Formulation optimization of berberine and magnolol co-loaded liposomes by Box-Behnken response sur-face method
OBJECTIVE To optimize the formulation of berberine and magnolol co-loaded liposomes(Lip-MB)by Box-Behnken response surface method.METHODS The content of berberine and magnolol was determined by high performance liq-uid chromatography(HPLC).Lip-MB was prepared by thin-film dispersion plus pH gradient method.Based upon the results of single factor experiment,Box-Behnken response surface method was employed for optimizing the formulation with berberine and magnolol encapsulation efficiency as dependent variables.Morphology,particle size,zeta potential and in vitro release of Lip-MB were evaluated.RESULTS The optimal formulation process was as follow:mass ratio of hydrogenated soybean phosphotidyl-choline(HSPC)to cholesterol(CHOL)3.6∶1,drug-to-lipid ratio 1∶23,pH value of external aqueous phase 8.4 and incubation temperature of 59℃.The encapsulation efficiencies of berberine and magnolol in Lip-MB were(91.74±1.91)％and(83.17± 1.05)％.Average particle size of liposomes was(106.6±2.60)nm and Zeta potential(-9.88±2.33)mV.Cumulative release rates of berberine and magnolol were 98.41％and 81.83％within 84h respectively.CONCLUSION The model established by Box-Behnken design-response surface method may be employed for optimizing the formulation of Lip-MB.And optimized lipo-somes offer high encapsulation efficiency,small particle size,uniform distribution and slow release effect.
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