An evaluation of the transmembrane ammonium sulfate gradients method in lipid system to improve trapping capacity of amphipathic weak base drugs

Aim and Liposomal vesicles provide the possibility of loading lipophilic drugs into phospholipids bilayers and water-soluble (hydrophilic) aqueous phase. The present study was aimed on the evaluation of the properties of liposomal doxorubicin loaded into liposome by both active and passive procedures in terms of drug loading and release.
Material and Dipalmitoyl glycerol phospholipid glycerol, cholesterol and DSPE-mPEG 2000 was used for synthesis of nanoliposome. Then, doxorubicin loading was performed by passive (thin film hydration) and active (according to pH gradient) methods. The average diameter of nanoparticls was measured with Zeta Sizer. And the amount of drug loading and release was performed using dialysis.
The average size of nanoparticles were 138.6 ± 4.9 nm and 105.9 ± 3.8 nm for thin film hydration method, and pH gradient method, respectively. And drug loading efficacy of doxorubicin-containing nanoliposomes was 89±4.35 for pH gradient method and 15.65±8.65 for thin film method. The accumulated amount of drug release during 48 hours in PBS at pH=7.4, was determined 78% and 24% for hydration thin film method pH gradient method, respectively.
This study shows that nanoliposomal doxorubicin prepared by active method, was more effective than that the passive method. Our prepared nanoformulation was also sensitive to pH of medium.