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Article ; Online: Silicones in dermatological topical drug formulation: Overview and advances.

Sounouvou, Hope T / Lechanteur, Anna / Piel, Géraldine / Evrard, Brigitte

2022 Volume 625, Page(s) 122111

Abstract: Silicones, more specifically those of the polydimethylsiloxane type, have been widely used in the pharmaceutical industry for decades, particularly in topical applications. In the dermatological field, in addition to provide undeniable textural and ... ...

Abstract	Silicones, more specifically those of the polydimethylsiloxane type, have been widely used in the pharmaceutical industry for decades, particularly in topical applications. In the dermatological field, in addition to provide undeniable textural and sensory benefits, they can play important functions in the physicochemical properties, stability and biopharmaceutical behavior of these formulations. However, despite the notable advances that can be attributed to the family of silicones, the reputation of these compounds is quite bad. Indeed, silicones, even if they derive from sand, are synthetic compounds. Moreover, they are not biodegradable. They flow into our wastewater and oceans, accumulating in the fauna and flora. This obviously raises many concerns in the common imagination. Do silicones represent a danger for our environment? Should the human species worry about long term toxic effects? Are the claimed benefits really that important? After exploring the various applications of silicone excipients in topical dermatological formulations with a special focus on recent advances which open breathtaking prospects for dermatological applications, this paper shed light on the specific challenges involved in preparation of silicone-based drug as well as, the in vivo behavior of these polymers, the toxicological and environmental risks associated with their application.
MeSH term(s)	Chemistry, Pharmaceutical ; Drug Carriers/chemistry ; Drug Compounding ; Excipients/chemistry ; Humans ; Silicones/chemistry
Chemical Substances	Drug Carriers ; Excipients ; Silicones
Language	English
Publishing date	2022-08-13
Publishing country	Netherlands
Document type	Journal Article ; Review
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2022.122111
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Article ; Online: Innovative lipoplexes formulations with enhanced siRNA efficacy for cancer treatment: Where are we now?

Berger, Manon / Lechanteur, Anna / Evrard, Brigitte / Piel, Géraldine

International journal of pharmaceutics

2021 Volume 605, Page(s) 120851

Abstract: Over the past two decades, RNA interference has become an extensively studied mechanism to silence gene and treat diseases including cancer. siRNA appears as a promising strategy that could avoid some side effects related to traditional chemotherapy. ... ...

Abstract	Over the past two decades, RNA interference has become an extensively studied mechanism to silence gene and treat diseases including cancer. siRNA appears as a promising strategy that could avoid some side effects related to traditional chemotherapy. Considering the weak stability of naked siRNA in blood, vectors like cationic liposomes or Lipid Nanoparticles (LNPs) are widely used to carry and protect siRNA until it reaches the tumor targeted. Despite extensive research, only three RNAi drugs are currently approved by the Food and Drug Administration, including only one LNP formulation of siRNA to treat hereditary ATTR amyloidosis. This shows the difficulty of lipoplexes clinical translation, in particular in cancer therapy. To overcome the lipoplexes limitations, searches are made on innovative lipoplexes formulations with enhanced siRNA efficacy. The present review is focusing on the recent use of pH-sensitive lipids, peptides and cell-penetrating peptides or polymers. The incorporation of some of these components in the lipoplex formulation induces a fusogenic property or an enhanced endosomal escape, an enhanced cellular uptake, an enhanced tumor targeting, an improved stability in the blood stream …These innovations appear critical to obtain an efficient siRNA accumulation in tumor cells with effective antitumor effect considering the complex tumor environment.
MeSH term(s)	Humans ; Lipids ; Liposomes ; Nanoparticles ; Neoplasms/drug therapy ; RNA Interference ; RNA, Small Interfering
Chemical Substances	Lipids ; Liposomes ; RNA, Small Interfering
Language	English
Publishing date	2021-07-01
Publishing country	Netherlands
Document type	Journal Article ; Review
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2021.120851
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Article ; Online: Use of liposome-encapsulated estetrol for treatment of neonatal hypoxic-ischemic encephalopathy.

Tskitishvili, Ekaterine / Palazzo, Claudio / Foidart, Jean-Michel / Piel, Géraldine / Pequeux, Christel

Brain research

2023 Volume 1809, Page(s) 148369

Abstract: Estetrol (E4) is a natural estrogen synthesized only during pregnancy. It has strong neuroprotective and antioxidative activities. The aim of the present study was to define the neuroprotective potency of E4 encapsulated either in liposome (Lipo-E4) or ... ...

