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Pegylation and antibiotics

Wei Hong, Yining Zhao, Yuru Guo, Chengcheng Huang, Peng Qiu, Jia Zhu, Chun Chu, Hong Shi, Mingchun Liu
Although nano-self-assemblies of hydrophobic-modified bacitracin A with PLGA (Nano-BAPLGA) have demonstrated promising antibacterial activities, the application of Nano-BAPLGA was severely compromised by low water solubility. In this study, a series of PEGylated PLGA copolymers were selected to conjugate the N-terminus of bacitracin A in order to construct PEGylated self-assembled Nano-BAs and to further develop nano-self-assemblies of bacitracin A with strong antibacterial potency and high solubility. Compared with Nano-BAPLGA, all PEGylated Nano-BAs, except Nano-BA5K, exhibited strong antibacterial efficiency against both gram-positive and gram-negative bacteria by inducing loss of cytoplasmic membrane potential, membrane permeabilization and leakage of calcein from artificial cell membranes...
March 8, 2018: ACS Applied Materials & Interfaces
Kathryn A Guerriero, Steven R Wilson, Nabil E Boutagy, Chi Liu, Albert J Sinusas, Caroline J Zeiss
An adult female beagle (Canis lupus familiaris) used in a model of doxorubicin-induced cardiomyopathy presented with epithelial desquamation on the shoulders and ventrum after receiving the 8th weekly intravenous dose of the free form of doxorubicin (20 mg/m2; total accumulation, 160 mg/m2). The lesions were empirically treated with topical disinfectants and topical and systemic antibiotics. Despite treatment, the lesions progressed and ulcerated. Bacterial culture revealed Staphylococcus aureus, but trichogram, skin scraping, and fungal culture were negative for microorganisms...
February 1, 2018: Comparative Medicine
Pradeep Pushparaj Selvadoss, Jayshree Nellore, Malathy Balaraman Ravindrran, Uma Sekar
Pseudomonas aeruginosa is a problematic human pathogen resistant to almost all available antibiotics. The important prerequisite for these drugs to target this bacterium is an efficient delivery system. Siderophore-mediated drug delivery system is a promising approach to carry out antibiotics to the cells. Pyochelin, a siderophore of P. aeruginosa, was successfully synthesized in a five-step procedure. PEGylated liposomal pyochelin-antibiotic (L-Pch-Ab) carrier was fabricated by thin-film hydration method. L-Pch-Ab had an average size of 90...
November 27, 2017: Artificial Cells, Nanomedicine, and Biotechnology
H Q Huang, B Bai, Y H Gao, D H Zou, S H Zou, H Tan, Y P Song, Z Y Li, J Jin, W Li, H Su, Y P Gong, M Z Zhong, Y R Shuang, J Zhu, J Q Zhang, Z Cai, Q L Teng, W J Sun, Y Yang, Z J Xia, H L Chen, L M Hua, Y Y Bao, N Wu
Objective: To evaluate the efficacy and safety of pegylated recombinant human granulocyte colony-stimulating factor (PEG-rhG-CSF) in prophylaxis neutropenia after chemotherapy in patients with lymphoma. Methods: This was a multicenter, single arm, open, phase Ⅳ clinical trial. Included 410 patients with lymphoma received multiple cycles of chemotherapy and PEG-rhG-CSF was administrated as prophylactic. The primary endpoint was the incidence of Ⅲ/Ⅳ grade neutropenia and febrile neutropenia (FN) after each chemotherapy cycle...
October 14, 2017: Zhonghua Xue Ye Xue za Zhi, Zhonghua Xueyexue Zazhi
J A S Ritsema, E M A Herschberg, S E Borgos, C Løvmo, R Schmid, Y M Te Welscher, G Storm, C F van Nostrum
In the field of nanomedicine, nanoparticles are developed to target antibiotics to sites of bacterial infection thus enabling adequate drug exposure and decrease development of resistant bacteria. In the present study, we investigated the encapsulation of two antibiotics with different polarity into different PEGylated polymeric nanoparticles based on aliphatic polyesters, to obtain a better understanding of critical factors determining encapsulation and release. The nanoparticles were prepared from diblock copolymers comprising of a poly(ethylene glycol) block attached to an aliphatic polyester block of varying polarity: poly(lactic-co-glycolic acid) (mPEG-PLGA), poly(lactic-co-hydroxymethyl glycolic acid) (mPEG-PLHMGA) and poly(lactic-co-benzyloxymethyl glycolic acid) (mPEG-PLBMGA)...
November 11, 2017: International Journal of Pharmaceutics
Guo-Bin Qi, Di Zhang, Fu-Hua Liu, Zeng-Ying Qiao, Hao Wang
To date, numerous nanosystems have been developed as antibiotic replacements for bacterial infection treatment. However, these advanced systems are limited owing to their nontargeting accumulation and the consequent side effects. Herein, transformable polymer-peptide biomaterials have been developed that enable specific accumulation in the infectious site and long-term retention, resulting in enhanced binding capability and killing efficacy toward bacteria. The polymer-peptide conjugates are composed of a chitosan backbone and two functional peptides, i...
