Enhanced transdermal delivery of ondansetron using nanovesicular systems: Fabrication, characterization, optimization and ex-vivo permeation study-Box-Cox transformation practical example

Habib, Basant A; Sayed, Sinar; El-Sayed, Ghada M.

doi:10.1016/j.ejps.2018.01.044

Cited by 52 publications

(27 citation statements)

References 52 publications

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“…The precipitated cake was appropriately dissolved and diluted with ethanol followed by spectrophotometric estimation of the entrapped VRC quantity (model UV-1601 PC, Shimadzu, Kyoto, Japan) at predetermined λ max =256 nm using a blank of corresponding plain PNs treated by the same way. Drug EE % was determined conferring to the subsequent equation: 29 …”

Section: Methodsmentioning

confidence: 99%

<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: Methodsmentioning

confidence: 99%

<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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“…The supernatant obtained after centrifugation was appropriately diluted with methanol and the amount of unentrapped BRT was measured spectrophotometrically (model UV-1601 PC, Shimadzu, Kyoto, Japan) using methanol as a blank at λ max = 320 nm. Drug EE% was determined according to the following equation (Habib et al., 2018): …”

Section: Methodsmentioning

confidence: 99%

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

2019

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Brimonidine tartrate (BRT) is a hydrophilic a 2 adrenergic agonist used for the treatment of glaucoma. Glaucoma is an ocular disease affecting the anterior segment of the eye requiring lifetime treatment. Owing to the obstacles facing ocular delivery systems and hydrophilicity of BRT, frequent administration of the eye drops is required. Niosomes have been widely used to improve the ocular bioavailability of the topically applied drugs and to enhance the ocular residence time. However, they have drawbacks as physical instability, aggregation, and loss of the entrapped drug. For this reason, BRT proniosomes were prepared to overcome niosomal instability issues. A D-optimal design was utilized to determine the optimum conditions for preparation of the proniosomal gels. Independent variables were amount of surfactant, surfactant:cholesterol ratio, and type of surfactant used. The dependent variables were entrapment efficiency (EE%), particle size, percentage of drug released after 2 h (Q 2h), and percentage of drug released after 24 h (Q 24h). The optimum formula was suggested with desirability 0.732 and the composition of 540 mg Span 60 and 10:1 surfactant:cholesterol ratio. The results obtained after reconstitution were; EE% of 79.23 ± 1.12% particle size of 810.95 ± 16.758 nm, polydispersity index (PDI) 0.6785 ± 0.213, zeta potential 59.1 ± 0.99 mV, Q 2h 40.98 ± 1.29%, Q 8h 63.35 ± 6.07%, and Q 24h ¼ 91.11 ± 1.76%. Transmission electron microscope imaging of the formula showed the typical spherical shape of niosomes. In-vivo pharmacodynamic study assured the improved ocular bioavailability of BRT selected formula when compared with Alphagan V R P with relative AUC 0-24 of 5.024 and 7.90 folds increase in the mean residence time (MRT). Lack of ocular irritation of the formula was assured by Draize test.

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“…The supernatant was taken, diluted and measured spectrophotometrically (UV-1601 PC shimadzu, Kyoto, Japan) at λ max =254 nm. EE% was calculated using the following formula (Habib et al., 2018 ): …”

Section: Methodsmentioning

confidence: 99%

“…PS and PDI of the formed niosomes as well as their ZP were determined using Malvern zeta sizer (Malvern Instrument Ltd., Worcestshire, UK). The niosomal dispersions were appropriately diluted with distilled water before measurements (Habib et al., 2018 ).…”

Section: Methodsmentioning

confidence: 99%

“…Q n was calculated according to Habib et al. ( 2018 ) with modifications: where, Q n is the current cumulative percent of drug released, C n represents the receptor medium current concentration at n th sample, V r is the receptor medium volume, V s is the volume of each sample removed for analysis, and denotes the summed total of the previously measured concentrations.…”

Section: Methodsmentioning

confidence: 99%

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Sustained ocular delivery of Dorzolamide-HCl via proniosomal gel formulation: in-vitro characterization, statistical optimization, and in-vivo pharmacodynamic evaluation in rabbits

et al. 2018

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Glaucoma is the second cause of blindness worldwide. Frequent administration of traditional topical dosage forms may lead to patient incompliance and failure of treatment. Our study aims to formulate proniosomal gel formulations that sustain the release of the water-soluble anti-glaucoma drug Dorzolamide-HCl (Dorz). Proniosomal gel formulations were prepared using coacervation phase separation method according to a 52 full factorial design. The effects of Cholesterol and surfactant (Span 40) amounts (independent variables) on the percentage entrapment efficiency (EE%), particle size (PS), and the percent of drug released after 8 h (Q8h) (dependent variables (DVs)) were investigated. An optimized formulation (OF) was chosen based on maximizing EE% and Q8h and minimizing PS. An intraocular pressure (IOP) pharmacodynamic study was performed in rabbits to evaluate the in-vivo performance of the OF-gel compared to the marketed Trusopt® eye drops. The results showed that the independent variables studied significantly affected EE%, PS, and Q8h. OF was the one containing 60 mg Cholesterol and 540 mg Span 40. It had desirability of 0.885 and its actually measured DVs deviated from the predicted ones by a maximum of 4.8%. The in-vivo pharmacodynamic study showed that OF could result in higher reduction in IOP, significantly sustain that reduction in IOP and increase Dorz bioavailability compared to Trusopt® eye drops. Thus the OF-gel is very promising for being used in glaucoma treatment.

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Enhanced transdermal delivery of ondansetron using nanovesicular systems: Fabrication, characterization, optimization and ex-vivo permeation study-Box-Cox transformation practical example

Cited by 52 publications

References 52 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>

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

Sustained ocular delivery of Dorzolamide-HCl via proniosomal gel formulation: in-vitro characterization, statistical optimization, and in-vivo pharmacodynamic evaluation in rabbits

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