School of Life Sciences, Pharmacy, and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, UK.
National Heart and Lung Institute, Imperial College London, Guy Scadding Building, Royal Brompton Campus, London, SW3 6LY, UK.
Sci Rep. 2020 Jul 21;10(1):12010. doi: 10.1038/s41598-020-68722-8.
Neisseria gonorrhoeae bacteria are acknowledged as an urgent threat to human health because this species has developed resistances to all of the antibiotics used clinically to treat its infections. N. gonorrhoeae causes the sexually transmitted disease gonorrhoea, but also causes blindness when the bacteria infect the eyes. Infants are particularly susceptible, acquiring the infection from their mothers at birth. We have shown that the monoglyceride monocaprin rapidly kills N. gonorrhoeae and other bacterial species and is non-irritating in ocular assays. Here we show that the physical and chemical properties of monocaprin make it ideal for use in a thickened eye drop formulation to combat eye infections. Monocaprin-containing formulations were assessed using analytical techniques and for antimicrobial activity in vitro and in ex vivo infections. Monocaprin-containing formulations retained activity after three years and are non-irritating, unlike preparations of povidone iodine in our assays. A recommended formulation for further development and investigation is 0.25% monocaprin in 1% HPMC with 1% polysorbate 20.
淋病奈瑟菌被认为是对人类健康的一个紧急威胁，因为该物种已经对所有临床上用于治疗其感染的抗生素产生了耐药性。淋病奈瑟菌会引起性传播疾病淋病，但当细菌感染眼睛时也会导致失明。婴儿特别容易受到感染，他们会在出生时从母亲那里感染这种疾病。我们已经表明，单甘油脂辛酸单酯可以迅速杀死淋病奈瑟菌和其他细菌，并且在眼部试验中无刺激性。在这里，我们表明辛酸单甘酯的物理和化学性质使其非常适合用于浓稠的滴眼剂配方，以对抗眼部感染。使用分析技术评估了含有辛酸单甘酯的制剂，并评估了其在体外和体内感染中的抗菌活性。辛酸单甘酯制剂在三年后仍保持活性，而且与我们试验中的聚维酮碘制剂不同，它无刺激性。进一步开发和研究的推荐配方是 0.25%辛酸单甘酯在 1% HPMC 中，含有 1%聚山梨酯 20。
