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Pharmaceutics
Special Issues
PEGylation in Drug Delivery Systems
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PEGylation in Drug Delivery Systems

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (31 October 2020) | Viewed by 18793

Special Issue Editors

Prof. Dr. Kang Choon Lee

E-Mail Website
Guest Editor
College of Pharmacy, Sungkyunkwan University, Suwon, Korea
Interests: PEGylation; bioconjugation; protein/peptide delivery; oral peptide delivery
Prof. Dr. Dong Hee Na

E-Mail Website
Guest Editor
College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea
Interests: PEGylation; protein stability; nanomedicine; dendrimers; targeted drug delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

PEGylation is a pharmaceutical technology that attaches polyethylene glycol (PEG) to therapeutic molecules or drug carriers and results in improving their pharmaceutical properties. In the case of drug conjugates, the enlargement of the molecular size due to PEGylation leads to reduced renal excretion resulting in a prolonged circulation time of drugs. PEG coating of drug carriers has been a useful approach to avoid immune system recognition followed by rapid clearance from the body. Since the first PEGylated enzyme products appeared on the market in the early 1990s, currently over 15 PEGylated products have been approved and launched.

This Special Issue of Pharmaceutics focuses on PEGylation approaches for the development of novel drug conjugates and stealth drug carriers for drug delivery. We welcome articles dealing with all aspects of PEGylation technologies in drug delivery systems and invite researchers in academia and industry to publish their original research work or review articles containing expert opinions and perspectives for PEGylation technology.

Prof. Dr. Kang Choon Lee
Prof. Dr. Dong Hee Na
Guest Editors

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. Pharmaceutics 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

  • PEGylation
  • proteins
  • peptides
  • aptamers
  • stability
  • long-acting formulation
  • nanocarriers
  • nanomedicine
  • PEGylated dendrimers
  • stealth liposomes
  • biopolymers

Published Papers (5 papers)

