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Titolo:
DISPOSITION OF POSITIVELY CHARGED BOWMAN-BIRK PROTEASE INHIBITOR CONJUGATES IN MICE - INFLUENCE OF PROTEIN CONJUGATE CHARGE-DENSITY AND SIZE ON LUNG TARGETING
Autore:
EKRAMI H; KENNEDY AR; SHEN WC;
Indirizzi:
UNIV SO CALIF,JOHN STAUFFER PHARMACEUT SCI CTR,DEPT PHARMACEUT SCI,1985 ZONAL AVE,ROOM 404B LOS ANGELES CA 90033 UNIV SO CALIF,JOHN STAUFFER PHARMACEUT SCI CTR,DEPT PHARMACEUT SCI LOS ANGELES CA 90033 UNIV PENN,SCH MED,DEPT RADIAT ONCOL PHILADELPHIA PA 19104
Titolo Testata:
Journal of pharmaceutical sciences
fascicolo: 4, volume: 84, anno: 1995,
pagine: 456 - 461
SICI:
0022-3549(1995)84:4<456:DOPCBP>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
RADIATION-INDUCED TRANSFORMATION; BLOOD-BRAIN-BARRIER; C3H-10T1/2 CELLS; ORAL CARCINOGENESIS; DIETARY ADDITION; EPITHELIAL-CELLS; IMMUNOGLOBULIN-G; DIMETHYLHYDRAZINE; POLYLYSINE; RAT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
37
Recensione:
Indirizzi per estratti:
Citazione:
H. Ekrami et al., "DISPOSITION OF POSITIVELY CHARGED BOWMAN-BIRK PROTEASE INHIBITOR CONJUGATES IN MICE - INFLUENCE OF PROTEIN CONJUGATE CHARGE-DENSITY AND SIZE ON LUNG TARGETING", Journal of pharmaceutical sciences, 84(4), 1995, pp. 456-461

Abstract

The influence of conjugate charge density and size on the targeting of cationic Bowman-Birk inhibitor (BBI) conjugates to the lungs was studied in mice. The biodistribution of BBI, either as the native proteinor in the conjugated form (conjugated to a dicationic, tetracationic,or polycationic carrier), indicated that by increasing the charge density of BBI conjugates, the lung accumulation of the conjugates administered intravenously (iv) can be increased. The order of lung accumulation in these studies was as follows: polycationic- > tetracationic- >dicationic-conjugated BBI > BBI. The influence of conjugate size on lung accumulation was studied in three experiments. First, the biodistribution of poly(D-lysine) carriers of equal charge density but different molecular weight demonstrated that lung accumulation of polycationic carriers increases with an increase in carrier size. Second, the biodistributions of BBI, tyramine-derivatized poly(D-lysine)(3 kDa), and poly(D-lysine)(3) kDa conjugated to BBI indicated that an increase in conjugate size alone is not sufficient to promote the lung accumulation of cationic BBI conjugates. Finally, the biodistribution poly(D-lysine) complexed with heparin showed that targeting of a conjugate to thelungs can be abolished by neutralizing the charge on the carrier. Collectively, data in this paper demonstrate that the carrier-mediated targeting of BBI to the lungs is dependent on (a) cationization of BBI, (b) the conjugate positive charge density, and (c) the size of the cationic conjugate if the charge density is maintained. Also, the data show that the size of the conjugate alone does not make a significant impact on lung accumulation.

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Documento generato il 20/09/20 alle ore 04:34:40