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The present approach enumerates the effectiveness of tuftsin tagged nano-liposome for the cytosolic transport of 2,6-di-isopropylphenol-linolenic acid conjugate against liver cancer in mice. Initially, the conjugate in its free form was examined for anticancer potential on HepG2 liver cancer cells. Induction of apoptosis and suppression of migration and adhesion of HepG2 cells confirmed the effectiveness of conjugate as an anticancer agent. After this, role of the conjugate entrapped in a nano-carrier was evaluated in animal model. The nano-formulation comprising of conjugate bearing tuftsin tagged liposome was firsly characterized and then its therapeutic effect was determined. The nano-formulation had 100–130 nm size nanoparticles and showed sustained release of the conjugate in the surrounding milieu. The nano-formulation distinctly reduced the expression of COX-2, an important molecule that is vastly expressed in hepatocellular carcinoma. The utilization of in-house engineered nano-formulation was also successful in significantly up-regulating Bax and down-regulating bcl-2 gene expression eventually helping in better survival of treated mice. Histopathological analysis also revealed positive recovery of the general architecture and the violent death of cancer cells by apoptosis at tumor specific site. The site specific delivery of conjugate entrapped in tuftsin tagged liposomes was highly safe as well as efficaceous. Nano-formulation based approach showed a visible chemotherapeutic effect on liver cancer progression in experimental mice thereby making it a potential candidate for treatment of liver cancer in clinical settings. 相似文献
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Yi Peng Lu Chen Sheng Ye Yu Kang Junqing Liu Su Zeng Lushan Yu 《Asian Journal of Pharmaceutical Sciences》2020,15(2):220-236
In recent years,the continuous occurrence of multi-drug resistance in the clinic has made people pay more attention to the transporter.Changes in the expression and activity of transporters can cause corresponding changes in drug pharmacokinetics and pharmacodynamics.The drug-drug interactions(DDI)caused by transporters can seriously affect drug effectiveness and toxicity.In the development of pharmaceutical preparations,people have increasingly concerned about the effects and regulation of transporters in drug effects.To improve the targeting and physicochemical properties of drugs,the development of targeted agents is very rapid.Among them,novel nano-formulations are the best.With the continuous innovation and development of nano-formulation,its application has become more and more extensive.Nano-formulation has exerted certain advantages in the drug development based on transporters,and is also involved in the combination of targeted transporters.This review focuses on the application of novel nano-agents targeting transporters and the introduction of drug-transporter-based nano-formulations. 相似文献
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