摘要

ClGa 5,10,15,20-Tetrakis (4-bromophenyl) porphyrinato (ClGaTBrPP) and its metal free derivative were successfully synthesized and incorporated into Pluronic F127 polymeric micelles that has been conjugated to folic acid (FA) to form ClGaTBrPP-F127-FA (or H2TBrPP-F127-FA). For comparison, ClGaTBrPP-F127 and H2TBrPP-F127 (without FA) were also formed. The singlet oxygen quantum yield for ClGaTBrPP-F127-FA was higher (Phi(Delta) = 0.44) than that of H2TBrPP-F127-FA (Phi(Delta) = 0.37), due to the heavy atom effect of Ga in the former which encourages intersystem crossing to the triplet state. The same applies to ClGaTBrPP-F127 (Phi(Delta) = 0.47) and H2TBrPP-F127 (Phi(Delta) = 0.41). Thus, F. values decreased in the presence of FA, but still high enough for practical application of the nanodrug system. The binding constants K-b were determined to be 1.08 x 10(4) M-1, 2.51 x 105 M-1, 1.52 x 10(3) and 2.68 x 10(3) for H2TBrPP+F127-FA, ClGaTBrPP+F127-FA, ClGaTBrPP-F127 and H2TBrPP-F127, respectively. The K-p values were determined in biphasic octanol and water system.

  • 出版日期2018-2