A new nanovesicular system for nasal drug administration

Touítou, Elka; Duchi, Shaher; Natsheh, Hiba

doi:10.1016/j.ijpharm.2020.119243

Cited by 19 publications

(22 citation statements)

References 31 publications

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“…Results of DSC measurements have indicated a difference of 16.51 • C in the Tm of the phospholipid vesicles of this nasal nanocarrier when compared to classic liposomes. These data suggest the presence of vesicles with fluid phospholipid bilayers in the nanocarrier [10].…”

Section: Phospholipid Nanovesicles Containing Ethanol and Propylene Gmentioning

confidence: 62%

“…Levels of O-desmethyl tramadol (M1), the main active metabolite of tramadol, were also measured in sheep plasma. As detected by liquid chromatography-mass spectrometry (LC-MS/MS), M1 plasma concentration in animals treated with tramadol nasally was similar to the levels in those receiving the drug by i.v administration [10].…”

Section: Active Molecules Incorporated In Phospholipid-altered Vesiclmentioning

confidence: 81%

“…The drug delivery-enhancing properties of this carrier were tested in several studies. Touitou et al [10] measured the ability of soft phospholipid vesicles containing 15% w/w ethanol and 20% w/w propylene glycol to increase the in vivo penetration into rats' nasal mucosa of fluorescent probes. CLSM data showed enhanced penetration of three probes: FITC, FITC-bacitracin and rhodamine B into the nasal mucosa only from the nanovesicular carrier, and not from a simple solution.…”

Section: Phospholipid Nanovesicles Containing Ethanol and Propylene Gmentioning

confidence: 99%

“…Drugs loaded in this carrier were efficient for the treatment of various diseases in animal models, including multiple sclerosis (MS), hot flushes, pain, inflammation, migraine and insomnia [9,10,31,151]. Drugs loaded in this carrier were efficient for the treatment of various diseases in animal models, including multiple sclerosis (MS), hot flushes, pain, inflammation, migraine and insomnia [9,10,31,151].…”

Section: Phospholipid Nanovesicles Containing Ethanol and Propylene Gmentioning

confidence: 99%

“…However, the ability of liposomes to facilitate drug penetration into the deep skin layers is limited [4,5]. Over the last three decades, an increasing attention has been given to phospholipid vesicles altered by surfactants and by ethanol to be used for delivery of active agents for dermal/transdermal and nasal administration [4,[6][7][8][9][10][11]. These types of vesicular carriers were not investigated for oral or parenteral administration.…”

Section: Introductionmentioning

confidence: 99%

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Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties

Natsheh

Touítou

2020

Molecules

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This is a comprehensive review on the use of phospholipid nanovesicles for dermal/transdermal and nasal drug administration. Phospholipid-based vesicular carriers have been widely investigated for enhanced drug delivery via dermal/transdermal routes. Classic phospholipid vesicles, liposomes, do not penetrate the deep layers of the skin, but remain confined to the upper stratum corneum. The literature describes several approaches with the aim of altering the properties of these vesicles to improve their penetration properties. Transfersomes and ethosomes are the most investigated penetration-enhancing phospholipid nanovesicles, obtained by the incorporation of surfactant edge activators and high concentrations of ethanol, respectively. These two types of vesicles differ in terms of their structure, characteristics, mechanism of action and mode of application on the skin. Edge activators contribute to the deformability and elasticity of transfersomes, enabling them to penetrate through pores much smaller than their own size. The ethanol high concentration in ethosomes generates a soft vesicle by fluidizing the phospholipid bilayers, allowing the vesicle to penetrate deeper into the skin. Glycerosomes and transethosomes, phospholipid vesicles containing glycerol or a mixture of ethanol and edge activators, respectively, are also covered. This review discusses the effects of edge activators, ethanol and glycerol on the phospholipid vesicle, emphasizing the differences between a soft and an elastic nanovesicle, and presents their different preparation methods. To date, these differences have not been comparatively discussed. The review presents a large number of active molecules incorporated in these carriers and investigated in vitro, in vivo or in clinical human tests.

