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Temozolomide-Loaded Solid Lipid Nanoparticles@Hydrogel for Local Treatment of Tumour
Australian Journal of Chemistry ( IF 1.1 ) Pub Date : 2020-07-15 , DOI: 10.1071/ch20018
Weiwei Ji , Zhilan Liu

Temozolomide (TMZ) is a significant anticancer agent especially for chemotherapy of glioblastoma. In order to reduce the recurrence rate of cancer, in this work an injectable hydrogel composed of TMZ-loaded solid lipid nanoparticles (SLNs) was designed for filling the cavity of a glioblastoma operation. First, TMZ-loaded SLNs (T-SLNs) were prepared by emulsion solvent diffusion and evaporation technology. The optimised formulation showed a particle size of 190.8 ± 15.3 nm, a Zeta potential of −20.2 ± 1.7 mV, an entrapment efficiency (EE%) of 99.3 ± 0.5 %, and drug loading (DL%) of 15.1 ± 2.7 %. The optimised formulation was freeze-dried and characterised by scanning electron microscopy (SEM), differential thermogravimetry (DTG), X-ray diffraction (XRD), and stability tests. The freeze-dried T-SLNs were then incorporated into a hydroxypropyl chitosan (HPCS)/diarylaldehyde PEG (PEG-DF) hydrogel bonded with an MRI contrast agent. The hydrogels were evaluated for in vitro drug release and cytotoxicity. The results indicated that compared with free TMZ, the T-SLNs@hydrogel prolonged drug release, and both blank SLNs and hydrogel materials did not exhibit cytotoxicity, suggesting the therapeutic efficacy of TMZ was reserved. Thus, comparing with its conventional oral administration, the obtained TMZ-loaded SLNs and the hydrogel could be more potent for local treatment of glioblastoma after an operation.



中文翻译:

替莫唑胺负载的固体脂质纳米颗粒@水凝胶用于肿瘤的局部治疗

替莫唑胺(TMZ)是一种重要的抗癌药,尤其适用于胶质母细胞瘤的化疗。为了降低癌症的复发率,在这项工作中,设计了一种由TMZ负载的固体脂质纳米颗粒(SLNs)组成的可注射水凝胶,用于填充胶质母细胞瘤手术的空腔。首先,通过乳液溶剂扩散和蒸发技术制备了负载TMZ的SLN(T-SLN)。优化的制剂显示出190.8±15.3 nm的粒径,-20.2±1.7 mV的Zeta电位,99.3±0.5%的包封效率(EE%)和15.1±2.7%的载药量(DL%)。将优化的制剂冷冻干燥并通过扫描电子显微镜(SEM),差示热重分析(DTG),X射线衍射(XRD)和稳定性测试进行表征。然后将冻干的T-SLNs掺入与MRI造影剂结合的羟丙基壳聚糖(HPCS)/二芳基醛PEG(PEG-DF)水凝胶中。评价了水凝胶的体外药物释放和细胞毒性。结果表明,与游离TMZ相比,T-SLNs @水凝胶可延长药物释放,空白的SLNs和水凝胶材料均无细胞毒性,提示保留了TMZ的疗效。因此,与常规的口服给药相比,所获得的TMZ负载的SLN和水凝胶对于术后胶质母细胞瘤的局部治疗可能更有效。T-SLNs @水凝胶延长了药物的释放,空白的SLNs和水凝胶材料均未显示出细胞毒性,表明保留了TMZ的治疗功效。因此,与常规的口服给药相比,所获得的TMZ负载的SLN和水凝胶对于术后胶质母细胞瘤的局部治疗可能更有效。T-SLNs @水凝胶延长了药物的释放,空白的SLNs和水凝胶材料均未显示出细胞毒性,表明保留了TMZ的治疗功效。因此,与常规的口服给药相比,所获得的TMZ负载的SLN和水凝胶对于术后胶质母细胞瘤的局部治疗可能更有效。

更新日期:2020-08-20
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