Intranasal niosomes of nefopam with improved bioavailability: preparation, optimization, and in-vivo evaluation

Abou-Taleb, Heba A; Khallaf, Rasha A.; Abdel-Aleem, Jelan A.

doi:10.2147/dddt.s177746

Cited by 46 publications

(26 citation statements)

References 38 publications

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“…The amphiphilc characters of cholesterol with the surfactant together form hydrogen bonding that improves the FLB content and solubility within the niosomal core, which leads to improved drug release [ 16 ]. In addition, the lipidic property, nano-size of the niosomes, and the presence of nonionic surfactant (Span ® ) that act as permeation enhancers could contribute to the enhanced diffusion of the drug via the nasal mucosa [ 14 ].…”

Section: Resultsmentioning

confidence: 99%

“…The proposed enhanced drug permeation across nasal mucosa could be interpreted on the basis of the niosomes’ nano-size and lipophilic nature, which facilitate the passage of drug across the nasal mucosal epithelium with consequent efficient delivery into the bloodstream [ 33 ]. Furthermore, the increased concentration of the drug in the brain foreshadows the ability of the proposed niosomes to enhance the direct delivery of the drug to the CNS delivery through the nasal olfactory region BBB [ 14 ]. The improved CNS delivery could be ascribed the ability of the intact lipid-based niosomes to pass the BBB by receptor-mediated endocytosis.…”

Section: Resultsmentioning

confidence: 99%

“…Compared to phospholipid-based vesicles, niosomes demonstrate greater physical stability and reduced handling and storage costs. Moreover, niosomes have been reported as efficient carriers for targeting drugs and increasing their accumulation in organs as liver and brain [ 12 , 13 , 14 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

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RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

et al. 2020

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Flibanserin (FLB) is a multifunctional serotonergic agent that was recently approved by the FDA for the oral treatment of premenopausal women with hypoactive sexual desire disorder. FLB is a centrally acting drug that has a low oral bioavailability of 33% owing to its exposure to the hepatic first-pass effect, as well as its pH-dependent solubility, which could be an obstacle hindering the drug dissolution and absorption via mucosal barriers. Thus, this work aimed at overcoming the aforementioned drawbacks and promoting the nose-to-brain delivery of FLB via the formulation of an intra-nasal in situ niosomal gel. The Box–Behnken design was employed to study the impact of Span® 85 concentration (X1), hydration time (X2), and pH of the hydrating buffer (X3) on the vesicle size and drug entrapment. The optimized formulation exhibited a spherical shape with a vesicular size of 46.35 nm and entrapment efficiency of 92.48%. The optimized FLB niosomes integrated into gellan gum-based in situ gel exhibited enhanced ex vivo permeation and improved plasma and brain concentrations after nasal administration in rats compared to raw FLB. These findings highlight the capability of the proposed intra-nasal FLB niosomal in situ gel to boost the drug bioavailability and to promote its direct delivery to the brain.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

et al. 2020

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“…All niosome formulations prepared with Cremophor RH 40 gave considerably ( p < 0.05) higher release rates as compared to those prepared with Tween 80 and Span 60 at the same molar ratios. This could be clarified on the basis that niosomes show a release pattern dependent on the alkyl chain length, and the greater the alkyl chain length, the lesser the rate of drug release [ 71 ]. Span 60 has the longest saturated alkyl chain as compared to Tween 80 and Cremophore RH40, thus it exhibited the slowest drug release.…”

Section: Discussionmentioning

confidence: 99%

Fabrication and Appraisal of Simvastatin via Tailored Niosomal Nanovesicles for Transdermal Delivery Enhancement: In Vitro and In Vivo Assessment

