Design and Optimization of In Situ Gelling Mucoadhesive Eye Drops Containing Dexamethasone

Szalai, Boglárka; Jójárt-Laczkovich, Orsolya; Kovács, Anita; Berkó, Szilvia; Balogh, György Tibor; Katona, Gábor; Budai-Szűcs, Mária

doi:10.3390/gels8090561

Cited by 9 publications

(5 citation statements)

References 59 publications

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“…An increase in the concentration of Pluronic F-127 and Pluronic F-68 led to a decrease in the gelling time. The higher gelation time results in the decrease in the residence time, whereas a gelation time of less than 2 min disturbs the distribution of the gel in the nasal cavity . The lag time of gelation was analyzed, which showed that the HJ7DG (in situ gel of the optimized formulation HJ7D in the HJ3G gelling system) formulation possessed the shortest lag time in between 3 and 4 min.…”

Section: Resultsmentioning

confidence: 99%

“…The remaining fluoxetine concentration 332.35 ± 0.35 μg/mL was absorbed in the olfactory region of the brain. In the case of fluoxetine-loaded cubosomal in situ gel, it displayed a sustained release profile for 24 The results of the biodistribution study proposed that both the cubosomal formulations presented the improvement in the brain targeting in contrast to the drug solution (p value <0.001) with an enhanced nasal retention time for the drug to target the brain region. Fluoxetine drug solution revealed lower nasal retention time due to nasal drainage with a C max (97.92 ± 0.35 μg/mL) that was lower than that of formulation HJ7D.…”

Section: Ex Vivo Permeation Study Of In Situmentioning

confidence: 99%

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Potentiation of Brain Bioavailability Using Thermoreversible Cubosomal Formulation

Jain,

Prabhakar,

Shende

2024

Mol. Pharmaceutics

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The aim of the present study was to develop and evaluate intranasal formulations of the thermoreversible fluoxetine cubosomal in situ gel. This gel was intended for permeation and bioavailability enhancement to target the brain effectively by bypassing the blood−brain barrier (BBB). Fluoxetine-loaded cubosomes were prepared by the homogenization method followed by the cold method approach to develop in situ gel. Fluoxetineloaded cubosomes displayed a higher encapsulation efficiency (82.60 ± 1.25%) than fluoxetine. This might be due to the solubilizing activity of the polymer to cause partitioning of the lipophilic drug into the aqueous phase during the change from the cubic gel phase to cubosomes. In vitro analysis of fluoxetine-loaded cubosomal in situ gel showed a sustained release profile (93.22 ± 2.47%) due to limited diffusion of fluoxetine. The formation of strong affinity bonds of the drug with GMO (drug transporter) decreased the drug release in comparison to that with fluoxetine-loaded cubosomes (90.68 ± 1.74%). The ex vivo drug release profile revealed the drug release of 96.31 ± 2.88% by the end of 24 h. This is attributed to the higher capability of the intranasal cubosomal in situ gel to prolong the retention and enable better permeation through the nasal mucosa. In male Wistar rats, in vivo biodistribution studies for cubosomal in situ gel administered via the intranasal route at a dose of 3.5 mg/kg demonstrated an increase in pharmacokinetic parameters like the AUC (406 ± 75.35 μg/mL), C max (368.07 ± 0.23 μg/mL), T max (4 h), and t 1/2 (14.06 h). The mucoadhesive nature of the in situ gel led to an increase in the residence time of the gel in the nasal mucosa. The biodistribution study of intranasal in situ cubosomal gel improved the bioavailability 2.21-fold in comparison to that with the cubosomal dispersion but 2.83-fold in comparison to that with the drug solution. Therefore, fluoxetine-loaded cubosomal in situ gel proved as a promising carrier for effective transportation of fluoxetine via the intranasal route with significant brain bioavailability.

