Gao Jingrong, Kumari Ankita, Zeng Xin-An, Chan Siewyin, Farooq Muhammad Adil, Alee Mahafooj, Khan Shaheer Hasan, Rahaman Abdul, He Shan, Xin Xiong, Mehmood Tariq
School of Food and Pharmacy, Zhejiang Ocean University, Zhoushan, China.
School of Food Science and Engineering, South China University of Technology, Guangzhou, China.
Front Chem. 2023 Feb 8;11:1044953. doi: 10.3389/fchem.2023.1044953. eCollection 2023.
Breast cancer is the second most common cancer around the world. Triple-negative breast cancer (TNBC) is characterized by the absence of three receptors: progesterone, estrogen, and human epidermal growth factor-2 receptor (HER2). Various synthetic chemotherapies have gained attention but they caused unwanted side effects. Therefore, some secondary therapies are now becoming famous against this disease. For instance, natural compounds have been extensively researched against many diseases. However, enzymatic degradation and low solubility remain a major concern. To combat these issues, various nanoparticles have been synthesized and optimized from time to time, which increases its solubility and hence therapeutic potential of a particular drug increases. In this study, we have synthesized Poly D,L-lactic-co-glycolic acid (PLGA) loaded thymoquinone (TQ) nanoparticle (PLGA-TQ-NPs) and then coated them by chitosan (CS) (PLGA-CS-TQ-NPs), which was characterized by different methods. Size of non-coated NPs was 105 nm with PDI value of 0.3 and the size of coated NPs was 125 nm with PDI value of 0.4. Encapsulation efficiency (EE%) and Drug loading (DL%) was found to be 70.5 ± 2.33 and 3.38 for non-coated and 82.3 ± 3.11 and 2.66 for coated NPs respectively. We have also analysed their cell viability against MDA-MB-231 and SUM-149 TNBC cell lines. The resultant, nanoformulations exhibit anti-cancerous activity in a dose and time-dependent manner for MDA-MB-231 and SUM-149 cell lines with an IC value of (10.31 ± 1.15, 15.60 ± 1.25, 28.01 ± 1.24) and (23.54 ± 1.24, 22.37 ± 1.25, 35 ± 1.27) for TQ free, PLGA-TQ-NPs and PLGA-CS-TQ-NPs respectively. For the first time, we have developed a nanoformulations of PLGA loaded TQ coated with CS NPs (PLGA-CS-TQ-NPs) against TNBC which led to their enhanced anti-cancerous effects.
乳腺癌是全球第二常见的癌症。三阴性乳腺癌（TNBC）的特征是缺乏三种受体：孕激素、雌激素和人表皮生长因子-2受体（HER2）。各种合成化疗方法受到了关注，但它们会产生不良副作用。因此，一些二线治疗方法现在在对抗这种疾病方面越来越出名。例如，天然化合物已针对多种疾病进行了广泛研究。然而，酶降解和低溶解度仍然是一个主要问题。为了解决这些问题，人们不时地合成并优化了各种纳米颗粒，这增加了其溶解度，从而提高了特定药物的治疗潜力。在本研究中，我们合成了负载百里醌（TQ）的聚D，L-乳酸-乙醇酸共聚物（PLGA）纳米颗粒（PLGA-TQ-NPs），然后用壳聚糖（CS）对其进行包覆（PLGA-CS-TQ-NPs），并通过不同方法对其进行了表征。未包覆纳米颗粒的尺寸为105nm，PDI值为0.3，包覆纳米颗粒的尺寸为125nm，PDI值为0.4。未包覆纳米颗粒的包封率（EE%）和载药量（DL%）分别为70.5±2.33和3.38，包覆纳米颗粒的包封率和载药量分别为82.3±3.11和2.66。我们还分析了它们对MDA-MB-231和SUM-149 TNBC细胞系的细胞活力。结果表明，纳米制剂对MDA-MB-231和SUM-149细胞系具有剂量和时间依赖性的抗癌活性，TQ游离物、PLGA-TQ-NPs和PLGA-CS-TQ-NPs的IC值分别为（10.31±1.15、15.60±1.25、28.01±1.24）和（23.54±1.24、22.37±1.25、35±1.27）。我们首次开发了一种负载TQ并包覆CS纳米颗粒的PLGA纳米制剂（PLGA-CS-TQ-NPs）用于对抗TNBC，这增强了它们的抗癌效果。
