Chitosan-coated liposome dry-powder formulations loaded with ghrelin for nose-to-brain delivery

Salade, Laurent; Wauthoz, Nathalie; Vermeersch, Marjorie; Amighi, Karim; Goole, Jonathan

doi:10.1016/j.ejpb.2018.06.011

Cited by 49 publications

(27 citation statements)

References 56 publications

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“…The high drug recovery in the olfactory region, a site for the transportation of drug to the central nervous system, suggests that chitosan-coated liposomes are suitable for a nose-to-brain delivery. However, it is important to indicate that the nasal cast is not suitable for the evaluation of mucociliary clearance mechanism [118]. In vitro study of the formulation from a USB aerosol on artificial nasal cavity indicated that the total recovered drug was 23% in the nasal valves section, 25% in the turbinates section, 0% in the rhinopharynx and filter sections, and 52% in the olfactory region [118] Fexofenadine Chitosan Particle size of 359 nm.…”

Section: Emulsionsmentioning

confidence: 99%

Chitosan-Based Nanocarriers for Nose to Brain Delivery

Aderibigbe

Naki

2019

Applied Sciences

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In the treatment of brain diseases, most potent drugs that have been developed exhibit poor therapeutic outcomes resulting from the inability of a therapeutic amount of the drug to reach the brain. These drugs do not exhibit targeted drug delivery mechanisms, resulting in a high concentration of the drugs in vital organs leading to drug toxicity. Chitosan (CS) is a natural-based polymer. It has unique properties such as good biodegradability, biocompatibility, mucoadhesive properties, and it has been approved for biomedical applications. It has been used to develop nanocarriers for brain targeting via intranasal administration. Nanocarriers such as nanoparticles, in situ gels, nanoemulsions, and liposomes have been developed. In vitro and in vivo studies revealed that these nanocarriers exhibited enhanced drug uptake to the brain with reduced side effects resulting from the prolonged contact time of the nanocarriers with the nasal mucosa, the surface charge of the nanocarriers, the nano size of the nanocarriers, and their capability to stretch the tight junctions within the nasal mucosa. The aforementioned unique properties make chitosan a potential material for the development of nanocarriers for targeted drug delivery to the brain. This review will focus on chitosan-based carriers for brain targeting.

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Section: Emulsionsmentioning

confidence: 99%

Chitosan-Based Nanocarriers for Nose to Brain Delivery

Aderibigbe

Naki

2019

Applied Sciences

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“…An insert with a surface area of 4.2 cm 2 was then placed below these instead of the cap (tip-cell layer distance = 12 cm). From the initial amount of powder loaded in the device (25 mg), 99.6% ± 1.5% was delivered and 64 ± 4.8% deposited on the Calu-3 cell monolayer on the insert, with a very good reproducibility (< 10%) (Salade et al, 2018). Of course, the reproducibility of the method could change according to the properties of the powder studied (e.g.…”

Section: Formulation Deposition Methodsmentioning

confidence: 99%

“…The residual moisture of the formulation can be estimated by weight evaluation before and after desiccation, by thermogravimetric analysis or by accurately determining the water content using a Karl Fisher test. The residual moisture in the formulation is an important parameter for powder properties as well as for drug stability (Salade et al, 2018). The flowability of the powder may be improved by the presence of small amounts of residual moisture as water can act as a lubricant by reducing electrostatic charges.…”

Section: Powder Formulationsmentioning

confidence: 99%

“…Thus, experiments on a nasal cast make it possible to compare new techniques of targeted administration and thus to select the most promising. Another experiment also targeted nose-to-brain delivery but with a powder formulation containing chitosan-coated liposomes loaded with ghrelin (Salade et al, 2018). This approach adjusted the physicochemical properties of the powder developed and used the Unit-Dose System device from Aptar Pharma® (Le Vaudreuil, France).…”

Section: Deposition Studies In Nasal Cavities Using a Nasal Castmentioning

confidence: 99%

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How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods

Salade

Wauthoz

Goole

et al. 2019

International Journal of Pharmaceutics

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Nasal delivery offers many benefits over other conventional routes of delivery (e.g. oral or intravenous administration). Benefits include, among others, a fast onset of action, non-invasiveness and direct access to the central nervous system. The nasal cavity is not only limited to local application (e.g. rhinosinusitis) but can also provide direct access to other sites in the body (e.g. the central nervous system or systemic circulation). However, both the anatomy and the physiology of the nose impose their own limitations, such as a small volume for delivery or rapid mucociliary clearance. To meet nasal-specific criteria, the formulator has to complete a plethora of tests, in vitro and ex vivo, to assess the efficacy and tolerance of a new drug-delivery system. Moreover, depending on the desired therapeutic effect, the delivery of the drug should target a specific pathway that could potentially be achieved through a modified release of this drug. Therefore, this review focuses on specific techniques that should be performed when a nasal formulation is developed. The review covers both the tests recommended by regulatory agencies (e.g. the Food and Drug Administration) and other complementary experiments frequently performed in the field.

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“…peptides) and conventional small drug molecules (Chaturvedi et al, 2011). Furthermore, It has been previously reported that drug bioavailability can be improved when microparticles are given intranasally as powders compared to the corresponding liquid formulations (Ishikawa et al, 2001; Rassu et al, 2015;Salade et al, 2018).…”

Section: Introductionmentioning

confidence: 99%

Spray-dried alginate microparticles for potential intranasal delivery of ropinirole hydrochloride: development, characterization and histopathological evaluation

Hussein

Omer

Ismael

et al. 2019

Pharmaceutical Development and Technology

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Ropinirole hydrochloride (RH) is an anti-Parkinson drug with relativity low oral bioavailability owing to its extensive hepatic first pass metabolism. Spray-dried mucoadhesive alginate microspheres of RH were developed and characterized followed by histopathological evaluation using nasal tissue isolated from sheep. Spherical microparticles having high product yield (around 70%) were obtained when the inlet temperature of spray drying was 140°C. Fourier Transform Infrared (FTIR) studies revealed the compatibility of the drug with the polymer, and scanning electron microscopy (SEM) showed that drug-loaded microparticles were spherical, and the apparent surface roughness was inversely related to the ratio of polymer to drug. Furthermore, size of the spray-dried particles were in the range of 2.5-4.37 µm, depending on formulation. All formulations had high drug encapsulation efficiencies (101-106%). Drug loaded into the polymeric particles was in the amorphous state and drug molecules were molecularly dispersed in the polymeric matrix of the microparticles which were revealed by X-ray diffraction and differential scanning calorimetry (DSC), respectively. The in vitro drug release was influenced by polymer concentration. Histopathological study demonstrated that RH-loaded sodium alginate microparticles was safe to nasal epithelium. In conclusion, spray drying of RH using sodium alginate polymer has produced microparticles of suitable characteristics for potential intranasal administration.

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Chitosan-coated liposome dry-powder formulations loaded with ghrelin for nose-to-brain delivery

Cited by 49 publications

References 56 publications

Chitosan-Based Nanocarriers for Nose to Brain Delivery

Chitosan-Based Nanocarriers for Nose to Brain Delivery

How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods

Spray-dried alginate microparticles for potential intranasal delivery of ropinirole hydrochloride: development, characterization and histopathological evaluation

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