ocular tissue. Pickering emulsions stabilised with nanoparticles have been gaining attention in recent years for a range of biomedical applications because of their biocompatibility. Here, Pickering emulsions were evaluated for the first time for the confinement of organic components for potential application in ocular drug delivery. For a model system, we used nanodiamond (ND) nanoparticles functionalised with covalently-bonded two-tail (2T) oligoglycine C(NGly) to make Pickering oil-in-water emulsions, which were stable over three months of storage under neutral pH. We proved the non-toxicity of ND-2T Pickering emulsions, comparable to buffer solution, an bovine corneal permeability and opacity test. The retention of the oil phase in the ND-2T stabilised emulsions on corneal tissue is significantly increased because of the mucoadhesive properties arising from the positively-charged terminal amino groups of 2T. Our formulated emulsions have a surface tension, pH and salt concentration comparable to that of tear fluid. The high retention of the ND-2T-stabilised emulsions on the corneal surface, in combination with their non-toxicity, gives them distinct advantages for ocular drug delivery. The principles of this model system could be applied in the future design of a range of formulations for drug delivery.
水包油乳液,由常规表面活性剂稳定,常用于眼部药物输送的眼药水。然而,表面活性剂的存在有时会刺激组织。此外,常规乳液在眼部组织上的保留时间通常较短。近年来,由于其生物相容性,由纳米颗粒稳定的 Pickering 乳液在各种生物医学应用中受到关注。在这里,首次评估了 Pickering 乳液在有机成分的限制方面的应用,以用于眼部药物输送。对于模型体系,我们使用纳米金刚石 (ND) 纳米颗粒,其表面通过共价键连接两个尾端(2T)寡甘氨酸 C(NGly),以制造 Pickering 水包油乳液,在中性 pH 值下储存三个月后仍稳定。我们证明了 ND-2T Pickering 乳液的非毒性,与缓冲溶液相当,牛眼角膜通透性和不透明度测试也是如此。由于 2T 的末端氨基带正电荷,因此 ND-2T 稳定的乳液在角膜组织上的油相保留率显著增加,具有黏膜黏附性。我们配方的乳液的表面张力、pH 值和盐浓度与泪液相当。ND-2T 稳定的乳液在角膜表面的高保留率,结合其非毒性,使它们在眼部药物输送方面具有明显的优势。该模型体系的原理可应用于未来一系列药物输送配方的设计。