YANG Yi-hua, LI Ying-xuan, ZHANG Xin, et al. Optimization of Preparation Technology of Ligustrazine Hydrochloride Liposomes by Orthogonal Design[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(22): 20-23.
YANG Yi-hua, LI Ying-xuan, ZHANG Xin, et al. Optimization of Preparation Technology of Ligustrazine Hydrochloride Liposomes by Orthogonal Design[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(22): 20-23. DOI: 10.13422/j.cnki.syfjx.2014220020.
Objective:To optimize preparation technology of ligustrazine hydrochloride liposomes which provides a reference for clinical application of ligustrazine. Method: Ligustrazine hydrochloride was quantified by HPLC method
mobile phase consisted of methanol-0.2% triethylamine solution(glacial acetic acid adjusted pH to 5.0)(60: 40) with detection wavelength of 295 nm.Ligustrazine hydrochloride liposomes were prepared by film dispersion method with phospholipid and cholesterol as raw materials
taking encapsulation efficiency as index
orthogonal design was adopted to optimize preparation process with hydration time
weight ratio of cholesterol to phospholipid
weight ratio of ligustrazine hydrochloride to phospholipid and the concentration of phospholipid as factors.encapsulation efficiency
morphology
particle size
Zeta potential and stability of ligustrazine hydrochloride liposomes were investigated. Result: Optimum preparation technology was as follows:hydration time of 30 min
ratio of cholesterol to phospholipid 1: 2
ratio of ligustrazine hydrochloride to phospholipid 1: 15
the concentration of phospholipid 3%;under these conditions
liposomes were nearly spherical with average encapsulation efficiency of (70.27±0.58)%
particle size of (22.9±6.8)nm and Zeta potential of (-29.79±1.24)mV
they were stable under 4 ℃ for 2 weeks. Conclusion: This optimized preparation technology is rational and stable
which can help to improve absorption and prolong effective time.