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Pegylation and antibiotics

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https://www.readbyqxmd.com/read/27890573/pegylated-oleic-acid-a-promising-amphiphilic-polymer-for-nano-antibiotic-delivery
#1
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...
November 23, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27799220/covalent-immobilisation-of-enoxacin-onto-ti-implant-surfaces-for-inhibiting-multiple-bacteria-species-infection-and-in-vivo-mrsa-infection-prophylaxis
#2
Bin'en Nie, Teng Long, Haiyong Ao, Jianliang Zhou, Tingting Tang, Bing Yue
Infection is the one of the most important causes of titanium implants failure in vivo A developing prophylactic method involves immobilisation of antibiotics, especially vancomycin, on the surface of the titanium implants. However, these methods have limited effect in curbing multiple bacteria infection due to the antibiotic specificity. In the current study, enoxacin was covalently bound to the amine-functionalised Ti surface by a polyethylene glycol (PEG) spacer, and the bactericidal effectiveness was investigated in vitro and in vivo, respectively...
October 31, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27673346/the-alternative-strategy-for-designing-covalent-drugs-through-kinetic-effects-of-pi-stacking-on-the-self-assembled-nanoparticles-a-model-study-with-antibiotics
#3
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
https://www.readbyqxmd.com/read/27499189/physiological-proteins-in-therapeutics-a-current-review-on-interferons
#4
REVIEW
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
https://www.readbyqxmd.com/read/27471672/self-enhanced-targeted-delivery-of-a-cell-wall-and-membrane-active-antibiotics-daptomycin-against-staphylococcal-pneumonia
#5
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
https://www.readbyqxmd.com/read/26875538/vancomycin-loaded-superparamagnetic-mnfe2o4-nanoparticles-coated-with-pegylated-chitosan-to-enhance-antibacterial-activity
#6
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
https://www.readbyqxmd.com/read/26854965/fatal-outcome-of-human-coronavirus-nl63-infection-despite-successful-viral-elimination-by-ifn-alpha-in-a-patient-with-newly-diagnosed-all
#7
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
https://www.readbyqxmd.com/read/26809007/targeting-of-pegylated-liposomal-mitomycin-c-prodrug-to-the-folate-receptor-of-cancer-cells-intracellular-activation-and-enhanced-cytotoxicity
#8
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
https://www.readbyqxmd.com/read/26473831/effect-of-relative-arrangement-of-cationic-and-lipophilic-moieties-on-hemolytic-and-antibacterial-activities-of-pegylated-polyacrylates
#9
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
https://www.readbyqxmd.com/read/26005932/pegylated-ofloxacin-nanoparticles-render-strong-antibacterial-activity-against-many-clinically-important-human-pathogens
#10
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
https://www.readbyqxmd.com/read/25888864/novel-pegylated-silver-coated-carbon-nanotubes-kill-salmonella-but-they-are-non-toxic-to-eukaryotic-cells
#11
Atul A Chaudhari, Shanese L Jasper, Ejovwoke Dosunmu, Michael E Miller, Robert D Arnold, Shree R Singh, Shreekumar Pillai
BACKGROUND: Resistance of food borne pathogens such as Salmonella to existing antibiotics is of grave concern. Silver coated single walled carbon nanotubes (SWCNTs-Ag) have broad-spectrum antibacterial activity and may be a good treatment alternative. However, toxicity to human cells due to their physico-chemical properties is a serious public health concern. Although pegylation is commonly used to reduce metal nanoparticle toxicity, SWCNTs-Ag have not been pegylated as yet, and the effect of pegylation of SWCNTs-Ag on their anti-bacterial activity and cell cytotoxicity remains to be studied...
2015: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/25848270/poly-lactic-co-glycolic-acid-nanoparticles-conjugated-with-cd133-aptamers-for-targeted-salinomycin-delivery-to-cd133-osteosarcoma-cancer-stem-cells
#12
Miaozhong Ni, Min Xiong, Xinchao Zhang, Guoping Cai, Huaiwen Chen, Qingmin Zeng, Zuochong Yu
BACKGROUND: Cancer stem cells (CSCs) possess the characteristics associated with normal stem cells and are responsible for cancer initiation, recurrence, and metastasis. CD133 is regarded as a CSCs marker of osteosarcoma, which is the most common primary bone malignancy in childhood and adolescence. Salinomycin, a polyether ionophore antibiotic, has been shown to kill various CSCs, including osteosarcoma CSCs. However, salinomycin displayed poor aqueous solubility that hinders its clinical application...