Abstract	Estetrol (E4) is a natural estrogen synthesized only during pregnancy. It has strong neuroprotective and antioxidative activities. The aim of the present study was to define the neuroprotective potency of E4 encapsulated either in liposome (Lipo-E4) or in drug-in cyclodextrin (HP-β-CD) in liposome (DCL) system, and compare them with a single use of E4. In vitro studies were performed in an oxidative stress model of primary hippocampal neuronal cell cultures, followed by the lactate dehydrogenase activity and cell proliferation assays. In vivo studies were conducted by using a model of neonatal hypoxic-ischemic encephalopathy in immature rat pups. Brain samples were studied by (immuno)histochemistry for the detection of survived cells, expression of microtubule-associated protein-2, myelin basic protein, doublecortin and vascular-endothelial growth factor. Concentrations of glial fibrillary acidic protein in blood serum were studied by ELISA. In vitro, cell proliferation was significantly up-regulated in cultures treated either by DCL-E4 or E4 compared to the control cells, whereas DCL-E4 treated cells had significantly higher survival rate than the cells treated by E4 alone. Evaluation of brain samples showed that DCL-E4 and a high dose of E4 alone significantly preserve the grey and the white matter loses, and diminish GFAP expression in blood. Although DCL-E4 and E4 have similar effect on neurogenesis in the hippocampus and the cortex, DCL-E4 treatment significantly up-regulates angiogenesis in the hippocampus compared to a single use of E4. Present work reveals for the first time that liposome-encapsulated E4 might be a better alternative to a single use of E4.
MeSH term(s)	Rats ; Animals ; Estetrol/metabolism ; Estetrol/pharmacology ; Estetrol/therapeutic use ; Liposomes/metabolism ; Liposomes/pharmacology ; Hypoxia-Ischemia, Brain/drug therapy ; Hypoxia-Ischemia, Brain/metabolism ; Estrogens/metabolism ; Neurons/metabolism
Chemical Substances	Estetrol (ENB39R14VF) ; Liposomes ; Estrogens
Language	English
Publishing date	2023-04-13
Publishing country	Netherlands
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1200-2
ISSN	1872-6240 ; 0006-8993
ISSN (online)	1872-6240
ISSN	0006-8993
DOI	10.1016/j.brainres.2023.148369
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Article ; Online: A supercritical fluid technology for liposome production and comparison with the film hydration method.

Penoy, Noémie / Grignard, Bruno / Evrard, Brigitte / Piel, Géraldine

International journal of pharmaceutics

2020 Volume 592, Page(s) 120093

Abstract: Liposomes were produced by an innovative method using supercritical carbon dioxide as a dispersing agent. A quality by design strategy was used to find optimal production conditions with specific parameters (lipid concentration, dispersion volume, ... ...

Abstract	Liposomes were produced by an innovative method using supercritical carbon dioxide as a dispersing agent. A quality by design strategy was used to find optimal production conditions with specific parameters (lipid concentration, dispersion volume, agitation rate, temperature and pressure) allowing the production of liposomes with predicted physicochemical characteristics (particles size and PdI). Two conditions were determined with specific production parameters. It was shown that these two conditions allowed the production of liposomes of different compositions and that most of the liposome formulations had size and dispersity in accordance with the prediction values. The condition involving the higher lipid concentration showed a higher variability in terms of size and dispersity. However, this variability remained acceptable. This innovative supercritical method allowed the production of liposomes with physicochemical characteristics similar to those obtained by the conventional thin film hydration method. This new supercritical carbon dioxide method easily scalable in GMP conditions is a one-step production method contrarily to conventional methods which generally need an additional step as extrusion to homogenize the size of liposomes.
MeSH term(s)	Carbon Dioxide ; Drug Compounding ; Liposomes ; Particle Size ; Technology
Chemical Substances	Liposomes ; Carbon Dioxide (142M471B3J)
Language	English
Publishing date	2020-11-16
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2020.120093
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Article ; Online: Therapeutic peptides for chemotherapy: Trends and challenges for advanced delivery systems.

Ilangala, Ange B / Lechanteur, Anna / Fillet, Marianne / Piel, Géraldine

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

2021 Volume 167, Page(s) 140–158

Abstract: The past decades witnessed an increasing interest in peptides as clinical therapeutics. Rightfully considered as a potential alternative for small molecule therapy, these remarkable pharmaceuticals can be structurally fine-tuned to impact properties such ...

