Radeva Lyubomira, Zaharieva Maya M, Spassova Ivanka, Kovacheva Daniela, Pencheva-El Tibi Ivanka, Najdenski Hristo, Yoncheva Krassimira
Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.
The Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.
Pharmaceuticals (Basel). 2024 Jan 31;17(2):186. doi: 10.3390/ph17020186.
In this study, doxorubicin was loaded in a chitosan-albumin nanogel with the aim of improving its stability and exploring the potential of the system in the treatment of skin cancer. Infrared spectroscopy and X-ray diffraction confirmed the encapsulation of the drug. Transmission electron microscopy revealed the spherical shape of the nanogel particles. The drug-loaded nanogel was characterized with a small diameter of 29 nm, narrow polydispersity (0.223) and positive zeta potential (+34 mV). The exposure of encapsulated doxorubicin to light (including UV irradiation and daylight) did not provoke any degradation, whereas the nonencapsulated drug was significantly degraded. In vitro studies on keratinocytes (HaCaT) and epidermoid squamous skin carcinoma cells (A-431) disclosed that the encapsulated doxorubicin was more cytotoxic on both cell lines than the pure drug was. More importantly, the cytotoxic concentration of encapsulated doxorubicin in carcinoma cells was approximately two times lower than that in keratinocytes, indicating that it would not affect them. Thus, the loading of doxorubicin into the developed chitosan-albumin nanogel definitely stabilized the drug against photodegradation and increased its antineoplastic effect on the skin cancer cell line.
在本研究中,将阿霉素负载于壳聚糖 - 白蛋白纳米凝胶中,目的是提高其稳定性,并探索该体系在皮肤癌治疗中的潜力。红外光谱和X射线衍射证实了药物的包封。透射电子显微镜显示纳米凝胶颗粒呈球形。负载药物的纳米凝胶的特征在于直径小(29nm)、多分散性窄(0.223)和正的zeta电位(+34mV)。包封的阿霉素暴露于光(包括紫外线照射和日光)下不会引起任何降解,而未包封的药物则会显著降解。对角质形成细胞(HaCaT)和表皮样鳞状皮肤癌细胞(A - 431)的体外研究表明,包封的阿霉素对两种细胞系的细胞毒性均高于纯药物。更重要的是,包封的阿霉素在癌细胞中的细胞毒性浓度比在角质形成细胞中低约两倍,表明它不会对它们产生影响。因此,将阿霉素负载到所制备的壳聚糖 - 白蛋白纳米凝胶中确实使药物对光降解具有稳定性,并增强了其对皮肤癌细胞系的抗肿瘤作用。