Preparation and process optimization of gemcitabine hydrochloride stealth liposomes
Pages: 382-388
Year: 2017 Issue: 5
Journal: Chinese Journal of Antibiotics
Abstract: Objective Two statistical designs were used in this case study.The anti-cancer drug gemcitabine hydrochloride was used as a model compound to optimize the formulation of liposomes,and to investigate the characteristics of drug release in vitro.Methods The modified thin film method and the freeze thaw method was used to prepare gemcitabine hydrochloride stealth liposomes.First design (Plackett-Burman) was used to determine the factors that significantly affected the drug entrapment efficiency.It was discovered that the mass ratio of hydrogenated soybean phospholipids (HSPE),cholesterol,drugs and DSPE-PEG2k had significant effects on the drug encapsulation efficiency.This allowed the use of a central composite design (CCD) to elucidate the relationship between the these factors and the encapsulation efficiency.The drug release curve of the preparated gemcitabine hydrochloride stealth liposomes was drawn.Results Using this developed model,the optimal conditions included that the mass ratio of HSPE∶ cholesterol∶drugs∶ DSPE-PEG2k was 60∶3∶20∶4.8;the PBS concentration was 0.1mmol/L;the hydration time was 1h;the ultrasonic time was 3min (80W,3s/3s);and the freeze-thaw cycles were 4 times.Under the optimized conditions,encapsulation efficiency was 65.85％±0.48％,which increased by nearly 25％ compared with the original condition,and the release curve was fitted with ambiexponent equation.Conclusion Response surface analysis can effectively balance the interactions between various factors,and thus is suitable for the liposome preparation process and prescription screening.
Year: 2017 Issue: 5
Journal: Chinese Journal of Antibiotics
Abstract: Objective Two statistical designs were used in this case study.The anti-cancer drug gemcitabine hydrochloride was used as a model compound to optimize the formulation of liposomes,and to investigate the characteristics of drug release in vitro.Methods The modified thin film method and the freeze thaw method was used to prepare gemcitabine hydrochloride stealth liposomes.First design (Plackett-Burman) was used to determine the factors that significantly affected the drug entrapment efficiency.It was discovered that the mass ratio of hydrogenated soybean phospholipids (HSPE),cholesterol,drugs and DSPE-PEG2k had significant effects on the drug encapsulation efficiency.This allowed the use of a central composite design (CCD) to elucidate the relationship between the these factors and the encapsulation efficiency.The drug release curve of the preparated gemcitabine hydrochloride stealth liposomes was drawn.Results Using this developed model,the optimal conditions included that the mass ratio of HSPE∶ cholesterol∶drugs∶ DSPE-PEG2k was 60∶3∶20∶4.8;the PBS concentration was 0.1mmol/L;the hydration time was 1h;the ultrasonic time was 3min (80W,3s/3s);and the freeze-thaw cycles were 4 times.Under the optimized conditions,encapsulation efficiency was 65.85％±0.48％,which increased by nearly 25％ compared with the original condition,and the release curve was fitted with ambiexponent equation.Conclusion Response surface analysis can effectively balance the interactions between various factors,and thus is suitable for the liposome preparation process and prescription screening.
Related Articles