title: Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies.
abstract: CB13 (1-Naphthalenyl[4-(pentyloxy)-1-naphthalenyl]methanone)-loaded poly(lactic-co-glycolic acid) nanoparticles (NPs) were produced by nanoprecipitation and tested for their in vitro release behavior and in vitro cytotoxicity assays. The effects of several formulation parameters such as polymer type, surfactant concentration, and initial drug amount were studied. NPs had a particle size 90-300 nm in diameter. Results obtained show that the main influence on particle size was the type of polymer employed during the particle production: the greater the hydrophobicity, the smaller the particle size. In terms of encapsulation efficiency (%), high values were achieved (∼68%-90%) for all formulations prepared due to the poor solubility of CB13 in the external aqueous phase. Moreover, an inverse relationship between release rate and NP size was found. On the other hand, low molecular weight and low lactide content resulted in a less hydrophobic polymer with increased rates of water absorption, hydrolysis, and erosion. NPs showed no cytotoxicity and may be considered to be appropriate for drug-delivery purposes.
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, Seville, Spain.
authors.forename: Lucía
authors.initials: L
authors.lastname: Martín-Banderas
authors.forename: Josefa
authors.initials: J
authors.lastname: Alvarez-Fuentes
authors.forename: Matilde
authors.initials: M
authors.lastname: Durán-Lobato
authors.forename: José
authors.initials: J
authors.lastname: Prados
authors.forename: Consolación
authors.initials: C
authors.lastname: Melguizo
authors.forename: Mercedes
authors.initials: M
authors.lastname: Fernández-Arévalo
authors.forename: Maria Ángeles
authors.initials: MÁ
authors.lastname: Holgado
mesh_terms: D000284:Administration, Oral; D002470:Cell Survival / Q000187:drug effects; D003106:Colon / Q000166:cytology / Q000187:drug effects*; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry* / Q000633:toxicity*; D053769:Nanocapsules / Q000737:chemistry* / Q000633:toxicity* / Q000648:ultrastructure; D009281:Naphthalenes / Q000008:administration & dosage / Q000737:chemistry* / Q000633:toxicity*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry* / Q000633:toxicity*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D053769:Nanocapsules; D009281:Naphthalenes; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C524107:naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone