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白藜芦醇和紫檀芪水芯纳米胶囊的双重组合用于集成前列腺癌靶向治疗。

Dual combination of resveratrol and pterostilbene aqueous core nanocapsules for integrated prostate cancer targeting.

机构信息

Faculty of Pharmacy, Raja Balwant Singh Engineering Technical Campus, Bichpuri, Agra, Uttar Pradesh, India.

Institute of Pharmaceutical Research (IPR), GLA University, NH-2, Delhi Mathura Road, PO- Chaumuhan, Mathura, Uttar Pradesh, India.

出版信息

Ther Deliv. 2024;15(9):685-698. doi: 10.1080/20415990.2024.2380239. Epub 2024 Aug 12.

Abstract

Development and evaluation of aqueous core nanocapsules (ACNs) of BCS-II-class drug like resveratrol (RSV) and pterostilbene (PTE) for prostate cancer. Identify synergistic effects of molar ratios of RSV and PTE against PC-3 cell. Selected ratio of drugs was added to ACNs by double-emulsification-method using Box-Behnken design. Further, assessed for physicochemical characterization, release kinetics, compatibility, cytotoxicity, pharmacokinetic and biodistribution studies. Selected 1:1 ratio of RSV and PTE had greatest synergy potential have smaller particle-size (128.1 ± 3.21 nm), zeta-potential (-22.12 ± 0.2 mV), 0.53 PDI, improved encapsulation (87% for RSV, 72% for PTE), stable, no systemic toxicity, high biodistributed/accumulated in prostate cells. ACNs exhibited high t (12.42 ± 1.92 hs) and 8.20 ± 8.21 hs Mean Residence Time and lower clearance, proving the high effectiveness for prostate cancer.

摘要

开发和评价水芯毫微粒(ACNs)的 BCS-II 类药物,如白藜芦醇(RSV)和紫檀芪(PTE),用于前列腺癌。确定 RSV 和 PTE 的摩尔比对 PC-3 细胞的协同作用。通过双乳化法,使用 Box-Behnken 设计,将选定的药物比例添加到 ACNs 中。进一步评估理化特性、释放动力学、相容性、细胞毒性、药代动力学和生物分布研究。选择 RSV 和 PTE 的 1:1 比例具有最大的协同潜力,具有较小的粒径(128.1±3.21nm)、zeta 电位(-22.12±0.2mV)、0.53PDI、提高的包封率(87%的 RSV,72%的 PTE)、稳定、无全身毒性、在前列腺细胞中高分布/积累。ACNs 表现出高 t(12.42±1.92hs)和 8.20±8.21hs 平均驻留时间和较低的清除率,证明对前列腺癌具有高疗效。

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