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      Micellar Carriers of Active Substances Based on Amphiphilic PEG/PDMS Heterograft Copolymers: Synthesis and Biological Evaluation of Safe Use on Skin

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          Abstract

          Amphiphilic copolymers containing polydimethylsiloxane (PDMS) and polyethylene glycol methyl ether (MPEG) were obtained via an azide-alkyne cycloaddition reaction between alkyne-functionalized copolymer of MPEG methacrylate and azide-functionalized PDMS. “Click” reactions were carried out with an efficiency of 33–47% increasing grafting degrees. The grafted copolymers were able to carry out the micellization and encapsulation of active substances, such as vitamin C (VitC), ferulic acid (FA) and arginine (ARG) with drug loading content (DLC) in the range of 2–68% (VitC), and 51–89% (FA or ARG). In vitro release studies (phosphate buffer saline, PBS; pH = 7.4 or 5.5) demonstrated that the maximum release of active substances was mainly after 1–2 h. The permeability of released active substances through membrane mimicking skin evaluated by transdermal tests in Franz diffusion cells indicated slight diffusion into the solution (2–16%) and their remaining in the membrane. Studies on the selected carrier with FA showed no negative effect on cell viability, proliferation capacity or senescence, as well as cell apoptosis/necrosis differences or cell cycle interruption in comparison with control cells. These results indicated that the presented micellar systems are good candidates for carriers of cosmetic substances according to physicochemical characterization and biological studies.

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          Most cited references44

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          Cytotoxicity study of polyethylene glycol derivatives

          Cytotoxicity of PEG oligomers (with different molecular weights) and PEG based monomers (with different chain end groups) was studied in detail. Polyethylene glycol (PEG) derivatives have been widely used in bio-related research. However, PEG oligomers (with different molecular weights) or PEG based monomers (with different chain end groups) actually have different chemical and physical properties, which might lead to potential toxicity. In this work, the cytotoxicity of a series of PEG derivatives (oligomers and monomers) has been measured using human cervical cancer cells (HeLa) and a cell line of fibroblasts derived from mice (L929) as model cells. Most of the PEG oligomers are safe to both types of cells except triethylene glycol (TEG), which is toxic at high concentrations to L929 cells. On the other hand, PEG-based monomers including poly(ethylene glycol) methyl ether acrylate (mPEGA) and poly(ethylene glycol) methyl ether methacrylate (mPEGMA) showed obvious cytotoxicity. Subsequently, those toxic PEG derivatives have been studied to reveal the different mechanisms of their toxicity. This current research evaluated the cytotoxicity of PEG derivatives and pointed out the potential hazard of ‘safe’ biomaterials, which might offer a useful reference for people to use the PEG derivatives in future biomedical research.
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            Controlled release of cisplatin from pH-thermal dual responsive nanogels.

            In this study, a pH-thermal dual responsive nanogel was applied for cisplatin (CDDP) delivery. CDDP was loaded into the nanogels via conjugation with the carboxyl groups in the nanogels. The conjugation was confirmed by FTIR and XPS. The bonding between CDDP and COOH can be broken by the H(+) or Cl(-). We found that the CDDP released much faster at more acidic environment. The Cl(-) concentration in the human body is about 95-105 mm. The conjugated bond could be easily attacked by Cl(-) while the nanosystem is injected into the body. In order to diminish the Cl(-) triggering release of CDDP from the nanogels, we introduced a thermal-responsive units-NIPAm into the nanogel structure. After NIPAm introduced, the CDDP released much slower from the nanogels at 37 °C in pH = 7.38 buffer in the present of Cl(-) (150 mm) than that without NIPAm. And the CDDP also released slower from the nanogels at 37 °C than at 25 °C. By in vitro release behavior studying, we found that CDDP release from the NIPAm containing nanogels can be accelerated by H(+) attacking and reduced by temperature arising. By cellular uptake observation, we found that the nanogels were mainly localized in the cytoplasm of the cancer cells. The CDDP-loaded nanogels exhibited longer circulation time in vivo while compared to free CDDP. And it has better anti-cancer performance than free CDDP in vivo therapy of breast cancer in mice model. Furthermore, some side effects of CDDP, such as renal toxicity, phlebitis, bone marrow suppression etc. have also been reduced by nanogels loading. The in vitro and in vivo results demonstrated that the dual responsible nanogel is a suitable CDDP delivery candidate.
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              In situ growth of side-chain PEG polymers from functionalized human growth hormone-a new technique for preparation of enhanced protein-polymer conjugates.

              The application of atom transfer radical polymerization (ATRP) for preparation of a novel class of protein-polymer bioconjugates is described, exemplified by the synthesis of a recombinant human growth hormone (rh-GH) poly(ethylene glycol) methyl ether methacrylate (PEGMA) hybrid. The rh-GH protein was activated via a bromo-ester functionalized linker and used as a macroinitiator to polymerize the hydrophilic monomer PEGMA under solely aqueous conditions at 4 degrees C. ATRP conditions resulted in controlled polymer growth from rh-GH with low-polydispersity polyPEGMA chains. The rh-GH PEGMA product exhibited properties consistent with the presence of attached hydrophilic polymer chains, namely, high stability to denaturation and proteolysis. The polymerization conditions and conjugation proceeded with retention of the biological activity of the hormone. The rh-GH PEGMA was administered subcutaneously to rats and the activity compared to native rh-GH. The rh-GH PEGMA exhibited similar activity as the native rh-GH in vivo when a daily dose of 40 microg was administered. However, when a higher dose of 120 microg was administered with 3 days between injections the bioavailability of the rh-GH PEGMA was significantly better than that of the native. The results therefore demonstrate that ATRP can be successfully used as a general alternative approach to direct polymer conjugation, namely, PEGylation, to produce PEG-like protein conjugates. This technique can be exploited to design and synthesize protein-polymer derivatives with tailored therapeutic properties.
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                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Int J Mol Sci
                Int J Mol Sci
                ijms
                International Journal of Molecular Sciences
                MDPI
                1422-0067
                26 January 2021
                February 2021
                : 22
                : 3
                : 1202
                Affiliations
                [1 ]Department of Physical Chemistry and Technology of Polymers, Faculty of Chemistry, Silesian University of Technology, 44-100 Gliwice, Poland; justyna.odrobinska@ 123456polsl.pl
                [2 ]Department of Systems Biology and Engineering, Silesian University of Technology, Akademicka 16, 44-100 Gliwice, Poland; Magdalena.Skonieczna@ 123456polsl.pl
                [3 ]Biotechnology Centre, Silesian University of Technology, Krzywoustego 8, 44-100 Gliwice, Poland
                Author notes
                [* ]Correspondence: dneugebauer@ 123456polsl.pl
                Author information
                https://orcid.org/0000-0002-3448-8898
                https://orcid.org/0000-0002-6263-9585
                https://orcid.org/0000-0002-3802-744X
                Article
                ijms-22-01202
                10.3390/ijms22031202
                7865956
                33530445
                e2e501ba-0c78-426b-8b48-83ca37651ce3
                © 2021 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 28 December 2020
                : 22 January 2021
                Categories
                Article

                Molecular biology
                polydimethylsiloxane,heterografted copolymers,micellar carriers,franz diffusion cells,cytotoxicity

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