Dipartimento di Scienze della Salute, Università del Piemonte Orientale, Via Solaroli, 17, 28100 Novara, Italy.
Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via Pietro Giuria 9, 10124 Torino, Italy.
Int J Mol Sci. 2018 Jan 24;19(2):255. doi: 10.3390/ijms19020255.
AIM: To develop an innovative delivery system for temozolomide (TMZ) in solid lipid nanoparticles (SLN), which has been preliminarily investigated for the treatment of melanoma. MATERIALS AND METHODS: SLN-TMZ was obtained through fatty acid coacervation. Its pharmacological effects were assessed and compared with free TMZ in in vitro and in vivo models of melanoma and glioblastoma. RESULTS: Compared to the standard free TMZ, SLN-TMZ exerted larger effects, when cell proliferation of melanoma cells, and neoangiogeneis were evaluated. SLN-TMZ also inhibited growth and vascularization of B16-F10 melanoma in C57/BL6 mice, without apparent toxic effects. CONCLUSION: SLN could be a promising strategy for the delivery of TMZ, allowing an increased stability of the drug and thereby its employment in the treatment of aggressive malignacies.
目的:开发替莫唑胺(TMZ)的固体脂质纳米粒(SLN)新型递药系统,该系统初步用于治疗黑色素瘤。
材料与方法:通过脂肪酸共凝聚法获得 SLN-TMZ。评估其在黑色素瘤和神经胶质瘤的体外和体内模型中的药效,并与游离 TMZ 进行比较。
结果:与标准游离 TMZ 相比,当评估黑色素瘤细胞的细胞增殖和新生血管生成时,SLN-TMZ 发挥了更大的作用。SLN-TMZ 还能抑制 C57/BL6 小鼠中 B16-F10 黑色素瘤的生长和血管生成,且无明显毒性作用。
结论:SLN 可能是 TMZ 递药的一种有前途的策略,增加了药物的稳定性,从而可用于治疗侵袭性恶性肿瘤。
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