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Strong specificity for cancer cells is still the main challenge to deliver drugs for the therapy of cancer. Herein, we developed a convenient strategy to prepare a series of 5-boronopicolinic acid (BA) modified tumor-targeting drug delivery systems (T-DDSs) with strong tumor targeting function. An anti-tumor drug of camptothecin (CPT) was encapsulated into poly(lactide-co-glycolide)-g-polyethylenimine (PLGA-PEI) to form drug-loaded nanoparticles (NP/CPT). Then, the surface of NP/CPT was coated by BA with different polymer and BA molar ratios of 1:1, 1:5, 1:10 and 1:20 via electrostatic interaction to obtain T-DDSs with enhanced biocompatibility and specificity for tumor cells. The introduced BA can endow drug-loaded NPs with high targeting ability to tumor cells because of the overexpression of sialic acids (SA) in tumor cells, which possessed strong interaction with BA. Those T-DDSs exhibited good biocompatibility according to the results of MTT assay, hemolysis test and cellular uptake. Moreover, they were capable of decreasing the viability of breast cancer cell line 4T1 and MCF-7 cells with no obvious cytotoxicity for endothelial cells. Especially, T-DDS with 1:20 molar ratio displayed much higher cellular uptake than other groups, and also exhibited highly efficient in vivo anti-tumor effect. The significantly high targeting function and biocompatibility of T-DDSs improved their drug delivery efficiency and achieved good anti-tumor effect. The BA decorated T-DDSs provides a simple and robust strategy for the design and preparation of DDSs with good biocompatibility and strong tumor-specificity to promote drug delivery efficiency., (Copyright © 2020 Elsevier B.V. All rights reserved.)

Rheumatoid arthritis (RA) is a kind of systemic autoimmune disease, and patients with RA usually suffer serious pain, resulting in low quality of life. The development of drug delivery systems (DDSs) provides a valid approach for RA therapy via inhibiting the secretion of inflammatory cytokines from macrophages. As a prevailing drug nanocarrier with distinctive superiority, polymeric nanoparticles (NPs) have attracted much attention in recent years. However, low biocompatibility and limited exploitation of drug with high efficiency are still the main challenges in RA treatment. To overcome the limitations, we prepared a biocompatible copolymer methoxy-poly(ethylene glycol)-poly(lactide-co-glycolide) (mPEG-PLGA). Moreover, benzoylaconitine (BAC) with superior anti-inflammatory effect was selected as model drug. It was isolated from Aconitum kusnezoffii Reichb and encapsulated into mPEG-PLGA NPs (NP/BAC) to increase the bioavailablity of BAC. The NPs exhibited high cytocompatibility for activated macrophages and well compatibility with red blood cells. Furthermore, the anti-inflammatory property of NP/BAC was testified by substantially inhibiting secretion of pro-inflammatory cytokines. The TNF-α and IL-1β cytokines of NP/BAC group reduced 70 % and 66 % compared with that of activated macrophages. Especially, NP/BAC reduced the overexpression of NF-κB p65 to inhibit NF-κB signaling pathway, which was a critical regulator of inflammatory responses. NP/BAC also showed efficient in vivo anti-inflammatory effect with high ear (69.8 %) and paw (87.1 %) swelling suppressing rate. These results revealed the anti-inflammatory mechanism of NP/BAC and proved it was a suitable DDS to suppress inflammation, providing a promising strategy for RA therapy and research of Aconitum kusnezoffii Reichb., Competing Interests: Declaration of Competing Interest No conflict of interest exits in the submission of this manuscript, and the manuscript is approved by all authors for publication. I would like to declare on behalf of my co-authors that this work described was original research that has not been published previously, and not under consideration for publication elsewhere, in whole or in part. All the authors listed have approved the manuscript that is enclosed., (Copyright © 2020 Elsevier B.V. All rights reserved.)