Nanoencapsulation des huiles des plantes extraites par CO2 supercritique pour des applications pharmaceutiques

The use of plants for medicinal purposes has been known since ancient times in different cultures. In recent years, efforts have been devoted to the use of herbal medicine as a form of alternative therapy to avoid the adverse effects related with conventional chemically synthesized drugs. Among the vastness of plant products, essential and vegetable oils deserve peculiar attention. The use of plant oils is always confronted by their susceptibility to degradation and their reduced bioavailability in the human body. Therefore, nanoencapsulation systems (nanocarriers) were designed to overcome the aforementioned physicochemical drawbacks. The objective of this study was the nanoencapsulation of costus roots essential oil (Saussurea lappa CB Clarke). and date palm seeds vegetable oil (Phoenix dactylifera L.) extracted by an innovative and an environmentally friendly technique (Supercritical fluid extraction) in polymeric nanoparticles and the investigation of their therapeutic performances. Three axes were addressed in this work. The first one dealt with the extraction of oils and their qualitative and quantitative analysis by Gas chromatography- mass spectrometry. The second one is addressed to the encapsulation of plant oils in poly (methyl methacrylate) derivative (Eudragit® RS100) based- polymeric nanoparticles using the nanoprecipitation technique after having been optimized and the characterization of the obtained nanocapsules. The last part focused on the study of the anti-inflammatory, anti-Alzheimer, anti-diabetic and antioxidant activities. The results of the oil analysis showed the predominance of oleic acid (47.7%) and dehydrocostus lactone (55.4%) for vegetable and essential oils, respectively. Eudragit RS®100 is able to successfully encapsulate both types of oils in nanocapsules in the nanoscale range (from 145 to 217nm) with zeta potential between +45 and + 59mV and excellent stability at different temperatures and pH. In addition, the date seeds oil-loaded nanoparticles showed superior anti-diabetic activity than the standard drug, moderate anti-Alzheimer's activity, and low antioxidant activity. While costus oil loaded nanoparticles exerted relevant anti-inflammatory, anti-diabetic and anti-Alzheimer's activities. Through this thesis, we have demonstrated the promising potential of polymeric nanoparticles to improve the biological performance of natural oils and found that the studied oils-loaded nanoparticles constitute interesting alternatives of synthetic drugs in the management of Alzheimer, diabetes and inflammatory diseases.Le recours aux plantes à des fins médicinales est connu depuis la nuit des temps dans différentes cultures. Au cours de ces dernières années, des efforts ont été consacrés à la pratique de la phytothérapie en tant que médecine alternative ou complémentaire dans le but d’éviter les effets indésirables liés aux médicaments d’origine synthétiques. Parmi la diversité des constituants de plante utilisés en phytothérapie, les huiles essentielles et végétales continuent à être utilisées en première intention. L’utilisation des huiles est souvent confrontée par leur dégradation et leur biodisponibilité réduite dans le corps humain. Par conséquent, des systèmes de la nanoencapsulation sont conçus pour surmonter les contraintes physicochimiques susmentionnés. L'objectif de cette étude est la nanoencapsulation de l’huile essentielle des racines du costus indien (Saussurea lappa CB. Clarke.) et l’huile végétale des noyaux de dattes (Phoenix dactylifera L.) extraites par un procédé innovant et respectueux de l'environnement (extraction par dioxyde de carbone supercritique) dans des nanoparticules polymères et l’étude de leurs performances thérapeutiques. Trois axes ont été abordés dans ce travail. Le premier a porté sur l'extraction des huiles ainsi que leur analyse qualitative et quantitative par chromatographie en phase gazeuse couplée à la spectrométrie de masse. Le deuxième a porté sur l'encapsulation des huiles dans des nanoparticules polymères à base de dérivés de poly (méthyl méthacrylate) (Eudragit® RS100) par la technique de la nanoprécipitation après avoir été optimisée et la caractérisation des nanocapsules obtenues. Le dernier axe a porté sur l’étude de l’activité anti-inflammatoire, anti-Alzheimer, antidiabétique et antioxydante. Les résultats de l’analyse des huiles ont montré la prédominance de l’acide oléique (47.7%) et du dehydrocostus lactone (55.4%) pour l’huile végétale et essentielle, respectivement. L’Eudragit RS®100 est capable d’encapsuler avec succès les deux types d’huiles dans des particules de taille comprise entre 145 et 217 nm avec un potentiel ζ de +45 à +59mV et une excellente stabilité à différentes températures et pH. De plus, les nanoparticules chargées d’huile des noyaux de dattes ont montré une activité antidiabétique supérieure à celle du médicament standard, une activité anti-Alzheimer modérée et une faible activité antioxydante. Celles chargées d’huile de costus ont révélé des activités anti-inflammatoire, antidiabétique et anti-Alzheimer pertinentes. A travers cette thèse, nous avons mis en évidence le potentiel prometteur des nanoparticules polymères à améliorer les performances biologiques des huiles naturelles et qu’elles constituent des alternatives intéressantes par rapport aux différents médicaments d'origine synthétique dans la prise en charge de la maladie d'Alzheimer, du diabète et des maladies inflammatoires

