@article { author = {Ahmed, Hanaa and Galal, Asmaa F and Shalby, Aziza B and Abd-Rabou, Ahmed A and Mehaya, Fathy M}, title = {Improving Anti-Cancer Potentiality and Bioavailability of Gallic Acid by Designing Polymeric Nanocomposite Formulation}, journal = {Asian Pacific Journal of Cancer Prevention}, volume = {19}, number = {11}, pages = {3137-3146}, year = {2018}, publisher = {West Asia Organization for Cancer Prevention (WAOCP), APOCP's West Asia Chapter.}, issn = {1513-7368}, eissn = {2476-762X}, doi = {10.31557/APJCP.2018.19.11.3137}, abstract = {Objective: In this study, we investigated the in vivo antitumor activity and pharmacokinetic characteristics ofencapsulated GA-NC (gallic acid nanocomposite) in normal and hepatocellular carcinoma (HCC)-induced rats.Methods: Rats were distributed into 4 groups; negative control, HCC, gallic acid (GA), and GA-NC. Serum levels ofalpha-fetoprotein (AFP), endoglin (ENG), heat shock protein-70 (HSP-70), pro-caspase 3, lipocalin-2 (LCN-2) andβ-cell leukemia/lymphoma 2 (Bcl-2) were assayed by ELISA. The pharmacokinetic parameters for GA or GA-NCwere determined by means of non-compartmental approach based on the serum– concentration profiles of free GAand GA-NC after oral administration. Also, histological procedures were used for examination of liver tissue sections.Results: Anaplastic changes in liver tissues were observed in untreated HCC group, as well as a significant increasein the serum AFP level. In addition, significant elevation in the serum ENG level as an angiogenic marker and theserum levels of the apoptotic mediators; HSP-70, Bcl-2 and pro-caspase 3 beside significant amplification in the seruminflammatory modulator, LCN-2 were recorded. Treatment with free GA or GA-NC markedly recovered the anaplasticchanges in the rat liver tissues. In addition, they restored serum levels of AFP, ENG, HSP-70, Bcl-2, pro-caspase-3,and LCN-2. Pharmacokinetic analysis revealed that GA–NC displayed a characteristic sustained release profile with4-fold increase in bioavailability in normal and HCC-induced rats. Conclusions: The results of this study suggest thatencapsulation of GA into PLGA-CS-PEG enhances its oral bioavailability and anti-cancer activity. GA-NC may bea new therapeutic candidate for the mitigation of hepatocarcinogenesis.}, keywords = {Gallic acid,gallic acid nanocomposite,anti-cancer,pharmacokinetic,bioavailability}, url = {https://journal.waocp.org/article_73908.html}, eprint = {https://journal.waocp.org/article_73908_2ca79e2716b497094515799fff0446a1.pdf} }