The binding stoichiometry, binding constants, and inclusion mode of some water-soluble negatively charged cyclodextrin derivatives, i.e. heptakis-[6-deoxy-6-(3-sulfanylpropanoic acid)]-β-cyclodextrin(H1), heptakis-[6-deoxy-6-(2-sulfanylacetic acid)]-β-cyclodextrin(H2), mono-[6-deoxy-6-(3-sulfanylpropanoic acid)]-β-cyclodextrin (H3) and mono-[6-deoxy-6-(2-sulfanylacetic acid)]-β-cyclodextrin (H4), with three anticancer drugs, i.e. irinotecan hydrochloride; topotecan hydrochloride; doxorubicin hydrochloride, were investigated by means of ¹H NMR, UV–Vis spectroscopy, mass spectra and 2D NMR. Polyanionic cyclodextrins H1-H2 showed the significantly high binding abilities of up to 2.6 × 10⁴–2.0 × 10⁵ M⁻¹ towards the selected anticancer drugs, which were nearly 50–1000 times higher than the corresponding Ks values of native β-cyclodextrin. In addition, these polyanionic cyclodextrins also showed the pH-controlled release behaviors. That is, the anticancer drugs could be efficiently encapsulated in the cyclodextrin cavity at a pH value similar to that of serum but sufficiently released at an endosomal pH value of a cancer cell, which would make these cyclodextrin derivatives the potential carriers for anticancer drugs.

一些水溶性带负电荷的环糊精衍生物的结合化学计量，结合常数和包合方式，即七-[6-脱氧-6-（3-硫烷基丙酸）]-β-环糊精（H1），七-[6-]脱氧-6-（2-磺基乙酸）-β-环糊精（H2），单-[6-脱氧-6-（3-硫烷基丙酸）]-β-环糊精（H3）和单-[6-脱氧- 6-（2-磺基乙酸）-β-环糊精（H4），含三种抗癌药物，即盐酸伊立替康；盐酸托泊替康；用¹ H NMR，UV-Vis光谱，质谱和2D NMR研究了盐酸阿霉素。聚阴离子环糊精H1 - H2结果显示，对所选的抗癌药物具有高达2.6×10 ⁴ –2.0×10 ⁵ M ^-1的显着高结合能力，比天然β-环糊精的相应Ks值高近50–1000倍。另外，这些聚阴离子环糊精还显示出pH控制的释放行为。即，可以在类似于血清的pH值的pH值下将抗癌药有效地包封在环糊精腔中，但是在癌细胞的内体pH值下可以将其充分释放，这将使这些环糊精衍生物成为抗癌药的潜在载体。