References of "Lechanteur, Anna"
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See detailLipid gene nanocarriers for the treatment of skin diseases: current state-of-the-art
Bellefroid, Coralie ULiege; Lechanteur, Anna ULiege; Evrard, Brigitte ULiege et al

in European Journal of Pharmaceutics and Biopharmaceutics (2019)

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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; Collard, Laurence ULiege et al

Scientific conference (2018, December 19)

Water-solubility enhancement of atorvastatin using the hot melt extrusion for the production of a polymeric amorphous solid dispersion

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See detailEnhancement of skin penetration of lipid-based nanocarriers
Bellefroid, Coralie ULiege; Lechanteur, Anna ULiege; Evrard, Brigitte ULiege et al

Scientific conference (2018, December 19)

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See detailCationic Liposomes Carrying siRNA: Impact of Lipid Composition on Physicochemical Properties, Cytotoxicity and Endosomal Escape
Lechanteur, Anna ULiege; Sanna, Vincent; Duchemin, Amandine ULiege et al

Poster (2018, August)

In recent year, cationic liposomes have gained a lot of attention for siRNA delivery using different local routes of administration as the vaginal [1] or the pulmonary routes. However, lipoplexes have to ... [more ▼]

In recent year, cationic liposomes have gained a lot of attention for siRNA delivery using different local routes of administration as the vaginal [1] or the pulmonary routes. However, lipoplexes have to face several biological and intracellular barriers before releasing the genetic cargo. In this study, we focus our effort on intracellular barriers and more specifically on endosomal escape and cytosolic delivery of siRNA as well as on the cytotoxicity due to cationic lipids. Indeed, we have previously demonstrated that the surface charge of liposomes composed of the cationic lipid DOTAP is correlated to the induction of cytotoxicity [2]. In the present study, we have investigated the impact of different cationic lipids and co-lipids on the cytotoxicity and also on the endosomal escape of siRNA by flow cytometry, qRT-PCR and Western Blot assays [3]. To address these issues, we developed four liposomal formulations composed of two different cationic lipids (DOTAP and DC-Cholesterol) and different ratio of co-lipids (cholesterol and DOPE). Formulations were DOTAP/Cholesterol/DOPE 1/0.75/0.5, DOTAP/Cholesterol/DOPE 1/0.5/0.5, DOTAP/DOPE 1/1 and DC-Cholesterol/DOPE 1/1. Each type of liposomes were complexed to siRNA at six different N/P molar ratios and physico-chemical properties were characterized in terms of Z-average size, Zeta potential and complexation efficiency by gel retardation assay. Consequently, three N/P ratios (2.5, 5 and 10) were selected for in vitro experiments on A549 cells. First, we studied the cell viability of A549 cells treated during 24 h with liposomes complexed to inactive siRNA at different N/P molar ratios at siRNA concentrations of 40 and 100 nM. We have shown that the cytotoxicity is influenced by the N/P ratio, the concentration of cationic lipid as well as the nature of the cationic lipid. Secondly, the cellular uptake were evaluated by flow cytometry using the dry Trypan Blue® to quench the external fluorescence. Despite the fact the transfection rate were not significantly different, the mRNA knock-down efficiency were not similar between formulations. Liposomes containing 50% of DOPE induced a mRNA silencing of around 80% as well as the protein knock-down. This study allowed to highlight crucial parameters in order to develop lipoplexes which are safe and induce an efficient intracytoplasmic release of siRNA. Acknowledgments: The authors thank the Belgium National Fund for Scientific Research (FNRS, http://www.frs-fnrs.be) –Télévie for financial support and the Giga Cell Imaging and Flow Cytometry Platform for their collaboration. Anna Lechanteur is a FNRS-Télévie post-doctoral researcher. Amandine Duchemin is a FRIA FNRS Fellow. Denis Mottet is a FNRS Research Associate. References: 1. Lechanteur, A., Furst, T. Delvenne, P. et al., Promoting vaginal distribution of E7 and MCL-1 siRNA-silencing nanoparticles for cervical cancer treatment Molecular Pharmaceutics, 2017. 14: p. 1706-1717. 2. Lechanteur, A., Furst, T. Evrard, B. et al., PEGylation of lipoplexes: The right balance between cytotoxicity and siRNA effectiveness. Eur J Pharm Sci, 2016. 93: p. 493-503. 3. Lechanteur, A., Sanna, V. Duchemin, A. et al., Cationic Liposomes Carrying siRNA: Impact of Lipid Composition on Physicochemical Properties, Cytotoxicity and Endosomal Escape. Nanomaterials (Basel), 2018. 8(270): p. 1-12. [less ▲]

