References of "Lechanteur, Anna"
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See detailImpregnation of mesoporous silica with poor aqueous soluble molecule using pressurized carbon dioxide: is the solubility in the supercritical and subcritical phase a critical parameter?
Koch, Nathan ULiege; Jennotte, Olivier ULiege; Grignard, Bruno ULiege et al

in European Journal of Pharmaceutical Sciences (2020), 150

Recently, mesoporous silica (MS) has been used as a material able to maintain amorphous state of active compounds and therefore, enhance the oral bioavailability of BCSII drugs. Among impregnation methods ... [more ▼]

Recently, mesoporous silica (MS) has been used as a material able to maintain amorphous state of active compounds and therefore, enhance the oral bioavailability of BCSII drugs. Among impregnation methods of MS, techniques using supercritical carbon dioxide (sc-CO2) are promising tools. Solubility of compounds in sc-CO2 is reported as one of the most critical parameters, which usually limits its use in drug formulation. Indeed, most of compounds have poor solubility in sc-CO2. The aim of this work is to compare different MS and to study alternative processes using pressurized CO2 for insoluble molecule in sc-CO2. By using high pressure reactor, DSC, HPLC and in vitro dissolution tests, the crystallinity and dissolution profiles of MS with different pore size (6.6 nm, 25.0 nm and 2.5 nm) impregnated with fenofibrate (FF) under sc-CO2 were compared to select the most appropriate carrier. Then, the selected MS has been impregnated under supercritical, subcritical and atmospheric conditions. We have shown that the MS pore size of 6.6 nm provides the higher amorphous drug loading capacity as well as the faster and higher drug dissolution. In addition, FF-MS formulations produced with pressurized CO2 as fusion medium, both in subcritical and supercritical conditions; give similar crystallinity and dissolution results compared to those produced with supercritical fluids as solvent. Through this study, we show new possibilities of using CO2 for insoluble compounds in this fluid. [less ▲]

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See detailInfluence of Composition and Spray-Drying Process Parameters on Carrier-Free DPI Properties and Behaviors in the Lung: A review
Lechanteur, Anna ULiege; Evrard, Brigitte ULiege

in Pharmaceutics (2020)

Although dry powder inhalers (DPIs) have attracted great interest compared to nebulizers and metered-dose inhalers (MDIs), drug deposition in the deep lung is still insufficient to enhance therapeutic ... [more ▼]

Although dry powder inhalers (DPIs) have attracted great interest compared to nebulizers and metered-dose inhalers (MDIs), drug deposition in the deep lung is still insufficient to enhance therapeutic activity. Indeed, it is estimated that only 10%–15% of the drug reaches the deep lung while 20% of the drug is lost in the oropharyngeal sphere and 65% is not released from the carrier. The potentiality of the powders to disperse in the air during the patient’s inhalation, the aerosolization, should be optimized. To do so, new strategies, in addition to classical lactose-carrier, have emerged. The lung deposition of carrier-free particles, mainly produced by spray drying, is higher due to non-interparticulate forces between the carrier and drug, as well as better powder uniformity and aerosolization. Moreover, the association of two or three active ingredients within the same powder seems easier. This review is focused on a new type of carrier-free particles which are characterized by a sugar-based core encompassed by a corrugated shell layer produced by spray drying. All excipients used to produce such particles are dissected and their physico-chemical properties (Péclet number, glass transition temperature) are put in relation with the lung deposition ability of powders. The importance of spray-drying parameters on powders’ properties and behaviors is also evaluated. Special attention is given to the relation between the morphology (characterized by a corrugated surface) and lung deposition performance. The understanding of the closed relation between particle material composition and spray-drying process parameters, impacting the final powder properties, could help in the development of promising DPI systems suitable for local or systemic drug delivery. [less ▲]

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See detailCannabidiol aqueous solubility enhancement: comparison of three amorphous formulations strategies using different type of polymers
Koch, Nathan ULiege; Jennotte, Olivier ULiege; Gasparrini, Youri ULiege et al

in International Journal of Pharmaceutics (2020)

Poor aqueous solubility of terpenophenolic compound Cannabidiol (CBD) is a major issue in the widespread use of this promising therapeutic polyphenol. Moreover, choosing the appropriate strategy to ... [more ▼]