Nanoencapsulation of plant oils extracted by supercritical CO2 for pharmaceutical applications

Le recours aux plantes à des fins médicinales est connu depuis la nuit des temps dans différentes cultures. Au cours de ces dernières années, des efforts ont été consacrés à la pratique de la phytothérapie en tant que médecine alternative ou complémentaire dans le but d’éviter les effets indésirables liés aux médicaments d’origine synthétiques. Parmi la diversité des constituants de plante utilisés en phytothérapie, les huiles essentielles et végétales continuent à être utilisées en première intention. L’utilisation des huiles est souvent confrontée par leur dégradation et leur biodisponibilité réduite dans le corps humain. Par conséquent, des systèmes de la nanoencapsulation sont conçus pour surmonter les contraintes physicochimiques susmentionnés. L'objectif de cette étude est la nanoencapsulation de l’huile essentielle des racines du costus indien (Saussurea lappa CB. Clarke.) et l’huile végétale des noyaux de dattes (Phoenix dactylifera L.) extraites par un procédé innovant et respectueux de l'environnement (extraction par dioxyde de carbone supercritique) dans des nanoparticules polymères et l’étude de leurs performances thérapeutiques. Trois axes ont été abordés dans ce travail. Le premier a porté sur l'extraction des huiles ainsi que leur analyse qualitative et quantitative par chromatographie en phase gazeuse couplée à la spectrométrie de masse. Le deuxième a porté sur l'encapsulation des huiles dans des nanoparticules polymères à base de dérivés de poly (méthyl méthacrylate) (Eudragit® RS100) par la technique de la nanoprécipitation après avoir été optimisée et la caractérisation des nanocapsules obtenues. Le dernier axe a porté sur l’étude de l’activité anti-inflammatoire, anti-Alzheimer, antidiabétique et antioxydante. Les résultats de l’analyse des huiles ont montré la prédominance de l’acide oléique (47.7%) et du dehydrocostus lactone (55.4%) pour l’huile végétale et essentielle, respectivement. L’Eudragit RS®100 est capable d’encapsuler avec succès les deux types d’huiles dans des particules de taille comprise entre 145 et 217 nm avec un potentiel ζ de +45 à +59mV et une excellente stabilité à différentes températures et pH. De plus, les nanoparticules chargées d’huile des noyaux de dattes ont montré une activité antidiabétique supérieure à celle du médicament standard, une activité anti-Alzheimer modérée et une faible activité antioxydante. Celles chargées d’huile de costus ont révélé des activités anti-inflammatoire, antidiabétique et anti-Alzheimer pertinentes. A travers cette thèse, nous avons mis en évidence le potentiel prometteur des nanoparticules polymères à améliorer les performances biologiques des huiles naturelles et qu’elles constituent des alternatives intéressantes par rapport aux différents médicaments d'origine synthétique dans la prise en charge de la maladie d'Alzheimer, du diabète et des maladies inflammatoires.The use of plants for medicinal purposes has been known since ancient times in different cultures. In recent years, efforts have been devoted to the use of herbal medicine as a form of alternative therapy to avoid the adverse effects related with conventional chemically synthesized drugs. Among the vastness of plant products, essential and vegetable oils deserve peculiar attention. The use of plant oils is always confronted by their susceptibility to degradation and their reduced bioavailability in the human body. Therefore, nanoencapsulation systems (nanocarriers) were designed to overcome the aforementioned physicochemical drawbacks. The objective of this study was the nanoencapsulation of costus roots essential oil (Saussurea lappa CB Clarke). and date palm seeds vegetable oil (Phoenix dactylifera L.) extracted by an innovative and an environmentally friendly technique (Supercritical fluid extraction) in polymeric nanoparticles and the investigation of their therapeutic performances. Three axes were addressed in this work. The first one dealt with the extraction of oils and their qualitative and quantitative analysis by Gas chromatography- mass spectrometry. The second one is addressed to the encapsulation of plant oils in poly (methyl methacrylate) derivative (Eudragit® RS100) based- polymeric nanoparticles using the nanoprecipitation technique after having been optimized and the characterization of the obtained nanocapsules. The last part focused on the study of the anti-inflammatory, anti-Alzheimer, anti-diabetic and antioxidant activities. The results of the oil analysis showed the predominance of oleic acid (47.7%) and dehydrocostus lactone (55.4%) for vegetable and essential oils, respectively. Eudragit RS®100 is able to successfully encapsulate both types of oils in nanocapsules in the nanoscale range (from 145 to 217nm) with zeta potential between +45 and + 59mV and excellent stability at different temperatures and pH. In addition, the date seeds oil-loaded nanoparticles showed superior anti-diabetic activity than the standard drug, moderate anti-Alzheimer's activity, and low antioxidant activity. While costus oil loaded nanoparticles exerted relevant anti-inflammatory, anti-diabetic and anti-Alzheimer's activities. Through this thesis, we have demonstrated the promising potential of polymeric nanoparticles to improve the biological performance of natural oils and found that the studied oils-loaded nanoparticles constitute interesting alternatives of synthetic drugs in the management of Alzheimer, diabetes and inflammatory diseases