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Section: Resultsmentioning

confidence: 99%

Section: Ex Vivo Permeation Study Of In Situmentioning

confidence: 99%

Potentiation of Brain Bioavailability Using Thermoreversible Cubosomal Formulation

Jain,

Prabhakar,

Shende

2024

Mol. Pharmaceutics

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“…Viscosity, pH, and drug content were assessed at 1, 2, and 3 months to confirm the stability of the optimized formulations. [29]…”

Section: In Vivo Pharmacokinetics Studiesmentioning

confidence: 99%

Untitled

2024

AJP

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Aim: This study focused on the formulation and evaluation of ocular in situ gels containing blueberry extract for potential therapeutic applications. Materials and Methods: Various parameters were assessed to determine the physical characteristics, stability, and performance of the formulated gels. These parameters included clarity, transparency, pH, viscosity, gelling capacity, in vitro and ex vivo drug release, sterility, ocular irritation, intraocular pressure (IOP) reduction, and pharmacokinetic profiles. Total number of six formulations were prepared and evaluated for different parameters. Percentage drug release of all the formulations were carried out by modified Franz diffusion cell using simulated tear fluid. Results and Discussion: B6 formulation has shown maximum percentage release of 98.35% in 8 h. Ex vivo studies indicated that 80.23% of the drug permeated from the formulations, demonstrating a sustained effect. Furthermore, in situ gel of blueberry extract (B6) demonstrated a good percentage reduction in IOP, with a value of 29.96 ± 2.88 % mmHg. The in situ gel formulation achieved a C max of 10.5 ± 1.28 mg/mL after 4 h, which was approximately 10 times higher than the C max of the timolol eye drop (0.908 mg/mL) obtained after 2 h. Conclusion:The results indicated that the in situ gels demonstrated favorable physical properties, stable pH, excellent gelling capacity, sustained drug release, and sterility. Furthermore, the gels exhibited no ocular irritation and effectively reduced IOP, offering potential benefits for glaucoma treatment. Pharmacokinetic analysis revealed enhanced drug bioavailability with the in situ gel formulations compared to conventional eye drops. Stability studies confirmed the formulation's robustness under various environmental conditions. These findings highlight the suitability of the in situ gel formulations for ocular drug delivery, emphasizing their potential as effective and safe therapeutic options.

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“…Based on all of the above, designing new drug delivery systems that can deliver the appropriate therapeutic concentrations to target tissues and maintain them without or with minimal side effects is the main focus of current research in the field of ophthalmic preparations [ 42 , 43 ].…”

Section: Ocular Anatomy and Physiologymentioning

confidence: 99%

Biopolymers in Mucoadhesive Eye Drops for Treatment of Dry Eye and Allergic Conditions: Application and Perspectives

Račić

Krajišnik

2023

Pharmaceutics

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Dry eye syndrome and allergic conjunctivitis are the most common inflammatory disorders of the eye surface. Although eye drops are the most usual prescribed dosage form, they are characterized by low ocular availability due to numerous barrier mechanisms of the eye. The use of biopolymers in liquid ophthalmic preparations has numerous advantages, such as increasing the viscosity of the tear film, exhibiting bioadhesive properties, and resisting the drainage system, leading to prolonged retention of the preparation at the site of application, and improvement of the therapeutic effect. Some mucoadhesive polymers are multifunctional excipients, so they act by different mechanisms on increasing the permeability of the cornea. Additionally, many hydrophilic biopolymers can also represent the active substances in artificial tear preparations, due to their lubrication and moisturizing effect. With the modification of conventional ophthalmic preparations, there is a need for development of new methods for their characterization. Numerous methods for the assessment of mucoadhesiveness have been suggested by the literature. This review gives an overview related to the development of mucoadhesive liquid ophthalmic formulations for the treatment of dry eye and allergic conditions.

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Design and Optimization of In Situ Gelling Mucoadhesive Eye Drops Containing Dexamethasone

Cited by 9 publications

References 59 publications

Potentiation of Brain Bioavailability Using Thermoreversible Cubosomal Formulation

Potentiation of Brain Bioavailability Using Thermoreversible Cubosomal Formulation

Untitled

Biopolymers in Mucoadhesive Eye Drops for Treatment of Dry Eye and Allergic Conditions: Application and Perspectives

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