Exploring the potential of complex-vesicle based niosomal ocular system loaded with azithromycin: Development of in situ gel and ex vivo characterization

Akhtar, Nida; Singh, Rahul Kumar; Pathak, Kamala

doi:10.18869/acadpub.pbr.3.1.22

Cited by 13 publications

(7 citation statements)

References 17 publications

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“…60 The complete release of the pure drug from ocular inserts for 6 h was essential while the drug release from (VRC-Ns Ocu) was slower, taking a period of 8 h with lesser immediate burst effect than that of the niosomal suspension nearly 22.73±2.47% after half hour. This depicted that VRC was distributed and entrapped consistently into noisomes inside the ocusert matrix and gradually released out into the release medium that is in agreement with a study, 61 which demonstrated that viscosity-enhancing polymers like poloxamer and carbopol reduced the release rate of the drug via diffusion through gel matrix, but in our case, the viscosity-enhancing polymers were HPMC and carbopol 940 .…”

Section: In-vitro Drug Release Studysupporting

confidence: 92%

<p>Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies</p>

El-Emam¹,

Girgis²,

El‐Sokkary³

et al. 2020

IJN

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Background: Voriconazole (VRC) is a triazole broad spectrum antifungal drug, used in the management of versatile fungal infections, particularly fungal keratitis. The obligatory use of niosomal delivery of VRC may reduce the frequency of dosing intervals resulting from its short biological half time and consequently improve patient compliance. Methods: VRC loaded proniosomes (VRC-PNs) were set by the coacervation technique and completely characterized. The developed formula was comprehensively assessed concerning in-vitro release behavior, kinetic investigation, and its conflict against refrigerated and room temperature conditions. A selected noisomal formula was incorporated into ocusert (VRC-PNs Ocu) formulated by 1% w/w hydroxypropyl methyl cellulose HPMC and 0.1% w/w carbopol 940. Eventually, in vitro antifungal activity against Candida albicans and Aspergillus nidulans was assessed by the cup diffusion method. Results: The optimized VRC-PNs (Pluronic F127: cholesterol weight ratio 1:1 w/w) exhibited the highest entrapment efficiency (87.4±2.55%) with a spherical shape, proper size in nano range and a suitable Zeta potential of 209.7±8.13 nm and −33.5±1.85 mV, respectively. Assurance of drug encapsulation in nanovesicles was accomplished by several means such as attenuated total reflection Fourier-transform infrared spectroscopy, differential scanning calorimetry in addition to powder X-ray diffraction investigations. It displayed a biphasic in vitro release pattern and after 6 months of storage at a refrigerated temperature, the optimized formula preserved its stability. VRC-PNs Ocu proved a very highly significant antifungal activity matched with the free drug or nanosuspension which was extra assured by comparing its mean inhibition zone with that of 5% natamycin market eye drops. Conclusion: In conclusion, VRC-PNs Ocu could be considered as a promising stable sustained release topical ocular nanoparticulate system for the management of fungal infections.

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Section: In-vitro Drug Release Studysupporting

confidence: 92%

<p>Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies</p>

El-Emam¹,

Girgis²,

El‐Sokkary³

et al. 2020

IJN

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“…Here in the current procedure Cholesterol, span 60, and cetylpyridinium chloride weighed properly and dissolved inorganic phase containing di-ethyl ether and methanol in a ratio of 8:2. Prepared organic phase solution finally transferred through 22 gauge needle in a beaker containing 20 ml phosphate buffer pH 6.8 and drug solution whose stirring speed of 75rpm and temperature of 65 C was maintained throughout the time period of 45 min., which is a must require a process to confirm properly shaped vesicles and for high drug loading and also provide an advantage to ensure that organic solution was fully evaporated [12]. In the end, 3 2 full factorial designs utilize to check out the total number of preparation and concentration of independent variables.…”

Section: Methods Of Preparationmentioning

confidence: 99%

“…To conduct the preliminary study, blank niosomes were prepared through various types of surfactants and methods of preparation, out of which best niosomal preparation was selected on the basis of visual observation through photograph and optical microscopy at 40X [12].…”