Abstract	The past decades witnessed an increasing interest in peptides as clinical therapeutics. Rightfully considered as a potential alternative for small molecule therapy, these remarkable pharmaceuticals can be structurally fine-tuned to impact properties such as high target affinity, selectivity, low immunogenicity along with satisfactory tissue penetration. Although physicochemical and pharmacokinetic challenges have mitigated, to some extent, the clinical applications of therapeutic peptides, their potential impact on modern healthcare remains encouraging. According to recent reports, there are more than 400 peptides under clinical trials and 60 were already approved for clinical use. As the demand for efficient and safer therapy became high, especially for cancers, peptides have shown some exciting developments not only due to their potent antiproliferative action but also when used as adjuvant therapies, either to decrease side effects with tumor-targeted therapy or to enhance the activity of anticancer drugs via transbarrier delivery. The first part of the present review gives an insight into challenges related to peptide product development. Both molecular and formulation approaches intended to optimize peptide's pharmaceutical properties are covered, and some of their current issues are highlighted. The second part offers a comprehensive overview of the emerging applications of therapeutic peptides in chemotherapy from bioconjugates to nanovectorized therapeutics.
MeSH term(s)	Animals ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Drug Delivery Systems ; Humans ; Nanoparticles ; Neoplasms/drug therapy ; Peptides/administration & dosage ; Peptides/chemistry ; Peptides/pharmacology
Chemical Substances	Antineoplastic Agents ; Peptides
Language	English
Publishing date	2021-07-24
Publishing country	Netherlands
Document type	Journal Article ; Review
ZDB-ID	1065368-5
ISSN	1873-3441 ; 0939-6411
ISSN (online)	1873-3441
ISSN	0939-6411
DOI	10.1016/j.ejpb.2021.07.010
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Article ; Online: An innovative one step green supercritical CO

Penoy, Noémie / Delma, Kouka Luc / Tonakpon, Hermane Avohou / Grignard, Bruno / Evrard, Brigitte / Piel, Géraldine

International journal of pharmaceutics

2022 Volume 627, Page(s) 122212

Abstract: Budesonide and salbutamol-loaded liposomes were prepared using an innovative one step supercritical ... ...

Abstract	Budesonide and salbutamol-loaded liposomes were prepared using an innovative one step supercritical CO
MeSH term(s)	Liposomes/chemistry ; Carbon Dioxide/chemistry ; Trehalose ; Budesonide ; Albuterol ; Phosphatidylcholines ; Cholesterol ; Solvents ; Polyethylene Glycols ; Particle Size
Chemical Substances	Liposomes ; Carbon Dioxide (142M471B3J) ; Trehalose (B8WCK70T7I) ; Budesonide (51333-22-3) ; Albuterol (QF8SVZ843E) ; Phosphatidylcholines ; Cholesterol (97C5T2UQ7J) ; Solvents ; Polyethylene Glycols (3WJQ0SDW1A)
Language	English
Publishing date	2022-09-21
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2022.122212
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Article: Effect of PEG Anchor and Serum on Lipid Nanoparticles: Development of a Nanoparticles Tracking Method.

Berger, Manon / Degey, Manon / Leblond Chain, Jeanne / Maquoi, Erik / Evrard, Brigitte / Lechanteur, Anna / Piel, Géraldine

Pharmaceutics

2023 Volume 15, Issue 2

Abstract: Polyethylene glycol (PEG) is used in Lipid Nanoparticles (LNPs) formulations to confer stealth properties and is traditionally anchored in membranes by a lipid moiety whose length significantly impacts the LNPs fate in vivo. C18 acyl chains are ... ...

Abstract	Polyethylene glycol (PEG) is used in Lipid Nanoparticles (LNPs) formulations to confer stealth properties and is traditionally anchored in membranes by a lipid moiety whose length significantly impacts the LNPs fate in vivo. C18 acyl chains are efficiently anchored in the membrane, while shorter C14 lipids are quickly desorbed and replaced by a protein corona responsible for the completely different fate of LNPs. In this context, a method to predict the biological behavior of LNPs depending on the lipid-PEG dissociation was developed using the Nanoparticle Tracking Analysis (NTA) method in serum. Two formulations of siRNA-containing LNPs were prepared including CSL3 or SM-102 lipids and were grafted with different lipids-PEG (C18, C14 lipids-PEG, and Ceramide-PEG). The impact of the lipid-PEG on the interactions between LNPs and serum components was demonstrated by monitoring the mean particle size and the concentration over time. In vitro, these formulations demonstrated low toxicity and efficient gene knockdown on tumor MDA-MB-231 cells, but serum was found to significantly impact the efficiency of C18-PEG-based LNPs, while it did not impact the efficiency of C14-PEG-based LNPs. The NTA method demonstrated the ability to discriminate between the behaviors of LNPs according to serum proteins' interactions. CSL3 lipid and Cer-PEG were confirmed to have promise for LNP formulation.
Language	English
Publishing date	2023-02-10
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics15020597
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Article ; Online: Lipid gene nanocarriers for the treatment of skin diseases: Current state-of-the-art.

