物理化学学报 >> 2015, Vol. 31 >> Issue (11): 2043-2048.doi: 10.3866/PKU.WHXB201509141

热力学,动力学和结构化学 上一篇    下一篇

铁脂质体/水分配系数测定及影响因素考察

李妮娜1,耿丽娜1,*(),王琳1,元琳琳1,常彦忠2,张建军2   

  1. 1 河北师范大学化学与材料科学学院,石家庄050024
    2 河北师范大学分析测试中心,石家庄050024
  • 收稿日期:2015-05-15 发布日期:2015-11-13
  • 通讯作者: 耿丽娜 E-mail:genglina0102@126.com
  • 基金资助:
    国家自然科学基金(31201305);河北省自然科学基金-石药集团医药联合研究基金(C2012205082)

Determination of Iron Liposome/Water Partition Coefficients and Identification of Influencing Factors

Ni-Na. LI1,Li-Na. GENG1,*(),Lin. WANG1,Lin-Lin. YUAN1,Yan-Zhong. CHANG2,Jian-Jun. ZHANG2   

  1. 1 College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang 050024, P. R. China
    2 Testing and Analysis Center, Hebei Normal University Shijiazhuang 050024, P. R. China
  • Received:2015-05-15 Published:2015-11-13
  • Contact: Li-Na. GENG E-mail:genglina0102@126.com
  • Supported by:
    the National Natural Science Foundation of China(31201305);Natural Science Foundation of Hebei ProvinceShijiazhuang Pharmaceutical Group (CSPC) Foundation, China(C2012205082)

摘要:

采用薄膜旋转蒸发-超声法分别制备了柠檬酸铁脂质体(FAC-Lip)和血红素铁脂质体(Heme-Lip).通过测定铁脂质体的体外释放,发现两种铁脂质体均具有缓释性,并且Heme-Lip的缓释性比FAC-Lip的好;采用平衡透析法测定了脂质体/水分配系数(P),并考察影响分配系数的因素,初步探讨了FAC和Heme与脂质体膜结合的吉布斯自由能(ΔG),结果发现随着胆固醇含量和药脂比例的增加, P先增大后减小,当P最大时,药物与磷脂膜的氢键及静电作用力最大;在透析平衡时,计算得到了FAC-Lip和Heme-Lip中药物与脂质体膜层之间的吉布斯自由能分别为-12.7和-18.2 kJ·mol-1.

关键词: 柠檬酸铁, 血红素铁, 脂质体/水分配系数, 平衡透析, 吉布斯自由能

Abstract:

Ferric citrate liposomes (FAC-Lip) and heme liposomes (Heme-Lip) were successfully prepared by a rotary-evaporated film-ultrasonication method. The release of iron liposomes were studied in vitro, and results showed that both iron liposomes had sustained-released properties, with Heme-Lip showing superior sustained-released over FAC-Lip. The liposome/water partition coefficients (P) were determined by equilibrium dialysis and the influences on P were evaluated, as well as the binding Gibbs free energy between FAC (Heme) and liposome. The results show that P initially increased and then decreased with increasing cholesterol content and the ratio of lipid to drug. The hydrogen and electrostatic interactions were largest when P was at its maximum. At the dialysis equilibrium, the binding Gibbs free energies (ΔG) of FAC-Lip and Heme-Lip were -12.7 and -18.2 kJ·mol-1, respectively.

Key words: Ferric citrate, Heme, Liposome/water partition coefficient, Equilibrium dialysis, Gibbs free energy

MSC2000: 

  • O642.1