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Section: Phospholipid Nanovesicles Containing Ethanol and Propylene Gmentioning

confidence: 62%

Section: Active Molecules Incorporated In Phospholipid-altered Vesiclmentioning

confidence: 81%

Section: Phospholipid Nanovesicles Containing Ethanol and Propylene Gmentioning

confidence: 99%

Section: Phospholipid Nanovesicles Containing Ethanol and Propylene Gmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties

Natsheh

Touítou

2020

Molecules

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Advances in Stimuli‐Responsive Chitosan Hydrogels for Drug Delivery Systems

Xia,

Ma,

et al. 2023

Macromolecular Bioscience

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Sustainable and controllable drug transport is one of the most efficient ways of disease treatment. Due to high biocompatibility, good biodegradability, and low costs, chitosan and its derivatives are widely used in biomedical fields. Specifically, chitosan hydrogel enables drugs to pass through biological barriers because of their abundant amino and hydroxyl groups that can interact with human tissues. Moreover, the multi‐responsive nature (pH, temperature, ions strength, and magnetic field, etc.) of chitosan hydrogels makes precise drug release a possibility. Here, the synthesis methods, modification strategies, stimuli‐responsive mechanisms of chitosan‐based hydrogels, and their recent progress in drug delivery are summarized. Chitosan hydrogels that carry and release drugs through subcutaneous (dealing with wound dressing), oral (dealing with gastrointestinal tract), and facial (dealing with ophthalmic, ear, and brain) are reviewed. Finally, challenges toward clinic application and the future prospects of stimuli‐responsive chitosan‐based hydrogels are indicated.

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Rational development of fingolimod nano-embedded microparticles as nose-to-brain neuroprotective therapy for ischemic stroke

Zhang,

Su,

Shao

et al. 2024

Drug Deliv. and Transl. Res.

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Ischemic stroke is one of the major diseases causing varying degrees of dysfunction and disability worldwide. The current management of ischemic stroke poses significant challenges due to short therapeutic windows and limited efficacy, highlighting the pressing need for novel neuroprotective treatment strategies. Previous studies have shown that fingolimod (FIN) is a promising neuroprotective drug. Here, we report the rational development of FIN nano-embedded nasal powders using full factorial design experiments, aiming to provide rapid neuroprotection after ischemic stroke. Flash nanoprecipitation was employed to produce FIN nanosuspensions with the aid of polyvinylpyrrolidone and cholesterol as stabilizers. The optimized nanosuspension (particle size = 134.0 ± 0.6 nm, PDI = 0.179 ± 0.021, physical stability = 72 ± 0 h, and encapsulation efficiency of FIN = 90.67 ± 0.08%) was subsequently spray-dried into a dry powder, which exhibited excellent redispersibility (RdI = 1.09 ± 0.04) and satisfactory drug deposition in the olfactory region using a customized 3D-printed nasal cast (45.4%) and an Alberta Idealized Nasal Inlet model (8.6%) at 15 L/min. The safety of the optimized FIN nano-embedded dry powder was confirmed in cytotoxicity studies with nasal (RPMI 2650 and Calu-3 cells) and brain related cells (SH-SY5Y and PC 12 cells), while the neuroprotective effects were demonstrated by observed behavioral improvements and reduced cerebral infarct size in a middle cerebral artery occlusion mouse stroke model. The neuroprotective effect was further evidenced by increased expression of anti-apoptotic protein BCL-2 and decreased expression of pro-apoptotic proteins CC3 and BAX in brain peri-infarct tissues. Our findings highlight the potential of nasal delivery of FIN nano-embedded dry powder as a rapid neuroprotective treatment strategy for acute ischemic stroke. Graphical abstract

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A new nanovesicular system for nasal drug administration

Cited by 19 publications

References 31 publications

Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties

Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties

Advances in Stimuli‐Responsive Chitosan Hydrogels for Drug Delivery Systems

Rational development of fingolimod nano-embedded microparticles as nose-to-brain neuroprotective therapy for ischemic stroke

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