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用于递送辣椒素的聚乳酸-羟基乙酸共聚物纳米颗粒：提高包封效率及对肝癌细胞系（HEPG2）的促凋亡活性

PLGA nanoparticles for capsaicin delivery: enhanced encapsulation efficiency and pro-apoptotic activity in HEPG2 cells.

作者信息

Mulè Chiara, Caputo Tania Mariastella, Montefusco Antonio, Romanelli Antonio Massimiliano, Caputo Ivana, Paolella Gaetana, Aliberti Anna, Cusano Andrea

机构信息

Optoelectronics Group, Department of Engineering, University of Sannio, Benevento, Italy.

Department of Chemistry and Biology, University of Salerno, Fisciano, Italy.

出版信息

Front Bioeng Biotechnol. 2025 Jul 18;13:1617022. doi: 10.3389/fbioe.2025.1617022. eCollection 2025.

DOI:10.3389/fbioe.2025.1617022
PMID:40756642
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12313566/
Abstract

INTRODUCTION

Capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide) (Cap) is a lipophilic alkaloid derived from Capsicum annuum. It was observed that Cap has an antitumoral activity in several cancer types, in particular in liver, colon and breast cancer. Actually, the use of Cap in the cancer therapy is limited by its very low bioavailability, a short half-life and side effects as mouth and stomach irritations and burning sensation. To overcome these limitations, the Cap has been encapsulated in carriers in order to reduce the adverse effect and to help the delivery in the cancer cells. In this study, we synthesized Poly(lactic co-glycolic acid) (PLGA) nanoparticles (NPs) to encapsulate Cap (PLGA-Cap), optimizing the synthetic strategy and improving its efficiency and safety. This is the first time that PLGA-Cap NPs was tested on HepG2 cells line for Hepatocellular carcinoma (HCC) therapy.

METHODS

NPs are characterized by Dynamic Light Scattering (DLS), Fourier transform infrared spectroscopy (FTIR), Morphological analysis by scanning transmission electron microscopy (STEM) and Reverse-Phase High Liquid Chromatography (RP-HPLC) to study their physicochemical properties and the best condition in terms of size, PDI and encapsulation efficiency. In vitro biological MTT assay was performed on HepG2 cells to observe the cell proliferation in response to PLGA-Cap. The apoptosis induced by Cap was evaluated the enzymatic activity of caspase 3, Bcl2 and Bax expression by Western blot and ROS activity.

RESULTS AND DISCUSSION

Our preparation showed the highest Encapsulation Efficiency (96%) reported by the literature, showing an improvement of 21% compared to what is actually reported. In vitro experiments revealed that PLGA-Cap formulation induced similar biological effects in terms of cell viability compared to free Cap. Moreover, HepG2 cancer cells treated with PLGA-Cap exhibited increased caspase 3 activity respect to those treated with free Cap.

CONCLUSION

In conclusion we demonstrated that our preparation showed an improvement in encapsulation parameters and in pro-apoptotic and anticancer activity in HepG2 cells.

摘要

引言

辣椒素（反式-8-甲基-N-香草基-6-壬酰胺）（Cap）是一种源自辣椒的亲脂性生物碱。据观察，Cap在多种癌症类型中具有抗肿瘤活性，尤其是在肝癌、结肠癌和乳腺癌中。实际上，Cap在癌症治疗中的应用受到其极低的生物利用度、短半衰期以及诸如口腔和胃部刺激、灼烧感等副作用的限制。为克服这些局限性，Cap已被封装在载体中，以减少不良反应并有助于其在癌细胞中的递送。在本研究中，我们合成了聚乳酸-羟基乙酸共聚物（PLGA）纳米颗粒（NPs）来封装Cap（PLGA-Cap），优化合成策略并提高其效率和安全性。这是首次在肝癌（HCC）治疗的HepG2细胞系上测试PLGA-Cap NPs。

方法

通过动态光散射（DLS）、傅里叶变换红外光谱（FTIR）、扫描透射电子显微镜（STEM）进行形态分析以及反相高效液相色谱（RP-HPLC）对纳米颗粒进行表征，以研究其物理化学性质以及在尺寸、多分散指数（PDI）和包封率方面的最佳条件。在HepG2细胞上进行体外生物学MTT试验，以观察对PLGA-Cap的细胞增殖反应。通过蛋白质免疫印迹法评估Cap诱导的凋亡、半胱天冬酶3的酶活性、Bcl2和Bax的表达以及活性氧（ROS）活性。

结果与讨论

我们的制剂显示出文献报道的最高包封率（96%），与实际报道相比提高了21%。体外实验表明，与游离Cap相比，PLGA-Cap制剂在细胞活力方面诱导了相似的生物学效应。此外，用PLGA-Cap处理的HepG2癌细胞相对于用游离Cap处理的细胞，半胱天冬酶3活性增加。

结论

总之，我们证明了我们的制剂在包封参数以及HepG2细胞的促凋亡和抗癌活性方面有改善。

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