In vitro–in vivo evaluation of tetrahydrozoline‐loaded ocular in situ gels on rabbits for allergic conjunctivitis management

Okur, Neslihan Üstündağ; Yozgatlı, Vildan; Okur, Mesut

doi:10.1002/ddr.21677

Cited by 28 publications

(22 citation statements)

References 54 publications

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“…The results showed that the expression of CCL5 mRNA and IL-17 mRNA in conjunctiva tissue and the percentage of IL-17 in spleen single cell suspension of mice in the subcutaneous injection group and the positive control group (eye drop stimulation) bore a striking resemblance, suggesting that subcutaneous injection stimulation can more effectively induce allergic conjunctivitis in mice. [34][35][36]…”

Section: Discussionmentioning

confidence: 99%

In vivo and in vitro Evaluation of in situ Gel Formulation of Pemirolast Potassium in Allergic Conjunctivitis

Shen

Yang

2021

DDDT

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Background: To establish a novel delivery system of pemirolast potassium-loaded gellan gum in situ gel in allergic conjunctivitis therapy. Methods: The prepared in situ gels were studied in the following aspects: in vitro gelation, in vitro release, stability, viscosity measurement, in vivo tear kinetics and pharmacodynamics. Results: In this study, the results showed that the viscosity of the in situ gels significantly increased when the preparation was in contact with simulated tear fluid and it also exhibited good stability in a period of three months. In vitro release showed that the release of pemirolast potassium from in situ gels had a good sustained release ability. No ocular damage or abnormal clinical signs to the cornea, iris, or conjunctivae were visible. Consistent with the in vitro studies, pemirolast potassium in situ gels were highly efficient in suppressing the inflammatory symptoms and improving the ocular bioavailability. Conclusion: Pemirolast potassium ocular in situ gels are safe and promising therapeutic alternatives to the existing medications for allergic conjunctivitis therapy.

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Section: Discussionmentioning

confidence: 99%

In vivo and in vitro Evaluation of in situ Gel Formulation of Pemirolast Potassium in Allergic Conjunctivitis

Shen

Yang

2021

DDDT

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“…At 6 h, THZ was not detectable for the marketed product, while 1.029 µg/mL of THZ was detected for the developed formulation. In addition, the ocular damage was not observed in both the optimized formulation and commercial product [38]. In short, thermosensitive in situ gel is a favorable approach to increase the ocular retention time and drug release, simultaneously improving the bioavailability and therapeutic outcome of ocular allergy.…”

Section: Other Ocular Diseasesmentioning

confidence: 95%

“…Ex vivo penetration: 0.582 ± 0.035% of THZ was detected in corneal tissue. In vivo studies: the concentration of THZ (1.029 µg/mL) in tear sample was higher in optimized formulation compared to THZ marketed product (no drug detected) at 6 h. In vivo ocular irritation: non-irritant [38] To develop disulfiram solid dispersion thermosensitive in situ gel to enhance corneal permeability and aqueous solubility.…”

Section: Bacterial Conjunctivitis/ofloxacinmentioning

confidence: 99%

“…The use of thermosensitive in situ gelling systems in the treatment of other diseases including corneal neovascularization, ocular allergy, and cataract has been studied [37,38,[49][50][51][52]. Corneal neovascularization is related to the invasion of new blood vessels into the cornea from the limbus because of an imbalance between angiogenic and antiangiogenic factors, which can be caused by ocular injury and diseases [52].…”

Section: Other Ocular Diseasesmentioning

confidence: 99%

“…Ocular allergy is another common ocular disorder; the symptoms such as itchiness can negatively impact patients' quality of life and productivity, leading to economic burden. Topical therapeutic agents have been used to alleviate symptoms by suppressing inflammatory responses [38,50]. Recently, Üstünda and co-workers developed and evaluated a thermosensitive dispersion of tetrahydrozoline (THZ)-loaded in situ gel (composed of poloxamer 188 and poloxamer 407) for ocular allergy.…”

