scholarly journals Noncovalent Complexation of Amphotericin B with Poly(β-Amino Ester) Derivates for Treatment of C. Neoformans Infection

Polymers ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 270 ◽  
Author(s):  
Yang Yu ◽  
Li Peng ◽  
Guojian Liao ◽  
Zhangbao Chen ◽  
Chong Li
Keyword(s):  
Amphotericin B ◽  
Addition Reaction ◽  
Noncovalent Complex ◽  
Drug Loading ◽  
Amino Ester ◽  
Poly Ethylene Glycol ◽  
Improve Treatment ◽  
Michael Type Addition ◽  
Poly Ethylene

Our goal was to improve treatment outcomes for C. neoformans infection by designing nanocarriers that enhance drug-encapsulating capacity and stability. Thus, a noncovalent complex of methoxy poly(ethylene glycol)-poly(lactide)-poly(β-amino ester) (MPEG-PLA-PAE) and amphotericin B (AMB) was developed and characterized. The MPEG-PLA-PAE copolymer was synthesized by a Michael-type addition reaction; the copolymer was then used to prepare the AMB-loaded nanocomplex. AMB was in a highly aggregated state within complex cores. A high encapsulation efficiency (>90%) and stability of the AMB-loaded nanocomplex were obtained via electrostatic interaction between AMB and PAE blocks. This nanocomplex retained drug activity against C. neoformans in vitro. Compared with micellar AMB, the AMB nanocomplex was more efficient in terms of reducing C. neoformans burden in lungs, liver, and spleen, based on its improved biodistribution. The AMB/MPEG-PLA-PAE complex with enhanced drug-loading capacity and stability can serve as a platform for effective treatment of C. neoformans infection.

scholarly journals Polypeptides Micelles Composed of Methoxy-Poly(Ethylene Glycol)-Poly(l-Glutamic Acid)-Poly(l-Phenylalanine) Triblock Polymer for Sustained Drug Delivery

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 230 ◽  
Author(s):  
Xingzheng Liu ◽  
Rongrong Fan ◽  
Boting Lu ◽  
Yuan Le
Keyword(s):  
Drug Release ◽  
Ethylene Glycol ◽  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Poly Ethylene Glycol ◽  
Sustained Drug Release ◽  
Poly Ethylene ◽  
Triblock Polymers

Methoxy-poly(ethylene glycol)-poly(l-glutamic acid)-poly(l-phenylalanine) triblock polymers with different architecture were synthesized as drug carrier to obtain sustained and controlled release by tuning the composition. These triblock polymers were prepared by ring opening polymerization and poly(ethylene glycol) was used as an initiator. Polymerization was confirmed by 1H NMR, FT-IR and gel penetration chromatography. The polymers can self-assemble to form micelles in aqueous medium and their critical micelle concentrations values were examined. The micelles were spherical shape with size of 50–100 nm and especially can arranged in a regular manner. Sorafenib was selected as the model drug and the drug loading performance was dependent on the composition of the block copolymer. In vitro drug release indicated that the polymers can realize controlled and sustained drug release. Furthermore, in vitro cytotoxicity assay showed that the polymers were biocompatible and the drug-loaded micelles can increase toxicity towards tumor cells. Confocal fluorescence microscopy assays illustrated that the micelles can be uptaken quickly and release drug persistently to inhibit tumor cell growth.

The Preparation of pH- and Thermo-Sensitive Chitosan-Based Hydrogels by Michael-Type Addition Reaction

2011 ◽  
Vol 130-134 ◽  
pp. 2392-2395
Author(s):  
Hong Liang Wei ◽  
Cun Cai Ma ◽  
Hui Juan Chu ◽  
Jing Zhu
Keyword(s):  
Ethylene Glycol ◽  
Potential Application ◽  
Addition Reaction ◽  
Poly Ethylene Glycol ◽  
Amino Groups ◽  
Mild Conditions ◽  
Primary Amino ◽  
Michael Type Addition ◽  
Poly Ethylene ◽  
Maleimide Group

The hydrogels based on chitosan were prepared by Michael-type addition reaction between chitosan's primary amino groups and maleimide group terminating poly (ethylene glycol) (PEG) under mild conditions. The hydrogels were characterizatied by FTIR, TG, etc. The study on the swelling behavior indicated that the hydrogels possess pH-and thermo-sensitivity. The chitosan-based hydogels crosslinked by Michael-type addition reaction have a potential application on biomaterials due to its biodegradability, biocompatibility, less toxicity and hydrophilicity.

scholarly journals Evaluation of the Physicochemical Properties, Pharmacokinetics, and In Vitro Anticancer Effects of Docetaxel and Osthol Encapsulated in Methoxy Poly(ethylene glycol)-b-Poly(caprolactone) Polymeric Micelles

