Studies on PEG-modified SLNs loading vinorelbine bitartrate (I): Preparation and evaluation in vitro

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• 作者：Feng Wan ; Jian You ; Yu Sun ; Xing-Guo Zhang ; Fu-De Cui ; Yong-Zhong Du ; Hong Yuan ; Fu-Qiang Hu
• 关键词：PEG-modified SLNs ; Vinorelbine bitartrate ; Cellular uptake ; Anticancer activity
• 刊名：International Journal of Pharmaceutics
• 出版年：2008
• 期刊代码：24_03785173
• 类别：pha
• 出版时间：9 July 2008
• 卷：359
• 期：1-2
• 页码：104-110
• 文件大小：4783 K

摘要

In this study, the conjugate of PEG₂₀₀₀–stearic acid (PEG₂₀₀₀–SA) was used to prepare PEGylated solid lipid nanoparticles loading vinorelbine bitartrate (VB-pSLNs) by cold homogenization technique. The particle size and zeta potential of resulted VB-pSLNs ranged 180–250 nm and 0–10 mV, which were determined using a Zetasizer, respectively. Although the drug entrapment efficiency (EE) slightly decreased after the PEG modification of VB-SLNs, above 60%EE could be reached. The drug release tests in vitro indicated the faster drug release from VB-pSLNs than that from VB-SLNs without PEG modification. To investigate the cellular uptake of VB-pSLNs, the chemical conjugate of octadecylamine-fluorescein isothiocynate (FITC-ODA) was synthesized, and was used as a fluorescence marker to incorporate into nanoparticles. The results from cellular uptake indicated that the phagocytosis of VB-pSLNs by RAW264.7 cells was inhibited effectively by the PEG modification of SLNs, while the uptake by cancer cells (MCF-7 and A549) could be improved significantly. The assay of anticancer activity in vitro demonstrated that the anticancer activity of VB was significantly enhanced by the encapsulation of SLNs and pSLNs due to the increased cellular internalization of drug. The results suggested that SLNs and pSLNs could be excellent carrier candidates to entrap VB for tumor chemotherapeutics.