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Research

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19 pages, 4729 KiB  
Article
Immunostimulating RNA Delivered by P1500 PEGylated Cationic Liposomes Limits Influenza Infection in C57Bl/6 Mice
by Elena P. Goncharova, Aleksandra V. Sen‘kova, Innokenty A. Savin, Tat‘yana O. Kabilova, Marina A. Zenkova, Valentin V. Vlassov and Elena L. Chernolovskaya
Pharmaceutics 2020, 12(9), 875; https://doi.org/10.3390/pharmaceutics12090875 - 14 Sep 2020
Cited by 5 | Viewed by 2291
Abstract
The emergence of highly pathogenic viruses and a high speed of infection spread put forward the problem of the development of novel antivirals and their delivery vehicles. In this study, we investigated the antiviral effect of the previously identified immunostimulatory 19-bp dsRNA (isRNA) [...] Read more.
The emergence of highly pathogenic viruses and a high speed of infection spread put forward the problem of the development of novel antivirals and their delivery vehicles. In this study, we investigated the antiviral effect of the previously identified immunostimulatory 19-bp dsRNA (isRNA) with 3′-nucleotide overhangs, which stimulates interferon α synthesis when delivered using cationic liposomes consisting of 1,26-bis(cholest-5-en-3β-yloxycarbonylamino)-7,11,16,20-tetraazahexacosan tetrahydrochloride and lipid-helper dioleoylphosphatidylethanolamine and its PEGylated formulation P1500 in vitro and in vivo. In vitro data showed that isRNA/2X3-DOPE complexes protected L929 cells from encephalomyocarditis virus infection, while isRNA/P1500 complexes were not active, which correlates with their lower transfection activity in cell culture. Comparison of the interferon-inducing activity of isRNA in BALB/c, CBA and C57Bl/6 mice showed that PEGylated liposomes significantly enhance the interferon-inducing activity of isRNA in vivo. The antiviral efficacy of the isRNA in vivo was considerably affected by the delivery system. The cationic liposomes 2X3-DOPE did not enhance the antiviral properties of isRNA in vivo. Similar liposomes equipped with a PEGylated lipoconjugate provided a pronounced anti-influenza effect of the isRNA in vivo. Administration of isRNA to C57Bl/6 led to a decrease in virus titers in the lungs and a significant decrease in the severity of the infection. Administration of a similar formulation to BALB/c mice caused only a mild antiviral effect at the initial stages of the infection. The data show that isRNA in combination with the PEGylated delivery system can be considered an effective means of suppressing influenza A infection. Full article
(This article belongs to the Special Issue PEGylation in Drug Delivery Systems)
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14 pages, 2675 KiB  
Article
Preparation and Evaluation of Eudragit L100-PEG Proliponiosomes for Enhanced Oral Delivery of Celecoxib
by Min-Hwan Kim, Dong Hyun Kim, Duy-Thuc Nguyen, Han Sol Lee, Nae-Won Kang, Min-Jun Baek, Jiseon An, So-Yeol Yoo, Yong-Hyeon Mun, Wonhwa Lee, Ki-Taek Kim, Cheong-Weon Cho, Jae-Young Lee and Dae-Duk Kim
Pharmaceutics 2020, 12(8), 718; https://doi.org/10.3390/pharmaceutics12080718 - 30 Jul 2020
Cited by 6 | Viewed by 3273
Abstract
PEGylated Eudragit L100 (ELP)-containing proliponiosomes (PLNs) were developed for improved oral delivery of celecoxib (CXB). The successful introduction of PEG 2000 or 5000 to Eudragit L100 (EL) was confirmed via proton nuclear magnetic resonance analysis of which calculated molar substitution ratio of PEG [...] Read more.
PEGylated Eudragit L100 (ELP)-containing proliponiosomes (PLNs) were developed for improved oral delivery of celecoxib (CXB). The successful introduction of PEG 2000 or 5000 to Eudragit L100 (EL) was confirmed via proton nuclear magnetic resonance analysis of which calculated molar substitution ratio of PEG to EL was 36.0 or 36.7, respectively. CXB, ELP, phospholipid, and non-ionic surfactants were dissolved in dimethyl sulfoxide and lyophilized to produce CXB-loaded PLNs (CXB@PLNs). The physical state of CXB@PLNs was evaluated using differential scanning calorimetry and powder X-ray diffractometry, which revealed that crystalline CXB was transformed into amorphous form after the fabrication procedure. The reconstitution of CXB@PLNs in aqueous media generated CXB-loaded liponiosomes with nano-sized mean diameters and spherical morphology. CXB@PLNs displayed enhanced dissolution rate and permeability compared to CXB suspension. In vivo pharmacokinetic studies performed on rats demonstrated the improved oral bioavailability of CXB@PLNs compared to that of CXB suspension. No serious systemic toxicity was observed in the blood biochemistry tests performed on rats. These results suggest that the developed PLNs could be promising oral delivery systems for improving the bioavailability of poorly water-soluble drugs, such as CXB. Full article
(This article belongs to the Special Issue PEGylation in Drug Delivery Systems)
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13 pages, 1908 KiB  
Article
A Novel Star Like Eight-Arm Polyethylene Glycol-Deferoxamine Conjugate for Iron Overload Therapy
by Bohong Yu, Yinxian Yang, Qi Liu, Aiyan Zhan, Yang Yang and Hongzhuo Liu
Pharmaceutics 2020, 12(4), 329; https://doi.org/10.3390/pharmaceutics12040329 - 07 Apr 2020
Cited by 7 | Viewed by 3418
Abstract
The traditional iron chelator deferoxamine (DFO) has been widely used in the treatment of iron overload disease. However, DFO has congenital disadvantages, including a very short circular time and non-negligible toxicity. Herein, we designed a novel multi-arm conjugate for prolonging DFO duration in [...] Read more.
The traditional iron chelator deferoxamine (DFO) has been widely used in the treatment of iron overload disease. However, DFO has congenital disadvantages, including a very short circular time and non-negligible toxicity. Herein, we designed a novel multi-arm conjugate for prolonging DFO duration in vivo and reducing cytotoxicity. The star-like 8-arm-polyethylene glycol (8-arm-PEG) was used as the macromolecular scaffold, and DFO molecules were bound to the terminals of the PEG branches via amide bonds. The conjugates displayed comparable iron binding ability to the free DFO. Furthermore, these macromolecule conjugates could significantly reduce the cytotoxicity of the free DFO, and showed satisfactory iron clearance capability in the iron overloaded macrophage RAW 246.7. The plasma half-life of the 8-arm-PEG-DFO conjugate was about 190 times than that of DFO when applied to an intravenously administered rat model. In conclusion, research indicated that these star-like PEG-based conjugates could be promising candidates as long circulating, less toxic iron chelators. Full article
(This article belongs to the Special Issue PEGylation in Drug Delivery Systems)
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17 pages, 6431 KiB  
Article
Development of Folate-Functionalized PEGylated Zein Nanoparticles for Ligand-Directed Delivery of Paclitaxel
by Zar Chi Soe, Wenquan Ou, Milan Gautam, Kishwor Poudel, Bo Kyun Kim, Le Minh Pham, Cao Dai Phung, Jee-Heon Jeong, Sung Giu Jin, Han-Gon Choi, Sae Kwang Ku, Chul Soon Yong and Jong Oh Kim
Pharmaceutics 2019, 11(11), 562; https://doi.org/10.3390/pharmaceutics11110562 - 30 Oct 2019
Cited by 25 | Viewed by 3763
Abstract
In this study, we investigated the active targeted delivery of a hydrophobic drug, paclitaxel (PTX), via receptor-mediated endocytosis by folate receptors expressed on cancer cells using a protein-based nanoparticle system. PTX was loaded on zein nanoparticles and conjugated with folate (PTX/Zein-FA) to estimate [...] Read more.
In this study, we investigated the active targeted delivery of a hydrophobic drug, paclitaxel (PTX), via receptor-mediated endocytosis by folate receptors expressed on cancer cells using a protein-based nanoparticle system. PTX was loaded on zein nanoparticles and conjugated with folate (PTX/Zein-FA) to estimate its chemotherapeutic efficacy in folate receptor-expressing KB cancer cells. PTX/Zein-FA nanoparticles were successfully developed, with a nanoparticle size of ~180 nm and narrow polydispersity index (~0.22). Accelerated release of PTX in an acidic environment was observed for PTX/Zein-FA. An in vitro cellular study of PTX/Zein-FAs in KB cells suggested that PTX/Zein-FA improved the cytotoxic activity of PTX on folate receptors overexpressed in cancer cells by inducing proapoptotic proteins and inhibiting anti-apoptotic proteins. In addition, PTX/Zein-FA exhibited anti-migratory properties and could alter the cell cycle profile of KB cells. A549 cells, which are folate receptor-negative cancer cells, showed no significant enhancement in the in vitro cellular activities of PTX/Zein-FA. We describe the antitumor efficacy of PTX/Zein-FA in KB tumor-bearing mice with minimum toxicity in healthy organs, and the results were confirmed in comparison with free drug and non-targeted nanoparticles. Full article
(This article belongs to the Special Issue PEGylation in Drug Delivery Systems)
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Review

