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Review

Penetration Enhancers for Topical Drug Delivery to the Ocular Posterior Segment—A Systematic Review

1
Institute of Inflammation and Ageing, College of Medical and Dental Sciences, University of Birmingham, Birmingham B15 2TT, UK
2
Department of Science, Waterford Institute of Technology, Cork Road, Waterford X91 K0EK, Ireland
3
Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+DFarma, Facultad de Farmacia and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain
4
Experimentica Ltd., Microkatu 1, P.O. Box 1199, 70211 Kuopio, Finland
*
Author to whom correspondence should be addressed.
Academic Editor: Rocio Herrero-Vanrell
Pharmaceutics 2021, 13(2), 276; https://doi.org/10.3390/pharmaceutics13020276
Received: 24 January 2021 / Revised: 11 February 2021 / Accepted: 15 February 2021 / Published: 18 February 2021
(This article belongs to the Special Issue Innovative Technologies to Treat Diseases of the Back of the Eye)
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. View Full-Text
Keywords: topical drug delivery; penetration enhancers; neuroprotection; retina; retinal ganglion cells; posterior segment topical drug delivery; penetration enhancers; neuroprotection; retina; retinal ganglion cells; posterior segment
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MDPI and ACS Style

Thareja, A.; Hughes, H.; Alvarez-Lorenzo, C.; Hakkarainen, J.J.; Ahmed, Z. Penetration Enhancers for Topical Drug Delivery to the Ocular Posterior Segment—A Systematic Review. Pharmaceutics 2021, 13, 276. https://doi.org/10.3390/pharmaceutics13020276

AMA Style

Thareja A, Hughes H, Alvarez-Lorenzo C, Hakkarainen JJ, Ahmed Z. Penetration Enhancers for Topical Drug Delivery to the Ocular Posterior Segment—A Systematic Review. Pharmaceutics. 2021; 13(2):276. https://doi.org/10.3390/pharmaceutics13020276

Chicago/Turabian Style

Thareja, Abhinav, Helen Hughes, Carmen Alvarez-Lorenzo, Jenni J. Hakkarainen, and Zubair Ahmed. 2021. "Penetration Enhancers for Topical Drug Delivery to the Ocular Posterior Segment—A Systematic Review" Pharmaceutics 13, no. 2: 276. https://doi.org/10.3390/pharmaceutics13020276

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