Topical co-delivery of indomethacin and nigella sativa L. essential oil in poly-cappa-caprolactone nanoparticles: in vitro study of anti-inflammatory activity

Indomethacin is a potent, nonselective Non-steroidal Antiinflammatory Drug (NSAID) but its low water-solubility precludes its use as topical dosage form. As with other NSAIDs, the systemic delivery is associated with high risk of serious gastrointestinal adverse events including bleeding, ulceration and perforation of stomach and intestines. Here we demonstrate a safer way of administration i.e via topical demonstrating synergistic effects when co-delivered with Nigella sativa L. seeds essential oil (NSSEO) in the form of coencapsulated particles (~200 nm) of poly--caprolactone. The particles showed penetrability across stratum corneum to dermis layer in ex-vivo human skin. Further study in the xyline-induced ear edema in mice was performed, and co-encapsulated particles demonstrated highest antiinflammatory effect compared to indomethacin particles and indomethacin gels. Despite slower onset compared to indomethacin gels, the inflamed ear continued to show reduction in thickness over 8 hours of observation demonstrating synergistic and pro-longed effect contributed by NSSEO. In immunohistochemistry study of CD45+, the mice ears treated with co-encapsulated particles showed considerable reduction in lesions, epidermal-dermal separation and inflammatory cells (lymphocytes and neutrophils) infiltration as compared to other formulation. Based on microscopic evaluation, the anti-inflammatory inhibition effect of co-encapsulated particles is the highest (90%) followed by indomethacin particles (79%) and indomethacin gel (49%). The findings suggest not only skin permeability of indomethacin significantly improved but also the therapeutic effects, all provided by the presence of NSSEO in the particles. This study paves the way to more co-encapsulation of any other contemporary medicines in combination with this wholesome natural oil, NSSEO

Préparation de nanoparticules à base de polymère pour applications anti-inflammatoires topiques

The objective of this PhD thesis was to extract the Nigella Sativa L. Seeds Essential Oil and its encapsulation together with indomethacin within polymeric nanoparticles in order to reduce taken amount and to enhance indomethacin cutaneous penetration, and anti-inflammatory activity. To this direction poly-epsilon-caprolactone based nanoparticles were designed using nanoprecipitation method. A systematic study was performed to figure out the effect of process and formulation parameters on the characteristics of obtained nanoparticles. Once the effects of all parameters were studied, then indomethacin and Nigella Sativa L. Seeds Essential Oil was encapsulated separately. Consequently, both together indomethacin and Nigella Sativa L. Seeds Essential Oil was encapsulated. Then prepared nanoparticles were characterized in terms of stability, encapsulation efficiency. In addition, ex vivo skin penetration and in vivo anti-inflammatory activity of designed nanoparticles was investigatedL'objectif de cette thèse est d’encapsuler l'indométacine dans des nanoparticules polymériques en association à l’huile essentielle de Nigella Sativa L. extraite à partir de ses graines afin d’optimiser son utilisation par voie cutanée et potentialiser son activité anti-inflammatoire.Pour ce faire, des nanoparticules à base de poly-epsilon-caprolactone ont été préparées par nanoprécipitation. Une étude systématique a été menée pour comprendre l'effet de la variation des paramètres de préparation sur les propriétés colloïdales des nanoparticules obtenues. Une fois les différents paramètres optimisés, l'indométacine et l'huile essentielle de Nigella Sativa L. ont été encapsulées séparément dans les nanoparticules polymériques. Puis, l’ensemble, indométacine et huile essentielle de Nigella Sativa L. a été encapsulé. Les nanoparticules préparées ont à chaque fois été caractérisées notamment en termes de stabilité et de performance d’encapsulation. Ensuite, nous avons mené une étude ex vivo et in vivo des nanoparticules obtenues afin d’évaluer le potentiel de pénétration cutanée d’une part, et le potentiel clinique dans la prise en charge de l’inflammatio

Biodegradable Polymer Based Nanoparticles: Dermal and Transdermal Drug Delivery

International audienc

Elaboration of Nanoparticles Containing Indomethacin: Argan Oil for Transdermal Local and Cosmetic Application

International audienc

Effect of process and formulation parameters on polycaprolactone nanoparticles prepared by solvent displacement

International audienc

Natural Products as Source of Molecules with Therapeutic Potential

International audienc

Encapsulation of NSAIDs for inflammation management: Overview, progress, challenges and prospects

International audienc

Nanoencapsulation of Essential Oils as Natural Food Antimicrobial Agents: An Overview

International audienceThe global demand for safe and healthy food with minimal synthetic preservatives is continuously increasing. Natural food antimicrobials and especially essential oils (EOs) possess strong antimicrobial activities that could play a remarkable role as a novel source of food preservatives. Despite the excellent efficacy of EOs, they have not been widely used in the food industry due to some major intrinsic barriers, such as low water solubility, bioavailability, volatility, and stability in food systems. Recent advances in nanotechnology have the potential to address these existing barriers in order to use EOs as preservatives in food systems at low doses. Thus, in this review, we explored the latest advances of using natural actives as antimicrobial agents and the different strategies for nanoencapsulation used for this purpose. The state of the art concerning the antibacterial properties of EOs will be summarized, and the main latest applications of nanoencapsulated antimicrobial agents in food systems will be presented. This review should help researchers to better choose the most suitable encapsulation techniques and materials

Plant extracts: from encapsulation to application

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Polycaprolactone Based Nanoparticles Loaded with Indomethacin for Anti-Inflammatory Therapy: From Preparation to Ex Vivo Study

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