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23 pages, 4780 KiB  
Review
Molecular Simulations of PEGylated Biomolecules, Liposomes, and Nanoparticles for Drug Delivery Applications
by Hwankyu Lee
Pharmaceutics 2020, 12(6), 533; https://doi.org/10.3390/pharmaceutics12060533 - 10 Jun 2020
Cited by 38 | Viewed by 5252
Abstract
Since the first polyethylene glycol (PEG)ylated protein was approved by the FDA in 1990, PEGylation has been successfully applied to develop drug delivery systems through experiments, but these experimental results are not always easy to interpret at the atomic level because of the [...] Read more.
Since the first polyethylene glycol (PEG)ylated protein was approved by the FDA in 1990, PEGylation has been successfully applied to develop drug delivery systems through experiments, but these experimental results are not always easy to interpret at the atomic level because of the limited resolution of experimental techniques. To determine the optimal size, structure, and density of PEG for drug delivery, the structure and dynamics of PEGylated drug carriers need to be understood close to the atomic scale, as can be done using molecular dynamics simulations, assuming that these simulations can be validated by successful comparisons to experiments. Starting with the development of all-atom and coarse-grained PEG models in 1990s, PEGylated drug carriers have been widely simulated. In particular, recent advances in computer performance and simulation methodologies have allowed for molecular simulations of large complexes of PEGylated drug carriers interacting with other molecules such as anticancer drugs, plasma proteins, membranes, and receptors, which makes it possible to interpret experimental observations at a nearly atomistic resolution, as well as help in the rational design of drug delivery systems for applications in nanomedicine. Here, simulation studies on the following PEGylated drug topics will be reviewed: proteins and peptides, liposomes, and nanoparticles such as dendrimers and carbon nanotubes. Full article
(This article belongs to the Special Issue PEGylation in Drug Delivery Systems)
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