Preparation and characterization of APGA modified artemether liposomes / 中草药

ABSTRACT

Objective To optimize the formulation ratio and preparation process of the APGA modified artemether liposomes, and evaluate its physical and chemical properties. Methods The encapsulation efficiency of artemether was evaluated as index, and the preparation method of APGA modified artemether liposomes was optimized. The preparation process of APGA modified artemether liposomes was optimized by orthogonal experiments. Laser particle analyzer and transmission electron microscopy were used to evaluate the particle size, Zeta potential, and appearance of liposomes, and dialysis method was used to study the release of liposomes in vitro. Results The best prescription was as follow EPC-Chol-TPGS at 950.53, 5% APGA-PEG-DSPE, the artemether-lipid ratio at 120, film-forming temperature 30 ℃, probe ultrasound time 8 min. The resulting liposomes exhibited a pale blue opalescent appearance. The average particle size, polydispersity index, and zeta potential of artemether liposomes was (99.97 ± 1.67) nm, 0.185 ± 0.021, and (-0.023 ± 0.080) mV, respectively. Transmission electron micrograph image showed that artemether liposomes were spherical vesicles with uniform sizes. The encapsulation efficiency of artemether in liposomes was (90.06 ± 1.15)%. In vitro cumulative release rate of artemether from the liposomes in the simulated body fluids was (57.07 ± 6.09)% after 48 h. Conclusion The optimized APGA modified artemether liposomes was successfully developed. It had the following characters round shape, uniform particle size, high drug encapsulation efficiency and good sustained-release effect.