Abstract
PNAPR2 is a peptide nucleic acid (PNA) complementary to a sequence of the viral protease-encoding gene, effective in blocking HIV release, when used at high doses. Erythrocytes (RBC) were used to target PNA PR2 to the macrophage compartment. The antiviral activity was assessed in human HIV-infected macrophages both as inhibition of p24 production and reduction of HIV DNA content. PNAPR2, either added to the medium at a concentration of 100 μM or loaded into RBC at about 40 μM, inhibited p24 production 80 compared with infected samples and reduced HIV DNA content by 83 and 90, respectively. The results show that (1) a stronger anti-HIV effect is achievable with higher doses of PNAPR2, both when given free and encapsulated into RBC; (2) the antiviral effect obtained by free PNA PR2 at a concentration of 100 μM is achievable by encapsulating it into RBC at a concentration of 40 μM, suggesting that RBC can be used as a delivery system to increase the antisense effect of PNAPR2.
| Original language | English |
|---|---|
| Pages (from-to) | 278-285 |
| Number of pages | 8 |
| Journal | Journal of Drug Targeting |
| Volume | 17 |
| Issue number | 4 |
| DOIs | |
| Publication status | Published - May 2009 |
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Keywords
- Delivery
- Erythrocytes (RBC)
- HIV
- Macrophages
- Peptide nucleic acid (PNA)
ASJC Scopus subject areas
- Pharmaceutical Science
Cite this
Erythrocytes as carriers of antisense PNA addressed against HIV-1 gag-pol transframe domain. / Fraternale, Alessandra; Paoletti, Maria Filomena; Casabianca, Anna; Orlandi, Chiara; Millo, Enrico; Balestra, Emanuela; Damonte, Gianluca; Perno, Carlo Federico; Magnani, Mauro.
In: Journal of Drug Targeting, Vol. 17, No. 4, 05.2009, p. 278-285.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Erythrocytes as carriers of antisense PNA addressed against HIV-1 gag-pol transframe domain
AU - Fraternale, Alessandra
AU - Paoletti, Maria Filomena
AU - Casabianca, Anna
AU - Orlandi, Chiara
AU - Millo, Enrico
AU - Balestra, Emanuela
AU - Damonte, Gianluca
AU - Perno, Carlo Federico
AU - Magnani, Mauro
PY - 2009/5
Y1 - 2009/5
N2 - PNAPR2 is a peptide nucleic acid (PNA) complementary to a sequence of the viral protease-encoding gene, effective in blocking HIV release, when used at high doses. Erythrocytes (RBC) were used to target PNA PR2 to the macrophage compartment. The antiviral activity was assessed in human HIV-infected macrophages both as inhibition of p24 production and reduction of HIV DNA content. PNAPR2, either added to the medium at a concentration of 100 μM or loaded into RBC at about 40 μM, inhibited p24 production 80 compared with infected samples and reduced HIV DNA content by 83 and 90, respectively. The results show that (1) a stronger anti-HIV effect is achievable with higher doses of PNAPR2, both when given free and encapsulated into RBC; (2) the antiviral effect obtained by free PNA PR2 at a concentration of 100 μM is achievable by encapsulating it into RBC at a concentration of 40 μM, suggesting that RBC can be used as a delivery system to increase the antisense effect of PNAPR2.
AB - PNAPR2 is a peptide nucleic acid (PNA) complementary to a sequence of the viral protease-encoding gene, effective in blocking HIV release, when used at high doses. Erythrocytes (RBC) were used to target PNA PR2 to the macrophage compartment. The antiviral activity was assessed in human HIV-infected macrophages both as inhibition of p24 production and reduction of HIV DNA content. PNAPR2, either added to the medium at a concentration of 100 μM or loaded into RBC at about 40 μM, inhibited p24 production 80 compared with infected samples and reduced HIV DNA content by 83 and 90, respectively. The results show that (1) a stronger anti-HIV effect is achievable with higher doses of PNAPR2, both when given free and encapsulated into RBC; (2) the antiviral effect obtained by free PNA PR2 at a concentration of 100 μM is achievable by encapsulating it into RBC at a concentration of 40 μM, suggesting that RBC can be used as a delivery system to increase the antisense effect of PNAPR2.
KW - Delivery
KW - Erythrocytes (RBC)
KW - HIV
KW - Macrophages
KW - Peptide nucleic acid (PNA)
UR - http://www.scopus.com/inward/record.url?scp=70749123774&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=70749123774&partnerID=8YFLogxK
U2 - 10.1080/10611860902737474
DO - 10.1080/10611860902737474
M3 - Article
C2 - 19255894
AN - SCOPUS:70749123774
VL - 17
SP - 278
EP - 285
JO - Journal of Drug Targeting
JF - Journal of Drug Targeting
SN - 1061-186X
IS - 4
ER -