Development and Characterization of a Microemulsion Containing a Cannabidiol Oil and a Hydrophilic Extract from Sambucus ebulus for Topical Administration.

Cannabidiol (CBD) is a safe and non-psychotropic phytocannabinoid with a wide range of potential therapeutic anti-inflamatory and antioxidant activities. Due to its lipophilicity, it is normally available dissolved in oily phases. The main aim of this work was to develop and characterize a new formulation of a microemulsion with potential anti-inflammatory and antioxidant activity for the topical treatment of inflammatory skin disorders. The microemulsion system was composed of a 20% CBD oil, which served as the hydrophobic phase; Labrasol/Plurol Oleique (1:1), which served as surfactant and cosurfactant (S/CoS), respectively; and an aqueous vegetal extract obtained from Sambucus ebulus L. (S. ebulus) ripe fruits, which has potential anti-oxidant and anti-inflammatory activity and which served as the aqueous phase. A pseudo-ternary phase diagram was generated, leading to the selection of an optimal proportion of 62% (S/CoS), 27% CBD oil and 11% water and, after its reproducibility was tested, the aqueous phases were replaced by the vegetal hydrophilic extract. The defined systems were characterized in terms of conductivity, droplet size (by laser scattering), compatibility of components (by differential scanning calorimetry) and rheological properties (using a rotational rheometer). The designed microemulsion showed good stability and slight pseudo-plastic behavior. The release properties of CBD from the oil phase and caffeic acid from the aqueous phase of the microemulsion were studied via in vitro diffusion experiments using flow-through diffusion cells and were compared to those of a CBD oil and a microemulsion containing only CBD as an active substance. It was found that the inclusion of the original oil in microemulsions did not result in a significant modification of the release of CBD, suggesting the possibility of including hydrophilic active compounds in the formulation and establishing an interesting strategy for the development of future formulations.

Assessment of In Vitro Release Testing Methods for Colloidal Drug Carriers: The Lack of Standardized Protocols.

Although colloidal carriers have been in the pipeline for nearly four decades, standardized methods for testing their drug-release properties remain to be established in pharmacopeias. The in vitro assessment of drug release from these colloidal carriers is one of the most important parameters in the development and quality control of drug-loaded nano- and microcarriers. This lack of standardized protocols occurs due to the difficulties encountered in separating the released drug from the encapsulated one. This review aims to compare the most frequent types of release testing methods (i.e., membrane diffusion techniques, sample and separate methods and in situ detection techniques) in terms of the advantages and disadvantages of each one and of the key parameters that influence drug release in each case.

In situ forming PLA and PLGA implants for the parenteral administration of Cannabidiol.

Cannabidiol (CBD) is the main non-psychotropic cannabinoid. It has attracted a great deal of interest in the treatment of several diseases such as inflammatory disorders and cancer. Despite its promising clinical interest, its administration is very challenging. In situ forming implants (ISFIs) could be a simple and cheap strategy to administer CBD while obtaining a prolonged effect with a single administration. This work aims to design, develop, and characterize for the first time ISFIs for the parenteral administration of CBD with potential application in cancer disease. Formulations made of PLGA-502, PLGA-502H, and PLA-202 in NMP or DMSO and PLA-203 in DMSO at a polymer concentration of 0.25 mg/µL and loaded with CBD at a drug: polymer ratio of 2.5:100 and 5:100 (w/w) were developed. The formulations prepared with NMP exhibited a faster drug release. CBD implants elaborated with PLGA-502 and DMSO with the highest CBD: polymer ratio showed the most suitable drug release for one month. This formulation was successfully formed in ovo onto the chorioallantoic chick membrane without exhibiting signs of toxicity and exhibited a superior antiangiogenic activity than CBD in solution administered at the same doses. Consequently, implants made of PLGA-502 and DMSO represent a promising strategy to effectively administer CBD subcutaneously as combination therapy in cancer disease.

La nanotecnología aplicada al desarrollo de medicamentos / Nanotechnology applied to drug development

En este trabajo se realiza una revisión de las principales estrategias definidas hasta la fecha para el desarrollo de sistemas nanoparticulares farmacéuticos y de su interés en terapéutica, Se trata de liposomas, nanopartículas poliméricas o lipídicas, micelas poliméricas, dendrímeros, conjugados poliméricos y con anticuerpos, nanotubos de carbono y otros nanotransportadores, que tras su administración posibilitan la vectorización o localización selectiva de la sustancia que transportan a nivel de un órgano, de un tejido, de un tipo específico de células o incluso a nivel de orgánulos celulares concretos. En la actualidad, las principales dianas en vectorización son las células tumorales y la neovascularización tumoral, las células del sistema fagocítico mononuclear y las células somáticas dañadas. La vectorización a estas dianas se puede alcanzar mediante un mecanismo pasivo, un mecanismo mediado por un desencadenante externo 0 un mecanismo activo.

This paper reviews the main strategies defined to date for the development of pharmaceutical nanoparticle systems and their interest in therapy. These are Iiposomes, polymeric or lipid nanoparticles, polymeric micelles, dendrimers, polymer conjugates and antibodies, carbon nanotubes and other nanocarriers, which upon administration enable targeting or selective localization of substance transporting at level of an organ, a tissue, a specific cell type or even at specific cellular organelles. Currently, the main targets in drug targeting are tumor cells and tumor neovascularization, the mononuclear phagocyte system cells and somatic cells damaged. Drug localization to these targets can be achieved by a passive mechanism, a mechanism mediated by an external trigger or an active mechanism.