Encapsulation of Essential Oils via Nanoprecipitation Process: Overview, Progress, Challenges and Prospects

Essential oils are of paramount importance in pharmaceutical, cosmetic, agricultural, and food areas thanks to their crucial properties. However, stability and bioactivity determine the effectiveness of essential oils. Polymeric nanoencapsulation is a well-established approach for the preservation of essential oils. It offers a plethora of benefits, including improved water solubility, effective protection against degradation, prevention of volatile components evaporation and controlled and targeted release. Among the several techniques used for the design of polymeric nanoparticles, nanoprecipitation has attracted great attention. This review focuses on the most outstanding contributions of nanotechnology in essential oils encapsulation via nanoprecipitation method. We emphasize the chemical composition of essential oils, the principle of polymeric nanoparticle preparation, the physicochemical properties of essential oils loaded nanoparticles and their current applications

Plant oils: From chemical composition to encapsulated form use

International audienceThe last decade has witnessed a burgeoning global movement towards essential and vegetable oils in the food, agriculture, pharmaceutical, cosmetic, and textile industries thanks to their natural and safe status, broad acceptance by consumers, and versatile functional properties. However, efforts to develop new therapy or functional agents based on plant oils have met with challenges of limited stability and/or reduced efficacy. As a result, there has been increased research interest in the encapsulation of plant oils, whereby the nanocarriers serve as barrier between plant oils and the environment and control oil release leading to improved efficacy, reduced toxicity and enhanced patient compliance and convenience. In this review, special concern has been addressed to the encapsulation of essential and vegetable oils in three types of nanocarriers: polymeric nanoparticles, liposomes and solid lipid nanoparticles. First, the chemical composition of essential and vegetable oils was handled. Moreover, we gather together the research findings reported by the literature regarding the different techniques used to generate these nanocarriers with their significant findings. Finally, differences and similarities between these nanocarriers are discussed, along with current and future applications that are warranted by their structures and properties

Carbamazepine solubility enhancement in tandem with swellable polymer osmotic pump tablet: A promising approach for extended delivery of poorly water-soluble drugs

