Hydroxycamptothecin (
HCPT) loaded PEG modified nanostructured
lipid carriers (
HCPT-PEG-NLC) and nanostructured
lipid carriers (
HCPT-NLC) were prepared by melt emulsification and homogenization method. The morphology, particle size and encapsulation efficiency of them were investigated.
HCPT concentrations in plasma, heart, liver, spleen, lung, kidney and ovary were determined after iv of
HCPT injection,
HCPT-PEG-NLC and
HCPT-NLC in mice. The targeting indexes of
HCPT-PEG-NLC and
HCPT-NLC were calculated. The transmission electron microscope imaging showed that
HCPT-PEG-NLC and
HCPT-NLC exhibited a spherical shape. The particle sizes of them were (88.6 +/- 22.5) and (127.2 +/- 43.4) nm. The encapsulation efficiency were (90.51 +/- 3.29)% and (84.37 +/- 2.81)%, respectively. After iv injection into the tail vein of mice,
HCPT plasma concentrations of
HCPT-PEG-NLC and
HCPT-NLC were higher than that of
HCPT injection at each sampling time. They also showed longer elimination time in every tissue.
HCPT-NLC accumulated in endothelial system (RES), Re and Ce of it in liver and spleen were significantly higher than
HCPT-PEG-NLC. HPCT-PEG-NLC prolonged circulation time and increased bioavailability of
HCPT. MRT and AUC0-24 h of it were 19.80 and 17.02 times higher than those of
HCPT injection. It also significantly reduced phagocytosis of RES, and showed lung targeting effect (Re and Ce were 14.51 and 41.35). To summarize,
HCPT-PEG-NLC could prolong the circulation time of
HCPT in vivo, and had the lung targeting effect. It was a promising carrier to increase
therapeutic effect of
HCPT in treating
lung cancer.