Optimization on Preparation of Saussureae Involucratar Herba Extract-composite Phospholipid Liposome by Central Composite Design-response Surface Method

JIANG Wen1 ZENG Cheng2,3 YU Ning2 TAN Mei-e2 XING Jian-guo2

(1.Department of Pharmacy, the Sixth Affiliated Hospital of Xinjiang Medical University, Urumqi, China 830002)
(2.Xinjiang Institute of Materia Medica, Urumqi, China 830004)
(3.Institute of Traditional Chinese Medicine, Xinjiang Medical University, Urumqi, China 830054)

【Abstract】 Objective To optimize the preparation of Saussureae Involucratae Herba extract (SIHE)-composite phospholipid liposome (CPL) by the central composite design-response surface methodology (CCD-RSM) and to investigate the in vitro release of drugs. Methods The method of ammonium sulfate transmembrane gradients was adopted to prepare SIHE-CPL. The single factor experiments were used for the key experimental factors and their test ranges. Based on the single factor experiments, with the size of SIHE-CPL, polymey disperse index (PDI), encapsulation efficiency (EE), and Zeta potential as dependent variables, central composite design was adopted to optimize the preparation technology by taking the content of phospholipid and the content of cholesterol as independent variables; test results were fitted by multiple linear and binomial nonlinear equations, and optimum formulation was selected by RSM; then the in vitro release behavior of the drug was studied with method of dynamic dialysis. Infrared (IR) spectroscopy and X-ray diffraction (XRD) pattern were used to analyze the spectroscopic properties of SIHE-CPL. Results The second-order polynomial equation was superior to the linear one, and the observed values agreed well with model predicted values. The optimal process conditions were as follows: size of SIHE-CPL was (102.7 ± 5.1) nm, PDI was 0.154 ± 0.017, EE of chlorogenic acid and rutin was (87.68 ± 2.57)% and (84.18 ± 2.97)%, Zeta potential was (−28.4 ± 2.2) mV, SIHE-CPL and solution of SIHE were both accorded with the first order model, and IR analysis and XRD proved the formation of SIHE-CPL. Conclusion The size and PDI of SIHE-CPL are low and the EE and Zeta potential of SIHE-CPL are high. CCD-RSM could be successfully used to optimize the prescription of SIHE-CPL.

【Keywords】 Saussureae Involucratae Herba extract; composite phospholipid liposome; central composite design-response surface methodology; in vitro release; infrared spectroscopic analysis; X-ray diffraction;


【Funds】 National Natural Science Foundation of China (81260681)

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This Article


CN: 12-1108/R

Vol 47, No. 01, Pages 57-64

January 2016


Article Outline


  • 1 Instruments and materials
  • 2 Methods and results
  • 3 Discussion
  • References