Preparation of cRGD-modified harmine hydrochloride stealth liposomes
- Author:
Mei WANG
1
Author Information
- Publication Type:Journal Article
- Keywords: Entrapment efficiency; Harmine hydrochloride; Liposome; Particle size
- From: Chinese Pharmaceutical Journal 2015;50(8):689-694
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To prepare cRGD-modified harmine hydrochloride long circulating liposomes, investigate its characteristics in vitro, and finally establish its best preparation method. METHODS: Firstly the content determination method was established, and secondly harmine hydrochloride liposomes were prepared through reverse phase evaporation method. Both active and passive drug loading methods were investigated to entrap the drug. Thirdly, cRGD-DSPE-2000 was prepared by conjugation method, and then cRGD modified harmine hydrochloride long circulating liposomes were prepared. Finally the particle sizes, Zeta potential and the entrapment efficiency were determined. The release of the liposomes in vitro was measured. RESULTS: The standard curves all had good linearities except for the one using 100% methanol as solvent. The particle sizes of the liposomes prepared by passive loading method, active loading method, and long circulating cRGD modified liposomes were 227.2, 246.3 and 241.9 nm, respectively, and the Zeta potentials were about 20-30 mV. The entrapment efficiency were (36.78 ± 6.82)%, (81.77 ± 7.61)%, and (80.02 ± 1.27)%, respectively. The release of cRGD liposomes was slower than the liposomes without cRGD and HM solution. CONCLUSION: cRGD-modified long circulating harmine hydrochloride liposomes can be made through reverse phase evaporation method and active loading method. KEY
