Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Sensors (Basel). 2022 Feb 10;22(4):1364. doi: 10.3390/s22041364.
Breast cancer is the most common cancer in females and ranked second after skin cancer. The use of natural compounds is a good alternative for the treatment of breast cancer with less toxicity than synthetic drugs. The aim of the present study is to develop and characterize hybrid Apigenin (AN) Nanoparticles (NPs) for oral delivery (AN-NPs). The hybrid AN-NPs were prepared by the self-assembly method using lecithin, chitosan and TPGS. Further, the NPs were optimized by Box-Behnken design (3-factor, 3-level). The hybrid NPs were evaluated for particle size (PS), entrapment efficiency (EE), zeta potential (ZP), and drug release. The optimized hybrid NPs (ON2), were further evaluated for solid state characterization, permeation, antioxidant, cytotoxicity and antimicrobial study. The formulation (ON2) exhibited small PS of 192.6 ± 4.2 nm, high EE 69.35 ± 1.1%, zeta potential of +36.54 mV, and sustained drug release (61.5 ± 2.5% in 24 h), as well as significantly ( < 0.05) enhanced drug permeation and antioxidant activity. The IC of pure AN was found to be significantly ( < 0.05) lower than the formulation (ON2). It also showed significantly greater ( < 0.05) antibacterial activity than pure AN against and . From these findings, it revealed that a hybrid AN polymeric nanoparticle is a good carrier for the treatment of breast cancer.
乳腺癌是女性最常见的癌症，发病率仅次于皮肤癌。与合成药物相比，使用天然化合物是治疗乳腺癌的一种较好的替代方法，其毒性更小。本研究的目的是开发和表征具有口服递送（AN-NPs）的新型橙皮苷（AN）纳米粒子（NPs）。通过使用卵磷脂、壳聚糖和 TPGS 的自组装方法制备了混合的 AN-NPs。进一步，通过 Box-Behnken 设计（3 因素，3 水平）对 NPs 进行了优化。通过测定粒径（PS）、包封效率（EE）、Zeta 电位（ZP）和药物释放，对混合 NPs 进行了评价。对优化后的混合 NPs（ON2）进行了进一步的固态特性、渗透、抗氧化、细胞毒性和抗菌研究。该制剂（ON2）表现出较小的 PS（192.6 ± 4.2 nm）、高 EE（69.35 ± 1.1%）、Zeta 电位（+36.54 mV）和持续的药物释放（24 h 内释放 61.5 ± 2.5%），并且显著（ < 0.05）增强了药物渗透和抗氧化活性。纯 AN 的 IC 发现明显低于制剂（ON2）。与纯 AN 相比，它对 和 显示出更强的抗菌活性。从这些发现中，表明混合的 AN 聚合物纳米粒子是治疗乳腺癌的良好载体。
