000086125 001__ 86125
000086125 005__ 20200716101448.0
000086125 0247_ $$2doi$$a10.1016/j.ejpb.2018.11.020
000086125 0248_ $$2sideral$$a109739
000086125 037__ $$aART-2019-109739
000086125 041__ $$aeng
000086125 100__ $$aAparicio-Blanco, J.
000086125 245__ $$aLipid nanocapsules decorated and loaded with cannabidiol as targeted prolonged release carriers for glioma therapy: In vitro screening of critical parameters
000086125 260__ $$c2019
000086125 5060_ $$aAccess copy available to the general public$$fUnrestricted
000086125 5203_ $$aThe therapeutic potential of cannabinoids has been truly constrained heretofore due to their strong psychoactive effects and their high lipophilicity. In this context, precisely due to the lack of psychoactive properties, cannabidiol (CBD), the second major component of Cannabis sativa, arises as the phytocannabinoid with the most auspicious therapeutic potential. Hence, the incorporation of CBD in lipid nanocapsules (LNCs) will contribute to overcome the dosing problems associated with cannabinoids. Herein, we have prepared LNCs decorated and loaded with CBD for glioma therapy and screened in vitro their critical parameters. On the one hand, we have encapsulated CBD into the oily core of LNCs to test their in vitro efficacy as extended-release carriers against the human glioblastoma cell line U373MG. The in vitro antitumor effect was highly dependent on the size of LNCs due to its pivotal role in the extent of CBD release. Effectively, a comparison between two differently-sized LNCs (namely, 20-nm and 50-nm sized carriers) showed that the smaller LNCs reduced by 3.0-fold the IC50 value of their 50-nm sized counterparts. On the other hand, to explore the potential of this phytocannabinoid to target any of the cannabinoid receptors overexpressed in glioma cells, we decorated the LNCs with CBD. This functionalization strategy enhanced the in vitro glioma targeting by 3.4-fold in comparison with their equally-sized undecorated counterparts. Lastly, the combination of CBD-loading with CBD-functionalization further reduced the IC50 values. Hence, the potential of these two strategies of CBD incorporation into LNCs deserves subsequent in vivo evaluation.
000086125 540__ $$9info:eu-repo/semantics/openAccess$$aby-nc-nd$$uhttp://creativecommons.org/licenses/by-nc-nd/3.0/es/
000086125 590__ $$a4.604$$b2019
000086125 591__ $$aPHARMACOLOGY & PHARMACY$$b40 / 270 = 0.148$$c2019$$dQ1$$eT1
000086125 592__ $$a1.059$$b2019
000086125 593__ $$aBiotechnology$$c2019$$dQ1
000086125 593__ $$aPharmaceutical Science$$c2019$$dQ1
000086125 593__ $$aMedicine (miscellaneous)$$c2019$$dQ1
000086125 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/acceptedVersion
000086125 700__ $$0(orcid)0000-0002-6873-5244$$aSebastián, V.$$uUniversidad de Zaragoza
000086125 700__ $$aBenoit, J.P.
000086125 700__ $$aTorres-Suárez, A.I.
000086125 7102_ $$15005$$2555$$aUniversidad de Zaragoza$$bDpto. Ing.Quím.Tecnol.Med.Amb.$$cÁrea Ingeniería Química
000086125 773__ $$g134 (2019), 126-137$$pEur. j. pharm. biopharm.$$tEuropean Journal of Pharmaceutics and Biopharmaceutics$$x0939-6411
000086125 8564_ $$s1474180$$uhttps://zaguan.unizar.es/record/86125/files/texto_completo.pdf$$yPostprint
000086125 8564_ $$s205190$$uhttps://zaguan.unizar.es/record/86125/files/texto_completo.jpg?subformat=icon$$xicon$$yPostprint
000086125 909CO $$ooai:zaguan.unizar.es:86125$$particulos$$pdriver
000086125 951__ $$a2020-07-16-09:04:28
000086125 980__ $$aARTICLE