Nanostructured liquid crystalline formulation as a remarkable new drug delivery system of anti-epileptic drugs for treating children patients

El-Enin, Hadel A. Abo; Alshanbari, Areej

doi:10.1016/j.jsps.2018.04.004

Cited by 44 publications

(19 citation statements)

References 56 publications

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“…The F1 formulation released 71 ± 4% of the drug after 4 h compared to 79 ± 8% from F2, and without any statistically significant difference (p < .05). Meanwhile, the F3 formulation and NT suspension showed lower NT releases of 30 ± 3 and 39 ± 1%, respectively, after 4 h. It can be seen that F1 and F2 provide a sustained release of NT, which agrees with a previous study that reported sustained drug release by cubosomes (El-Enin & AL-Shanbari, 2018). Interestingly, there was no burst release from the F1 and F2 formulations, also agreeing with reported studies that show drug release without a burst effect from cubosomes (Luechtefeld et al, 2016).…”

Section: In Vitro Releasesupporting

confidence: 90%

Nanocubosomal based in situ gel loaded with natamycin for ocular fungal diseases: development, optimization, in-vitro , and in-vivo assessment

et al. 2021

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Natamycin (NT) is a synthetic broad-spectrum antifungal used in eye drops. However, it has low solubility and high molecular weight, limiting its permeation, and generally causes eye discomfort or irritation when administered. Therefore, the present study aimed to develop an ophthalmic in situ gel formulation with NT-loaded cubosomes to enhance ocular permeation, improve antifungal activity, and prolong the retention time within the eye. The NT-loaded cubosome (NT-Cub) formula was first optimized using an I-optimal design utilizing phytantriol, PolyMulse, and NT as the independent formulation factors and particle size, entrapment efficiency %, and inhibition zone as responses. Phytantriol was found to increase particle size and entrapment efficiency %. Higher levels of PolyMulse slightly increased the inhibition zone whereas a decrease in particle size and EE% was observed. Increasing the NT level initially increased the entrapment efficiency % and inhibition zone. The optimized NT-Cub formulation was converted into an in situ gel system using 1.5% Carbopol 934. The optimum formula showed a pH-sensitive increase in viscosity, favoring prolonged retention in the eye. The in vitro release of NT was found to be 71 ± 4% in simulated tear fluid. The optimum formulation enhanced the ex vivo permeation of NT by 3.3 times compared to a commercial formulation and 5.2 times compared to the NT suspension. The in vivo ocular irritation test proved that the optimum formulation is less irritating than a commercial formulation of NT. This further implies that the developed formulation produces less ocular irritation and can reduce the required frequency of administration.

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Section: In Vitro Releasesupporting

confidence: 90%

Nanocubosomal based in situ gel loaded with natamycin for ocular fungal diseases: development, optimization, in-vitro , and in-vivo assessment

et al. 2021

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“…They facilitate a more targeted and efficient brain delivery and reduce side effects at the same time [223]. The advantage of using nanotechnology-based drug delivery systems has been shown for different CNS indications, such as epilepsy, psychosis-related disorders and glioma [152,[223][224][225][226][227].…”

Section: Systemic and Cns Side Effectsmentioning

confidence: 99%

Intranasal drug delivery: opportunities and toxicologic challenges during drug development

Keller

Merkel

Popp

2021

Drug Deliv. and Transl. Res.

271

178

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Over the past 10 years, the interest in intranasal drug delivery in pharmaceutical R&D has increased. This review article summarises information on intranasal administration for local and systemic delivery, as well as for CNS indications. Nasal delivery offers many advantages over standard systemic delivery systems, such as its non-invasive character, a fast onset of action and in many cases reduced side effects due to a more targeted delivery. There are still formulation limitations and toxicological aspects to be optimised. Intranasal drug delivery in the field of drug development is an interesting delivery route for the treatment of neurological disorders. Systemic approaches often fail to efficiently supply the CNS with drugs. This review paper describes the anatomical, histological and physiological basis and summarises currently approved drugs for administration via intranasal delivery. Further, the review focuses on toxicological considerations of intranasally applied compounds and discusses formulation aspects that need to be considered for drug development. Graphical abstract

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“…In previous studies, Nasr et al and Abo El-Enin et al found that the drug-loaded cubosomes were nearly spherical with irregular polyangular shapes. 10,37 This might be due to the GTP, which leads to a semi-cubic (semi-spherical) shape as it is reported in previous studies that GTP formed dense spherical nanoparticles. 50,51 The scanned cubosomes showed numerous water channels in their structure as the GMO is self-assembled in water and form a liquid crystalline cubic phase consisted of bicontinuous lipid bilayers with networks of water channels.…”

Section: Tem Imagingmentioning

confidence: 66%

“…Increasing the concentration of PF127 stabilized the system sterically and made an efficient distribution of the crystalline structure of the cubosomes. 36,37 Besides, increasing PF127 decreased the surface tension, which facilitated the formation of cubosomes with smaller PS. In a previous study, Abdelrahman, F.E.…”

Section: Characterization Of the Prepared In Situ Cubo-gels Ps Pdi mentioning

confidence: 99%

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<p>Brain Targeting of Duloxetine HCL via Intranasal Delivery of Loaded Cubosomal Gel: In vitro Characterization, ex vivo Permeation, and in vivo Biodistribution Studies</p>

Elsenosy¹,

Abdelbary²,

Elshafeey³

et al. 2020

IJN

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Purpose: Duloxetine (DLX) is dual serotonin and norepinephrine reuptake inhibitor suffering from limited bioavailability (≈ 40%) due to extensive hepatic metabolism. This work aims to formulate and evaluate DLX intranasal thermoreversible cubosomal gels to enhance its bioavailability and ensure efficient brain targeting. Materials and Methods: Cubo-gels were prepared by 3 3 central composite design with three independent factors, lipid ratio (glycerol monooleate: glycerol tripalmitate), Pluronic F127%, and Pluronic F68%. The prepared formulations were evaluated for their particle size (PS), gelling temperature (GT), entrapment efficiency (EE%), and in vitro release. The cubogel with the highest desirability (0.88) was chosen as the optimized formulation. DLX cubogel was evaluated using differential scanning calorimetry, Fourier-transform infrared spectroscopy, X-ray powder diffraction, and transmission electron microscopy. Cytotoxicity study, ex vivo permeation study and in vivo bio-distribution study were conducted to evaluate the safety and efficacy of brain targeting. Results: The optimum cubo-gel was composed of 3.76 lipid ratio, 20% w/v PF127, and 5% w/v PF68. It had PS of 265.13 ± 9.85 nm, GT of 32 ± 0.05°C, EE% of 98.13 ± 0.50%, and showed controlled release behavior where 33% DLX was released within 6 hrs. The plain in situ cubo-gel had a significantly higher IC 50 compared to DLX solution and DLX-loaded in situ cubo-gel. The ex vivo permeation study showed 1.27 enhancement in the drug permeation from DLX in situ cubo-gel. According to the in vivo bio-distribution study in plasma and brain, the intranasal DLX in situ cubo-gel showed a 1.96 fold improvement in brain bioavailability compared to the intranasal solution. Its BTE% and DTP% were 137.77 and 10.5, respectively, indicating efficient brain targeting after intranasal administration. Conclusion: Accordingly, intranasal DLX in situ cubo-gel can be considered as an innovative nano-carrier delivery system for bioavailability enhancement and efficient brain targeting of DLX to maximize its effect.

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Nanostructured liquid crystalline formulation as a remarkable new drug delivery system of anti-epileptic drugs for treating children patients

Abstract: Cubosomal-gel could be considered an innovative dosage-form for Cl through the transdermal route.

Cited by 44 publications

References 56 publications

Nanocubosomal based in situ gel loaded with natamycin for ocular fungal diseases: development, optimization, in-vitro , and in-vivo assessment

Nanocubosomal based in situ gel loaded with natamycin for ocular fungal diseases: development, optimization, in-vitro , and in-vivo assessment

Intranasal drug delivery: opportunities and toxicologic challenges during drug development

<p>Brain Targeting of Duloxetine HCL via Intranasal Delivery of Loaded Cubosomal Gel: In vitro Characterization, ex vivo Permeation, and in vivo Biodistribution Studies</p>

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