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Int J Mol Sci. 2018 Mar 6;19(3). pii: E748. doi: 10.3390/ijms19030748.

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

Author information

1
CNR NANOTEC-Istituto di Nanotecnologia, Via Monteroni, 73100 Lecce, Italy. nemany.hanafy@nanotec.cnr.it.
2
Department of Mathematics and Physics "E. De Giorgi", University of Salento, Via Monteroni, 73100 Lecce, Italy. nemany.hanafy@nanotec.cnr.it.
3
CNR NANOTEC-Istituto di Nanotecnologia, Via Monteroni, 73100 Lecce, Italy. alessandra.quarta@nanotec.cnr.it.
4
Department of Biological and Environmental Sciences and Technologies (DiSTeBA), University of Salento, Via Monteroni, 73100 Lecce, Italy. marzia.mferraro@gmail.com.
5
Department of Biological and Environmental Sciences and Technologies (DiSTeBA), University of Salento, Via Monteroni, 73100 Lecce, Italy. luciana.dini@unisalento.it.
6
CNR NANOTEC-Istituto di Nanotecnologia, Via Monteroni, 73100 Lecce, Italy. concetta.nobile@nanotec.cnr.it.
7
Department of Mathematics and Physics "E. De Giorgi", University of Salento, Via Monteroni, 73100 Lecce, Italy. marialuisa.degiorgi@unisalento.it.
8
CNR NANOTEC-Istituto di Nanotecnologia, Via Monteroni, 73100 Lecce, Italy. sonia.carallo@nanotec.cnr.it.
9
CNR NANOTEC-Istituto di Nanotecnologia, Via Monteroni, 73100 Lecce, Italy. cinzia.citti@gmail.com.
10
Department of Biological and Environmental Sciences and Technologies (DiSTeBA), University of Salento, Via Monteroni, 73100 Lecce, Italy. cinzia.citti@gmail.com.
11
CNR NANOTEC-Istituto di Nanotecnologia, Via Monteroni, 73100 Lecce, Italy. antonio.gaballo@nanotec.cnr.it.
12
Life Science Department, University of Modena e Reggio Emilia, Via G. Campi, 41125 Modena, Italy. giuseppe.cannazza@unimore.it.
13
Department of Mathematics and Physics "E. De Giorgi", University of Salento, Via Monteroni, 73100 Lecce, Italy. ross.rinaldi@unisalento.it.
14
National Institute of Gastroenterology "S. De Bellis" Research Hospital, Via Turi, 70013 Castellana Grotte (BA), Italy. gianluigi.giannelli@irccsdebellis.it.
15
CNR NANOTEC-Istituto di Nanotecnologia, Via Monteroni, 73100 Lecce, Italy. stefano.leporatti@nanotec.cnr.it.

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.

KEYWORDS:

Cargo-carriers; LY2157299; Liver Cancer Cells; drug delivery; nano-micelles

PMID:
29509706
PMCID:
PMC5877609
DOI:
10.3390/ijms19030748
[Indexed for MEDLINE]
Free PMC Article

Conflict of interest statement

The abstract of this paper was presented at the 50th Annual Scientific Meeting of the European Society for Clinical Investigation in Paris as a poster presentation with interim findings. The poster’s abstract was published in “Poster Abstracts” in EUROPEAN JOURNAL OF CLINICAL INVESTIGATION, Volume: 46 Special Issue: SI Supplement: 1 Pages: 30 Meeting Abstract: 3.07 Published: APR 2016.

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