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Stability Test of PACAP in Eye Drops.
Journal of Molecular Neuroscience ( IF 3.1 ) Pub Date : 2020-04-22 , DOI: 10.1007/s12031-020-01532-9
Anita K Kovacs 1 , Tamas Atlasz 2, 3 , Dora Werling 2, 4 , Edina Szabo 2 , Dora Reglodi 2 , Gabor K Toth 1
Affiliation  

PACAP is a neuropeptide with widespread distribution and diverse biological functions. It has strong cytoprotective effects mediated mainly through specific PAC1 receptors. Experimental data show protective effects of PACAP in the retina and cornea in several pathological conditions. Although intravitreal injections are a common practice in some ocular diseases, delivery of therapeutic agents in the form of eye drops would be more convenient and would lead to fewer side effects. We have previously shown that PACAP, in the form of eye drops, is able to pass through the ocular barriers and can exert retinoprotective effects. As eye drops represent a promising form of administration of PACAP in ocular diseases, it is important to investigate the stability of PACAP in solutions used in eye drops. In this study, the stability of PACAP1-27 and PACAP1-38 in eye drops was measured in four common media and a commercially available artificial tear solution at both room temperature and +4 °C. Mass spectrometry results show that the highest stability was gained with PACAP1-38 in water and 0.9% saline solution at +4 °C, representing 80-90% drug persistence after 2 weeks. PACAP1-38 in the artificial tear showed very fast degradation at room temperature, but was stable at +4 °C. In summary, PACAP1-38 has higher stability than PACAP1-27, with highest stability at +4 °C in water solution, but both peptides in each medium can be stored for relatively longer periods without significant degradation. These data can provide reference for future therapeutic use of PACAP in eye drops.

中文翻译:

PACAP 在滴眼液中的稳定性测试。

PACAP是一种分布广泛、生物学功能多样的神经肽。它具有主要通过特定 PAC1 受体介导的强细胞保护作用。实验数据显示 PACAP 在几种病理条件下对视网膜和角膜的保护作用。虽然玻璃体内注射是一些眼部疾病的常见做法,但以滴眼液的形式递送治疗剂会更方便,并且会导致更少的副作用。我们之前已经表明,滴眼剂形式的 PACAP 能够穿过眼部屏障并发挥视网膜保护作用。由于滴眼液代表了 PACAP 在眼部疾病中的一种有前景的给药形式,因此研究 PACAP 在滴眼液中使用的溶液中的稳定性非常重要。在这项研究中,PACAP1-27 和 PACAP1-38 在滴眼液中的稳定性在四种常见介质和市售人工泪液中在室温和 +4 °C 下进行测量。质谱结果表明,PACAP1-38 在水和 0.9% 盐水溶液中在 +4 °C 下获得最高稳定性,代表 2 周后 80-90% 的药物持久性。人工泪液中的 PACAP1-38 在室温下显示出非常快的降解,但在 +4 °C 时稳定。综上所述,PACAP1-38 比 PACAP1-27 具有更高的稳定性,在 +4°C 的水溶液中稳定性最高,但两种肽在每种介质中都可以储存相对较长的时间而不会显着降解。这些数据可为今后PACAP在滴眼液中的治疗应用提供参考。
更新日期:2020-04-23
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