Formulation and Particle Size Reduction Improve Bioavailability of Poorly Water-Soluble Compounds with Antimalarial Activity

Table 4

Summary of orally dosed DQ distribution in the liver and in the blood.

PK values and	Nanoparticle (0.39 μm)		Microsuspension (36.88 μm)
Ratios of liver/plasma	PO 80 mg/kg	PO 80 mg/kg	PO 400 mg/kg	PO 400 mg/kg
AUC liver (ng·h/mL)	6055.50		1096.20
𝐶max liver (ng/mL or g)		407.30		93.40
AUC plasma (ng·h/mL)	795.50		51.40
𝐶max plasma (ng/mL or g)		25.30		6.10
Ratio of AUC liver/AUC plasma	81.20		21.30
Ratio of 𝐶max liver/𝐶max plasma		16.10		15.30

Data are derived from Table 3. DQ: decoquinate; PO: oral dose; AUC: area under the curve; 𝐶_max: maximal concentration; DQ was orally dosed at 80 mg/kg for nanoparticle formulations and at 400 mg/kg for microsuspensions.