Targeted nano-delivery of novel omega-3 conjugate against hepatocellular carcinoma: Regulating COX-2/bcl-2 expression in an animal model.

Journal Article

Bhat., A. A. Khan, A. M. Alanazi, M. Jabeen, I Hassan, M. A. . 2016

• المجلة \ الصحيفة: Biomedicine & Pharmacotherapy
• رقم الإصدار السنوي: 81
• الصفحات: 394-401

مستخلص المنشور

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