Development and investigation of timolol maleate niosomal formulations for the treatment of glaucoma

Ramadan, Afaf A.; Eladawy, Shereen A.; El-Enin, Amal S M Abu; Hussein, Zeinab M.

doi:10.1007/s40005-019-00427-1

Cited by 36 publications

(13 citation statements)

References 36 publications

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“…This is also in agreement with the fact that at room temperature, Span 60 molecules are present in the ordered gel state in bilayer structures. However, Span 80 molecules are in the disordered liquid-crystalline state [ 44 , 45 ].…”

Section: Resultsmentioning

confidence: 99%

Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

et al. 2021

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The present study aimed to investigate the potential of nanospanlastics for boosting the bioavailability of epigallocatechin gallate (EGCG). EGCG has valuable effects like anti-inflammation, anti-oxidation, and anti-tumorigenesis. Unfortunately, it has a low oral bioavailability due to its limited permeation and poor stability. To overcome these pitfalls, EGCG was fabricated as a nanospanlastic. Nanospanlastics are flexible nanovesicles that are composed of surfactants and edge activators (EAs). EAs improve the deformability of spanlastics by acting as a destabilizing factor of their vesicular membranes. EGCG-loaded spanlastics were prepared by an ethanol injection method, according to 23 factorial design, to explore the impact of different independent variables on entrapment efficiency (EE%), % drug released after 12 h (Q12h), and particle size (PS). In vitro characterization, ex vivo intestinal permeation test, and pharmacokinetic study of the optimized formula were performed. A newly developed RP-HPLC technique was adopted for the estimation of EGCG. The optimized formula (F4) demonstrated more prolonged drug release and a significant improvement in the EE%, permeability, deformability and stability than the corresponding niosomes. The pharmacokinetic study investigated that F4 had a more sustained drug release and a higher bioavailability than the conventional niosomes and free drugs. Nanospanlastics could be a promising approach for improving the bioavailability of EGCG.

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Section: Resultsmentioning

confidence: 99%

Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

et al. 2021

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“…Surfactants with high phase transition temperatures provide high entrapment for the drug and vice versa. 40,41 The fact that PLu F127 and Sp 60 exhibit high EE % was ascribed to various causes for instance; being solid at room temperature with positive phase transition temperature (Tc=25ºC and 53ºC, respectively). This is the main reason for further involvement in more rigid bilayers, reducing drug leaching from the vesicles; therefore improving entrapment efficiency.…”

Section: Effect Of Type Of Nonionic Surfactantsmentioning

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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“…Recently, Ramadan et al utilized TFH method for production of niosomes with various kind of surfactants and different ratios of surfactants to cholesterol. They encapsulated drug, timolol maleate which is used for treatment of glaucoma by lowering intraocular pressure (IOP), with an encapsulation efficiency (EE%) of 98.8% [ 28 ].…”

Section: Niosomes As New Drug Delivery Systemsmentioning

confidence: 99%

“…Niosomal formulations prolonged drug release successfully in several studies in comparison with free drug formulations. Timolol maleate loaded niosomes developed for the treatment of glaucoma showed a prolonged release profile and entire drug was released from the vesicles in about 24 h, while its free form was completely released in 4 h [ 28 ]. Free drug solution of brimonidine tartrate, another drug used for glaucoma treatment, shown to release 75% of the drug within 2 h, whereas niosomal formulation released 22% of the drug in 8 h [ 58 ].…”

Section: Niosomes As New Drug Delivery Systemsmentioning

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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Development and investigation of timolol maleate niosomal formulations for the treatment of glaucoma

Cited by 36 publications

References 36 publications

Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

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

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

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