Poor aqueous solubility of terpenophenolic compound Cannabidiol (CBD) is a major issue in the widespread use of this promising therapeutic polyphenol. Moreover, choosing the appropriate strategy to overcome this challenge is time-consuming and based on trial-error processes. The amorphous form of CBD provided higher aqueous solubility as well as faster dissolution rate in comparison with crystalline CBD. Nevertheless, amorphous forms of CBD tend to recrystallize. The aim of this study was to use three different strategies based on the stabilization of the amorphous form. Cyclodextrins (CH3CD, HPβCD and HPγCD.), mesoporous silicas (Silsol® and Syloid® AL-1FP) and water soluble polymers (Kollidon® VA64, Kollidon® 12PF and Soluplus®) were processed by using the following techniques: freeze-drying, spray-drying, subcritical carbon dioxide impregnation or hot-melt extrusion. All the obtained formulations provided complete amorphous CBD, although the drug loading depend highly of the excipients. CBD-cyclodextrin formulations, processed by freeze-drying or spray-drying, and CBD-mesoporous silica formulations, processed by subcritical CO2 or by atmospheric impregnation, provided significant increase of aqueous solubility. While the use of Kollidon® 12PF did not provided significant increased solubility within 90 min, Kollidon® VA64 has been highlighted as the excipient that exhibits the highest increase of aqueous solubility of this study. Finally, all formulations, excepted CBD-ALFP formulations, showed adequate stability within at least two months. [less ▲]

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See detailLiposomal Encapsulated Curcumin Effectively Attenuates Neuroinflammatory and Reactive Astrogliosis Reactions in Glia Cells and Organotypic Brain Slices
Schmitt, Christina; Lechanteur, Anna ULiege; Cossais, François et al

in International Journal of Nanomedicine (2020), 15

Introduction: The polyphenolic spice and food coloring ingredient curcumin has beneficial effects in a broad variety of inflammatory diseases. Amongst them, curcumin has been shown to attenuate microglia ... [more ▼]

Introduction: The polyphenolic spice and food coloring ingredient curcumin has beneficial effects in a broad variety of inflammatory diseases. Amongst them, curcumin has been shown to attenuate microglia reaction and prevent from glial scar formation in spinal cord and brain injuries. Methods: We developed a protocol for the efficient encapsulation of curcumin as a model for anti-inflammatory drugs yielding long-term stable, non-toxic liposomes with favorable physicochemical properties. Subsequently, we evaluate the effects of liposomal curcumin in experimental models for neuroinflammation and reactive astrogliosis. Results: We could show that liposomal curcumin can efficiently reduce the reactivity of human microglia and astrocytes and preserve tissue integrity of murine organotypic cortex slices. Discussion and Perspective: In perspective, we want to administer this curcumin formulation in brain implant coatings to prevent neuroinflammation and glial scar formation as foreign body responses of the brain towards implanted materials. [less ▲]

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See detailThree-dimensional printing technology as a promising tool in bioavailability enhancement of poorly water-soluble molecules: a review
Jennotte, Olivier ULiege; Koch, Nathan ULiege; Lechanteur, Anna ULiege et al

in International Journal of Pharmaceutics (2020)

Poor aqueous solubility of active pharmaceutical ingredients (API) is nowadays a major issue in the pharmaceutical field. The combinatorial chemistry provides more and more API with a great therapeutic ... [more ▼]

Poor aqueous solubility of active pharmaceutical ingredients (API) is nowadays a major issue in the pharmaceutical field. The combinatorial chemistry provides more and more API with a great therapeutic potential, but with a low aqueous solubility. Among the strategies to overcome this drawback, the use of amorphous solid dispersions (ASD), as well as the increase of surface area, is widely used. The three dimensional (3D) printing technologies appear to be innovative tools allowing the construction of any unconventional forms with different composition, structure or infill; especially by using ASD materials. This review aims to deliver notions about the different 3D printing techniques found in the literature to improve aqueous solubility of several API, namely nozzle-based method, inkjet methods and laser-based methods, as well as guide formulator in terms of formulation parameters that have to be optimized to allow the most suitable impression of innovative medicines. [less ▲]

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See detailIn vitro skin penetration enchancement techniques: a combined approach of ethosomes and microneedles
Bellefroid, Coralie ULiege; Lechanteur, Anna ULiege; Evrard, Brigitte ULiege et al

in International Journal of Pharmaceutics (2019), 572

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See detailImprovement water-solubility of ellagic acid for use as an antimalarial drug through oral administration
Nyamba, Isaïe ULiege; Lechanteur, Anna ULiege; Evrard, Brigitte ULiege et al

Poster (2019, December 11)

Ellagic acid (EA) is a polyphenolic compound, classed as a BCS IV drug, having anti-plasmodial activity on plasmodium-infected cell cultures. However, this class of molecules has a low oral ... [more ▼]

