Pharmaceuticals

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Special Issue Editor

Prof. Dr. Peter Turecek

E-Mail Website1 Website2 Website3
Guest Editor

1. Shire, Vienna, Austria
2. Department of Pharmacology and Toxicology, University of Vienna, Vienna, Austria
Interests: protein modification; protein purification and characterization; plasma fractionation; virus inactivation; molecular biology; recombinant proteins; coagulation physiology; biochemical and analytical techniques; diagnostics; pharmaceutical biotechnology; pharmacology and toxicology

Special Issue Information

Dear Colleagues,

Polyethylene glycol (PEG) is a synthetic, highly water soluble, inert polymer that is produced in a wide range of molecular sizes and structures. PEGs of various molecular weights have been widely used in cosmetics, pharmaceuticals and other consumer care products. For the past 20 years, PEG has also been used for the chemical modification of drugs and particularly of biopharmaceuticals, known as PEGylation technology. Over the years, several second-generation biologicals have used PEGylation to provide pharmacologically-improved drug molecules.

There is a clear need to further improve pharmacologic and pharmaceutical properties of biopharmaceuticals to reduce treatment frequency or to allow more convenient routes of administration. As a result of its successful and safe use, many other PEGylated drugs are currently under non-clinical and clinical development. Consequently, we are seeing more PEG derivatives, enhanced PEGylation reagents, and linker and coupling chemistries, and completely new PEGylation approaches. These are applied to essentially all classes of drug molecules, biologicals, such as peptides, proteins, aptamers, and new pharmaceutical formulations and drug delivery systems, such as liposomes and nanospheres. At the same time, PEG continues to be a ubiquitously used polymer with a high exposure to humans.

In this Special Issue, we seek submissions corresponding to all aspects of PEG used in pharmaceutical and medical applications. We call for reports on methods of PEGylation, uses of PEG in various applications, synthesis of PEG derivatives—essentially all preparative work with PEG in pharmacy. Moreover, we will review analytical methods related to PEG and PEG derivatives. Manuscripts dealing with experiences of PEG in formulation and drug delivery are also welcome.

Related publications:

PEGylation of Biopharmaceuticals: A Review of Chemistry and Nonclinical Safety Information of Approved Drugs. https://www.ncbi.nlm.nih.gov/pubmed/26869412
Noncovalent PEGylation, An Innovative Subchapter in the Field of Protein Modification. https://www.ncbi.nlm.nih.gov/pubmed/26523632
Process for protein PEGylation. https://www.ncbi.nlm.nih.gov/pubmed/24531008
PEGylated Biopharmaceuticals: Current Experience and Considerations for Nonclinical Development. https://www.ncbi.nlm.nih.gov/pubmed/26239651

Prof. Dr. Peter Turecek
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

polyethylene glycol
PEG
PEGylation
Biopharmaceuticals
PEGylation chemistry

Published Papers (2 papers)

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Research

16 pages, 1091 KiB

Open AccessArticle

Polyethylene Glycol Exposure with Antihemophilic Factor (Recombinant), PEGylated (rurioctocog alfa pegol) and Other Therapies Indicated for the Pediatric Population: History and Safety

by Reinhard Stidl, Michael Denne, Jimena Goldstine, Bill Kadish, Katherine I. Korakas and Peter L. Turecek

Pharmaceuticals 2018, 11(3), 75; https://doi.org/10.3390/ph11030075 - 26 Jul 2018

Cited by 16 | Viewed by 8651

Abstract

Polyethylene glycol (PEG) is an inert, water soluble polymer, used for decades in pharmaceuticals. Although PEG is considered safe, concerns persist about the potential adverse effects of long-term exposure to PEG-containing therapies, specifically in children, following the introduction of PEGylated recombinant factor products used for the treatment of hemophilia. Given the absence of long-term surveillance data, and to evaluate the potential risk, we estimated PEG exposure in the pediatric population receiving PEGylated therapies with pediatric indications administered intravenously or intramuscularly. We used a range of pediatric weights and doses based on prescribing information (PI) or treatment guidelines. PIs and reporting websites were searched for information about adverse events (AEs). For a child weighing 50 kg on the highest prophylactic dose of a FVIII product, the range of total PEG exposure was 40–21,840 mg/year; for factor IX (FIX) products, the range was 13–1342 mg/year; and for other products, the range was 383–26,743 mg/year, primarily as a derivative excipient. No AE patterns attributable to PEG were found for any of these products, including potential renal, neurological, or hepatic AEs. Our analyses suggest the pediatric population has had substantial exposure to PEG for several decades, with no evidence of adverse consequences. Full article

(This article belongs to the Special Issue Polyethylene Glycol (PEG) and PEGylation in Pharmacy)

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16 pages, 3304 KiB

Open AccessArticle

Improved Intranasal Retentivity and Transnasal Absorption Enhancement by PEGylated Poly-l-ornithine

by Yusuke Kamiya, Tsutomu Yamaki, Shigehiro Omori, Masaki Uchida, Kazuo Ohtake, Mitsutoshi Kimura, Hiroshi Yamazaki and Hideshi Natsume

Pharmaceuticals 2018, 11(1), 9; https://doi.org/10.3390/ph11010009 - 25 Jan 2018

Cited by 9 | Viewed by 3863

Abstract

We reported that the introduction of polyethylene glycol (PEG) to poly-l-ornithine (PLO), which is an homopolymeric basic amino acid having absorption-enhancement ability, prolonged retention time in an in vitro inclined plate test, probably due to an increase in viscosity caused by PEGylation. The aim of the present study is to investigate whether the introduction of PEG chains to PLO improves intranasal retention and transnasal absorption in vivo. We performed intranasal administration experiments using PLO and PEG-PLO with a model drug, fluorescein isothiocyanate dextran (FD-4), in rats under closed and open systems. In the open system, transition of plasma FD-4 concentration after co-administration with unmodified PLO was low, and the area under the plasma concentration-time curve (AUC) decreased to about 60% of that in the closed system. In contrast, the AUC after co-administration with PEG-PLO in the open system was about 90% of that in the closed system, and the transition of plasma FD-4 concentration and FD-4 absorption profile were similar to those of the closed system. These findings indicate that introducing PEG chains to homopolymeric basic amino acids (HPBAAs) is a very useful method for developing a functional absorption enhancer that can exhibit an efficient in vivo absorption-enhancing effect. Full article

(This article belongs to the Special Issue Polyethylene Glycol (PEG) and PEGylation in Pharmacy)

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