Abstract

Aim

To develop docetaxel (DT) and curcumin (CUR) co-loaded nanostructured lipid carriers (DTCR-NLCs) for ratiometric co-targeting to non-small cell lung carcinoma (NSCLC) cells.

Methods

The DTCR-NLCs were developed by employing a high-pressure homogenisation technique and optimised by employing a rotatable central composite design response surface methodology (RCCD-RSM) via the design of experiments (DoE) approach.

Results

The optimised DTCR-NLCs had a particle size (D90) of 150.2 ± 5.2 nm, Pdi of 0.263 ± 0.15, zeta potential of +26.3 ± 5.2 mv. The % drug loading (% DL) of DT and CUR was observed to be 1.38 ± 0.98 and 2.99 ± 1.24, respectively. Dissolution studies depicted a pH-independent drug release (≈98% drug release at 144 h). The DTCR-NLCs were stable and haemocompatible. MTT cell viability assay of DTCR-NLCs demonstrated considerably increased cytotoxicity towards NCI-H460 cells.

Conclusions

The developed DTCR-NLCs heralds the future of an efficacious and safer Taxane therapy for NSCLC.

中文翻译：

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多西紫杉醇和姜黄素共载纳米结构脂质载体的制备、优化和体外评估，以提高对非小细胞肺癌的抗肿瘤活性。

摘要

目的

开发多西紫杉醇 (DT) 和姜黄素 (CUR) 共载纳米结构脂质载体 (DTCR-NLC)，用于非小细胞肺癌 (NSCLC) 细胞的比例共靶向。

方法

DTCR-NLC 是通过采用高压均质技术开发的，并通过实验设计 (DoE) 方法采用可旋转中心复合设计响应面方法 (RCCD-RSM) 进行优化。

结果

优化后的 DTCR-NLC 的粒径 (D90) 为 150.2 ± 5.2 nm，Pdi 为 0.263 ± 0.15，zeta 电位为 +26.3 ± 5.2 mv。观察到 DT 和 CUR 的载药量 (% DL) 分别为 1.38 ± 0.98 和 2.99 ± 1.24。溶出度研究描述了不依赖于 pH 值的药物释放（在 144 小时时约 98% 的药物释放）。DTCR-NLCs 是稳定和血液相容的。DTCR-NLC 的 MTT 细胞活力测定表明对 NCI-H460 细胞的细胞毒性显着增加。

结论

开发的 DTCR-NLC 预示着一种有效且更安全的紫杉烷治疗非小细胞肺癌的未来。