References of "Lechanteur, Anna"
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See detailAmphiphilic N-vinyl pyrrolidone-based polymers as PEG alternatives to avoid blood proteins adsorption around liposomes
Berger, Manon ULiege; Toussaint, François ULiege; Pairoux, Charlotte ULiege et al

Conference (2021, April 06)

Introduction: After a systemic administration, liposomes are quickly covered by proteins leading to the formation of a protein corona. This corona is responsible for a change of physicochemical properties ... [more ▼]

Introduction: After a systemic administration, liposomes are quickly covered by proteins leading to the formation of a protein corona. This corona is responsible for a change of physicochemical properties (as an increase of the size), pharmacokinetics, biodistribution, targeting ability, … [1]. Polyethylene glycol (PEG) is generally grafted onto the liposomes surface to reduce these non-specific interactions with blood components [2]. Since PEG faces some issues [3], alternatives are searched which should optimally prevent the formation of this corona. The goal of this study is to evaluate the protein corona formation around cationic liposomes (DOTAP/Chol/DOPE 1/0.75/0.5 molar ratio) encapsulating a model siRNA. Method: Different formulations were tested: naked liposomes, PEGylated liposomes (15% molar ratio of total lipids) and liposomes grafted with the new synthetic amphiphilic N-vinyl pyrrolidone-based polymers. Liposomes were incubated in FBS for two hours and their sizes were compared before and after incubation. Measurements were performed by DLS and NTA. An increase in liposomes size is related to the adsorption of proteins around the particles. Results: Results show that 15% PEG allows to prevent a significant size increase. However, 15% amphiphilic N-vinyl pyrrolidone-based polymers are not able to prevent corona formation since both analyses revealed a huge increase of particles sizes. A higher concentration (40%) was necessary to hinder a significant size increase meaning probably that their insertion/coating into/onto lipoplexes is different compared to PEG. Conclusions: To conclude, we showed that new synthetic amphiphilic N-vinyl pyrrolidone-based polymers were able to prevent protein corona formation around lipoplexes. Further studies are ongoing in order to evaluate the transfection capacity of these coated-vectors carrying siRNA. [less ▲]

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See detailHow do infill density and polymer composition of tablets produced by hotmelt extrusion coupled with Fused Deposition Modeling 3D printing influence the dissolution profile of a BCS II molecule ?
Parulski, Chloé ULiege; Gresse, Eva ULiege; Jennotte, Olivier ULiege et al

Conference (2021, April 06)

Introduction: During last years, the use of three-dimensional (3D) printing for drug manufacturing has considerably increased in the field of pharmaceutical research. The development of complex geometries ... [more ▼]

Introduction: During last years, the use of three-dimensional (3D) printing for drug manufacturing has considerably increased in the field of pharmaceutical research. The development of complex geometries leading to different drug release profiles is an application that make 3D printing and, more specifically, Fused Deposition Modeling (FDM) a promising tool. In fact, many active pharmaceutical ingredients are classified in the Biopharmaceutics Classification System class II (BCS II) since they are poorly soluble. Thus, the goal of this work is to enhance the solubility and the bioavaibilty of poorly soluble drugs by the use of hot-melt extrusion (HME) coupled with FDM to form of an amorphous solid dispersion. Method: The selected model drug was Itraconazole (ITZ), a BCS II active molecule. Hot-melt extrusion process was performed on three formulations containing 25% of ITZ and different proportions of Affinisol® 15LV (hydroxypropylmethylcellulose) and Kollidon® VA 64 (vinylpyrrolidone-vinyl acetate copolymer). For each formulation, tablets with infill densities of 20%, 50% and 80% were printed (Figure 1). Results: Differential scanning calorimetry (DSC) analysis shows that the three formulations contain ITZ in its amorphous form. The results of dissolution tests in 0.1 M HCl indicate that the dissolution profile of the drug is influenced by the polymer composition and the infill density of the tablets. Conclusions: In conclusion, for the three formulations, the lower the tablet infill is, the higher the porosity and the faster the dissolution rate are. A solubility profile similar to that of Sporanox® (the correspondent commercialized drug in Belgium) is even obtained with one of the tablet formulations with an infill density of 20%, which is highly encouraging for future experiments. [less ▲]

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See detailImpact of amphiphilic copolymer used as PEG alternative on the formation of a protein corona around coated-liposomes encapsulating siRNA
Berger, Manon ULiege; Toussaint, François ULiege; Pairoux, Charlotte ULiege et al

