PEGylated nanostructured lipid carriers (PEG–NLC) as a novel drug delivery system for biochanin A

• DOI: 10.3109/03639045.2014.938082
• Publication Date: 2014-07-10T14:24:19Z
• Authors: Lei Wang; Qing Luo; Tongyuan Lin; Rui Li; Tingting Zhu; Kai Zhou; Zhaojie Ji; Jiawei Song; Buyun Jia; Caiyun Zhang; Weidong Chen; Guangyu Zhu
• Keywords: 0301 basic medicine; Drug Carriers; Calorimetry, Differential Scanning; Biological Availability; Antineoplastic Agents; Genistein; Lipids; Polyethylene Glycols; Rats; 3. Good health; Rats, Sprague-Dawley; 03 medical and health sciences; Drug Delivery Systems; Solubility; Area Under Curve; MCF-7 Cells; Animals; Humans; Nanoparticles; Emulsions; Female; Particle Size; Crystallization

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.