2015: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/25848262/alendronate-coated-long-circulating-liposomes-containing-99mtechnetium-ceftizoxime-used-to-identify-osteomyelitis
#13
Diego dos Santos Ferreira, Fernanda Alves Boratto, Valbert Nascimento Cardoso, Rogéria Serakides, Simone Odília Fernandes, Lucas Antônio Miranda Ferreira, Mônica Cristina Oliveira
Osteomyelitis is a progressive destruction of bones caused by microorganisms. Inadequate or absent treatment increases the risk of bone growth inhibition, fractures, and sepsis. Among the diagnostic techniques, functional images are the most sensitive in detecting osteomyelitis in its early stages. However, these techniques do not have adequate specificity. By contrast, radiolabeled antibiotics could improve selectivity, since they are specifically recognized by the bacteria. The incorporation of these radiopharmaceuticals in drug-delivery systems with high affinity for bones could improve the overall uptake...
2015: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/25793309/improved-biofilm-antimicrobial-activity-of-polyethylene-glycol-conjugated-tobramycin-compared-to-tobramycin-in-pseudomonas-aeruginosa-biofilms
#14
Ju Du, H M H N Bandara, Ping Du, Hui Huang, Khang Hoang, Dang Nguyen, Sri Vasudha Mogarala, Hugh D C Smyth
The objective of this study was to develop a functionally enhanced antibiotic that would improve the therapeutic activity against bacterial biofilms. Tobramycin was chemically conjugated with polyethylene glycol (PEG) via site-specific conjugation to form PEGylated-tobramycin (Tob-PEG). The antibacterial efficacy of Tob-PEG, as compared to tobramycin, was assessed on the planktonic phase and biofilms phase of Pseudomonas aeruginosa. The minimum inhibitory concentration (MIC80) of Tob-PEG was higher (13.9 μmol/L) than that of tobramycin (1...
May 4, 2015: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/25790806/bacterial-infection-as-an-adverse-effect-of-telaprevir-based-triple-therapy-for-chronic-hepatitis-c-infection
#15
MULTICENTER STUDY
Akira Kawano, Eiichi Ogawa, Norihiro Furusyo, Makoto Nakamuta, Eiji Kajiwara, Kazufumi Dohmen, Hideyuki Nomura, Kazuhiro Takahashi, Takeaki Satoh, Koichi Azuma, Yuichi Tanabe, Shinji Shimoda, Kazuhiro Kotoh, Jun Hayashi
OBJECTIVE: There is little information regarding the incidence of bacterial infections as an adverse effect of telaprevir (TVR)-based triple therapy. This study was performed in order to evaluate the baseline and on-treatment predictors of bacterial infections in patients treated with TVR-based triple therapy. METHODS: This multicenter study evaluated 430 patients with chronic hepatitis C who received 12 weeks of TVR in combination with 24 weeks of pegylated interferon α2b plus ribavirin...
2015: Internal Medicine
https://www.readbyqxmd.com/read/25576433/phase-iii-placebo-controlled-double-blind-randomized-trial-of-pegfilgrastim-to-reduce-the-risk-of-febrile-neutropenia-in-breast-cancer-patients-receiving-docetaxel-cyclophosphamide-chemotherapy
#16
RANDOMIZED CONTROLLED TRIAL
Yoshimasa Kosaka, Yoshiaki Rai, Norikazu Masuda, Toshimi Takano, Toshiaki Saeki, Seigo Nakamura, Ryutaro Shimazaki, Yoshinori Ito, Yutaka Tokuda, Kazuo Tamura
PURPOSE: Pegfilgrastim is a pegylated form of filgrastim, a recombinant protein of granulocyte colony-stimulating factor, that is used to reduce the risk of febrile neutropenia (FN). Here, we report the results of a phase III trial of pegfilgrastim in breast cancer patients receiving docetaxel and cyclophosphamide (TC) chemotherapy. METHODS: We conducted a double-blind, placebo-controlled, randomized trial to determine the efficacy of pegfilgrastim in reducing the risk of FN in early-stage breast cancer patients...