Elementary osmotic pump (EOP) is a unique extended release (ER) drug delivery system based on the principle of osmosis. It has the ability to minimize the amount of the drug, accumulation and fluctuation in drug level during chronic uses. Carbamazepine (CBZ), a poorly water-soluble antiepileptic drug, has serious side effects on overdoses and chronic uses. The aim of the present study was to design a new EOP tablet of CBZ containing a solubility enhancers and swellable polymer to reduce its side effects and enhance the patient compliance. Firstly, a combination of solubilizing carriers was selected to improve the dissolution of the slightly soluble drug. Then, designing the new EOP tablet and investigating the effect of different variables of core and coat formulations on drug release behavior by single parameter optimization and by Taguchi orthogonal design with analysis of variance (ANOVA), respectively. The results showed that CBZ solubility was successfully enhanced by a minimum amount of combined polyvinyl pyrrolidone (PVP K30) and sodium lauryl sulfate (SLS). The plasticizer amount and molecular weight (MW) together with the osmotic agent amount directly affect the release rate whereas the swellable polymer amount and viscosity together with the semi-permeable membrane (SPM) thickness inversely influence the release rate. In addition, the tendency of following zero order kinetics was mainly affected by the coat components rather than those of the core. Further, orifice size does not have any significant effect on the release behavior within the range of 0.1 mm to 0.8 mm. In this study we report the successful formulation of CBZ-EOP tablets, which were similar to the marketed product Tegretol CR 200 and able to satisfy the USP criterion limits and to deliver about 80% of CBZ at a rate of approximately zero order for up to 12 h

Nanonutraceuticals: The New Frontier of Supplementary Food

In the last few decades, the combination between nanotechnology and nutraceutics has gained the attention of several research groups. Nutraceuticals are considered as active compounds, abundant in natural products, showing beneficial effects on human health. Unfortunately, the uses, and consequently the health benefits, of many nutraceutical products are limited by their unsuitable chemico-physical features. For example, many nutraceuticals are characterized by low water solubility, low stability and high susceptibility to light and oxygen, poor absorption and potential chemical modifications after their administration. Based on the potential efficacy of nutraceuticals and on their limiting features, nanotechnology could be considered a revolutionary innovation in empowering the beneficial properties of nutraceuticals on human health, thus enhancing their efficacy in several diseases. For this reason, nanotechnology could represent a new frontier in supplementary food. In this review, the most recent nanotechnological approaches are discussed, focusing on their ability to improve the bioavailability of the most common nutraceuticals, providing an overview regarding both the advantages and the possible limitations of the use of several nanodelivery systems. In fact, although the efficacy of smart nanocarriers in improving health benefits deriving from nutraceuticals has been widely demonstrated, the conflicting opinions on the mechanism of action of some nanosystems still reduce their applicability in the therapeutic field

Nanocapsules containing Saussurea lappa essential oil: Formulation, characterization, antidiabetic, anti-cholinesterase and anti-inflammatory potentials

International audiencePlant-based remedies have been widely used for the management of variable diseases due to their safety and less side effects. In the present study, we investigated Saussurea lappa CB. Clarke. (SL) given its largely reported medicinal effects. Specifically, our objective was to provide an insight into a new polymethyl methacrylate based nanocapsules as carriers of SL essential oil and characterize their biologic functions. The nanoparticles were prepared by nanoprecipitation technique, characterized and analyzed for their cytotoxicity, anti-inflammatory, anti-Alzheimer and antidiabetic effects. The results revealed that the developed nanoparticles had a diameter around 145 nm, a polydispersity index of 0.18 and a zeta potential equal to +45 mV and they did not show any cytotoxicity at 25 μg·mL−1. The results also showed an anti-inflammatory activity (reduction in metalloprotease MMP-9 enzyme activity and RNA expression of inflammatory cytokines: TNF-α, GM-CSF and IL1β), a high anti-Alzheimer’s effect (IC50 around 25.0 and 14.9 μg·mL−1 against acetylcholinesterase and butyrylcholinesterase, respectively), and a strong antidiabetic effect (IC50 were equal to 22.9 and 75.8 μg·mL−1 against α-amylase and α-glucosidase, respectively). Further studies are required including the in vivo studies (e.g., preclinical), the pharmacokinetic properties, the bioavailability and the underlying associated metabolic pathways