Tao Yang, Hongling Xu, Cheng Li, Manlin Wang, Xin Zeng, Yongjian Huang, Hongying Abamo, Qiong Man, Yaxin Zheng, Yang Li
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引用次数: 0
Abstract
The effectiveness of liposome-based antitumor drugs is significantly limited by the poor tumor accumulation of liposomes. Herein, we report that resiquimod (R848) can selectively increase tumor accumulation of 7-Ethyl-10-hydroxycamptothecin (SN38)-loaded liposomes (SN38-LIPs) without significantly altering their pharmacokinetics. R848 enhanced the tumor distribution of SN38-LIPs and free SN38 by approximately 5-fold and 10-fold, respectively. This further resulted in greatly improved in vivo antitumor activity compared with those treated with R848 or SN38-LIPs alone (tumor inhibition rate: ∼95% versus ∼50%). The increased antitumor activity was associated with increased serum TNF-α and enhanced macrophage infiltration in the tumor. These results suggested that R848 held great potential to enhance the clinical antitumor effect of nanomedicine by increasing its tumor accumulation.
期刊介绍:
Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development.
Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.