Section: Other Ocular Diseasesmentioning

confidence: 99%

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Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research

et al. 2021

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Eyesight is one of the most well-deserved blessings, amid all the five senses in the human body. It captures the raw signals from the outside world to create detailed visual images, granting the ability to witness and gain knowledge about the world. Eyes are exposed directly to the external environment; they are susceptible to the vicissitudes of diseases. The World Health Organization has predicted that the number of individuals affected by eye diseases will rise enormously in the next decades. However, the physical barriers of the eyes and the problems associated with conventional ocular formulations are significant challenges in ophthalmic drug development. This has generated the demand for a sustained ocular drug delivery system, which serves to deliver effective drug concentration at a reduced frequency for consistent therapeutic effect and better patient treatment adherence. Recent advancement in pharmaceutical dosage design has demonstrated that a stimuli-responsive in situ gel system exhibits the favorable characteristics for providing sustained ocular drug delivery and enhanced ocular bioavailability. Stimuli-responsive in situ gels undergo a phase transition (solution–gelation) in response to the ocular environmental temperature, pH, and ions. These stimuli transform the formulation into a gel at the cul de sac to overcome the shortcomings of conventional eye drops, such as rapid nasolacrimal drainage and short contact time with the ocular surface This review highlights the recent successful research outcomes of stimuli-responsive in situ gelling systems in treating in vivo models with glaucoma and various ocular infections. Additionally, it also presents the mechanism, recent development, and safety considerations of stimuli-sensitive in situ gel as the potential sustained ocular delivery system for treating common eye disorders.

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Managing allergic conjunctivitis via ophthalmic microemulsions: Formulation, characterization, in vitro irritation studies based onEpiOcular™ eye irritation assay and in vivo studies in rabbit eye

Yozgatlı

Okur

et al. 2023

J Surfact & Detergents

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The purpose of this work was the development of an alternative ocular tetrahydrozoline hydrochloride (THZ) microemulsion for the management of allergic conjunctivitis. Pseudo‐ternary phase diagrams were used to produce the microemulsions. For the formulation of the microemulsions, isopropyl myristate was selected as oil. Furthermore, various surfactants were applied for the determination of their suitability; ME‐1 and ME‐4 were developed using Sorbitan monolaurate 80 and Polysorbate 80, for ME‐2 and ME‐5 Sorbitan monolaurate 80 and macrogolglycerol ricinoleate while for ME‐3 and ME‐6 Sorbitan monolaurate 80 and Polysorbate 20. For ME‐1, ME‐2, and ME‐3 propylene glycol and ethanol, for ME‐4, ME‐5, and ME‐6 ethanol and polyethylene glycol were used as co‐surfactants. Various characterization parameters of microemulsions were evaluated such as droplet size, conductivity, zeta potential, viscosity, and pH. In addition, the drug release, stability, sterility, safety, ex vivo, and in vivo experiments were studied. The characterization showed that the formulations can act as suitable carriers for eye application. In addition, it was revealed that microemulsions were found stable and sterile. The formulations released the drug in a sustained manner. Ex vivo diffusion studies exhibited that the microemulsions can be used for topical delivery to the eye. Assessment of in vitro ocular irritation was conducted by an in vivo prediction model, EpiOcular™ eye irritation test. Based on the in vivo studies, the chosen ideal microemulsion showed longer contact time to the cornea than the commercial product. Moreover, the developed ocular carrier was found to be safe from the viewpoint of in vitro ocular irritancy and mutagenicity. In conclusion, according to characterization results, the THZ microemulsions can act as a hopeful approach for topical eye application.

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In vitro–in vivo evaluation of tetrahydrozoline‐loaded ocular in situ gels on rabbits for allergic conjunctivitis management

Cited by 28 publications

References 54 publications

In vivo and in vitro Evaluation of in situ Gel Formulation of Pemirolast Potassium in Allergic Conjunctivitis

In vivo and in vitro Evaluation of in situ Gel Formulation of Pemirolast Potassium in Allergic Conjunctivitis

Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research

Managing allergic conjunctivitis via ophthalmic microemulsions: Formulation, characterization, in vitro irritation studies based onEpiOcular™ eye irritation assay and in vivo studies in rabbit eye

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