Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

Adnet, Thomas; Groo, Anne-Claire; Picard, Céline; Davis, Audrey; Corvaisier, Sophie; Since, Marc; Bounoure, F.; Rochais, Christophe; Pluart, Loïc Le; Dallemagne, Patrick; Malzert‐Fréon, Aurélie

doi:10.3390/pharmaceutics12030251

Cited by 54 publications

(20 citation statements)

References 67 publications

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“…Moreover, a decrease in the formulations' apparent viscosity with time was not observed, which indicates the absence of thixotropy (the upper and lower curves of the rheograms overlap). Other authors have reported the same behavior as desirable for nasal formulations [18][19][20]. Figure 1B also shows the effect of lipid-based nanosystems on the flow behavior.…”

Section: Rheological and Texture Analysissupporting

confidence: 66%

Thermosensitive Nasal In Situ Gels of Lipid-Based Nanosystems to Improve the Treatment of Alzheimer’s Disease

Cunha

Forbes

Lobo

et al. 2020

The 1st International Electronic Conference on Pharmaceutics

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Thermosensitive in situ gels are promising formulations for the management of Alzheimer’s disease (AD), since they increase the residence time of lipid-based nanosystems in the nasal cavity, improving drug therapeutic efficacy. The purpose of this study is to prepare thermosensitive in situ gels with anticholinesterase inhibitor (RVG)-loaded nanostructured lipid carriers (NLC) and nanoemulsions to improve the residence time of the formulations in the nasal cavity. Different concentrations of thermosensitive polymers were added to the RVG-loaded NLC and to the RVG-loaded nanoemulsion to optimize the gelation temperature of the in situ gels; concentrations of 17% (%, w/w) of Kolliphor® P407 and 0.3% (%, w/w) of MethocelTM K4M were selected. The in situ gels of the RVG-loaded NLC and RVG-loaded nanoemulsion had a particle size, PDI, ZP, and pH of, respectively: 141.70 ± 0.40 nm and 146.10 ± 1.73 nm; 0.45 ± 0.00 and 0.43 ± 0.02; −4.06 ± 1.03 mV and −4.09 ± 0.71 mV, 6.60 ± 0.01 and 7.00 ± 0.02. In addition, these in situ gels showed a non-Newtonian plastic behavior, and the texture parameters presented desirable values for nasal administration. From these results, we concluded that the developed in situ gels can be used to improve the treatment of AD through the nose-to-brain route.

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Section: Rheological and Texture Analysissupporting

confidence: 66%

Thermosensitive Nasal In Situ Gels of Lipid-Based Nanosystems to Improve the Treatment of Alzheimer’s Disease

Cunha

Forbes

Lobo

et al. 2020

The 1st International Electronic Conference on Pharmaceutics

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“…This hydrogel is also able to encapsulate curcumin and release it slowly, and although this hydrogel has not been tested yet in vivo, it could represent a promising therapeutic strategy [ 184 ]. Recently, a combinatory approach has also been tested, combining liposomes with hydrogels and delivering an active pharmaceutical ingredient, in order to improve bioavailability [ 185 ].…”

Section: The Role Of Scaffolds In Developing Regenerative Therapiementioning

confidence: 99%

Advances in Tissue Engineering and Innovative Fabrication Techniques for 3-D-Structures: Translational Applications in Neurodegenerative Diseases

Rey

Barzaghini

Nardini

et al. 2020

Cells

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In the field of regenerative medicine applied to neurodegenerative diseases, one of the most important challenges is the obtainment of innovative scaffolds aimed at improving the development of new frontiers in stem-cell therapy. In recent years, additive manufacturing techniques have gained more and more relevance proving the great potential of the fabrication of precision 3-D scaffolds. In this review, recent advances in additive manufacturing techniques are presented and discussed, with an overview on stimulus-triggered approaches, such as 3-D Printing and laser-based techniques, and deposition-based approaches. Innovative 3-D bioprinting techniques, which allow the production of cell/molecule-laden scaffolds, are becoming a promising frontier in disease modelling and therapy. In this context, the specific biomaterial, stiffness, precise geometrical patterns, and structural properties are to be considered of great relevance for their subsequent translational applications. Moreover, this work reports numerous recent advances in neural diseases modelling and specifically focuses on pre-clinical and clinical translation for scaffolding technology in multiple neurodegenerative diseases.

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“…pH values of NEs were measured between 3.25 and 3.56, which are in the acceptable range for nasal preparation (6 ± 3 ) [50].…”

Section: Physicochemical Characterization Of Nes Containingmentioning

confidence: 92%

Fabrication of a Thermosensitive In Situ Gel Nanoemulsion for Nose to Brain Delivery of Temozolomide

Bayanati

Khosroshahi

Alvandi

et al. 2021

Journal of Nanomaterials

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In this study, a thermosensitive in situ gel nanoemulsion was formulated by a low energy method for intranasal delivery of temozolomide to bypass the blood-brain barrier and optimize chemotherapy for glioblastoma. Various amounts of Labrasol, Transcutol®P, and Triacetin were chosen as nanoemulsion components based on the solubility and the partial pseudoternary phase diagrams studies. Poloxamer derivatives added to the selected nanoemulsion and gelling temperature optimized. The prepared in situ gel nanoemulsion containing temozolomide showed a mean droplet size of 16.25 ± 0.44 nm , a polydispersity index value of 0.35 ± 0.01 , and desirable pH and viscosity. In vitro release studies revealed that both nanoemulsion and in situ gel preparation have sustained release pattern in comparison to the control solution. Visual evaluation and droplet size and polydispersity index measurements showed both nanoemulsion and in situ gel nanoemulsion were stable during heating-cooling and freeze-thaw cycles and also centrifugation. Mucoadhesion percentage of in situ gel nanoemulsion was 37.037 ± 2.32 regarding ex vivo studies, which had a significant rise in comparison to control solution and nanoemulsion. Permeation across the nasal mucosa was 1.43- and 1.52-fold higher than the control solution for nanoemulsion and in situ nanoemulsion, respectively. Gamma scintigraphy study showed brain accumulation of developed nanoemulsion formulations. Our studies demonstrated optimized formulation has suitable physicochemical properties, desirable release profile, enhanced permeation across the nasal mucosa, and prolonged resistance time at the nasal mucosa. Therefore, in situ gel nanoemulsion would be an effective novel nasal delivery system for the treatment of glioblastoma.

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Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

Cited by 54 publications

References 67 publications

Thermosensitive Nasal In Situ Gels of Lipid-Based Nanosystems to Improve the Treatment of Alzheimer’s Disease

Thermosensitive Nasal In Situ Gels of Lipid-Based Nanosystems to Improve the Treatment of Alzheimer’s Disease

Advances in Tissue Engineering and Innovative Fabrication Techniques for 3-D-Structures: Translational Applications in Neurodegenerative Diseases

Fabrication of a Thermosensitive In Situ Gel Nanoemulsion for Nose to Brain Delivery of Temozolomide

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