Temozolomide (TMZ) – a chemotherapeutic agent possessing cytotoxic activity is used in single or combined therapies of human glioma. Difficulties in these applications, connected with low solubility and stability of temozolomide lead us to study the inclusion complexes between TMZ, and three cyclodextrins: β-cyclodextrin (βCD), monodeoxy-6-monoamino-β-cyclodextrin hydrochloride (βCDamine), and β-cyclodextrin containing galactosamine and triazole ring in the side group (βCDgal). The voltammetric and spectroscopy studies showed the improvement of the drug solubility and formation of stable complexes. Higuchi and Connors method was used to determine the solubilities of the drug in the presence of the selected cyclodextrins. Phase solubility diagrams showed increase of TMZ solubility and 1:1 stoichiometry of the complexes formed. The stability constant of TMZ- βCDgal complex was pH – dependent, larger at pH 7.4 (corresponding to the pH of the body fluids), than at pH 5.5, characteristic for the cancer cells environment. βCDgal ligand was an effective complexing agent for TMZ due to additional strong proton-acceptor π-π interactions between the triazole ring of the cyclodextrin and the ring of TMZ. The increased solubility and sustainability of TMZ complexes with βCDgal allow to propose this cyclodextrin as a promising TMZ carrier for further studies in the biological cell environment.

Temozolomide（TMZ）–具有细胞毒性活性的化学治疗剂被用于人类神经胶质瘤的单一或联合治疗。由于这些应用的困难以及替莫唑胺的低溶解度和稳定性，导致我们研究了TMZ与三种环糊精之间的包合配合物：β-环糊精（βCD），单脱氧-6-单氨基-β-环糊精盐酸盐（βCDamine）和β侧基中含有半乳糖胺和三唑环的β-环糊精（βCDgal）。伏安法和光谱法研究表明，药物溶解度得到了改善，并形成了稳定的复合物。在选定的环糊精存在下，使用Higuchi和Connors方法确定药物的溶解度。相溶解度图显示所形成的配合物的TMZ溶解度增加和化学计量比为1：1。TMZ-βCDgal复合物的稳定性常数是pH依赖性的，在pH 7.4（对应于体液的pH）下比在pH 5.5下更大，这是癌细胞环境的特征。βCDgal配体是TMZ的有效络合剂，这是因为环糊精的三唑环与TMZ环之间存在额外的强质子受体π-π相互作用。TMZ与βCDgal配合物的溶解度和可持续性的提高，使得该环糊精可以作为有希望的TMZ载体用于生物细胞环境中的进一步研究。βCDgal配体是TMZ的有效络合剂，这是因为环糊精的三唑环与TMZ环之间存在额外的强质子受体π-π相互作用。TMZ与βCDgal配合物的溶解度和可持续性的提高，使得该环糊精可以作为有希望的TMZ载体用于生物细胞环境中的进一步研究。βCDgal配体是TMZ的有效络合剂，这是因为环糊精的三唑环与TMZ环之间存在额外的强质子受体π-π相互作用。TMZ与βCDgal配合物的溶解度和可持续性的提高，使得该环糊精可以作为有希望的TMZ载体用于生物细胞环境中的进一步研究。