Thareja Abhinav, Hughes Helen, Alvarez-Lorenzo Carmen, Hakkarainen Jenni J, Ahmed Zubair
Institute of Inflammation and Ageing, College of Medical and Dental Sciences, University of Birmingham, Birmingham B15 2TT, UK.
Department of Science, Waterford Institute of Technology, Cork Road, Waterford X91 K0EK, Ireland.
Pharmaceutics. 2021 Feb 18;13(2):276. doi: 10.3390/pharmaceutics13020276.
There is an unmet clinical need for eye drop formulations to efficiently treat the diseases of the posterior ocular segment by non-invasive topical administration. Here, we systematically reviewed the literature on ocular penetration enhancers and their ability to transfer drugs to the posterior segment of the eye in experimental studies. Our aim was to assess which penetration enhancer is the most efficient at delivering drugs to the posterior segment of the eye, when topically applied. We conducted a comprehensive search in three electronic databases (Ovid Embase, Ovid MEDLINE, and PubMed) to identify all the relevant manuscripts reported on ocular penetration enhancers based on the PRISMA guidelines. We identified 6540 records from our primary database search and filtered them per our inclusion/exclusion criteria to select a final list of 14 articles for qualitative synthesis. Of these, 11 studies used cell penetrating peptides (CPPs), 2 used chitosan, and 1 used benzalkonium chloride (BAC) as the penetration enhancer. Cationic and amphipathic CPPs, transactivator of transcription (TAT), and penetratin can be inferred to be the best among all the identified penetration enhancers for drug delivery to the fundus oculi via topical eye drop instillation. Further high-quality experimental studies are required to ascertain their quantitative efficacy.
对于眼药水制剂而言，通过非侵入性局部给药有效治疗眼后节疾病存在未满足的临床需求。在此，我们系统回顾了关于眼部渗透促进剂及其在实验研究中将药物转运至眼后节能力的文献。我们的目的是评估哪种渗透促进剂在局部应用时将药物递送至眼后节的效率最高。我们在三个电子数据库（Ovid Embase、Ovid MEDLINE和PubMed）中进行了全面检索，以根据PRISMA指南识别所有关于眼部渗透促进剂的相关手稿。我们从主要数据库搜索中识别出6540条记录，并根据我们的纳入/排除标准对其进行筛选，以选择14篇文章的最终列表进行定性综合分析。其中，11项研究使用细胞穿透肽（CPPs），2项使用壳聚糖，1项使用苯扎氯铵（BAC）作为渗透促进剂。阳离子和两亲性CPPs、转录激活因子（TAT）和穿膜肽在所有已识别的渗透促进剂中可被推断为通过局部滴眼剂滴注将药物递送至眼底的最佳选择。需要进一步的高质量实验研究来确定它们的定量疗效。
