title: Poly-ε-caprolactone microspheres as a drug delivery system for cannabinoid administration: development, characterization and in vitro evaluation of their antitumoral efficacy.
abstract: Cannabinoids show promise for the treatment of various medical conditions such as emesis, anorexia, pain, cancer, multiple sclerosis, Parkinson's disease and glaucoma. However, their high lipohilicity and instability complicate their handling and dosing, and restrict their use as pharmaceuticals. The objective of the present work was to assess the feasibility of developing cannabinoid loaded poly-ε-caprolactone (PCL) microparticles prepared by the oil-in-water emulsion-solvent evaporation technique as a suitable dosage form for their administration. Spherical microparticles with a size range of 20-50 μm, and high entrapment efficiency (around 100%) were obtained. Cannabidiol (CBD) dissolved in the polymeric matrix of the microspheres was slowly released in vitro within 10 days. In vitro cell viability studies demonstrated the antitumoral activity of CBD released from microparticles. After 4 and 7 days of incubation, CBD in microspheres significantly inhibited the growth of MDA-MB-231 cells by 60% as compared to the 50% attained with free drug. The results suggest that PCL microparticles could be an alternative delivery system for long-term cannabinoid administration, showing potential therapeutic advantages over free drug.
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, Complutense University of Madrid, 28040 Madrid, Spain.
authors.forename: D
authors.initials: D
authors.lastname: Hernán Pérez de la Ossa
authors.forename: A
authors.initials: A
authors.lastname: Ligresti
authors.forename: M E
authors.initials: ME
authors.lastname: Gil-Alegre
authors.forename: M R
authors.initials: MR
authors.lastname: Aberturas
authors.forename: J
authors.initials: J
authors.lastname: Molpeceres
authors.forename: V
authors.initials: V
authors.lastname: Di Marzo
authors.forename: A I
authors.initials: AI
authors.lastname: Torres Suárez
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D002185:Cannabidiol / Q000008:administration & dosage* / Q000737:chemistry; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D006801:Humans; D008863:Microspheres; D011091:Polyesters / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011091:Polyesters; D002185:Cannabidiol; C016240:polycaprolactone