Ellagic acid (EA) is a polyphenolic compound, classed as a BCS IV drug, having anti-plasmodial activity on plasmodium-infected cell cultures. However, this class of molecules has a low oral bioavailability. The aim of our study is to increase the aqueous solubility and therefore the bioavailability of EA to allow its use orally as an antimalarial. To achieve this goal, solid dispersions of EA were made using the hot melt extrusion process. For this purpose, a Scamex® twin-screw corotative extruder was used for the production of extrudates from mixtures of EA powders (5% w/w) and polymers (95% w/w). Three polymers were used as Eudragit® EPO, Kollidon VA® 64 and Soluplus®. The release profile of the EA from the extrudates was evaluated in vitro by dissolution tests under non sink conditions in acidic medium (0.1N HCl) and close to neutrality (pH 6.8 phosphate buffer). Eudragit® EPO-based extrudates showed the best release profile of AE with a 94% release rate after 15 min while Kollidon VA® 64 and Soluplus® extrudates showed a dissolution of AE of 38.5% and 30.66%, respectively. The apparent solubility resulting from these release rates corresponded to a respective increase of 62, 25 and 20 times compared to the actual solubility of EA. Moreover, the supersaturated solutions of Eudragit® EPO and Soluplus® were stable for at least 1h30 min. In conclusion, the solid dispersion made of Eudragit® EPO and EA seems appropriated to enhance the oral bioavailability of the drug. [less ▲]

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See detailLC-UV as tool for nanovectorized anticancer peptide quality control: evaluation of encapsulation efficiency
Ilangala Booka, Ange ULiege; COBRAIVILLE, Gaël ULiege; EVRARD, Aude ULiege et al

Poster (2019, December 11)

Many peptides have today a recognized and growing therapeutic interest. However, their administration is not an easy task, since systemically administrated peptides may suffer from several issues such as ... [more ▼]

Many peptides have today a recognized and growing therapeutic interest. However, their administration is not an easy task, since systemically administrated peptides may suffer from several issues such as rapid elimination or unspecific biodistribution. Moreover, many compounds of this emerging class of therapeutics have their targets at the intracellular level, adding another challenge to their therapeutic success. LB19 is a peptidic selective inhibitors of LDHB that catalyzes the conversion of lactate + NAD to pyruvate + NADH + H+, a new therapeutic approach for cancer therapy. The necessity of intravenous administration of LB19 lead to the development of liposomes as drug carriers, combining the protective properties of PEG (stealth liposomes) with the transfection properties of pH-sensitive lipids. This general concept raises the need to develop analytical tools enabling the determination of the encapsulation efficiency of LB19 into these nanocarriers and quantitatively demonstrate their ability to achieve intracellular delivery of their payload. In this project, a LC-UV method was developed to selectively quantify this new anticancer peptide in liposomes. More particularly, we generated stability data of LB19 to support its formulation development. The LC-UV method was employed to study the adsorption of the peptide and demonstrate the impact of the adsorption behaviour on quantitative analysis during the evaluation of the encapsulation efficiency of liposomes. Altogether, this analytical part of our project has the potential to control the quality of the formulated LB19 loaded liposomes, and has also a goal to provide a LC-MS/MS method for the intracellular assay of the peptide on long run. [less ▲]

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See detailAssessment of the feasibility to develop a fast and easy reproducible 3D bronchial model growing at the air-liquid interface: Which critical culture parameters must be controlled?
Lechanteur, Anna ULiege; Evrard, Brigitte ULiege; Piel, Géraldine ULiege

Poster (2019, December 11)

The discovery and evaluation of new active drugs will be easier thanks to the development of 3D-epithelial model mimicking biological barriers (1). These models closer to in vivo conditions should help to ... [more ▼]

The discovery and evaluation of new active drugs will be easier thanks to the development of 3D-epithelial model mimicking biological barriers (1). These models closer to in vivo conditions should help to speed up the drug development process. Regarding lung administration, despite many studies exploring the development of 2D-model using Calu-3 cells, there are still multiple disparities about experimental methods and a standardization is needed. We investigated the impact of different culture parameters (time, cell densities,…) on the integrity and the morphology of a 2D model (2). Using permeability studies, electron microscopy and immunohistochemistry, we propose an easy and reproducible 2D-model with Calu-3 cells fully differentiated after 14 days of growing at the air-liquid interface. Moreover, based on these results, we went further with a 3D-bronchial model which consists of a collagen matrix, fibroblasts laid under the epithelial layer. We aim to assess the feasibility to develop a 3D cell-based model of the human airway growing at the air-liquid interface. Many parameters which have to be tightly controlled to develop an extracellular matrix equivalent without any shrinking of the gel encompassing alive fibroblasts as well as over epithelial cells have been identified. Overall, this in vitro model is a differentiated pseudo-stratified bronchial mucosa with mucus expression which is the basis for further optimization allowing the screening of pulmonary drugs in terms of permeability, cytotoxicity or particle-mucus interactions. (1) A. Lechanteur, et al. ADDR. 124 (2018) 50–63. (2) A. Lechanteur, et al. EJPB. 144 (2019) 2–10. [less ▲]

