Long-Term Prophylaxis and Pharmacokinetic Evaluation of Intramuscular Nano- and Microparticle Decoquinate in Mice Infected with P. berghei Sporozoites
Table 1
Long-term efficacy of depot IM-decoquinate (DQ) formulation (nano- and microsuspension) dosed with single intramuscular injection at 80, 120, or 240 mg/kg before treatment given 2, 4, 6, or 8 weeks early and monitoring by using in vivo imaging system (IVIS) in C3H mice ().
Test agents
Dose (mg/kg)
Regimen
Liver suppression rate (%)
Blood infection by FCM
Number of C3H mice
Effects
24 h
48 h
72 h
Challenged
Protected completely
Causal prophylaxis
IM nano-DQ (0.43 µm)
120
−8 weeks
71.8
70.5
65.7
5/5
5
0
0/5
Mild suppression
120
−6 weeks
79.0
90.8
92.5
4/5
5
1
1/5
Partial causal prophylaxis
120
−4 weeks
89.4
97.6
99.6
1/5
5
4
4/5
Partial causal prophylaxis
120
−2 weeks
97.9
100
100
0/5
5
5
5/5
Full causal prophylaxis
80
−2 weeks
100
91.7
100
1/5
5
4
4/5
Partial causal prophylaxis
IM nano-DQ(0.43 µm)
240
−8 weeks
100
100
100
0/5
5
5
5/5
Full causal prophylaxis
240
−6 weeks
100
98.9
100
0/5
5
5
5/5
Full causal prophylaxis
IM micro-DQ (8.31 µm)
120
−8 weeks
100
100
100
0/5
5
5
5/5
Full causal prophylaxis
120
−6 weeks
100
98.8
100
0/5
5
5
5/5
Full causal prophylaxis
120
−4 weeks
100
99.3
100
0/5
5
5
5/5
Full causal prophylaxis
120
−2 weeks
100
99.6
100
0/5
5
5
5/5
Full causal prophylaxis
IVIS study: decoquinate (DQ) injected 2, 4, 6, and 8 weeks early to the challenge with 10,000 sporozoites (SPZ) intravenously in C3H female mice, which will be monitored with IVIS on days 1, 2, and 3 after SPZ inoculation. The blood parasitemia will be measured by flow cytometry up to 30 days after inoculation.
