Encapsulation of the dual FLAP/mPEGS-1 inhibitor BRP-187 into acetalated dextran and PLGA nanoparticles improves its cellular bioactivity

Table 1 Overview of the NP properties

NP formulation	After purification		After lyophilization			EE (%)	LC (%)	PVA (%)
NP formulation	d_H (nm)	PDI	d_H (nm)	PDI	ζ (mV)	EE (%)	LC (%)	PVA (%)
Acdex	210 ± 26	0.17 ± 0.07	211 ± 35	0.26 ± 0.09	− 12 ± 2	–	–	0.01 ± 0.000
Acdex[BRP-187]	196 ± 51	0.16 ± 0.11	178 ± 26	0.13 ± 0.07	− 13 ± 8	59 ± 23	1.7 ± 0.6	0.01 ± 0.000
Acdex-RhodB[BRP-187]	163 ± 15	0.20 ± 0.06	189 ± 37	0.28 ± 0.11	− 24 ± 2	67 ± 10	2.0 ± 0.3	n.m.
PLGA	124 ± 6	0.06 ± 0.03	130 ± 2	0.09 ± 0.03	− 20 ± 2	–	–	0.02 ± 0.002
PLGA[BRP-187]	153 ± 41	0.17 ± 0.14	158 ± 35	0.12 ± 0.06	− 15 ± 3	76 ± 22	2.2 ± 0.6	0.03 ± 0.002
PLGA-DY635	143 ± 3	0.08 ± 0.03	154 ± 5	0.15 ± 0.02	− 20 ± 1	–	–	0.02 ± 0.006
PLGA-DY635[BRP-187]	153 ± 2	0.12 ± 0.01	168 ± 9	0.19 ± 0.05	− 19 ± 1	87 ± 6	2.5 ± 0.2	0.02 ± 0.002

Concentration of NPs used for the PVA assay was 3 mg mL⁻¹. SD for all measurements n ≥ 3. n.m.–not measured
d_H Hydrodynamic diameter obtained by DLS measurements. EE encapsulation efficiency. LC loading capacity

ISSN: 1477-3155