et al. 2021

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Simvastatin (SIM) is a HMG-CoA reductase inhibitor employed in the management of hyperlipidemia. However, its low bioavailability limits its clinical efficacy. The objective of this study was to overcome the poor bioavailability of SIM via the transdermal application of a SIM-loaded niosomal gel. Niosomes loaded with SIM were fabricated by means of the thin-film hydration method and optimized through a 33-factorial design utilizing Design Expert® software. The prepared niosomes were evaluated for entrapment efficiency (EE%), zeta potential, vesicle size, and cumulative percentage of drug release. The optimum niosomal formulation was loaded on the gel and evaluated for physical properties such as color, clarity, and homogeneity. It was also evaluated for spreadability, and the cumulative % drug release. The best niosomal gel formula was appraised for ex vivo permeation as well as pharmacokinetic study. The SIM-loaded niosomes showed EE% between 66.7–91.4%, vesicle size between 191.1–521.6 nm, and zeta potential ranged between −0.81–+35.6 mv. The cumulative percentage of drug released was ranged from 55% to 94% over 12 h. SIM-loaded niosomal gels were clear, homogenous, spreadable, and the pH values were within the range of physiological skin pH. Furthermore, about 73.5% of SIM was released within 24 h, whereas 409.5 µg/cm2 of SIM passed through the skin over 24 h in the ex vivo permeation study. The pharmacokinetic study revealed higher AUC0–∞ and Cmax with topical application of SIM-loaded niosomal gel compared to topical SIM gel or oral SIM suspension. The topical application of SIM-loaded niosomal gel ascertained the potential percutaneous delivery of SIM.

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“…Physical stability of the optimal ethosomal RP formulation was evaluated by examining changes of mean particle size, ZP, and EE% during storage at 4°C and 25°C protected from the light for 90 days. 12,36,37 Preparation of RP Ethosomal Hydrogel…”

Section: Physical Stabilitymentioning

confidence: 99%

Tailoring of Retinyl Palmitate-Based Ethosomal Hydrogel as a Novel Nanoplatform for Acne Vulgaris Management: Fabrication, Optimization, and Clinical Evaluation Employing a Split-Face Comparative Study

Salem¹,

Kharshoum²,

Awad³

et al. 2021

IJN

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Aim: Retinyl palmitate (RP), the most stable vitamin A derivative, is used to treat photoaging and other skin disorders. The need to minimize the adverse effects of topical drug administration has led to an enhanced interest in loading RP on ethosomes for topical drug delivery. The aim of the current study was to prepare and compare the performance of RP decorated ethosomal hydrogel with tretinoin cream in the treatment of acne vulgaris as an approach to improve drug efficacy and decrease its side effects. Methods: RP-loaded ethosomes were prepared using the injection sonication technique. A Box-Behnken design using Design Expert ® software was used for the optimization of formulation variables. Particle size, zeta potential (ZP), entrapment efficiency percent (EE %), % drug release, and permeation over 24 h of different formulations were determined. The optimal formulation was incorporated into a hydrogel. Finally, the efficacy and tolerability of the optimized RP ethosomal hydrogel were clinically evaluated for acne treatment using a split-face comparative clinical study. Results: The optimized ethosomal RP showed particle size of 195.8±5.45 nm, ZP of −62.1 ±2.85 mV, EE% of 92.63±4.33%, drug release % of 96.63±6.81%, and drug permeation % of 85.98 ±4.79%. Both the optimized RP ethosomal hydrogel and tretinoin effectively reduced all types of acne lesions (inflammatory, non-inflammatory, and total lesions). However, RP resulted in significantly lower non-inflammatory and total acne lesion count than the marketed tretinoin formulation. Besides, RP-loaded ethosomes showed significantly improved tolerability compared to marketed tretinoin with no or minimal skin irritation symptoms. Conclusion: RP ethosomal hydrogel is considerably effective in controlling acne vulgaris with excellent skin tolerability. Therefore, it represents an interesting alternative to conventional marketed tretinoin formulation for topical acne treatment.

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Intranasal niosomes of nefopam with improved bioavailability: preparation, optimization, and in-vivo evaluation

Cited by 46 publications

References 38 publications

RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

Fabrication and Appraisal of Simvastatin via Tailored Niosomal Nanovesicles for Transdermal Delivery Enhancement: In Vitro and In Vivo Assessment

Tailoring of Retinyl Palmitate-Based Ethosomal Hydrogel as a Novel Nanoplatform for Acne Vulgaris Management: Fabrication, Optimization, and Clinical Evaluation Employing a Split-Face Comparative Study

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