September 2017: Advanced Materials
Rita S Santos, George R Dakwar, Elisa Zagato, Toon Brans, Céu Figueiredo, Koen Raemdonck, Nuno F Azevedo, Stefaan C De Smedt, Kevin Braeckmans
The rising antimicrobial resistance contributes to 25000 annual deaths in Europe. This threat to the public health can only be tackled if novel antimicrobials are developed, combined with a more precise use of the currently available antibiotics through the implementation of fast, specific, diagnostic methods. Nucleic acid mimics (NAMs) that are able to hybridize intracellular bacterial RNA have the potential to become such a new class of antimicrobials and additionally could serve as specific detection probes...
September 2017: Biomaterials
Mohsen Chiani, Kayhan Azadmanesh, Mohammad Ali Shokrgozar, Mohammad Reza Mehrabi, Azim Akbarzadeh, Dariush Norouzian
Folate receptor (FR)-mediated drug delivery is a promising approach for active targeting of drugs to the FR-positive tumor cells. Bleomycin (BLM) is an antitumor antibiotic with poor therapeutic activity as a result of its limited diffusion into tumor cells. The aim of this study was to investigate whether FR-targeted PEGylated nanoliposomes (FPNL) can effectively deliver BLM to tumor cells and enhance its in vitro and in vivo efficacy. FPNL and PNL (non-targeted) were prepared by thin film hydration method, and their physiochemical properties, cellular uptake, tissue distribution and tumor inhibitory effects were investigated...
November 2017: Chemical Biology & Drug Design
Rongtao Zhao, Min Lv, Yang Li, Mingxuan Sun, Wen Kong, Lihua Wang, Shiping Song, Chunhai Fan, Leili Jia, Shaofu Qiu, Yansong Sun, Hongbin Song, Rongzhang Hao
The increasing occurrence of antibiotic-resistant pathogens, especially superbugs, is compromising the efficacy of traditional antibiotics. Silver nanoparticles (AgNPs) loaded graphene oxide (GO) nanocomposite (GO-Ag) has drawn great interest as a promising alternative antibacterial material. However, GO-Ag nanocomposite often irreversibly aggregates in physiological solutions, severely influencing its antibacterial capacity and practical application. Herein, a PEGylated and AgNPs loaded GO nanocomposite (GO-PEG-Ag) is synthesized through a facile approach utilizing microwave irradiation, while avoiding extra reducing agents...
April 28, 2017: ACS Applied Materials & Interfaces
Qiang Gao, Meng Yu, Yajuan Su, Meihua Xie, Xin Zhao, Peng Li, Peter X Ma
Numerous antimicrobial coatings have been developed for biomedical devices/implants, but few can simultaneously fulfill the requirements for antimicrobial and antifouling ability and biocompatibility. In this study, to develop an antimicrobial and antibiofilm surface coating, diblock amphiphilic molecules with antimicrobial and antifouling segments in a single chain were rationally designed and synthesized. Cationic antimicrobial polypeptides (AMP) were first synthesized by N-carboxyanhydride ring-opening polymerization (NCA-ROP)...
March 15, 2017: Acta Biomaterialia
Calvin A Omolo, Rahul S Kalhapure, Mahantesh Jadhav, Sanjeev Rambharose, Chunderika Mocktar, Valence M K Ndesendo, Thirumala Govender
Vancomycin (VM), a last resort to control methicillin-resistant S. aureus (MRSA) infections, is on the verge of becoming ineffective. Novel nano delivery systems of VM have the potential to combat MRSA. The search for novel materials for nanoantibiotic development is therefore an active research area. In this study, oleic acid (OA) was coupled with monomethoxy polyethylene glycol (mPEG) to obtain a novel bio-safe amphiphilic polymer, mPEG-OA. The critical micelle concentration of mPEG-OA, was found to be 4...
March 2017: European Journal of Pharmaceutics and Biopharmaceutics
Bin'en Nie, Teng Long, Haiyong Ao, Jianliang Zhou, Tingting Tang, Bing Yue
Infection is one of the most important causes of titanium implant failure in vivo A developing prophylactic method involves the immobilization of antibiotics, especially vancomycin, onto the surface of the titanium implant. However, these methods have a limited effect in curbing multiple bacterial infections due to antibiotic specificity. In the current study, enoxacin was covalently bound to an amine-functionalized Ti surface by use of a polyethylene glycol (PEG) spacer, and the bactericidal effectiveness was investigated in vitro and in vivo The titanium surface was amine functionalized with 3-aminopropyltriethoxysilane (APTES), through which PEG spacer molecules were covalently immobilized onto the titanium, and then the enoxacin was covalently bound to the PEG, which was confirmed by X-ray photoelectron spectrometry (XPS)...
January 2017: Antimicrobial Agents and Chemotherapy
Libo Du, Siqingaowa Suo, Han Zhang, Hongying Jia, Ke Jian Liu, Xue Ji Zhang, Yang Liu
It is still a huge challenge to find a new strategy for rationally designing covalent drugs because most of them are discovered by serendipity. Considering that the effect of covalent drugs is closely associated with the kinetics of the reaction between drug molecule and its target protein, here we first demonstrate an example of the kinetic effect of pi-stacking of drug molecules on covalent antimicrobial drug design. When PEGylated 7-aminocephalosporanic acid (PEG-ACA) is used as a substrate drug, pi-stacking of  the ACA group via the self-assembly of PEG-ACA on the surface of gold nanoparticles (i...
