000032743 001__ 32743
000032743 005__ 20210121114451.0
000032743 0247_ $$2doi$$a10.2147/IJN.S90849
000032743 0248_ $$2sideral$$a92815
000032743 037__ $$aART-2015-92815
000032743 041__ $$aeng
000032743 100__ $$aGuada, M.
000032743 245__ $$aLipid nanoparticles for cyclosporine a administration: Development, characterization, and in vitro evaluation of their immunosuppression activity
000032743 260__ $$c2015
000032743 5060_ $$aAccess copy available to the general public$$fUnrestricted
000032743 5203_ $$aCyclosporine A (CsA) is an immunosuppressant commonly used in transplantation for prevention of organ rejection as well as in the treatment of several autoimmune disorders. Although commercial formulations are available, they have some stability, bioavailability, and toxicity related problems. Some of these issues are associated with the drug or excipients and others with the dosage forms. With the aim of overcoming these drawbacks, lipid nanoparticles (LN) have been proposed as an alternative, since excipients are biocompatible and also a large amount of surfactants and organic solvents can be avoided. CsA was successfully incorporated into LN using the method of hot homogenization followed by ultrasonication. Three different formulations were optimized for CsA oral administration, using different surfactants: Tween® 80, phosphatidylcholine, taurocholate and Pluronic® F127 (either alone or mixtures). Freshly prepared Precirol nanoparticles showed mean sizes with a narrow size distribution ranging from 121 to 202 nm, and after freeze-drying were between 163 and 270 nm, depending on the stabilizer used. Surface charge was negative in all LN developed. High CsA entrapment efficiency of approximately 100% was achieved. Transmission electron microscopy was used to study the morphology of the optimized LN. Also, the crystallinity of the nanoparticles was studied by X-ray powder diffraction and differential scanning calorimetry. The presence of the drug in LN surfaces was confirmed by X-ray photoelectron spectroscopy. The CsA LN developed preserved their physicochemical properties for 3 months when stored at 4°C. Moreover, when the stabilizer system was composed of two surfactants, the LN formulations were also stable at room temperature. Finally, the new CsA formulations showed in vitro dose-dependent immunosuppressive effects caused by the inhibition of IL-2 levels secreted from stimulated Jurkat cells. The findings obtained in this paper suggest that new lipid nanosystems are a good alternative to produce physicochemically stable CsA formulations for oral administration.
000032743 540__ $$9info:eu-repo/semantics/openAccess$$aby-nc$$uhttp://creativecommons.org/licenses/by-nc/3.0/es/
000032743 590__ $$a4.32$$b2015
000032743 591__ $$aPHARMACOLOGY & PHARMACY$$b40 / 255 = 0.157$$c2015$$dQ1$$eT1
000032743 591__ $$aNANOSCIENCE & NANOTECHNOLOGY$$b26 / 83 = 0.313$$c2015$$dQ2$$eT1
000032743 592__ $$a1.323$$b2015
000032743 593__ $$aBioengineering$$c2015$$dQ1
000032743 593__ $$aBiomaterials$$c2015$$dQ1
000032743 593__ $$aBiophysics$$c2015$$dQ1
000032743 593__ $$aOrganic Chemistry$$c2015$$dQ1
000032743 593__ $$aMedicine (miscellaneous)$$c2015$$dQ1
000032743 593__ $$aNanoscience and Nanotechnology$$c2015$$dQ1
000032743 593__ $$aDrug Discovery$$c2015$$dQ1
000032743 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/publishedVersion
000032743 700__ $$0(orcid)0000-0002-6873-5244$$aSebastián, V.$$uUniversidad de Zaragoza
000032743 700__ $$0(orcid)0000-0002-2966-9088$$aIrusta, S.$$uUniversidad de Zaragoza
000032743 700__ $$aFeijoó, E.
000032743 700__ $$aDios-Viéitez, M.C.
000032743 700__ $$aBlanco-Prieto, M.
000032743 7102_ $$15005$$2555$$aUniversidad de Zaragoza$$bDpto. Ing.Quím.Tecnol.Med.Amb.$$cÁrea Ingeniería Química
000032743 773__ $$g10 (2015), 6541-6553$$pInt. j. nanomed.$$tInternational Journal of Nanomedicine$$x1176-9114
000032743 8564_ $$s4855156$$uhttps://zaguan.unizar.es/record/32743/files/texto_completo.pdf$$yVersión publicada
000032743 8564_ $$s76035$$uhttps://zaguan.unizar.es/record/32743/files/texto_completo.jpg?subformat=icon$$xicon$$yVersión publicada
000032743 909CO $$ooai:zaguan.unizar.es:32743$$particulos$$pdriver
000032743 951__ $$a2021-01-21-10:45:53
000032743 980__ $$aARTICLE