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See detailAssessment of skin penetration of classical and deformable liposomes
Bellefroid, Coralie ULiege; Lechanteur, Anna ULiege; Evrard, Brigitte ULiege et al

Conference (2018, July 12)

The skin is the largest organ of the human body representing an alternative route of administration by providing an easy and pain-free drug delivery option. Cutaneous drug delivery is not associated with ... [more ▼]

The skin is the largest organ of the human body representing an alternative route of administration by providing an easy and pain-free drug delivery option. Cutaneous drug delivery is not associated with a significant drug loss compared to systemic administration due to low enzymatic degradation and a negligible clearance. Moreover, the systemic toxicity resulting from cutaneous application is limited and side effects are easy to observe and to handle [1]. Thanks to these advantages there is a great interest in using the skin as a route of administration. Besides physical and active methods involving the disruption of the stratum corneum (SC) to increase the penetration of drugs in the underlying layers, passive methods using of non-viral vectors, particularly lipid-based nanovectors, is one of the most attractive method [2]. They were developed to increase topical macromolecules penetration through the SC barrier and to promote the intracellular delivery of large molecules such as nucleic acids. However, it has become obvious that conventional liposomes do not promote the skin penetration without enhancement techniques [3]. The aim of this study is to assess the skin penetration of lipid-based nanocarriers according to their composition. The skin penetration of conventional liposomes was compared to the penetration of deformable liposomes with ethanol and/or edge activators (EA). 25% (w/w) of ethanol was added to conventional liposomes (DOTAP/DOPE) to form ethosomes. Sodium Cholate and Tween®80 were used as EA to develop deformable liposomes. Formulations were characterized in terms of size, polydispersity index and surface charge. Ex vivo skin penetration experiment were performed using pig ear skin on Franz cells. In order to visualize the penetration through the skin using confocal microscopy, nanocarriers were fluorescently labeled with a fluorescent lipid (NBD-PC). A kinetic of application was performed (from 3h to 24h) and each condition was done with or without tape stripping. In this study, we showed that all the formulations were not able to penetrate the skin, even for deformable formulations. However, when the SC was removed, formulations containing ethanol allowed penetration into the epidermis. Moreover, the addition of an EA seems to encourage deeper penetration. Acknowledgments: Authors thank the Walloon Region and FEDER for financial supports. References: 1. Zakrewsky, M., S. Kumar, and S. Mitragotri, Nucleic acid delivery into skin for the treatment of skin disease: Proofs-of-concept, potential impact, and remaining challenges. J Control Release, 2015. 219: p. 445-56. 2. Geusens, B., et al., Lipid-mediated gene delivery to the skin. Eur J Pharm Sci, 2011. 43(4): p. 199-211. 3. Sala, M., et al., Lipid nanocarriers as skin drug delivery systems: Properties, mechanisms of skin interactions and medical applications. Int J Pharm, 2018. 535(1-2): p. 1-17. [less ▲]

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See detailMucoadhesive chitosan-coated PLGA nanoparticles for oral delivery of ferulic acid
Angeli de Lima, Isabela; Maissar Khalil, Najeh; Toyomi Tominaga, Tania et al

in Artificial Cells, Nanomedicine and Biotechnology (2018)

This paper describes the development and in vitro evaluation of poly(lactic-co-glycolic acid) (PLGA) nanoparticles coated with chitosan (CS) for oral delivery of ferulic acid (FA). Nanoparticles were ... [more ▼]

