Preparation of liposomes containing zedoary turmeric oil using freeze-drying of liposomes via TBA/water cosolvent systems and evaluation of the bioavailability of the oil.
The purpose of this study was to enhance the absorption of zedoary turmeric oil (ZTO) in vivo and develop new formulations of a water-insoluble oily drug. This study described a method for preparing ZTO liposomes, which involved freeze-drying (FD) of liposomes with TBA/water cosolvent systems. The TBA/water cosolvent systems were used to investigate a feasible method of liposomes manufacture; the two factors, sugar/lipid mass ratio and TBA content (concentration), of the preparation process were evaluated in this study. The results showed that the addition of TBA content could significantly enhance the sublimation of ice resulting in short FD cycles time, and reduce the entrapment efficiency of liposomes. In addition, the residual TBA solvents levels were determined to be less than 0.37% under all optimum formulations and processing conditions. Several physical properties of liposomes were examined by H-600 transmission electron microscope (TEM) and zetamaster analyser system. The results revealed that the liposomes were smooth and spherical with an average particle size of 457 +/- 7.8 nm and the zeta potential was more than 3.65 Mv. The bioavailability of the liposomes was evaluated in rabbits, compared with the conventional self-emulsifying formulation for oral administration. Compared with the conventional self-emulsifying formulation, the plasma concentration-time profiles with improved sustained-release characteristics were achieved after oral administration of the liposomes with a bioavailability of 257.7% (a good strategy for improving the bioavailability of an oily drug). In conclusion, the present experimental findings clearly demonstrated the usefulness of ZTO liposome vesicles in improving therapeutic efficacy by enhancing oral bioavailability. Our study offered an alternative method for designing sustained-release preparations of oily drugs.
Department of Pharmaceutical Sciences, Gannan Medical College, Jiangxi, China. menghua001@sina.com
Zhiwen
Z
Yang
Songlin
S
Yu
Dahua
D
Fu
D000818:Animals; D000840:Anisoles / Q000737:chemistry*; D019540:Area Under Curve; D001682:Biological Availability; D030024:Curcuma / Q000737:chemistry*; D005612:Freeze Drying; D006207:Half-Life; D008081:Liposomes / Q000737:chemistry*; D010938:Plant Oils / Q000737:chemistry / Q000493:pharmacokinetics*; D011817:Rabbits; D014867:Water / Q000737:chemistry*
D000840:Anisoles; D008081:Liposomes; D010938:Plant Oils; D014867:Water; C484217:2,4,6-tribromoanisole