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Mycophenolate co-administration with quercetin via lipid-polymer hybrid nanoparticles for enhanced breast cancer management.
Nanomedicine: Nanotechnology, Biology and Medicine ( IF 4.2 ) Pub Date : 2019-12-26 , DOI: 10.1016/j.nano.2019.102147 Gopal Patel 1 , Neeraj Singh Thakur 2 , Varun Kushwah 3 , Mahesh D Patil 4 , Shivraj Hariram Nile 5 , Sanyog Jain 3 , Guoyin Kai 5 , Uttam Chand Banerjee 2
Nanomedicine: Nanotechnology, Biology and Medicine ( IF 4.2 ) Pub Date : 2019-12-26 , DOI: 10.1016/j.nano.2019.102147 Gopal Patel 1 , Neeraj Singh Thakur 2 , Varun Kushwah 3 , Mahesh D Patil 4 , Shivraj Hariram Nile 5 , Sanyog Jain 3 , Guoyin Kai 5 , Uttam Chand Banerjee 2
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Mycophenolic acid (MPA) has promising anticancer properties; however, it has limited clinical applications in vivo due to hydrophobic nature, high first-pass metabolism, lack of targeting, etc. These associated problems could be addressed by developing a suitable delivery vehicle, inhibiting the first-pass metabolism and additive/synergistic pharmacodynamic effect. Thus, MPA loaded highly stable lipid polymer hybrid nanoparticles (LPNs) were developed and investigated with the combination of quercetin (QC), a CYP 450 inhibitor cum anticancer. LPNs of MPA and QC (size; 136 ± 12 and 176 ± 35 nm, respectively) demonstrated higher cellular uptake and cytotoxicity of combination therapy (MPA-LPN + QC-LPN) compared to individual congeners in MCF-7 cells. In vivo pharmacokinetics demonstrated 2.17 fold higher T1/2 value and significantly higher pharmacodynamic activity in case of combination therapy compared to free MPA. In nutshell, the combinatory therapeutic regimen of MPA and QC could be a promising approach in improved breast cancer management.
中文翻译：
霉酚酸酯通过脂质-聚合物杂化纳米颗粒与槲皮素共同给药，可增强乳腺癌的治疗效果。
麦考酚酸（MPA）具有良好的抗癌特性；然而，由于疏水性，高首过代谢，缺乏靶向性等原因，它在体内的临床应用受到限制。这些相关的问题可以通过开发合适的递送载体，抑制首过代谢和加性/协同药代动力学来解决。影响。因此，开发了载有MPA的高度稳定的脂质聚合物杂化纳米颗粒（LPN），并结合了槲皮素（QC），一种CYP 450抑制剂和抗癌药进行了研究。与MCF-7细胞中的单个同类物相比，MPA和QC的LPN（大小；分别为136±12和176±35 nm）表现出更高的细胞摄取和联合治疗（MPA-LPN + QC-LPN）的细胞毒性。体内药代动力学证明2。与游离MPA相比，联合治疗时的T1 / 2值高17倍，药理活性显着提高。简而言之，MPA和QC的联合治疗方案可能是改善乳腺癌管理的一种有前途的方法。
更新日期：2019-12-27
中文翻译：
霉酚酸酯通过脂质-聚合物杂化纳米颗粒与槲皮素共同给药，可增强乳腺癌的治疗效果。
麦考酚酸（MPA）具有良好的抗癌特性；然而，由于疏水性，高首过代谢，缺乏靶向性等原因，它在体内的临床应用受到限制。这些相关的问题可以通过开发合适的递送载体，抑制首过代谢和加性/协同药代动力学来解决。影响。因此，开发了载有MPA的高度稳定的脂质聚合物杂化纳米颗粒（LPN），并结合了槲皮素（QC），一种CYP 450抑制剂和抗癌药进行了研究。与MCF-7细胞中的单个同类物相比，MPA和QC的LPN（大小；分别为136±12和176±35 nm）表现出更高的细胞摄取和联合治疗（MPA-LPN + QC-LPN）的细胞毒性。体内药代动力学证明2。与游离MPA相比，联合治疗时的T1 / 2值高17倍，药理活性显着提高。简而言之，MPA和QC的联合治疗方案可能是改善乳腺癌管理的一种有前途的方法。
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