Conference (2021, March 04)

After a systemic administration, liposomes are quickly covered by blood proteins leading to the formation of a protein corona. This corona is responsible for liposomes with a change of physicochemical ... [more ▼]

After a systemic administration, liposomes are quickly covered by blood proteins leading to the formation of a protein corona. This corona is responsible for liposomes with a change of physicochemical properties (as an increase of the size), pharmacokinetics, biodistribution, targeting ability and cellular uptake, complement activation and liposomes rapid clearance. To decrease this phenomenon, polyethylene glycol (PEG) is generally grafted onto liposomes surface to reduce non-specific interactions with blood components. Since PEG faces some issues, alternatives are searched which should optimally protect the liposomes surface from proteins adsorption. The goal of this study was to evaluate the protein corona formation around cationic liposomes (DOTAP/Chol/DOPE 1/0.75/0.5 molar ratio) encapsulating siRNA (N/P ratio of 2.5). Different formulations were tested: naked liposomes, PEGylated liposomes (15% molar ratio of total lipids) and liposomes grafted with new synthetic amphiphilic N-vinyl pyrrolidone-based copolymers used as PEG alternatives (B15b and B19a differing by the number of monomer units). Liposomes were incubated in Fetal Bovine Serum for two hours and their sizes were compared before and after incubation. An increase in liposomes size was related to the adsorption of proteins around the particles. Measurements were performed with Malvern Zetasizer® and Malvern NanoSight®. Results showed that PEG was already effective at 15% to prevent a significant increase of the size. However, both alternatives used at this concentration were not able to prevent corona formation since both analyses revealed a huge increasing of particles sizes. Higher concentration (40%) was necessary to hinder a significant increase of the size meaning probably that their insertion/coating into lipoplexes are different compared to PEG. These polymers may therefore be a great alternative able to face PEG limitations. To conclude, through this project, we have proven that our new amphiphilic copolymers were able to prevent protein corona formation around lipoplexes. Further studies are ongoing in order to evaluate the transfection capacity of these coated-vectors carrying siRNA. [less ▲]

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See detailInvestigation of the impact of polymer composition and infill density of solid oral forms produced by hot-melt extrusion coupled with 3D printing on the dissolution rate of itraconazole
Parulski, Chloé ULiege; Gresse, Eva ULiege; Jennotte, Olivier ULiege et al

Conference (2021, March 04)

In recent years, scientific interest in using three-dimensional (3D) printing for drug manufacturing has considerably increased. Modification of drug release profiles by the elaboration of complex ... [more ▼]

In recent years, scientific interest in using three-dimensional (3D) printing for drug manufacturing has considerably increased. Modification of drug release profiles by the elaboration of complex geometries is an application that make 3D printing and, more precisely, Fused Deposition Modeling (FDM) a promising tool for the pharmaceutical field. In fact, nowadays, many active pharmaceutical ingredients are classified in the Biopharmaceutics Classification System class II (BCS II) since they are poorly soluble. Therefore, the aim of this work is to improve the solubility, thus, the bioavaibilty of poorly soluble drugs by the formation of an amorphous solid dispersion by the use of hot-melt extrusion (HME) coupled with FDM 3D printing. Itraconazole (ITZ), a BCS II active molecule, was selected as the model drug. Three formulations containing different proportions of Affinisol® 15LV (hydroxypropylmethylcellulose) and Kollidon® VA 64 (vinylpyrrolidone-vinyl acetate copolymer) and a constant proportion of 25% of ITZ were hot-melt extruded. For each formulation, tablets with infill densities of 20%, 50% and 80% and constant weight were successfully printed (Figure 1). The results obtained with the differential scanning calorimetry (DSC) analysis show that ITZ is in an amorphous form in all the three formulations. The results of dissolution tests in 0.1 M HCl indicate that the polymer composition of the tablets has an influence on the dissolution profile of the drug. Moreover, the dissolution rate of the tablets is also influenced by their infill density. To conclude, we have found that, for the three formulations, the lower the tablet infill is, the higher the porosity and the faster the dissolution rate are. One of the tablet formulations with an infill density of 20% even have a solubility profile similar to that of Sporanox® (the correspondent commercialized drug in Belgium) which is highly encouraging for future experiments. [less ▲]

