The relative roles of charge and a recognition peptide in luminal targeting of colorectal cancer by fluorescent polyacrylamide

A multifactorial analysis of complex pharmaceutical platforms: an application of design of experiments to targetable polyacrylamide and ultrasound contrast agents

“…[11,10,3] For this reason, the DoE analysis was conducted on the Flu-CPAA-100 (maximal cationic charge), while Flu-CPAA-20 (minimal cationic charge) served as a control polymer that represents a minimal cell-binding competency, yet baring a sufficient cationic charge necessary for the conjugation reaction with both IR-783-S-Ph-COOH fluorophore and the VRPMPLQ recognition peptide.…”

“…In a preliminary study, it was verified that the increase in specific binding to colon cancer cells [10] as well as malignant tissues of the rat colon [3] was directly proportional to the increase in the charge density of Flu-CPAA. [10] Therefore, Flu-CPAA-100 (maximal charge density, containing 100 mol% of the cationic monomer) was tested and compared with Flu-CPAA-20 (minimal charge density, containing 20 mol% of the cationic monomer, sufficient for the conjugation reaction with the VRPMPLQ peptide and the IR-783-S-Ph-COOH). The latter was selected to serve as a control polymer; (b) the presence of the recognition peptide VRPMPLQ on the Flu-CPAA.…”

“…Frequency analysis of the in vivo studies (polymers specific binding to malignant tissues in the rat colon, the cationic charge density of the CPAA can identify metastatic stage in colon cancer because of the increased expression of the negatively charged sialic acid on the surface of the cancer cells. [10] Under certain circumstances the addition of a recognition peptide may improve the recognition capabilities of the system. [13,14,4] To protect the polymeric detecting platform (Flu-CPAA) from premature protein interactions we incorporated them into an exposing platform, made of PLA MBs, aimed at releasing its recognition cargo in the vicinity of the tissue of interest, under focused US insonation, in the form of polymerloaded SPF.…”

“…[9,10] Briefly, the tested polymeric products were suspended in phosphate buffered saline (PBS) and administered (500 μL each) rectally or intravenously (IV), to anesthetized rats (DMH-induced or non-treated healthy controls). In the rectal administration part of the study, 20 min after the administration, the colon of each anesthetized rat was rinsed and 3 h later the whole colons were exteriorized by laparotomy, cut open, spread on a polyethylene sheet with the mucosal aspect upwards, and imaged.…”

Synthesis and characterization of new optically active poly(acrylamide/methacrylurea-co-vinyl acetate) copolymers with dansyl units

“…[9] The method frequently used to obtain chiral polymers consists of the polymerization of optically active monomers [5,10,11] or by means of a polycondensation reaction, [2] free radical polymerization, [9] and dispersion polymerization. [12] Based on their chiral structure, the optically active poly(meth)acrylamides have found potential applications in biomedicine, [13,14] pharmacy, [15] high-performance liquid chromatography, [16] catalytic activity in asymmetric transformations, as well as high chiral recognition ability, [10,[17][18][19] and for the elimination of different environmentally toxic metal ion/counterion couples. [20] The most important reason to utilize these compounds are primarily a good biocompatibility with DNA in vitro, and secondly low cost, relatively easy copolymerization, and versatility in applications.…”