Chair in Pharmaceutical Technology, School of Pharmacy, Queen's University Belfast, 97 Lisburn Road, Belfast, BT9 7BL, UK.
Drug Deliv Transl Res. 2021 Oct;11(5):2169-2185. doi: 10.1007/s13346-020-00883-5. Epub 2021 Jan 15.
As microneedle (MN) patches progress towards commercialisation, there is a need to address issues surrounding their translation from the laboratory to the end-user. One important aspect of MN patches moving forward is appropriate primary packaging. This research focuses on MN patches containing amoxicillin (AMX) sodium for the potential treatment of neonatal sepsis in hot and humid countries. A MN patch consists of a hydrogel-forming MN array and a drug-containing reservoir. Improper primary packaging in hot and humid countries may result in degradation of active pharmaceutical ingredients, with the use of substandard medicines a major health concern. The research presented here, for the first time, seeks to investigate the integrity of MN patches in different primary packaging when stored under accelerated storage conditions, according to international guidelines. At pre-defined intervals, the performance of the MN patch was investigated. Major causes of drug instability are moisture and temperature. To avoid unnecessary degradation, suitable primary packaging was sought. After 168 days, the percentage of AMX sodium recovered from drug-containing reservoirs packaged in Protect™ 470 foil was 103.51 ± 7.03%. However, packaged in poly(ester) foil, the AMX sodium content decreased significantly (p = 0.0286), which is likely due to the degradation of AMX sodium by the imbibed moisture. Therefore, convincing evidence was provided as to the importance of investigating the stability of MN patches in primary packaging intended for MN-mediated transdermal delivery so that they are 'fit for purpose' when it reaches the end-user. Future work will include qualitative studies to assess MN patch usability.
随着微针(MN)贴片向商业化发展,需要解决从实验室到最终用户的转化问题。MN 贴片向前发展的一个重要方面是适当的初级包装。这项研究专注于含有阿莫西林(AMX)钠的 MN 贴片,用于治疗湿热国家的新生儿败血症。MN 贴片由水凝胶形成的 MN 阵列和含有药物的储库组成。在湿热国家,如果初级包装不当,可能会导致活性药物成分降解,使用劣质药物是一个主要的健康问题。这里介绍的研究首次根据国际指南,试图研究在加速储存条件下不同初级包装中的 MN 贴片的完整性。在预定义的间隔时间内,研究 MN 贴片的性能。药物不稳定性的主要原因是湿度和温度。为了避免不必要的降解,需要寻找合适的初级包装。在 168 天后,保特(Protect)470 箔片中包装的含药储库中回收的 AMX 钠百分比为 103.51±7.03%。然而,在聚酯箔中,AMX 钠含量显著下降(p=0.0286),这可能是由于吸收的水分导致 AMX 钠降解。因此,提供了令人信服的证据,证明在 MN 介导的经皮给药中,对初级包装中 MN 贴片的稳定性进行调查的重要性,以便当它们到达最终用户时,它们是“适合目的”的。未来的工作将包括定性研究,以评估 MN 贴片的可用性。