Wang Lei, Luo Qing, Lin Tongyuan, Li Rui, Zhu Tingting, Zhou Kai, Ji Zhaojie, Song Jiawei, Jia Buyun, Zhang Caiyun, Chen Weidong, Zhu Guangyu
The Pharmacokinetics Lab, Anhui University of Chinese Medicine , Hefei , China .
Drug Dev Ind Pharm. 2015;41(7):1204-12. doi: 10.3109/03639045.2014.938082. Epub 2014 Jul 10.
With the aim to develop a lipid nanoparticle for biochanin A (BCA) by emulsion-evaporation and low temperature-solidification technique. The results revealed that BCA-PEG-NLC not only have small mean particle (148.5 ± 2.88 nm) with narrow polydispersity index (PI) (0.153 ± 0.01), encapsulation capacity (99.62 ± 0.06%), payload (9.06 ± 0.01%), zeta potential (-19.83 ± 1.19 mV), but also slower release rate compared with BCA suspension over 48 h by the dialysis method (n=3). The crystallinity of lipid matrix within BCA-PEG-NLC was evaluated by differential scanning calorimetry (DSC) which verified the BCA successfully into the nanoparticles. Particularly, in pharmacokinetic, the BCA-PEG-NLC of Cmax values and AUC (area under curve) was higher than BCA suspension (approximately 15.8 and 2.9 times, respectively), meanwhile, the mean residence time (MRT) was significantly longer. Furthermore, in vitro cytotoxicity BCA-PEG-NLC showed higher cytotoxicity against MCF-7 cell line compared with BCA suspension. This study suggested that PEG-NLC is a novel anti-cancer nanoparticle, which could provide attractive treatment for a wide variety of tumors and improved the oral bioavailability of poorly water-soluble drug.
旨在通过乳化蒸发和低温固化技术开发一种用于生物chanin A（BCA）的脂质纳米颗粒。结果表明，BCA-PEG-NLC不仅具有小的平均粒径（148.5±2.88nm）和窄的多分散指数（PI）（0.153±0.01）、包封率（99.62±0.06%）、载药量（9.06±0.01%）、zeta电位（-19.83±1.19mV），而且通过透析法在48小时内与BCA悬浮液相比释放速率更慢（n=3）。通过差示扫描量热法（DSC）评估了BCA-PEG-NLC内脂质基质的结晶度，证实BCA成功载入纳米颗粒。特别是，在药代动力学方面，BCA-PEG-NLC的Cmax值和AUC（曲线下面积）高于BCA悬浮液（分别约为15.8倍和2.9倍），同时，平均驻留时间（MRT）明显更长。此外，体外细胞毒性实验表明，与BCA悬浮液相比，BCA-PEG-NLC对MCF-7细胞系具有更高的细胞毒性。本研究表明，PEG-NLC是一种新型抗癌纳米颗粒，可为多种肿瘤提供有吸引力的治疗方法，并提高难溶性药物的口服生物利用度。