Bellefroid, Coralie / Lechanteur, Anna / Evrard, Brigitte / Piel, Géraldine

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

2019 Volume 137, Page(s) 95–111

Abstract: Nucleic acids carried by non-viral nanovectors have demonstrated high potential as a therapeutic strategy for gene-related diseases. The dermal or transdermal gene delivery allow to target local skin diseases or to reach the blood stream. However, the ... ...

Abstract	Nucleic acids carried by non-viral nanovectors have demonstrated high potential as a therapeutic strategy for gene-related diseases. The dermal or transdermal gene delivery allow to target local skin diseases or to reach the blood stream. However, the skin is the first defense barrier of the body and must be overcome to distribute nucleic acids. Many intracellular barriers as cellular uptake, endosomal escape or cytosolic gene trafficking have to be crossed for the gene to achieve its therapeutic action. All hurdles to skin nucleic acid therapy are precisely described. Physical, active or passive methods have been proposed to improve the penetration through the stratum corneum. Lipidic-nanocarriers represent one of the most attractive methods because any skin disruption technique is requested. We give an overview of deformable lipidic-nanocarriers that have been developed to promote the skin penetration of nucleic acids. Moreover, this review describes the potential of deformable liposomes for cutaneous disorders.
MeSH term(s)	Animals ; Gene Transfer Techniques ; Genetic Therapy/methods ; Humans ; Lipids/chemistry ; Liposomes ; Nucleic Acids/administration & dosage ; Nucleic Acids/metabolism ; Skin/metabolism ; Skin Absorption ; Skin Diseases/therapy
Chemical Substances	Lipids ; Liposomes ; Nucleic Acids
Language	English
Publishing date	2019-02-19
Publishing country	Netherlands
Document type	Journal Article ; Review
ZDB-ID	1065368-5
ISSN	1873-3441 ; 0939-6411
ISSN (online)	1873-3441
ISSN	0939-6411
DOI	10.1016/j.ejpb.2019.02.012
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Article ; Online: Assessment 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 / Evrard, Brigitte / Piel, Géraldine

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

2019 Volume 144, Page(s) 2–10

MeSH term(s)	Bronchi/cytology ; Bronchi/drug effects ; Cell Culture Techniques/methods ; Cell Line ; Drug Evaluation, Preclinical/methods ; Epithelial Cells ; Feasibility Studies ; Fibroblasts ; Humans ; Reproducibility of Results ; Respiratory Mucosa/cytology ; Respiratory Mucosa/drug effects ; Respiratory System Agents/pharmacology ; Time Factors
Chemical Substances	Respiratory System Agents
Language	English
Publishing date	2019-09-04
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	1065368-5
ISSN	1873-3441 ; 0939-6411
ISSN (online)	1873-3441
ISSN	0939-6411
DOI	10.1016/j.ejpb.2019.09.001
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Article ; Online: Development and optimization of a one step process for the production and sterilization of liposomes using supercritical CO

Penoy, Noémie / Delma, Kouka Luc / Homkar, Nirmayi / Karim Sakira, Abdoul / Egrek, Sabrina / Sacheli, Rosalie / Sacré, Pierre-Yves / Grignard, Bruno / Hayette, Marie-Pierre / Somé, Touridomon Issa / Semdé, Rasmané / Evrard, Brigitte / Piel, Géraldine

International journal of pharmaceutics

2024 Volume 651, Page(s) 123769

Abstract: Liposomes are very interesting drug delivery systems for pharmaceutical and therapeutic purposes. However, liposome sterilization as well as their industrial manufacturing remain challenging. Supercritical carbon dioxide is an innovative technology that ... ...

Abstract	Liposomes are very interesting drug delivery systems for pharmaceutical and therapeutic purposes. However, liposome sterilization as well as their industrial manufacturing remain challenging. Supercritical carbon dioxide is an innovative technology that can potentially overcome these limitations. The aim of this study was to optimize a one-step process for producing and sterilizing liposomes using supercritical CO
MeSH term(s)	Humans ; Liposomes/chemistry ; Carbon Dioxide/chemistry ; Drug Delivery Systems ; Sterilization ; Infertility
Chemical Substances	Liposomes ; Carbon Dioxide (142M471B3J)
Language	English
Publishing date	2024-01-04
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2024.123769
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