Kazmi Imran, Al-Abbasi Fahad A, Imam Syed Sarim, Afzal Muhammad, Nadeem Muhammad Shahid, Altayb Hisham N, Alshehri Sultan
Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Pharmaceutics. 2022 Apr 3;14(4):783. doi: 10.3390/pharmaceutics14040783.
Apigenin (AGN) is a potent phytochemical with strong antioxidant and anticancer potential. But its therapeutic efficacy is limited due to its high lipophilic characteristics. Therefore, the present investigation aimed to develop AGN-loaded polymer-lipid hybrid nanoparticles (AGN-PLHNPs). Herein, we successfully developed AGN-PLHNPs and optimized them by a 33-Box-Behnken de-sign. The poly (lactic-co-glycolic acid) (PLGA; coded as F1), phospholipon 90 G (PL-90G; coded as F2), and poloxamer 188 (P-188; coded as F3) were considered as the independent factors while particle size (PS; coded as R1), entrapment efficiency (%EE; R2), and cumulative drug release (%CDR; R3) were selected as dependent responses. The average PS, %EE, and %CDR of the AGN-PLHNPs were observed in the range of 101.93 nm to 175.26 nm, 58.35% to 81.14%, and 71.21% to 93.31%, respectively. The optimized AGN-PLHNPs revealed better homogeneity (poly-dispersity index < 0.2) and colloidal stability with high zeta potential (>25 mV). It also exhibited fast release in the initial 4 h after that sustained release up to 48 h of study. Moreover, the results of both DPPH as well as ABTS assays revealed significant improvement in the antioxidant activity. Furthermore, the optimized AGN-PLHNPs exhibited enhanced cytotoxicity efficacy against MCF-7 as well as MDA-MB-231 breast cancer cell lines.
芹菜素(AGN)是一种具有强大抗氧化和抗癌潜力的有效植物化学物质。但其治疗效果因其高亲脂性特征而受到限制。因此,本研究旨在开发负载AGN的聚合物-脂质杂化纳米粒(AGN-PLHNPs)。在此,我们成功开发了AGN-PLHNPs,并通过三因素三水平的Box-Behnken设计对其进行了优化。聚(乳酸-乙醇酸)共聚物(PLGA;编码为F1)、磷脂90G(PL-90G;编码为F2)和泊洛沙姆188(P-188;编码为F3)被视为独立因素,而粒径(PS;编码为R1)、包封率(%EE;R2)和药物累积释放率(%CDR;R3)被选为相关响应指标。AGN-PLHNPs的平均粒径、%EE和%CDR分别在101.93 nm至175.26 nm、58.35%至81.14%和71.21%至93.31%范围内。优化后的AGN-PLHNPs显示出更好的均一性(多分散指数<0.2)和具有高zeta电位(>25 mV)的胶体稳定性。它在最初4小时内表现出快速释放,之后在长达48小时的研究中持续释放。此外,DPPH和ABTS试验结果均显示抗氧化活性有显著提高。此外,优化后的AGN-PLHNPs对MCF-7和MDA-MB-231乳腺癌细胞系表现出增强的细胞毒性作用。