In this study, we designed and prepared liposomal structures for the encapsulation of the novel small cyclic KRX29 peptide, that shows a potent and selective inhibition of the GRK2 activity whose high levels result in heart failure [7, 8]. The ultrasound assisted method is applied to produce tailored nanovesicles able to entrap the KRX29 peptide. Taking into account that the formulation choice is of crucial importance to achieve a suitable peptide-vector, nanoliposomes were produced exploring three different formulations by changing the charge ratio (-/+) between the anionic phosphatidylglycerol (PG) and the cationic KRX29. The charge effect on both peptide encapsulation and recovery efficiencies in liposomes were studied through an analytical HPLC protocol accurately developed for this purpose.
LIPOSOMAL STRUCTURES DESIGN FOR PEPTIDE DELIVERY IN HEART FAILURE THERAPY
BOCHICCHIO , SABRINA;SALA, MARINA;SPENSIERO, ANTONIA;SCALA, MARIA CARMINA;CAMPIGLIA, Pietro;DALMORO, ANNALISA;LAMBERTI, Gaetano;BARBA, Anna Angela
2016-01-01
Abstract
In this study, we designed and prepared liposomal structures for the encapsulation of the novel small cyclic KRX29 peptide, that shows a potent and selective inhibition of the GRK2 activity whose high levels result in heart failure [7, 8]. The ultrasound assisted method is applied to produce tailored nanovesicles able to entrap the KRX29 peptide. Taking into account that the formulation choice is of crucial importance to achieve a suitable peptide-vector, nanoliposomes were produced exploring three different formulations by changing the charge ratio (-/+) between the anionic phosphatidylglycerol (PG) and the cationic KRX29. The charge effect on both peptide encapsulation and recovery efficiencies in liposomes were studied through an analytical HPLC protocol accurately developed for this purpose.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
