Nanoparticles of amphiphilic α-, β-, and γ-cyclodextrins were obtained by formulation of cyclodextrins enzymatically transesterified with vinyl decanoate. The product of this synthesis is a mixture of bioesterified cyclodextrins with various degrees of substitution (DS) presenting for a same DS different regio-isomers. In a first step, the efficiency of a MALDI-TOF procedure to characterize the average molecular weight of the derivative bulk mixture was demonstrated by comparing the results with those obtained from complementary NMR and HPLC techniques. In a second step, the ultrastructure of nanoparticles prepared from three different batches of synthesis was investigated and correlated with the average molecular weight and DS of the parent derivative.
Ocular inflammation is one of the most common symptom of eye disorders and diseases. The therapeutic management of this inflammation must be rapid and effective in order to avoid deleterious effects for the eye and the vision. Steroidal (SAID) and non-steroidal (NSAID) anti-inflammatory drugs and immunosuppressive agents have been shown to be effective in treating inflammation of the ocular surface of the eye by topical administration. However, it is well established that the anatomical and physiological ocular barriers are limiting factors for drug penetration. In addition, such drugs are generally characterized by a very low aqueous solubility, resulting in low bioavailability as only 1% to 5% of the applied drug permeates the cornea. The present review gives an updated insight on the conventional formulations used in the treatment of ocular inflammation, i.e., ointments, eye drops, solutions, suspensions, gels, and emulsions, based on the commercial products available on the US, European, and French markets. Additionally, sophisticated formulations and innovative ocular drug delivery systems will be discussed. Promising results are presented with micro- and nanoparticulated systems, or combined strategies with polymers and colloidal systems, which offer a synergy in bioavailability and sustained release. Finally, different tools allowing the physical characterization of all these delivery systems, as well as in vitro, ex vivo, and in vivo evaluations, will be considered with regards to the safety, the tolerance, and the efficiency of the drug products.
Nowadays, colloidal drug carriers represent an alternative to solve drug bioavailabily problems. During the past two decades, colloidal drug carriers have proved to improve the therapeutic index of drugs and thus increase their efficacy and/or reduce their toxicity. However, the major challenge in the development of these drug carriers remains the search for materials able to self-organize into stable nanoscale systems. In particular, amphiphilic α-, β- and γ-cyclodextrins (CDs), grafted on their secondary or primary side with different aliphatic chains, have been investigated as drug delivery vehicles due to their ability to self-assemble and form various stable colloidal systems such as micellar aggregates, nanoreservoirs or nanoparticles exhibiting a matricial, multilamellar or hexagonal supramolecular organization. These self-assembled CD-based nanodevices show some advantages in terms of stability, good ability to associate lipophilic drugs and good in vivo tolerance. This review focuses on the potential of the structured nanoparticles obtained from nonionic amphiphilic CDs in drug delivery and targeting. We discuss the synthesis and characterization of the building blocks as well as the preparation and characterization of colloidal particles made from these materials. We also considered some pharmaceutical applications and identified opportunities for an optimum use of this CD-based nanotechnology approach in addressing worldwide priority health problems.
Artemisinin and its derivatives are currently recommended by World Health Organization for the treatment of malaria. Severe malaria requires a parenteral administration of artemisinin-based formulations. However, the effective use of artemisinin is limited by the pharmacokinetic characteristics of the drug (low water solubility, poor bioavailability and short half-life). To overcome some of these drawbacks, artemisinin-loaded surface-decorated nanoparticles were prepared by conanoprecipitation of γ-cyclodextrin bioesterified with C 10 alkyl chains and polyethylene glycol (PEG) derivatives (polysorbate 80 and DMPE-mPEG2000). Using a single dose (1.5 mg.kg -1 or 2 mg.kg -1 ) by intravenous administration, we investigated the in vivo pharmacokinetic properties in healthy rats of two types of artemisinin-loaded nanoparticle formulations, namely, nanosphere and nanoreservoir systems versus ethanolic-aqueous solution of artemisinin as reference. Significantly enhanced pharmacokinetic parameters were obtained with artemisinin-loaded nanoparticles. In comparison to reference formulation, the geometric mean exposures in plasma (AUC 0-t ) exhibited 2.35 and 3.26-fold increases when artemisinin was loaded in nanoreservoir and nanosphere systems, respectively. Its plasma half-life increased 4.00 and 6.25-fold and its clearance decreased up to 2.5 and 4.72-fold.Artemisinin was successfully administered intravenously by means of surface-decorated amphiphilic -cyclodextrin nanostructures and showed a longer elimination half-life with respect to an artemisinin solution in ethanol. Therefore, these systems are likely to provide significant advantages for the intravenous treatment of severe malaria.
