Design, synthesis, and characterization of glycyrrhetinic acid-mediated multifunctional liver-targeting polymeric carrie
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Design, synthesis, and characterization of glycyrrhetinic acid-mediated multifunctional liver-targeting polymeric carrier materials Qingxia Guan1, Xue Zhang1, Yue Zhang1, Xin Yu1, Weibing Zhang1, Liping Wang1, Shuang Sun1, Xiuyan Li1, Yanhong Wang1, Shaowa Lv1,a), Yongji Li1,b) 1
College of Pharmacy, Heilongjiang University of Chinese Medicine, Heilongjiang 150040, China Address all correspondence to these authors. e-mail: [email protected] b) e-mail: [email protected] a)
Received: 16 September 2019; accepted: 6 April 2020
The purpose of this study was to construct a glycyrrhetinic acid (GA)-mediated, breakable, intracellular, nanoscale drug-delivery carrier via amide and esterification reactions. The structures were identified by Fouriertransformed infrared (FTIR) and 1H-nuclear magnetic resonance (1H-NMR) spectrophotometry. The compatibility and safety of the carrier were evaluated using hemolysis and cytotoxicity tests. The GA-copolymer micelle was prepared using the solvent evaporation method. FTIR and 1H-NMR detection demonstrated the successful construction of the polymer. No hemolysis occurred in any concentration of polymer within 3 h, and the hemolysis rate was less than 5%. 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) experimental results showed that the novel polymer reduced the cell survival rate and had significant cytotoxic effects. The blank nanoparticles were liquid with light blue opalescence. Transmission electron microscopy revealed that the empty micelles were uniform spheres, with an average size of 62 nm and a zeta potential of −13 mV. The novel GA-mediated polymeric carrier material developed here has the potential to effectively kill human SMMC-7721 cancer cells within 3 days when the dose is above 500 ug/mL.
Introduction Primary liver cancer is a major problem in China, and hepatocellular carcinoma (HCC) accounts for about 80% [1, 2] of cases. HCC is a type of malignant tumor occurring in the liver. The incidence of HCC is associated with hepatitis B or C viral infections of hepatocytes, the abuse of toxic chemicals, aflatoxin, drinking polluted water, alcohol abuse, liver cirrhosis, and the presence of certain trace elements. Mortality rates for HCC patients are high in both developed and developing countries. Conventional chemotherapeutic drugs used to treat cancers have some disadvantages, such as low bioavailability and short action durations. Although these agents often inhibit tumor growth, they typically also induce systemic toxicity and significant side effects; the rate of effective liver cancer treatment is less than 20% [3, 4]. It is thus vital that tumortargeting agents are developed that can target HCC cells, facilitating the selective release of drugs in or near tumor cells to specifically suppress tumor cell proliferation. In recent years,
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tumor-targeting agents have mainly included physicochemical, passive, and active targeting agents [5, 6, 7]. Physicochemical targeting preparations are based on the physical and chemical
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