物理化学学报 >> 2010, Vol. 26 >> Issue (12): 3243-3248.doi: 10.3866/PKU.WHXB20101207

胶体及界面化学 上一篇    下一篇

Pluronic嵌段共聚物F127胶团对布洛芬的增溶

万东华, 郑欧, 周燕, 吴莉瑜   

  1. 福州大学化学化工学院, 福州350108
  • 收稿日期:2010-04-29 修回日期:2010-09-01 发布日期:2010-12-01
  • 通讯作者: 万东华 E-mail:wendlt1999@yahoo.com.cn
  • 基金资助:

    福州大学科技发展基金(2009-XY-07)资助项目

Solubilization of Ibuprofen in Pluronic Block Copolymer F127 Micelles

WAN Dong-Hua, ZHENG Ou, ZHOU Yan, WU Li-Yu   

  1. College of Chemistry and Chemical Engineering, Fuzhou University, Fuzhou 350108, P. R. China
  • Received:2010-04-29 Revised:2010-09-01 Published:2010-12-01
  • Contact: WAN Dong-Hua E-mail:wendlt1999@yahoo.com.cn
  • Supported by:

    The project was supported by the Science and Technology Development Fund of Fuzhou University, China (2009-XY-07).

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摘要：

研究了Pluronic F127 胶团溶液对药物布洛芬（IBU)的增溶作用. 通过芘探针荧光法测定了不同温度下F127在水溶液和0.01 mol·L-1 pH 7.4磷酸盐缓冲生理(PBS)溶液中的临界胶束浓度(cmc), 采用高效液相色谱(HPLC)测定了F127溶液中布洛芬的溶解度, 并依据公式计算了增溶参数(摩尔增溶量χ 和胶团-水分配系数K), 考察了温度、溶剂和F68 的加入对F127 胶团化行为及其对布洛芬增溶作用的影响. 结果表明: 布洛芬的溶解度随F127 质量分数的提高线性增加; 随着温度升高, cmc 急剧下降, 胶团内核的疏水性增强, χ和K 稍有增大; 与水溶液相比, 在PBS溶液中cmc减小, χ几乎不变, K 显著降低; F68 的加入对F127 胶团的性质几乎无影响, 对增溶的影响也不明显. 对增溶参数的分析表明,K 反映的是药物布洛芬的性质, χ则可反映嵌段共聚物F127的溶解效能, 并证实了布洛芬是通过F127胶团的内核和栅栏层而实现增溶的.

关键词: Pluronic 嵌段共聚物, 增溶, F127, 布洛芬, 胶团

Abstract:

We studied the effect of Pluronic F127 micelle solution on the solubility of ibuprofen (IBU). The critical micelle concentration (cmc) of F127 in both water and 0.01 mol·L-1 pH 7.4 phosphate buffer salt (PBS) solution at different temperatures was determined by the pyrene fluorescence method. The concentration of the solubilized IBU was determined using high-performance liquid chromatography (HPLC). We calculated the solubility descriptors (molar solubilization capacity, χ, and micelle-water partition coefficient, K). The influences of temperature, medium properties, and additional copolymer F68 on the micellization of F127 and the solubilization of IBU were also investigated. The results showed that the solubility of IBU increased linearly with an increase in the F127 mass fraction. With an increase in temperature, a significant decrease in the cmc was apparent and a less polar microenvironment was present in the micelle core. Slight increases in χ and K were found with an increase in temperature. The cmc of F127 in PBS solution was much less than that in water, χ was essentially the same and K decreased significantly in PBS solution. F127 micelle property and the solubilization capacity of the F127 micelles were only slightly affected in the presence of F68. An analysis of the solubility descriptors indicates that the K is particularly unique for the drug IBU, and the χ is useful in determining the solubility effectiveness of copolymer F127. We also demonstrated that IBU was predominantly in the micelle core and core-corona interface.

Key words: Pluronic block copolymer, Solubilization, F127, Ibuprofen, Micelle