Protective Effects of a Quercetin-Rich Fluorocarbon-Modified Chitosan Eyedrop from Radish (Raphanus sativus L.) Leaves Against Streptozotocin-induced Diabetic Retinopathy in Rats: An In Silico and In Vivo Study

DOI

10.2991/978-94-6239-836-8_10How to use a DOI?

Keywords

Quercetin; Raphanus sativus L.; Fluorocarbon-Modified Chitosan; Molecular Docking; VEGF-A; Diabetic Retinopathy; Ocular Drug Delivery

Abstract

Diabetic retinopathy (DR) is a major microvascular complication of diabetes, in which chronic hyperglycaemia, oxidative stress, and vascular endothelial growth factor A (VEGF-A) overexpression drive pathological retinal angiogenesis. Current anti-VEGF therapy requires repeated intravitreal injections, motivating the search for noninvasive alternatives. This study developed and evaluated a topical quercetin eye drop derived from radish (Raphanus sativus L.) leaves, encapsulated in fluorocarbon-modified chitosan (FCS), using in silico, physicochemical, and in vivo assessments. Molecular docking against VEGF-A (PDB 3QTK) showed that quercetin had the second most favourable binding energy (−8.21 kcal/mol; inhibition constant 9.089 μM) among the four candidate flavonols, after the anti-VEGF comparator faricimab (−8.93 kcal/mol), and shared several binding pocket residues with it. Leaves extracted by 70% ethanol maceration yielded 23.20% extract (moisture 7.85%) with positive flavonoid, alkaloid, saponin, tannin, triterpenoid, and phenolic reactions; HPLC confirmed quercetin at 125.430 ppm. The FTIR spectrum of the FCS carrier showed an FTIR spectrum 99.48% correlation with the chitosan standard. Three eye drop variants containing 100, 50, and 25 mg of extract (V1–V3) were clear, odourless, and sterile liquids at pH 7, with viscosities of 2.809, 2.505, and 2.214 cP; mean particle size was 24.67 nm, encapsulation efficiency ranged from 84.72–93.85%, and refractive indices fell within the accepted ocular range. In streptozotocin-induced diabetic rats, the highest-dose formulation (P1) produced the greatest fasting blood glucose reduction (62.47 ± 0.45%) and the lowest retinal histopathological damage score (4.00 ± 0.63) compared with the diabetic control (14.33 ± 1.21; Kruskal–Wallis test, p < 0.05). These findings provide preliminary, biologically plausible evidence that quercetin-FCS eye drops may protect against diabetic retinal injury, supported in silico by favourable VEGF-A binding affinity; however, direct in vivo VEGF quantification is still required before a VEGF-targeted mechanism can be confirmed.

Copyright

© 2026 The Author(s)

Open Access

Open Access This chapter is licensed under the terms of the Creative Commons Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/), which permits any noncommercial use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license and indicate if changes were made.

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TY  - CONF
AU  - Zahra Ramadhani
AU  - Setia Nurhidayah
AU  - Husnul Fikri
AU  - Dzaki Ahmad Lubis
AU  - Kaysha Natania Nurdin Putri
AU  - Humairah Medina Liza Lubis
PY  - 2026
DA  - 2026/11/11
TI  - Protective Effects of a Quercetin-Rich Fluorocarbon-Modified Chitosan Eyedrop from Radish (Raphanus sativus L.) Leaves Against Streptozotocin-induced Diabetic Retinopathy in Rats: An In Silico and In Vivo Study
BT  - Proceedings of the3rd Malikussaleh International Conference on Health and Disaster Medicine 2026  (MICOHEDMED 2026)
PB  - Atlantis Press
SP  - 91
EP  - 104
SN  - 2468-5739
UR  - https://doi.org/10.2991/978-94-6239-836-8_10
DO  - 10.2991/978-94-6239-836-8_10
ID  - Ramadhani2026
ER  -