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  • Enhanced cellular uptake and biodistribution of a synthetic cannabinoid loaded in surface-modified poly(lactic-co-glycolic acid) nanoparticles.

Enhanced cellular uptake and biodistribution of a synthetic cannabinoid loaded in surface-modified poly(lactic-co-glycolic acid) nanoparticles.

Journal of biomedical nanotechnology (2014-04-23)
Matilde Durán-Lobato, Inmaculada Muñoz-Rubio, M Angeles Holgado, Josefa Alvarez-Fuentes, Mercedes Fernández-Arévalo, Lucía Martín-Banderas
ABSTRACT

This article aimed to produce, characterize and evaluate different surface-modified naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone (CB13) loaded poly(lactic-co-glycolic acid) nanoparticles in order to improve their oral absorption and in vivo biodistribution. Plain and surface-modified PLGA nanoparticles were successfully prepared using a nanoprecipitation method. Chitosan, Eudragit RS, lecithin and vitamin E were used as surface modifying agents. The NPs were evaluated in terms of mean diameter and size distribution, zeta potential, morphology, drug loading, drug release profiles, mucoadhesive properties, in vitro cell viability and uptake and in vivo biodistribution. Mean particle size distributions in the range of 253-344 nm, spherical shape and controlled zeta potential values were observed depending on the additive employed. High values of entrapment efficiency were obtained for all the formulations. Lecithin and vitamin E modified particles showed higher release rates when compared to the rest of formulations. A clear improvement in ex vivo mucoadhesion properties was observed in the case of chitosan- and Eudragit RS-modified nanoparticles. Chitosan-poly(lactic-co-glycolic acid) nanoparticles showed the highest uptake values on Caco-2 cells. Biodistribution assays proved that most of the particles were accumulated in liver and spleen. An important goal has been achieved in this investigation: CB13, a highly lipophilic drug with low water solubility, can reach the interior of cells more efficiently when it is included in these surface-modified polymeric carriers.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Lactic acid, 85%, FCC
Sigma-Aldrich
Lactic acid, natural, ≥85%
Sigma-Aldrich
Lactic acid, meets USP testing specifications
Supelco
Lactic acid, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
DL-Lactic acid, ~90% (T)
Sigma-Aldrich
DL-Lactic acid, 85 % (w/w), syrup
Sigma-Aldrich
Lactic acid solution, ACS reagent, ≥85%
USP
Lactic acid, United States Pharmacopeia (USP) Reference Standard