This paper describes the development and in vitro evaluation of poly(lactic-co-glycolic acid) (PLGA) nanoparticles coated with chitosan (CS) for oral delivery of ferulic acid (FA). Nanoparticles were obtained by an emulsion evaporation technique and characterized. Furthermore, we evaluated the scavenging activity over hypochlorous acid (HOCl), the cytotoxicity over tumour cells and the in vitro intestinal permeability. Nanoparticles were spherical with a mean diameter of 242 nm, positive zeta potential and 50% of encapsulation efficiency. The in vitro release in phosphate buffered saline (PBS) (pH 7.4) demonstrated a prolonged and biphasic profile diffusion-controlled. In simulated gastrointestinal fluids, about 15% of FA was released in gastric fluid and a negligible release was observed in the intestinal fluid. In the HOCl scavenging activity and cytotoxicity over B16-F10 and HeLa cells, FA-loaded nanoparticles presented the same efficacy of the free drug. Besides, in the antioxidant and cytotoxic assay, CS contributed to FA effects. In the intestinal permeability study, FA-loaded nanoparticles exhibited a permeation of 6% through the Caco-2 monolayer and 20% through the Caco-2/HT29-MTX/Raji B co-culture. CS-coated PLGA nanoparticles are promising carriers for oral delivery of FA. [less ▲]

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See detailCationic Liposomes Carrying siRNA: Impact of Lipid Composition on Physicochemical Properties, Cytotoxicity and Endosomal Escape
Lechanteur, Anna ULiege; Sanna, Vincent; Duchemin, Amandine ULiege et al

in Nanomaterials (2018), 8(5),

Abstract: In recent year, cationic liposomes have gained a lot of attention for siRNA delivery. Despite this, intracellular barriers as endosomal escape and cytosolic delivery of siRNA still represent a ... [more ▼]

Abstract: In recent year, cationic liposomes have gained a lot of attention for siRNA delivery. Despite this, intracellular barriers as endosomal escape and cytosolic delivery of siRNA still represent a challeng, as well as the cytotoxicity due to cationic lipids. To address these issues, we developed four liposomal formulations, composed of two different cationic lipids (DOTAP and DC-Cholesterol) and different ratio of co-lipids (cholesterol and DOPE). The objective is to dissect these impacts on siRNA efficacy and cytotoxicity. Liposomes were complexed to siRNA at six different N/P molar ratios, physico-chemical properties were characterized, and consequently, N/P 2.5, 5 and 10 were selected for in vitro experiments. We have shown that cytotoxicity is influenced by the N/P ratio, the concentration of cationic lipid, as well as the nature of the cationic lipid. For instance, cell viability decreased by 70% with liposomes composed of DOTAP/Cholesterol/DOPE 1/0.75/0.5 at a N/P ratio 10, whereas the same formulation at a N/P ratio of 2.5 was safe. Interestingly, we have observed differences in terms of mRNA knock-down efficiency, whereas the transfection rate was quite similar for each formulation. Liposomes containing 50% of DOPE induced a mRNA silencing of around 80%. This study allowed us to highlight crucial parameters in order to develop lipoplexes which are safe, and which induce an efficient intracytoplasmic release of siRNA. [less ▲]

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See detailCationic Liposomes Carrying siRNA: Impact of Lipid Composition on Physicochemical Properties, Cytotoxicity and Endosomal Escape
Lechanteur, Anna ULiege; Sanna, Vincent; Duchemin, Amandine ULiege et al

in Cationic liposomes carrying siRNA: impact of lipid composition on physicochemical properties, cytotoxicity and endosomal escape (2018, April)

In recent year, cationic liposomes have gained attention for siRNA delivery using different local routes of administration as the vaginal [Lechanteur et al, Mol Pharm.2017] or the pulmonary routes ... [more ▼]

In recent year, cationic liposomes have gained attention for siRNA delivery using different local routes of administration as the vaginal [Lechanteur et al, Mol Pharm.2017] or the pulmonary routes. However, lipoplexes have to face several biological and intracellular barriers before releasing the genetic cargo. In this study, we focus our effort on intracellular barriers and more specifically on endosomal escape and cytosolic delivery of siRNA as well as on the cytotoxicity due to cationic lipids. Indeed, we have previously demonstrated that the surface charge of liposomes composed of the cationic lipid DOTAP is correlated to the induction of cytotoxicity [Lechanteur et al. EJPS.2016]. In the present study, we have investigated the impact of different cationic lipids and co-lipids on the cytotoxicity and also on the endosomal escape of siRNA by flow cytometry, qRT-PCR and Western Blot assays [Lechanteur et al. Nanomat.2018]. To address these issues, we developed four liposomal formulations composed of two different cationic lipids (DOTAP and DC-Cholesterol) and different ratio of co-lipids (cholesterol and DOPE). Formulations were DOTAP/Cholesterol/DOPE 1/0.75/0.5, DOTAP/Cholesterol/DOPE 1/0.5/0.5, DOTAP/DOPE 1/1 and DC-Cholesterol/DOPE 1/1. Each type of liposomes were complexed to siRNA at six different N/P molar ratios and physico-chemical properties were characterized in terms of Z-average size, Zeta potential and complexation efficiency. Consequently, three N/P ratios (2.5, 5 and 10) were selected for in vitro experiments on A549 cells. We studied the cell viability of cells with liposomes complexed to inactive siRNA at different N/P molar ratios at two siRNA concentrations. We have shown that the cytotoxicity is influenced by the N/P ratio, the concentration of cationic lipid as well as the nature of the cationic lipid. The cellular uptake were evaluated using the dye Trypan Blue® to quench the external fluorescence. Despite the fact the transfection rate were not significantly different, the mRNA knock-down efficiency were not similar between formulations. Liposomes containing 50% of DOPE induced a mRNA silencing of around 80% as well as the protein knock-down. This study allowed to highlight crucial parameters in order to develop lipoplexes which are safe and induce an efficient intracytoplasmic release of siRNA. [less ▲]

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See detailMucoadhesive nanostructured polyelectrolytes complexes modulate the intestinal permeability of methotrexate
Boni, Fernanda Isadora; Almeida, Andreia; Lechanteur, Anna ULiege et al

in European Journal of Pharmaceutical Sciences (2018), 111

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See detail3D Model Replicating the Intestinal Function to Evaluate Drug Permeability
Pereira, Ines; Lechanteur, Anna ULiege; Sarmento, Bruno

in Epithelial Cell Culture: Methods and Protocols (2018)

Animal models are essential in drug development but present many concerns in the practical and ethical sense. To avoid the unnecessary use of animals other models are used in the beginning of any ... [more ▼]

Animal models are essential in drug development but present many concerns in the practical and ethical sense. To avoid the unnecessary use of animals other models are used in the beginning of any scientific discovery, the in vitro models. The relevance of in vitro cell based culture models for studying intestinal drug absorption and transcytosis during early stages of drug development is undeniable. Several in vitro co-culture models have been described for this purpose, however excluding the integration of the complex intestinal architecture and neglecting different physiological mechanisms involved in the drug transport. 2-D cell cultures are the current standard, but despite their widely use, they no longer are considered the most trustworthy in vitro models since they do not mimic many aspects that happen in vivo. The simulation of a complete microenvironment capable of mimicking the intestinal mucosa requires therefore further investigation, particularly focused in addressing the abovementioned unmet needs. 3D models came as bridge between the in vitro and in vivo models. These models are proven to be influential of the drug effect in cells, being the most adequate to mimic the live tissue especially in drug development. Supported by the great amount of studies using simple and reductionist co-culture monolayers, and pushing forward an innovative model previously reported by our group, the present study aims to describe a sophisticated and highly reproducible in vitro 3D co-culture intestinal model. Here, the components are assembled in a multistage process into Transwell filters by co-culturing human colon carcinoma Caco-2 and mucusproducing HT29-MTX cells over a layer of collagen embedding intestinal myofibroblasts (CCD-18Co). The 3D co-culture intestinal model described herein represents a particularly powerful and versatile tool that recapitulates the intestinal functioning regarding mucus production, tightness of the different cell types, and the 3D architecture, bridging the gap between simple monolayer cultures of epithelial cells and the complex in vivo physiological conditions. Importantly, it shows tremendous potential in predicting intestinal absorption of orally administered drugs when delivered alone, or encapsulated into micro- and nanosystems, the current leading force of pharmaceutical technology research. [less ▲]

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See detailPromoting vaginal distribution of two active siRNA-complexed in liposomes for cervical cancer treatment
Lechanteur, Anna ULiege; Furst, Tania; Delvenne, Philippe ULiege et al

Conference (2017, December 07)

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See detailPromoting vaginal distribution of two active siRNA-complexed in liposomes for cervical cancer treatment
Lechanteur, Anna ULiege; Furst, Tania; Delvenne, Philippe ULiege et al

