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Journal of Drug Delivery Science and Technology

Journal of Drug Delivery Science and Technology

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mPEG-PDLLA polymeric micelles loading a novel pyridazinone derivative IMB5036 for improving anti-tumor activity in hepatocellular carcinoma

Published:29 October 2023 DOI: 10.1016/j.jddst.2023.105101
Yanqun Dong , Yijia Zheng , Junyi Zhang , Xing Lv , Hanyu Hong , Yanbo Zheng , Ruiqi Wang , Jianhua Gong

Abstract

IMB5036 (N7) is a hydrophobic pyridazinone compound with antitumor activity, identified in our laboratory. To increase its water solubility, we utilized nanomicelles encapsulating N7 in this study. Monomethyl polyethylene glycol-polylactic acid (mPEG-PDLLA) polymer micelles were employed as drug carrier, and their characterizations were measured. IMB5036/mPEG-PDLLA (N7M) exhibited a particle size of approximately 28?nm and a polydispersity index of around 0.2. The optimal dosage ratio of N7 to mPEG-PDLLA was determined to be 10:90, with an encapsulation rate of (93.66?±?3.94)% and a drug loading efficiency of (9.59?±?1.26)%. The morphology of N7 micelles was spherical, with a uniform particle size distribution and good water solubility of approximately 1.17?mg/ml. Compared to the free drug, N7M demonstrated a higher tumor cell uptake rate and slow release profile, while maintaining similar tumor cell killing ability and apoptosis-inducing capacity. In vivo experiments confirmed that the nanomicelles improved tumor targeting, and N7M effectively inhibited tumor growth in a hepatoma xenograft model. Overall, N7M represents a successful injectable nanomicelle formulation for the treatment of hepatoma.

Substances (4)

Materials
Procduct Name CAS Molecular Formula Supplier Price
Coumarin 6 38215-36-0 C20H18N2O2S 278 suppliers $10.00-$807.00
Coumarin 6 38215-36-0 C20H18N2O2S 278 suppliers $10.00-$807.00
Coumarin 6 38215-36-0 C20H18N2O2S 278 suppliers $10.00-$807.00
Coumarin 6 38215-36-0 C20H18N2O2S 278 suppliers $10.00-$807.00

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