Stability of natural polyphenol fisetin in eye drops Stability of fisetin in eye drops

Krajčíková, Kristína; Suváková, Mária; Glinská, Gabriela; Ohlasová, Jana; Tomečková, Vladimı́ra

doi:10.1515/chem-2020-0029

Cited by 6 publications

(3 citation statements)

References 36 publications

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“…Despite higher solubility in the alkaline environment [38], the pKa of the OH group at the C7 position of FST is 7.27 in an aqueous and neutral medium. Therefore, when the pH is adjusted to 7.4, it would cause the deprotonation of FST, as shown in Figure S1 [39,40]. In this study, the release of FST within 24 h is between 10.8 and 19.9%, and the highest release is presented in the pH 7.4 medium, which fits the solubility in different pH conditions.…”

Section: In Vitro Releasesupporting

confidence: 67%

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

et al. 2021

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This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. The responses, including average particle size, polydispersity index, encapsulation efficiency, and zeta potential, were assessed. The optimized formulation possessed a mean particle size of 187.9 nm, the polydispersity index of 0.121, encapsulation efficiency of 79.3%, and zeta potential of −29.2 mV. The morphological observation demonstrated a globular shape for particles. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the encapsulated FST was presented as the amorphous state. The dissolution test indicated a 3.06-fold increase for the accumulating concentrations, and the everted gut sac test showed a 4.9-fold gain for permeability at the duodenum region. In conclusion, the optimized FST-loaded nanoparticle formulation in this work can be developed as an efficient oral delivery system of FST to improve its biopharmaceutic properties.

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Section: In Vitro Releasesupporting

confidence: 67%

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

et al. 2021

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“…Fisetin group: Treatment consisted of 0.1% fisetin in Hypromelóza—P (Unimed Pharma, Slovakia) eye drops (artificial tears) 3 times per day via 1 drop bilaterally for 14 days. Hypromelóza—P was used to ensure fisetin stability [ 39 ]. The fisetin dosage and duration of treatment were chosen based on the previous in vivo studies with polyphenols from the structurally same group—flavones [ 21 ].…”

Section: Methodsmentioning

confidence: 99%

The Effects of Fisetin on Cyclosporine-Treated Dry Eye Disease in Dogs

Krajčíková

Balicka²,

Lapšanská³

et al. 2023

IJMS

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Dry eye disease (DED) is a chronic debilitating ophthalmological disease with the current therapeutic options focused on the suppression of the symptoms. Among the possibilities of how to improve DED therapy, polyphenols have shown an enormous capacity to counteract DED functional changes. The study aimed to specifically target pathophysiological mechanisms by the addition of fisetin to the cyclosporine treatment protocol. We examined dog patients with DED on cyclosporine treatment that were administered 0.1% fisetin or fisetin-free eye drops. For the assessment of fisetin effects, tear film production and matrix metalloproteinase 9 (MMP-9) were studied in the tear film. Tear production was not recovered after 7 or 14 days (9.40 mm ± 6.02 mm, p = 0.47; 9.80 mm ± 6.83 mm, p = 0.53, respectively). MMP-9 levels significantly increased after 7 days and then dropped after 14 days (775.44 ng/mL ± 527.52 ng/mL, p = 0.05; 328.49 ng/mL ± 376.29 ng/mL, p = 1.00, respectively). Fisetin addition to cyclosporine DED treatment was not able to restore tear fluid production but influenced molecular pathological events through MMP-9.

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“…Compounds such as curcumin or quercetin have already exhibited encouraging results in both in vitro and in vivo models [ 51 ]. Improvement of marketed formulations with the addition of polyphenols, like in the case of Hypromelóza-P ® and fisetin, could also be a promising strategy [ 52 ].…”

Section: Ocular Pathologies Related To Oxidative Stress and Inflammentioning

confidence: 99%

Ocular Delivery of Polyphenols: Meeting the Unmet Needs

2021

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Nature has become one of the main sources of exploration for researchers that search for new potential molecules to be used in therapy. Polyphenols are emerging as a class of compounds that have attracted the attention of pharmaceutical and biomedical scientists. Thanks to their structural peculiarities, polyphenolic compounds are characterized as good scavengers of free radical species. This, among other medicinal effects, permits them to interfere with different molecular pathways that are involved in the inflammatory process. Unfortunately, many compounds of this class possess low solubility in aqueous solvents and low stability. Ocular pathologies are spread worldwide. It is estimated that every individual at least once in their lifetime experiences some kind of eye disorder. Oxidative stress or inflammatory processes are the basic etiological mechanisms of many ocular pathologies. A variety of polyphenolic compounds have been proved to be efficient in suppressing some of the indicators of these pathologies in in vitro and in vivo models. Further application of polyphenolic compounds in ocular therapy lacks an adequate formulation approach. Therefore, more emphasis should be put in advanced delivery strategies that will overcome the limits of the delivery site as well as the ones related to the polyphenols in use. This review analyzes different drug delivery strategies that are employed for the formulation of polyphenolic compounds when used to treat ocular pathologies related to oxidative stress and inflammation.

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Stability of natural polyphenol fisetin in eye drops Stability of fisetin in eye drops

Cited by 6 publications

References 36 publications

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

The Effects of Fisetin on Cyclosporine-Treated Dry Eye Disease in Dogs

Ocular Delivery of Polyphenols: Meeting the Unmet Needs

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