Pickering emulsions stabilised with oligoglycine-functionalised nanodiamond as a model system for ocular drug delivery applications.
Pickering emulsions stabilised with oligoglycine-functionalised nanodiamond as a model system for ocular drug delivery applications.
复制标题
用低聚甘氨酸功能化纳米金刚石稳定的皮克林乳液作为眼部药物输送应用的模型系统。
作者：
Huang Z
用常规表面活性剂稳定的水包油乳剂通常用于眼内给药的滴眼剂中。然而，表面活性剂的存在有时会刺激组织。此外，常规乳剂在眼组织上的滞留性通常较差。近年来，由于其生物相容性，用纳米颗粒稳定的Pickering乳液在一系列生物医学应用中获得了关注。在这里，皮克林乳液进行了评估，首次为限制的有机成分，在眼部药物输送的潜在应用。对于一个模型系统，我们使用nanodiamond（ND）纳米粒子功能化与共价键合的双尾（2T）寡聚甘氨酸C10（NGly4）2皮克林水包油乳液，这是稳定的超过三个月的存储在中性pH值。我们证明了ND-2T皮克林乳液的非毒性，相当于缓冲溶液，通过离体牛角膜渗透性和不透明度测试。ND-2T稳定乳剂中的油相在角膜组织上的保留显著增加，因为2T的带正电荷的末端氨基具有粘膜粘附特性。我们配制的乳液具有与泪液相当的表面张力、pH值和盐浓度。ND-2T稳定的乳剂在角膜表面上的高保留率以及它们的无毒性使它们具有用于眼部药物递送的独特优势。该模型系统的原理可以应用于未来设计的一系列制剂的药物输送。
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 C10(NGly4)2 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, via an ex vivo 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.