000070891 001__ 70891
000070891 005__ 20200221144328.0
000070891 0247_ $$2doi$$a10.1039/c6ra11056h
000070891 0248_ $$2sideral$$a106247
000070891 037__ $$aART-2016-106247
000070891 041__ $$aeng
000070891 100__ $$aMaione, S.
000070891 245__ $$aElectrospray loading and release of hydrophobic gramicidin in polyester microparticles
000070891 260__ $$c2016
000070891 5060_ $$aAccess copy available to the general public$$fUnrestricted
000070891 5203_ $$aGramicidin (GA), a very hydrophobic pentadecapeptide with important biological activities (i.e. in addition to its well-known antimicrobial and antibiotic activities, GA has been recently identified as a potent therapeutic agent against different carcinomas), has been loaded by electrospraying in poly(tetramethylene succinate) (PE44), a biodegradable and biocompatible aliphatic polyester. Microspheres (average diameter: 5.0 +/- 0.7 mm) were successfully obtained from the mixture of GA and PE44 solutions in ethanol and chloroform, respectively. The loading of the peptide, which has been proved by FTIR and X-ray photoelectron spectroscopies, essentially occurred at the surface of the microspheres, as was reflected by scanning electron microscopy micrographs and atomic force microscopy phase images. In spite of this, the thermal stability of the polyester matrix remained essentially unaltered, even though the wettability decreased. The release of GA in phosphate buffer saline (PBS) was limited by the very low solubility of the peptide in aqueous solution, a fast burst effect followed by the establishment of equilibrium after 5 days of being observed in this hydrophilic environment. The release behaviour was very different when the hydrophilicity of the medium was reduced by adding ethanol. In this case, a very fast but sustained release was identified during the first few hours. On the other hand, biological tests have demonstrated that GA retains its antimicrobial activity after loading and does not alter the biocompatibility of PE44. Our results prove that, despite its hydrophobicity and relatively large number of residues, the loading of GA in a polymeric matrix represents an alternative strategy for the release of this versatile peptide in cancer therapy.
000070891 536__ $$9info:eu-repo/grantAgreement/ES/DGA/E40$$9info:eu-repo/grantAgreement/ES/MINECO-FEDER/CTQ2013-40855-R$$9info:eu-repo/grantAgreement/ES/MINECO-FEDER/MAT2015-69367-R$$9info:eu-repo/grantAgreement/ES/MINECO-FEDER/MAT2015-69547-R
000070891 540__ $$9info:eu-repo/semantics/openAccess$$aby-nc$$uhttp://creativecommons.org/licenses/by-nc/3.0/es/
000070891 590__ $$a3.108$$b2016
000070891 591__ $$aCHEMISTRY, MULTIDISCIPLINARY$$b59 / 166 = 0.355$$c2016$$dQ2$$eT2
000070891 592__ $$a0.889$$b2016
000070891 593__ $$aChemistry (miscellaneous)$$c2016$$dQ1
000070891 593__ $$aChemical Engineering (miscellaneous)$$c2016$$dQ1
000070891 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/publishedVersion
000070891 700__ $$adel Valle, L.J.
000070891 700__ $$aPerez-Madrigal, M.M.
000070891 700__ $$0(orcid)0000-0003-3222-0828$$aCativiela, C.$$uUniversidad de Zaragoza
000070891 700__ $$aPuiggali, J.
000070891 700__ $$aAleman, C.
000070891 7102_ $$12013$$2765$$aUniversidad de Zaragoza$$bDpto. Química Orgánica$$cÁrea Química Orgánica
000070891 773__ $$g6, 77 (2016), 73045-73055$$pRSC ADVANCES$$tRSC Advances$$x2046-2069
000070891 8564_ $$s390965$$uhttps://zaguan.unizar.es/record/70891/files/texto_completo.pdf$$yVersión publicada
000070891 8564_ $$s114739$$uhttps://zaguan.unizar.es/record/70891/files/texto_completo.jpg?subformat=icon$$xicon$$yVersión publicada
000070891 909CO $$ooai:zaguan.unizar.es:70891$$particulos$$pdriver
000070891 951__ $$a2020-02-21-13:45:04
000070891 980__ $$aARTICLE