Surface‐Modified LPD Nanoparticles for Tumor Targeting

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Abstract
Abstract:  We have developed a tumor‐targeted LPD formulation (liposome‐polycation‐DNA complex) for siRNA. With surface modification, the targeted, PEGylated LPD increased the delivery efficiency by four‐fold and the gene‐silencing effect by two‐ to three‐fold. Downregulation of survivin in human lung cancer cells by targeted LPD induced 90% of apoptosis and sensitized the cells to cisplatin by four‐fold. PEGylated LPD formulation also significantly improved the tumor localization of siRNA in the NCI‐H460 human lung cancer xenograft model. The tumor appeared to be the major uptake organ for siRNA formulated in surface‐modified LPD. Our encouraging results indicate that surface‐modified LPD may be a potent carrier for RNAi‐based tumor therapy.