Conference (2017, December 05)

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See detailDevelopment and characterization of lipid-polymeric nanoparticles for oral insulin delivery
Sgorla, Débora; Lechanteur, Anna ULiege; Almeida, Andreia et al

in Expert Opinion on Drug Delivery (2017)

Introduction: The oral route is widely accepted as the most physiological path for exogenous administration of insulin, as it closely mimic the endogenous insulin pathway. Thus, in this work it is ... [more ▼]

Introduction: The oral route is widely accepted as the most physiological path for exogenous administration of insulin, as it closely mimic the endogenous insulin pathway. Thus, in this work it is proposed an innovative lipid-polymeric nanocarrier to delivery insulin orally. Areas covered: Nanoparticles were produced through a modified solvent emulsification-evaporation method, using ethyl palmitate and hydroxypropylmethylcellulose acetate succinate as matrix. Lipid-polymeric nanoparticles were around 300 nm in size, negatively charged (-20 mV) and associated insulin with efficiency higher than 80%. Differential scanning calorimetry suggested thermal stability of nanoparticles. In vitro release assays under simulated gastrointestinal conditions resulted in 9% and 14% of insulin released at pH 1.2 during 2 h and at pH 6.8 for 6 h, respectively, demonstrating the ability of those nanoparticles to protect insulin against premature degradation. Importantly, nanoparticles were observed to be safe at potential therapeutic concentrations as did not originate cytotoxicity to intestinal epithelial cells. Lastly, the permeability of nanoencapsulated insulin through Caco-2 monolayers and a triple Caco-2/HT29-MTX/Raji B cell model correlated well with slow release kinetics, and fosters the effectiveness of nanoparticles to promote intestinal absorption of peptidic drugs. Expert Opinion: Lipid-polymeric nanoparticles were developed to encapsulate and carry insulin through intestine. Overall, nanoparticles provide insulin stability and intestinal permeability. [less ▲]

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See detailThe role of mucus in cell-based models used to screen mucosal drug delivery
Lechanteur, Anna ULiege; das Neves, José; Sarmento, Bruno

in Advanced Drug Delivery Reviews (2017)

The increasing interest in developing tools to predict drug absorption through mucosal surfaces is fostering the establishment of epithelial cell-based models. Cell-based in vitro techniques for drug ... [more ▼]

The increasing interest in developing tools to predict drug absorption through mucosal surfaces is fostering the establishment of epithelial cell-based models. Cell-based in vitro techniques for drug permeability assessment are less laborious, cheaper and address the concerns of using laboratory animals. Simultaneously, in vitro barrier models that thoroughly simulate human epithelia or mucosae may provide useful data to speed up the entrance of new drugs and new drug products into the clinics. Nevertheless, standard cell-based in vitro models that intend to reproduce epithelial surfaces often discard the role of mucus in influencing drug permeation/absorption. Biomimetic models of mucosae in which mucus production has been considered may not be able to fully reproduce the amount and architecture of mucus, resulting in biased characterization of permeability/absorption. In these cases, artificial mucus may be used to supplement cell-based models but still proper identification and quantification are required. In this review, considerations regarding the relevance of mucus in the development of cell-based epithelial and mucosal models mimicking the gastro-intestinal tract, the cervico-vaginal tract and the respiratory tract, and the impact of mucus on the permeability mechanisms are addressed. From simple epithelial monolayers to more complexes 3D structures, the impact of the presence of mucus for the extrapolation to the in vivo scenario is critically analyzed. Finally, an overview is provided on several techniques and methods to characterize the mucus layer over cell-based barriers, in order to intimately reproduce human mucosal layer and thereby, improve in vitro/in vivo correlation. [less ▲]

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See detailElucidation of the impact of cell culture conditions of Caco-2 cell monolayer on barrier integrity and intestinal permeability
Lechanteur, Anna ULiege; Almeida, Andreia; Sarmento, Bruno

in European Journal of Pharmaceutics and Biopharmaceutics (2017)

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See detailPromoting vaginal distribution of two active siRNA-complexed in liposomes for cervical cancer treatment
Lechanteur, Anna ULiege; Furst Tania; Evrard, Brigitte ULiege et al

Conference (2017, April 25)

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