Response surface optimization, Ex vivo and In vivo investigation of nasal spanlastics for bioavailability enhancement and brain targeting of risperidone

Abdelrahman, Fatma Elzahraa; Elsayed, Ibrahim; Gad, Mary Kamal; Elshafeey, Ahmed Hassen; Mohamed, M. I.

doi:10.1016/j.ijpharm.2017.07.050

Cited by 66 publications

(31 citation statements)

References 53 publications

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“…CBZ and span 60 were dissolved in 10 ml absolute ethanol and injected slowly in the preheated aqueous phase (60 ˚C ) containing PVA and was stirred for 1 h on magnetic stirrer then, the formed dispersion was sonicated for 2 min. Eventually, the prepared formulations were left in the refrigerator until further investigation [13]. Experimental runs, independent variables and the measured dependent variables for the prepared formulations were given in table 1.…”

Section: Preparation Of Spanlastics Formulationsmentioning

confidence: 99%

“…On the other hand, dependent variables were PS (Y1), PDI (Y2), ZP (Y3) and EE (Y4). Desirability values were measured to identify the optimum formula based on analyzing the response surface of the obtained data [13]. [15].…”

Section: Statistical Optimization Of the Formulationsmentioning

confidence: 99%

“…The EE ranges for all prepared formulations was ranged from 44%-97.6%. According to equations (13) and (14), the positive coefficient of XA reveals that the EE increased as the drug amount which is used to load the niosomes or the spanlastics increased. This is may be due to the increase in the medium's saturation with the drug which will then be available to be encapsulated into the vesicles [32].…”

Section: The Effect Of Independent Formulation Variables On Entrapmenmentioning

confidence: 99%

“…The viscosity was nearly uniform and constant through the whole shear rate values (nearly 65 cps). This nearly high viscosity due to the presence of two highly viscous surfactants in the composition of spanlastics formulation so that the prepared formulation could be used without the need of incorporating a gelling agent [13]. The almost constant viscosity indicated that the flow of the optimized formulation is Newtonian flow.…”

Section: Viscosity Measurementmentioning

confidence: 99%

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Carbamazepine Loaded Vesicular Structures for Enhanced Brain Targeting via Intranasal Route: Optimization, in Vitro Evaluation, and in Vivo Study

2019

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Objective: Carbamazepine (CBZ) is used as a first line in the treatment of grand mal and partial seizures, but it suffers from many side effects on different systems of the body. The objective of the present study was optimization of CBZ vesicular structures using 23 multifactorial design for the most efficient targeting of CBZ to the brain via the intranasal route. Methods: The concentration of CBZ (10 and 20%), type of vesicles (niosomes and spanlastics) and speed of rotation (200 and 300 rpm) were considered as the independent variables XA, XB and XC respectively, while the dependent variables were particle size PS (Y1), polydispersity index PDI (Y2), zeta potential ZP (Y3) and entrapment efficiency EE (Y4). The study of the effect of different formulation variables was carried out using Design-Expert ® software. CBZ-loaded spanlastics and noisome were prepared by the ethanol injection method and thin film hydration method, respectively. The optimized formulation was subjected to viscosity measurement, in vitro drug release and physical stability studies. In vivo evaluations in rats for the optimized formulation in comparison to oral CBZ suspension was carried out using behavioral assessment by elevated plus maze test, determination of endothelial nitric oxide synthase (e-NOS), reduced glutathione (GSH) and ELISA estimation of TNFα. Results: The selected optimized formulation (F0) containing 20% CBZ and spanlastic vesicular structure showed PS, PDI, ZP, and the EE % of 350.09 nm, 0.830, 16.124mV and 82.777%, respectively. In vitro release study of F0 demonstrated the ability of the F0 to increase drug release in the range time from 10-60 min (p<0.05) when compared with CBZ suspension. The viscosity of F0 was nearly uniform (65 cps). The photomicrograph taken by the transmission electron microscopy (TEM) reveals the spherical shape of F0. Good physical stability for six months of storage at 25˚ C was found for F0. The optimized spanlastic formulation F0 showed a decrease in latency time in behavior assessment test using elevated plus Maze test, a decrease in serum eNOS and TNF-α and increase in GSH when compared with the oral CBZ suspension, in addition to the histopathological study that revealed the more CBZ uptake by the brain. Conclusion: The optimized spanlastic formulation F0 achieved better results when compared with the oral CBZ suspension for targeting the CBZ spanlastics vesicular structure to the brain via the nasal route.

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Section: Preparation Of Spanlastics Formulationsmentioning

confidence: 99%

Section: Statistical Optimization Of the Formulationsmentioning

confidence: 99%

Section: The Effect Of Independent Formulation Variables On Entrapmenmentioning

confidence: 99%

Section: Viscosity Measurementmentioning

confidence: 99%

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Carbamazepine Loaded Vesicular Structures for Enhanced Brain Targeting via Intranasal Route: Optimization, in Vitro Evaluation, and in Vivo Study

2019

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“…Bioadhesion has been widely studied in the development of pharmaceutics to improve local and systemic absorption. Transmucosal drug delivery has gained impressive momentum in the past decade, especially with nano drug delivery systems (133)(134)(135). Transmucosal drug delivery routes include ocular, nasal, oromucosal (buccal, sublingual and gingival), pulmonary, gastrointestinal and vaginal sites.…”

Section: Transmucosal Drug Deliverymentioning

confidence: 99%

Recent advances in non-ionic surfactant vesicles (niosomes): Fabrication, characterization, pharmaceutical and cosmetic applications

Chen

Hanning

Falconer

et al. 2019

European Journal of Pharmaceutics and Biopharmaceutics

331

176

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This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.

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The effect of edge activator on the evolution and application of a nonionic surfactant: The elastic vesicular system

Sarolia

Baldha

Chakraborthy

et al. 2023

J Surfact & Detergents

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Vesicular drug delivery as part of the colloidal system was evolved to entrap a hydrophobic drug as well as a hydrophilic drug. The tremendous potential of this system lies in ensuring the targeted and controlled release of the drug molecules to reduce the toxicity and side effects. Liposomes and niosomes are the first duos of the vesicular system to be used in the pharmaceutical and cosmetic fields. However, the lack of elasticity in this formulation prevents its success on the market. To overcome the obstacles, additional formulation changes were made to the existing vesicle. These modifications were attributed to the one component termed edge activator (EA), which added an elasticity factor to the vesicle system. Based on the formulation and EA, the vesicular system transits in the liposome to the spanlastic system. Spanlastics are surfactant‐based nanovesicles that are elastic, malleable, and given that it is a vesicular system with polar and nonpolar components, it can retain both hydrophilic and lipophilic medications. A modified method of medication delivery may also be possible. This review article discusses the recent approaches to the evolution of nonionic surfactant vesicular systems with respect to their method of preparation, effects of EA, and therapeutic application of spanlastic.

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Response surface optimization, Ex vivo and In vivo investigation of nasal spanlastics for bioavailability enhancement and brain targeting of risperidone

Cited by 66 publications

References 53 publications

Carbamazepine Loaded Vesicular Structures for Enhanced Brain Targeting via Intranasal Route: Optimization, in Vitro Evaluation, and in Vivo Study

Carbamazepine Loaded Vesicular Structures for Enhanced Brain Targeting via Intranasal Route: Optimization, in Vitro Evaluation, and in Vivo Study

Recent advances in non-ionic surfactant vesicles (niosomes): Fabrication, characterization, pharmaceutical and cosmetic applications

The effect of edge activator on the evolution and application of a nonionic surfactant: The elastic vesicular system

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