000097158 001__ 97158
000097158 005__ 20210902121859.0
000097158 0247_ $$2doi$$a10.3390/pharmaceutics12111062
000097158 0248_ $$2sideral$$a121132
000097158 037__ $$aART-2020-121132
000097158 041__ $$aeng
000097158 100__ $$0(orcid)0000-0003-0063-9456$$aAnselmo, M.S.$$uUniversidad de Zaragoza
000097158 245__ $$aJanus dendrimers to assess the anti-hcv activity of molecules in cell-assays
000097158 260__ $$c2020
000097158 5060_ $$aAccess copy available to the general public$$fUnrestricted
000097158 5203_ $$aThe use of nanocarriers has been revealed as a valid strategy to facilitate drug bioavailability, and this allows for expanding the drug libraries for the treatment of certain diseases such as viral diseases. In the case of Hepatitis C, the compounds iopanoic acid and 3, 3', 5-triiodothyroacetic acid (or tiratricol) were identified in a primary screening as bioactive allosteric inhibitors of viral NS3 protease, but they did not exhibit accurate activity inhibiting viral replication in cell-based assays. In this work, dendritic nanocarriers are proposed due to their unique properties as drug delivery systems to rescue the bioactivity of these two drugs. Specifically, four different amphiphilic Janus dendrimers synthesized by combining 2, 2'-bis(hydroxymethyl)propionic acid (bis-MPA) and 2, 2'-bis(glyciloxy)propionic acid (bis-GMPA) functionalized with either hydrophilic or lipophilic moieties at their periphery were used to entrap iopanoic acid and tiratricol. Interestingly, differences were found in the loading efficiencies depending on the dendrimer design, which also led to morphological changes of the resulting dendrimer aggregates. The most remarkable results consist of the increased water solubility of the bioactive compounds within the dendrimers and the improved antiviral activity of some of the dendrimer/drug aggregates, considerably improving antiviral activity in comparison to the free drugs. Moreover, imaging studies have been developed in order to elucidate the mechanism of cellular internalization.
000097158 536__ $$9info:eu-repo/grantAgreement/ES/MICINN-FEDER/PGC2018-097583-B-I00$$9info:eu-repo/grantAgreement/ES/MICINN-FEDER/PGC2018-093761-B-C31$$9info:eu-repo/grantAgreement/ES/MICINN-FEDER/FPU12-05210$$9info:eu-repo/grantAgreement/ES/MEC/FPU13-3870$$9info:eu-repo/grantAgreement/ES/MCIU/BES-2016-078774$$9info:eu-repo/grantAgreement/ES/ISCIII-ERDF-ESF/PI18-00349-Investing in your future$$9info:eu-repo/grantAgreement/ES/ISCIII-ERDF-ESF/PI15-00663-Investing in your future$$9info:eu-repo/grantAgreement/ES/ISCIII/CPII13-00017$$9info:eu-repo/grantAgreement/ES/ISCIII/CIBERehd$$9info:eu-repo/grantAgreement/ES/DGA-FSE/E47-20R$$9info:eu-repo/grantAgreement/ES/DGA/B25-17R
000097158 540__ $$9info:eu-repo/semantics/openAccess$$aby$$uhttp://creativecommons.org/licenses/by/3.0/es/
000097158 590__ $$a6.321$$b2020
000097158 591__ $$aPHARMACOLOGY & PHARMACY$$b29 / 275 = 0.105$$c2020$$dQ1$$eT1
000097158 592__ $$a1.054$$b2020
000097158 593__ $$aPharmaceutical Science$$c2020$$dQ1
000097158 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/publishedVersion
000097158 700__ $$0(orcid)0000-0001-6584-6603$$aLancelot, A.
000097158 700__ $$aEgido, J.E.
000097158 700__ $$aClavería-Gimeno, R.
000097158 700__ $$0(orcid)0000-0002-1273-754X$$aCasanova, Á.$$uUniversidad de Zaragoza
000097158 700__ $$0(orcid)0000-0001-9866-6633$$aSerrano, J.L.$$uUniversidad de Zaragoza
000097158 700__ $$0(orcid)0000-0003-3109-4284$$aHernández-Ainsa, S.$$uUniversidad de Zaragoza
000097158 700__ $$0(orcid)0000-0001-5664-1729$$aAbian, O.$$uUniversidad de Zaragoza
000097158 700__ $$0(orcid)0000-0001-7091-077X$$aSierra, T.$$uUniversidad de Zaragoza
000097158 7102_ $$11005$$2410$$aUniversidad de Zaragoza$$bDpto. Farmacología y Fisiolog.$$cÁrea Fisiología
000097158 7102_ $$12013$$2765$$aUniversidad de Zaragoza$$bDpto. Química Orgánica$$cÁrea Química Orgánica
000097158 7102_ $$11002$$2060$$aUniversidad de Zaragoza$$bDpto. Bioq.Biolog.Mol. Celular$$cÁrea Bioquímica y Biolog.Mole.
000097158 773__ $$g12, 11 (2020), 1062 [24 pp]$$pPharmaceutics$$tPharmaceutics$$x1999-4923
000097158 8564_ $$s999325$$uhttps://zaguan.unizar.es/record/97158/files/texto_completo.pdf$$yVersión publicada
000097158 8564_ $$s29591$$uhttps://zaguan.unizar.es/record/97158/files/texto_completo.jpg?subformat=icon$$xicon$$yVersión publicada
000097158 909CO $$ooai:zaguan.unizar.es:97158$$particulos$$pdriver
000097158 951__ $$a2021-09-02-10:34:49
000097158 980__ $$aARTICLE