November 4, 2016: Nanotechnology
Debosree Ghosh, Debjani Ghosh, Pratap Parida
Interferons are produced in vivo and are one of the prime components of natural defense system of animals. They are released by the viral infected cells and provide protection to the neighboring cells against viral infection. The cyto-protective property of the proteins ignited the thought of their pharmaceutical adaptation for therapeutic use against viral diseases in individuals in whom the interferons released naturally are not sufficient to combat the situation. Interferon supplements have been found to complement various antiviral drugs...
2016: Mini Reviews in Medicinal Chemistry
Hong Jiang, Meimei Xiong, Qiuyan Bi, Ying Wang, Chong Li
Considering that some antibacterial agents can identify the outer structure of pathogens like cell wall and/or cell membrane, we explored a self-enhanced targeted delivery strategy by which a small amount of the antibiotic molecules were modified on the surface of carriers as targeting ligands of certain bacteria while more antibiotic molecules were loaded inside the carriers, and thus has the potential to improve the drug concentration at the infection site, enhance efficacy and reduce potential toxicity. In this study, a novel targeted delivery system against methicillin-resistant Staphylococcus aureus (MRSA) pneumonia was constructed with daptomycin, a lipopeptide antibiotic, which can bind to the cell wall of S...
July 2016: Acta Pharmaceutica Sinica. B
Akbar Esmaeili, Sepideh Ghobadianpour
Increasing prevalence of antibiotic-resistant and failed-treatment make more investigations to deal with these problems. Hence new therapeutic approaches for effective treatment are necessary. Ferrite superparamagnetic nanoparticles have potentially antibacterial activity. In this study we prepared MnFe2O4 superparamagnetic nanoparticles as core by precipitation method and used chitosan crosslinked by glutaraldehyde as shell, then modified with PEG to increase stability of particles against RES. Chitosan coating not only improves the properties of ferrit nanoparticles but also has antibacterial activity...
March 30, 2016: International Journal of Pharmaceutics
Karin Mayer, Cordula Nellessen, Corinna Hahn-Ast, Martin Schumacher, Sandra Pietzonka, Anna M Eis-Hübinger, Christian Drosten, Peter Brossart, Dominik Wolf
INTRODUCTION: Human coronavirus NL63 (HCoV-NL63) is one of four common human respiratory coronaviruses. Despite high incidence, HCoV infections are grossly understudied. We here report a case of HCoV infection in a leukemia patient with fatal ARDS despite successful virus elimination by pegylated interferon-alpha (PEG-IFN-α). CASE: The 27-year-old female pre-T-ALL patient was treated according to the German-Multicenter Trial for Adult ALL protocol. No relevant infectious complications were seen until day 35 when the neutropenic patient developed fever without any clinical focus...
August 2016: European Journal of Haematology
Yogita Patil, Yasmine Amitay, Patricia Ohana, Hilary Shmeeda, Alberto Gabizon
Mitomycin C (MMC) is a powerful anti-bacterial, anti-fungal and anti-tumor antibiotic, often active against multidrug resistant cells. Despite a broad spectrum of antitumor activity, MMC clinical use is relatively limited due to its fast clearance and dose-limiting toxicity. To exploit the potential antitumor activity of MMC and reduce its toxicity we have previously developed a formulation of pegylated liposomes with a lipophilic prodrug of MMC (PL-MLP), activated by endogenous reducing agents which are abundant in the tumor cell environment in the form of different thiols...
March 10, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
Ashish Punia, Kevin Lee, Edward He, Sumit Mukherjee, Andrew Mancuso, Probal Banerjee, Nan-Loh Yang
Synthetic amphiphilic polymers have been established as potentially efficient agents to combat widespread deadly infections involving antibiotic resistant superbugs. Incorporation of poly(ethylene glycol) (PEG) side chains into amphiphilic copolymers can reduce their hemolytic activity while maintaining high antibacterial activity. Our study found that the incorporation of PEG has substantially different effects on the hemolytic and antibacterial activities of copolymers depending on structural variations in the positions of cationic centers relative to hydrophobic groups...
2015: International Journal of Molecular Sciences
Gregory Marslin, Ann Mary Revina, Vinoth Kumar Megraj Khandelwal, Krishnamoorthy Balakumar, Caroline J Sheeba, Gregory Franklin
The rise of bacterial resistance against important drugs threatens their clinical utility. Fluoroquinones, one of the most important classes of contemporary antibiotics has also reported to suffer bacterial resistance. Since the general mechanism of bacterial resistance against fluoroquinone antibiotics (e.g. ofloxacin) consists of target mutations resulting in reduced membrane permeability and increased efflux by the bacteria, strategies that could increase bacterial uptake and reduce efflux of the drug would provide effective treatment...
August 1, 2015: Colloids and Surfaces. B, Biointerfaces
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