Technology Pharmaceutical Laboratory, Department of Processes Engineering, Faculty of Technology; Associated Laboratory in Marine Ecosystems and Aquaculture, Faculty of Nature and Life Sciences, Universite de Bejaia, 06000 Bejaia, Algeria; Technology Pharmaceutical and Bio pharmaceutics Laboratory, UFR Medicine and Pharmacy, Rouen University, 22 Blvd. Gambetta, 76183, Rouen, France.
Associated Laboratory in Marine Ecosystems and Aquaculture, Faculty of Nature and Life Sciences, Universite de Bejaia; Centre de Recherche en Technologies Agro-Alimentaires, Campus Universitaire Tergua Ouzemour, Bejaia 06000, Algeria.
Cryo Letters. 2023 Mar-Apr;44(2):89-99.
Camptothecin (CPT) is an anticancer drug, and is not employed in the clinic because of its high hydrophobicity and low active form stability. CPT may also have potential for use in cold preservation.
To overcome these drawbacks, CPT solubility variations in the presence of cyclodextrins (CDs) and polyethylene glycol (PEG) were evaluated by Higuchi solubility experiments.
CPT was encapsulated in different cyclodextrins and polyethylene glycol using a co-evaporation method. The CPT interactions with CDs and PEG 6000 were investigated by Fourier-transformed infrared spectroscopy (FT-IR), and X-ray powder diffraction (XRPD). Then, CPT complexes were evaluated for in-vitro drug release. To evaluate the potential anticancer efficacy of the CPT complexes system, in-vitro cytotoxicity studies on human red blood cells were carried out using UV assay. The impact of the CPT complex systems on sperm motility protection during cold preservation at 4 degree C was studied using CASA.
The dissolution profile of these preparations shows the improvement of the dissolution of the CPT following a fickien diffusion. The CPT solubility and stability improvement were the cause of the cytotoxicity on the red blood cells test. However, CPT alone, encapsulated, dispersed, and chemically modified protected spermatozoids during cold preservation.
We confirm the interest in CPT encapsulated and dispersed in anticancer treatments. We also found that CPT encapsulated or dispersed could protect sperm against oxidative damage and improve the membrane integrity of human sperm. Consequently, CPT encapsulated our dispersed could eventually be beneficial for infertility therapy. Doi: 10.54680/fr23210110712.
喜树碱（CPT）是一种抗癌药物，但由于其高疏水性和低活性形式稳定性，并未在临床上使用。CPT 也可能有用于低温保存的潜力。
为了克服这些缺点，通过 Higuchi 溶解度实验评估了 CPT 在环糊精（CDs）和聚乙二醇（PEG）存在下的溶解度变化。
采用共蒸发法将 CPT 包封在不同的环糊精和聚乙二醇中。通过傅里叶变换红外光谱（FT-IR）和 X 射线粉末衍射（XRPD）研究了 CPT 与 CDs 和 PEG 6000 的相互作用。然后，对 CPT 配合物进行了体外药物释放评价。为了评估 CPT 配合物系统的潜在抗癌疗效，用人红细胞的紫外吸收法进行了体外细胞毒性研究。使用 CASA 研究了 CPT 配合物系统对 4 摄氏度低温保存期间精子活力保护的影响。
这些制剂的溶解曲线表明，CPT 的溶解度在菲克扩散后得到了改善。CPT 溶解度和稳定性的提高是导致红细胞测试细胞毒性的原因。然而，CPT 本身、包封、分散和化学修饰都能在低温保存期间保护精子。
我们证实了 CPT 包封和分散在抗癌治疗中的应用。我们还发现，CPT 包封或分散可以保护精子免受氧化损伤，提高人精子的膜完整性。因此，CPT 包封或分散最终可能有益于不孕治疗。doi：10.54680/fr23210110712。
