International Journal of Pharmaceutics 2012-11-15

Competitive molecular interaction among paeonol-loaded liposomes: differential scanning calorimetry and synchrotron X-ray diffraction studies.

Rui-guang Wu, Jun-dong Dai, Fu-gen Wu, Xiao-hua Zhang, Wei-heng Li, Yu-rong Wang

Index: Int. J. Pharm. 438(1-2) , 91-7, (2012)

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Abstract

Thermotropic phase behavior of 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) liposomes containing 5 mol% cholesterol, or 5 mol% stigmasterol, or 5 mol% paeonol have been investigated by differential scanning calorimetry (DSC) and synchrotron X-ray diffraction (XRD) techniques, to investigate the competitive molecular interaction among paeonol-loaded liposomes. The results show that both sterol and paeonol can incorporate into hydrophobic region and interact with acyl chains of DPPC. Both 5 mol% sterols and 5 mol% paeonol can promote the formation of rippled gel phase of DPPC liposomes at room temperature. 5 mol% paeonol can induce the occurrence of phase separation in DPPC liposomes, but 5 mol% cholesterol or 5 mol% stigmasterol cannot induce this phenomenon. Both the repeat distance and the correlation length of paeonol-poor domain are larger than those of coexisted paeonol-rich domain. Both calorimetric data and SAXS patterns show that sterols have more favorable, stabilizing interactions with DPPC than paeonol, implying that high concentrations of sterols will have a negative effect on the loading of paeonol. In addition, calorimetric data show that cholesterol have a little more favorable, stabilizing interactions with DPPC than stigmasterol. The results of this study will play an important role in optimizing the formulation of paeonol-loaded liposomes.Copyright © 2012 Elsevier B.V. All rights reserved.