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See detailSterilization methods of liposomes: drawbacks of conventional methods and perspectives
Delma, Kouka Luc ULiege; Lechanteur, Anna ULiege; Semde, Rasmané et al

in International Journal of Pharmaceutics (2021)

Liposomes are targeted drug delivery systems that are of great pharmaceutical and therapeutic interest. Parenteral route is the main way used for liposome administration. In this case, their sterility is ... [more ▼]

Liposomes are targeted drug delivery systems that are of great pharmaceutical and therapeutic interest. Parenteral route is the main way used for liposome administration. In this case, their sterility is a requirement. However, due to the particular sensitivity of liposomes and their tendency to physicochemical alterations, their sterilization remains a real challenge. Conventional sterilization methods such as heat, ethylene oxide, ultraviolet and gamma irradiations are considered as unsuitable for liposome sterilization and the recommended methods for obtaining sterility of liposomes are filtration and aseptic manufacturing. Unfortunately, these recommended methods are not without limitations. This review outlines the difficulties associated with the use of these different classical methods for obtaining liposome sterility. The effects on liposome physicochemical and biopharmaceutical characteristics as well as efficacy, toxicity and practical problems of these sterilization techniques have been discussed. The search for an alternative method being therefore necessary, the applicability of supercritical carbon dioxide (ScCO2) technology, which is nowadays a promising strategy for the sterilization of sensitive products such as liposomes, is also examined. It appears from this analysis that ScCO2 could effectively be an interesting alternative to achieve sterility of liposomes, but for this, sterilization assays including challenge tests and optimization studies are needed. [less ▲]

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See detailSystematic study of liposomes composition towards efficient delivery of plasmid DNA as potential application of dermal fibroblasts targeting
Bellefroid, Coralie ULiege; Reusch, Céline ULiege; Lechanteur, Anna ULiege et al

in International Journal of Pharmaceutics (2021), 592

The use of non-viral DNA vectors to topically treat skin diseases has demonstrated a high potential. However, vectors applied on the skin face extracellular barriers including the stratum corneum and ... [more ▼]

The use of non-viral DNA vectors to topically treat skin diseases has demonstrated a high potential. However, vectors applied on the skin face extracellular barriers including the stratum corneum and intracellular barriers such as the endosomal escape and the nuclear targeting of the plasmid DNA. The aim of this study was to develop a formulation suitable for dermal application and effective for delivering plasmid DNA into cells. Different formulations were prepared using different cationic lipids (DOTAP, DC-Chol, DOTMA) and co-lipids (DOPE, DSPE). Lipoplexes were produced by complexing liposomes with plasmid DNA at different pDNA/CL (w/w) ratios. Our results showed that appropriate pDNA/CL ratios allowing total complexation of plasmid DNA differed depending on the structure of the lipid used. The transfection rates showed that (i) higher rates were obtained with DOTMA lipoplexes, (ii) DC-Chol lipoplexes provided a transfection twice as important as DOTAP lipoplexes and (iii) when DSPE was added, the cytotoxicity decreased while transfection rates were similar. We found that formulations composed of DC-Chol:DOPE:DSPE or DOTMA:DOPE were appropriate to complex plasmid DNA and to transfect human primary dermal fibroblasts with efficacy and limited cytotoxicity. Therefore, these formulations are highly promising in the context of gene therapy to treat skin diseases. [less ▲]

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See detailPhysical formulation approaches for improving aqueous solubility and bioavailability of ellagic acid: A review
Nyamba, Isaïe ULiege; Lechanteur, Anna ULiege; Semdé, Rasmé et al

in European Journal of Pharmaceutics and Biopharmaceutics (2020)

Ellagic acid (EA) is a polyphenolic active compound with antimalarial and other promising therapeutic activities. However, its solubility and its permeability are both low (BCS IV). These properties ... [more ▼]

Ellagic acid (EA) is a polyphenolic active compound with antimalarial and other promising therapeutic activities. However, its solubility and its permeability are both low (BCS IV). These properties greatly compromise its oral bioavailability and clinical utilizations. To overcome these limitations of the physicochemical parameters, several formulation approaches, including particle size reduction, amorphization and lipid-based formulations, have been used. Although these strategies have not yet led to a clinical application, some of them have resulted in significant improvements in the solubility and bioavailability of EA. This critical review reports and analyses the different formulation approaches used by scientists to improve both the biopharmaceutical properties and the clinical use of EA. [less ▲]

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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 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 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 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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