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See detailHot-melt extrusion as a solvent-free technique for the formation of a polymeric amorphous solid dispersion of atorvastatin
Jennotte, Olivier ULiege; Koch, Nathan ULiege; Lechanteur, Anna ULiege et al

Conference (2019, December 11)

Hot-melt extrusion for the formation of an amorphous solid dispersion of atorvastatin in order to enhance its aqueous solubility

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See detailChromametric assessment of drug skin tolerance: A comparative study between Africans and Caucasians skins
Sounouvou, Axel Gérald Hope Tognidé ULiege; Lechanteur, Anna ULiege; Quetin-Leclercq, Joëlle et al

in Skin Research and Technology (2019)

Background/Aims: During dermatological forms development, one of the simplest non-invasive techniques used to evaluate cutaneous tolerance of formulations is to monitor the color changes using a ... [more ▼]

Background/Aims: During dermatological forms development, one of the simplest non-invasive techniques used to evaluate cutaneous tolerance of formulations is to monitor the color changes using a tristimulus chromameter. Most published tolerance studies involving chromametric measurements are performed on Caucasian subjects. However, in the context of drug formulation for African-type populations, it is not always relevant to transpose tolerance results obtained on Caucasians populations to African-type ones due to histological ethnic differences of the skin. The goal of this work was to assess whether tristimulus chromameter can be used to highlight color variations following the application of dermatological topics on black skin in order to validate skin tolerance studies made on African-type subjects. Materials and Methods: After application of two commercial creams with opposite side effects (skin irritation and skin blanching) in both Africans and Caucasians populations, color variations were evaluated using a tristimulus chromameter in L*a*b* color system and compared between both populations. L* indicating color brightness, a* represents green and red directions and b* represents blue and yellow directions. Results: While skin irritation resulted in a significant increase of a* parameter in both studied populations, the skin blanching resulted in a decrease of a* associated with an increase of L*. Conclusion: We established that tristimulus chromameter can be used to achieve in vivo skin tolerance study of dermatologic formulations in Africans despite their dark skin even though it appeared less sensitive. This study can speed up the development of dermatological forms dedicated to Africans and/or Caucasians subjects. [less ▲]

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See detailAssessment of the feasibility to develop a fast and easy reproducible 3D bronchial model growing at the air-liquid interface: Which critical culture parameters must be controlled?
Lechanteur, Anna ULiege; Evrard, Brigitte ULiege; Piel, Géraldine ULiege

in European Journal of Pharmaceutics and Biopharmaceutics (2019)

The discovery and evaluation of new active drugs will be easier thanks to the development of 3D-epithelial model mimicking biological barriers. These models close to in vivo conditions should help to ... [more ▼]

The discovery and evaluation of new active drugs will be easier thanks to the development of 3D-epithelial model mimicking biological barriers. These models close to in vivo conditions should help to speed up the drug development process while reducing in vivo animal testing. Regarding lung administration, despite many studies exploring the development of 2D-model using Calu-3 cells, there are still multiple disparities about experimental methods and a standardization is needed. We investigated the impact of different culture parameters (time, cell densities, Transwell™ membrane pore sizes or the culture media) on the integrity and the morphology of a 2D model. Using permeability studies, electron microscopy and immunohistochemistry, we propose an easy and reproducible 2D-model with Calu-3 cells fully differentiated after 14 days of growing at the air-liquid interface. Moreover, based on these results, we went further with a 3D-bronchial model which consists of a collagen matrix, fibroblasts laid under the epithelial layer. We aim to assess the feasibility to develop a 3D cell-based model of the human airway growing at the air-liquid interface. Many parameters which have to be tightly controlled to develop an extracellular matrix equivalent without any shrinking of the gel encompassing alive fibroblasts as well as over epithelial cells have been identified. Overall, this in vitro model is a differentiated pseudo-stratified bronchial mucosa with mucus expression which is the basis for further optimization allowing the screening of pulmonary drugs in terms of permeability, cytotoxicity or particle-mucus interactions. [less ▲]

Detailed reference viewed: 28 (2 ULiège)
See detailDevelopment of new manufacturing processes for amorphous solid dispersions
Jennotte, Olivier ULiege; Koch, Nathan ULiege; Rocks, Natacha ULiege et al

Conference (2019, May 20)

Use of the hot-melt extrusion form amorphous solid dispersions of atorvastatin calcium trihydrate with a selection of three polymers in order to enhance its aqueous solubility

Detailed reference viewed: 36 (5 ULiège)
See detailHot melt extrusion as a solvent-free technique for the formation of a polymeric amorphous solid dispersion of atorvastatin
Jennotte, Olivier ULiege; Koch, Nathan ULiege; Collard, Laurence ULiege et al

Poster (2019, March 26)

Hot-melt extrusion as a solvent-free technique for the enhancement of BCSII molecules.

Detailed reference viewed: 28 (6 ULiège)