Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi 110062, India.
Department of Pharmacy, National University of Singapore, 117559 Singapore.
Nanomedicine (Lond). 2020 Nov;15(26):2563-2583. doi: 10.2217/nnm-2020-0277. Epub 2020 Oct 20.
This study aims to load tamoxifen (TAM) and sulforaphane (SFN) into nanostructured lipid carriers (NLCs) to enhance their oral delivery. TAM-SFN-NLCs were prepared using Precirol ATO5 and Transcutol HP, characterized and evaluated and to assess the drug release profile and intestinal permeability, respectively. pharmacokinetic and acute toxicity assessment was performed in Wistar rats. Optimized TAM-SFN-NLCs exhibited a particle size of 121.9 ± 6.42 nm and zeta potential of -21.2 ± 2.91 mV. The NLCs enhanced intestinal permeability of TAM and SFN and augmented oral bioavailability of TAM and SFN 5.2-fold and 4.8-fold, respectively. SFN significantly reduced TAM-associated toxicity . This coencapsulation of a chemotherapeutic agent with a herbal bioactive in NLCs could pave a novel treatment approach against cancer.
本研究旨在将他莫昔芬(TAM)和萝卜硫素(SFN)载入纳米结构脂质载体(NLCs)中,以增强其口服递送。使用 Prectirol ATO5 和 Transcutol HP 制备 TAM-SFN-NLCs,分别进行了表征和评价,并评估了药物释放曲线和肠道通透性。在 Wistar 大鼠中进行了药代动力学和急性毒性评估。优化的 TAM-SFN-NLCs 的粒径为 121.9±6.42nm,zeta 电位为-21.2±2.91mV。NLCs 增强了 TAM 和 SFN 的肠道通透性,并分别使 TAM 和 SFN 的口服生物利用度增加了 5.2 倍和 4.8 倍。SFN 显著降低了 TAM 相关毒性。这种将化疗药物与植物生物活性物质共同包封在 NLCs 中可能为癌症治疗开辟一种新的治疗方法。