. Author manuscript; available in PMC: 2016 Jul 1.

Published in final edited form as: Nanomedicine. 2015 Mar 17;11(5):1133–1140. doi: 10.1016/j.nano.2015.02.020

Table 1.

Pharmacokinetic summary in multiple dose study in Sprague Dawley rats

Part A: PK of PLP after administration in its liposomal encapsulated or free form in rats
PLP		Weekly LN-PLP (in mg/kg)						Daily PLP (in mg/kg)
		0.5		2		8		15		60
		M	F	M	F	M	F	M	F	M	F
Day 1	Clearance (mL hour^-1 kg^-1)	0.70	1.09	0.59	0.64	0.49	0.62	8543	3968	7053	nc
	T½ (hours)	34.7	22.9	39.1	33.8	45.7	33.9	0.08	0.42	0.11	nc
	C_max (μg/mL)	14.2	13.8	60.4	63.6	248	262	6.48	5.91	31.8	38.9
	C_max/dose (μg/mL)/(mg/kg)	28.4	27.5	30.2	31.8	31.0	32.7	0.43	0.39	0.53	0.65

Day 22/28	Clearance (mL hour^-1 kg^-1)	0.59	0.96	0.50	0.51	0.30	0.48	6885	4104	6125	NR
	T½ (hours)	0.25	0.25	0.25	0.25	0.25	0.25	0.08	0.08	0.08	0.08
	C_max (μg/mL)	17.3	14.5	72.5	76.3	300	288	7.94	5.92	37.2	40.1
	C_max/dose (μg/mL)/(mg/kg)	34.6	29.1	36.2	38.1	37.5	36.0	0.53	0.40	0.62	0.67

*Part B:* Pharmacokinetics of the active metabolite PL after administration of PLP in liposomal encapsulated or its free form in rats
PL		Weekly LN-PLP (in mg/kg)						Daily PLP (in mg/kg)
		0.5		2		8		15		60
		M	F	M	F	M	F	M	F	M	F

Day 1	T½ (hours)	nc^*						0.40	0.37	0.38	0.37
	C_max (μg/mL)	0.34	0.17	1.18	0.67	6.27	3.66	7.99	10.2	37.9	45.4
	C_max/dose (μg/mL)/(mg/kg)	0.70	0.34	0.59	0.34	0.78	0.46	0.53	0.68	0.63	0.76

Day 22/28	T½ (hours)	nc^*						0.35	0.43	0.37	0.39
	C_max (μg/mL)	0.23	0.08	1.17	0.50	6.87	3.59	9.80	10.0	40.9	41.3
	C_max/dose (μg/mL)/(mg/kg)	0.47	0.17	0.58	0.25	0.86	0.45	0.65	0.67	0.68	0.69

C_max, maximal concentration; F, female rats; LN, liposomal nanoparticle; M, male rats; nc, not calculated; PL, prednisolone (active metabolite); PLP, prednisolone phosphate (prodrug); T½; terminal half-live.

not calculated because plasma concentrations result of indirect release.