April 2015: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/25151744/long-circulating-liposomal-daptomycin-enhances-protection-against-systemic-methicillin-resistant-staphylococcus-aureus-infection-with-improved-therapeutic-potential
#17
Xing-Liang Huang, Jin Wu, Ting-Ting Su, Yan-Hong Li, Zhang-Bao Chen, Chong Li
In the face of escalating problems with pathogen control, the development of proper formulations of existing antibiotics is as important as the development of novel antibiotics. Daptomycin is a lipopeptide antibiotic with potent activity against Gram-positive bacteria. Currently, only injectable solution of daptomycin has been approved for clinical use. In the present study, the formulation of PEGylated liposomal daptomycin (PLD) was prepared and optimized, and its efficacy against methicillin-resistant Staphylococcus aureus (MRSA252) strains was investigated...
May 2014: Yao Xue Xue Bao, Acta Pharmaceutica Sinica
https://www.readbyqxmd.com/read/25055566/-comparative-study-of-pharmacokinetics-of-ofloxacin-in-a-free-and-niosomal-forms-in-experiments-on-white-mice-when-administered-per-os
#18
COMPARATIVE STUDY
A N Kulichenko, M E Mikhaĭlova, D A Kovalev, S V Pisarenko, Iu V Siritsa, L V Liapustina
AIM: To study features of pharmacokinetics of ofloxacin as a part of anion PEGylated niosomes on a basis of sorbitan monostearate (Span 60) to experimental white mice per os. MATERIALS AND METHODS: Ofloxacin was entrapped in niosomes consisting of Span 60, cholesterol, PEG 4000 and dicetylphosphate. Sizes of niosomes estimated by means of probe microscopy. Efficiency of inclusion of an antibiotic in niosomes defined after removal of free drug by a centrifugation...
2014: Vestnik Rossiĭskoĭ Akademii Meditsinskikh Nauk
https://www.readbyqxmd.com/read/25019569/a-phase-1b-study-of-trebananib-in-combination-with-pegylated-liposomal-doxorubicin-or-topotecan-in-women-with-recurrent-platinum-resistant-or-partially-platinum-sensitive-ovarian-cancer
#19
Ignace Vergote, Russell J Schilder, Charles H Pippitt, Shirley Wong, Alan N Gordon, Sidney Scudder, Frederic Kridelka, Luc Dirix, Joseph W Leach, Sumitra Ananda, Nuwan Nanayakkara, Rebeca Melara, Michael B Bass, Jason Litten, Henry Adewoye, Robert M Wenham
OBJECTIVE: To examine the tolerability and antitumor activity of trebananib plus pegylated liposomal doxorubicin (PLD) or topotecan in recurrent platinum-resistant or partially platinum-sensitive ovarian cancer. METHODS: In this open-label phase 1b study, patients received trebananib 10 mg/kg or 15 mg/kg IV QW plus PLD 50 mg/m(2) (cohorts A1 and A3, respectively) or topotecan 4 mg/m(2) (cohorts B1 and B3, respectively). Endpoints were dose-limiting toxicity (DLT; primary); treatment-emergent adverse events (AEs), overall response rate, anti-trebananib antibodies, and pharmacokinetics (secondary)...
October 2014: Gynecologic Oncology
https://www.readbyqxmd.com/read/24965180/correlation-of-toxicity-and-efficacy-with-pharmacokinetics-pk-of-pegylated-liposomal-doxorubicin-pld-caelyx%C3%A2
#20
Marye J Boers-Sonderen, Carla M L van Herpen, Winette T A van der Graaf, Ingrid M E Desar, Mirjam G W Arens- van der Logt, Yvo M de Beer, Petronella B Ottevanger, Nielka P van Erp
PURPOSE: Pegylated liposomal doxorubicin (PLD) is used to treat patients with breast and gynecological cancers. In order to optimize treatment with PLD, we assessed the prognostic and predictive factors for efficacy of PLD. METHODS: Seventeen patients treated with PLD 30 or 40 mg/m(2) underwent pharmacokinetic sampling during the first cycle of treatment. PLD exposure was calculated. An univariate analysis was performed with the variables: hand-foot syndrome, mucositis, rash, neutropenia, age, tumor type, number of previous therapies, ECOG performance status and progression-free survival (PFS)...
September 2014: Cancer Chemotherapy and Pharmacology
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