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Int. J. Mol. Sci. 2018, 19(3), 748;

Polymeric Nano-Micelles as Novel Cargo-Carriers for LY2157299 Liver Cancer Cells Delivery

CNR NANOTEC-Istituto di Nanotecnologia, Via Monteroni, 73100 Lecce, Italy
Department of Mathematics and Physics “E. De Giorgi”, University of Salento, Via Monteroni, 73100 Lecce, Italy
Department of Biological and Environmental Sciences and Technologies (DiSTeBA), University of Salento, Via Monteroni, 73100 Lecce, Italy
Life Science Department, University of Modena e Reggio Emilia, Via G. Campi, 41125 Modena, Italy
National Institute of Gastroenterology “S. De Bellis” Research Hospital, Via Turi, 70013 Castellana Grotte (BA), Italy
Author to whom correspondence should be addressed.
Current Address: Sohag Cancer Center, Garb District, Sohag City, Egypt and Institute of Nanoscience and Nanotechnology, Kafrelsheikh University, 33516 Kafr ElSheikh, Egypt.
Received: 15 February 2018 / Revised: 1 March 2018 / Accepted: 3 March 2018 / Published: 6 March 2018
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
PDF [7773 KB, uploaded 6 March 2018]


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. View Full-Text
Keywords: nano-micelles; Cargo-carriers; LY2157299; Liver Cancer Cells; drug delivery nano-micelles; Cargo-carriers; LY2157299; Liver Cancer Cells; drug delivery

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Hanafy, N.A.N.; Quarta, A.; Ferraro, M.M.; Dini, L.; Nobile, C.; De Giorgi, M.L.; Carallo, S.; Citti, C.; Gaballo, A.; Cannazza, G.; Rinaldi, R.; Giannelli, G.; Leporatti, S. Polymeric Nano-Micelles as Novel Cargo-Carriers for LY2157299 Liver Cancer Cells Delivery. Int. J. Mol. Sci. 2018, 19, 748.

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