Section: Preliminary Study On Blank Niosomesmentioning

confidence: 99%

5-Fluorouracil Impregnated Niosomal-in Situ Gel (Thermo-Sensitive) for Oral Cancer: Design, Characterization, in Vitro/Ex Vivo Evaluation

Singh

DEORA²

2022

Int J App Pharm

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Objective: To formulate and characterize 5-fluorouracil loaded niosomal-in-situ gel for sustained drug delivery to reduce dosing frequency at the same time, follow a local drug delivery for cancer targeting. Methods: Cholesterol and span-60-based niosomes were prepared after following the modified ether injection method. Best formulation selected after characterization through FTIR, SEM, % Entrapment efficiency, zeta potential, polydispersity index, in vitro release, and vesicle size whereas, based on cold method niosomes encapsulated in-situ gel was formulated and characterized through gelling temperature and time, spreadability and syringe ability, gel strength, adhesive force, and drug release. Results: Based on various studies, included particle size, PDI, zeta potential value, % Entrapment efficiency and % drug release, F1 formulation was selected as a best formulation, as niosomal particle size of 388.3 nm proved a higher drug permeation through the buccal area, whereas PDI and zeta potential value of 0.304 and+50.5 are proved a uniform niosomal size with optimum charge distribution which helps to attain higher stability of the formulation, on the other hand % Entrapment efficiency of 87.825% proved that niosomes are capable to hold higher drug concentration; lastly 84.567% of drug release within 12 h of time period prove that higher amount of drug release occur by following sustained release pattern. On the other hand Mucoadhesion, gelling strength and in vitro permeation studies prove that niosomes containing in-situ gel has a capacity to adhere over the mucosa with minimum dissolution with saliva up to 12 h and is capable of 95% of drug permeation capacity. Lastly FTIR and SEM images confirmed about niosomal formation with optimum stability. Conclusion: 5-Fluorouracil encapsulated niosomal in-situ gel will be superior and effective alternative to parenteral dosage forms available in the market for mouth cancer treatment.

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“…The EE% of prepared niosomes (>30%) and niosomal in situ gel formulations (>63%) were high, and niosomes prolonged drug release up to 12 h with increased corneal permeation. The results indicate that temperature-sensitive niosomal in-situ ocular gel showed increased residence time and provide localized drug delivery effective for the treatment of bacterial conjunctivitis [ 62 ].…”

Section: Niosome Based Treatment Strategies In Ocular Diseasesmentioning

confidence: 99%

Niosomal Drug Delivery Systems for Ocular Disease—Recent Advances and Future Prospects

et al. 2020

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The eye is a complex organ consisting of several protective barriers and particular defense mechanisms. Since this organ is exposed to various infections, genetic disorders, and visual impairments it is essential to provide necessary drugs through the appropriate delivery routes and vehicles. The topical route of administration, as the most commonly used approach, maybe inefficient due to low drug bioavailability. New generation safe, effective, and targeted drug delivery systems based on nanocarriers have the capability to circumvent limitations associated with the complex anatomy of the eye. Nanotechnology, through various nanoparticles like niosomes, liposomes, micelles, dendrimers, and different polymeric vesicles play an active role in ophthalmology and ocular drug delivery systems. Niosomes, which are nano-vesicles composed of non-ionic surfactants, are emerging nanocarriers in drug delivery applications due to their solution/storage stability and cost-effectiveness. Additionally, they are biocompatible, biodegradable, flexible in structure, and suitable for loading both hydrophobic and hydrophilic drugs. These characteristics make niosomes promising nanocarriers in the treatment of ocular diseases. Hereby, we review niosome based drug delivery approaches in ophthalmology starting with different preparation methods of niosomes, drug loading/release mechanisms, characterization techniques of niosome nanocarriers and eventually successful applications in the treatment of ocular disorders.

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Exploring the potential of complex-vesicle based niosomal ocular system loaded with azithromycin: Development of in situ gel and ex vivo characterization

Cited by 13 publications

References 17 publications

<p>Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies</p>

<p>Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies</p>

5-Fluorouracil Impregnated Niosomal-in Situ Gel (Thermo-Sensitive) for Oral Cancer: Design, Characterization, in Vitro/Ex Vivo Evaluation

Niosomal Drug Delivery Systems for Ocular Disease—Recent Advances and Future Prospects

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