Les plantes constituent un réservoir pour les pharmacopées du monde. Plusieurs médicaments importants sont fabriqués à partir des substances actives d’origine végétales. En outre de nombreux médicaments modernes ont été fabriqués à partir de ces matières premières. Les plantes médicinales sont utilisées directement sous forme fraîche, sèche ou transformée, stabilisée, ou extrait ou formulée avec d’autres plantes ou excipients de synthèse. Dans tous les cas, la matière végétale utilisée pour fabriquer la forme posologique doit faire preuve de son efficacité, son innocuité et être de qualité conforme aux exigences de la Pharmacopée Européenne pour les phytomédicaments, garantissant ainsi sa sécurité d’emploi. Pour ce faire, l’Organisation Mondiale de la Santé (OMS) a mis à la disposition des états membres des guides et standards permettant d’harmoniser et de sécuriser leur utilisation. Ainsi de nombreux pays africains ont adopté ces outils après des modifications appropriées pour faire progresser la recherche et le développement (R&D) de médicaments à base de plante. Le but de ce travail était de faire une synthèse des différentes étapes de production, de contrôle qualité et de standardisation des matières premières issues des plantes médicinales et des médicaments à base de plantes médicinales.Mots clés : Pharmacopée, médicaments, médecine traditionnelle, sécurité d’emploi, phytomédicaments. English title: Production of raw materials and manufacturing of drugs from medicinal plants Plants are a reservoir for the world's pharmacopoeias. Several important medicines are made from active substances of plant origin. In addition, many modern medicines have been made from these raw materials. Medicinal plants are used directly in fresh, dry or processed, stabilized, or extracted form or formulated with other plants or synthetic excipients. In all cases, the herbal material used to manufacture the dosage form must demonstrate its efficacy, safety and be of a quality that meets the requirements of the European Pharmacopoeia for phytomedicines, thus ensuring its safe use. To this end, the World Health Organization (WHO) has made available to Member States guides and standards to harmonize and secure their use. Thus, many African countries have adopted these tools after appropriate modifications to advance research and development (R&D) of plant-based drugs. The aim of this work was to make a synthesis of the different stages of production, quality control and standardization of raw materials from medicinal plants and herbal medicines.Keywords: Pharmacopoeia, drugs, traditional medicine, safe use, phytomedicines.
Furosemide is a diuretic frequently used in the therapeutic management of edema associated with cardiac, renal, and hepatic failure and hypertension. However, there are a very low number of pharmaceutical dosage forms containing furosemide that are suitable for children under 6- years old. Therefore, there is a real need to develop hospital preparations, especially in the hospital. Four oral pediatric solutions of furosemide (2 mg/Ml) were formulated. Two of those solutions did not contain ethanol. For each formulation, 12 batches of 1600.0 Ml were prepared and packaged in 250.0 Ml brown glass bottles with polypropylene screw caps. The physicochemical properties (visual appearance, pH, osmolarity, drug content) and microbiological quality of the finished product were determined on the freshly prepared solutions and after 90 days of storage at 30°C/65% RH. The physicochemical and microbiological characteristics of the freshly prepared solutions were within the prescribed specifications. After 90 days of storage at 30°C/65% RH, the solutions containing sucrose and those without ethanol showed a slight decrease in pH and furosemide content of about 2.5%–4.5% (w/w). Despite this slight decrease, the characteristics remained within the prescribed specifications. Based on the stability profile of the ethanol-free solution containing sorbitol, it could be implemented in hospitals for the care of pediatric patients.
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