| Literature DB >> 29509706 |
Nemany Abdelhamid Nemany Hanafy1,2, Alessandra Quarta3, Marzia Maria Ferraro4, Luciana Dini5, Concetta Nobile6, Maria Luisa De Giorgi7, Sonia Carallo8, Cinzia Citti9,10, Antonio Gaballo11, Giuseppe Cannazza12, Rosaria Rinaldi13, Gianluigi Giannelli14, Stefano Leporatti15.
Abstract
LY2157299 (LY), which is very small molecule bringing high cancer diffusion, is a pathway antagonist against TGFβ. LY dosage can be diluted by blood plasma, can be captured by immune system or it might be dissolved during digestion in gastrointestinal tract. The aim of our study is to optimize a "nano-elastic" carrier to avoid acidic pH of gastrointestinal tract, colon alkaline pH, and anti-immune recognition. Polygalacturonic acid (PgA) is not degradable in the gastrointestinal tract due to its insolubility at acidic pH. To avoid PgA solubility in the colon, we have designed its conjugation with Polyacrylic acid (PAA). PgA-PAA conjugation has enhanced their potential use for oral and injected dosage. Following these pre-requisites, novel polymeric nano-micelles derived from PgA-PAA conjugation and loading LY2157299 are developed and characterized. Efficacy, uptake and targeting against a hepatocellular carcinoma cell line (HLF) have also been demonstrated.Entities:
Keywords: Cargo-carriers; LY2157299; Liver Cancer Cells; drug delivery; nano-micelles
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Year: 2018 PMID： 29509706 PMCID： PMC5877609 DOI： 10.3390/ijms19030748
Source DB: PubMed Journal: Int J Mol Sci ISSN： 1422-0067 Impact factor: 5.923