2020 ◽  
Vol 22 (1) ◽  
pp. 231
Author(s):  
Min Jeong Jo ◽  
Yu Jin Lee ◽  
Chun-Woong Park ◽  
Youn Bok Chung ◽  
Jin-Seok Kim ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Pharmacokinetic Studies ◽  
Poly Ethylene Glycol ◽  
Drug Release Profile ◽  
Anticancer Effects ◽  
Poly Ethylene ◽  
Poly Caprolactone

Docetaxel (DTX), a taxane-based anticancer drug, and osthol (OTH), a coumarin-derivative compound, have shown anticancer effects against different types of cancers through various mechanisms. However, these drugs have low solubility in water and low oral bioavailability, and thus their clinical application is difficult. To overcome these problems, we encapsulated DTX and OTH in methoxy poly(ethylene glycol)-b-poly(caprolactone) (mPEG-b-PCL) and conducted studies in vitro and in vivo. We selected a 1:4 ratio as the optimal ratio of DTX and OTH, through combination index analysis in A549 cancer cells, and prepared micelles to evaluate the encapsulation efficiency, drug loading, particle size, and zeta potential. The in vitro drug-release profile showed that DTX/OTH-loaded mPEG-b-PCL micelles could slowly release DTX and OTH. In the clonogenic assay, DTX/OTH-loaded mPEG-b-PCL micelles showed 3.7 times higher inhibitory effect than the DTX/OTH solution. Pharmacokinetic studies demonstrated that micelles in combination with DTX and OTH exhibited increased area under curve and decreased clearance values, as compared with single micelles.

scholarly journals Novel 4-Arm Poly(Ethylene Glycol)-Block-Poly(Anhydride-Esters) Amphiphilic Copolymer Micelles Loading Curcumin: Preparation, Characterization, and In Vitro Evaluation

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Li Lv ◽  
Yuanyuan Shen ◽  
Min Li ◽  
Xiaofen Xu ◽  
Mingna Li ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Hela Cells ◽  
Drug Loading ◽  
Amphiphilic Copolymer ◽  
Phase Cell ◽  
Hydrodynamic Diameter ◽  
Dependent Manner ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene

A novel 4-arm poly(ethylene glycol)-block-poly(anhydride-esters) amphiphilic copolymer (4-arm PEG-b-PAE) was synthesized by esterization of 4-arm poly(ethylene glycol) and poly(anhydride-esters) which was obtained by melt polycondensation ofα-,ω-acetic anhydride terminated poly(L-lactic acid). The obtained 4-arm PEG-b-PAE was characterized by1H-NMR and gel permeation chromatography. The critical micelle concentration of 4-arm PEG-b-PAE was 2.38 μg/mL. The curcumin-loaded 4-arm PEG-b-PAE micelles were prepared by a solid dispersion method and the drug loading content and encapsulation efficiency of the micelles were 7.0% and 85.2%, respectively. The curcumin-loaded micelles were spherical with a hydrodynamic diameter of 151.9 nm. Curcumin was encapsulated within 4-arm PEG-b-PAE micelles amorphously and released from the micelles, faster in pH 5.0 than pH 7.4, presenting one biphasic drug release pattern with rapid release at the initial stage and slow release later. The hemolysis rate of the curcumin-loaded 4-arm PEG-b-PAE micelles was 3.18%, which was below 5%. The IC50value of the curcumin-loaded micelles against Hela cells was 10.21 μg/mL, lower than the one of free curcumin (25.90 μg/mL). The cellular uptake of the curcumin-loaded micelles in Hela cell increased in a time-dependent manner. The curcumin-loaded micelles could induce G2/M phase cell cycle arrest and apoptosis of Hela cells.

scholarly journals Self-targeting, zwitterionic micellar dispersants enhance antibiotic killing of infectious biofilms—An intravital imaging study in mice

2020 ◽  
Vol 6 (33) ◽  
pp. eabb1112 ◽  
Author(s):  
Shuang Tian ◽  
Linzhu Su ◽  
Yong Liu ◽  
Jingjing Cao ◽  
Guang Yang ◽  
...  
Keyword(s):  
Infection Control ◽  
Extracellular Polymeric Substances ◽  
Polymeric Micelles ◽  
Imaging Study ◽  
Amino Ester ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Positively Charged

Extracellular polymeric substances (EPS) hold infectious biofilms together and limit antimicrobial penetration and clinical infection control. Here, we present zwitterionic micelles as a previously unexplored, synthetic self-targeting dispersant. First, a pH-responsive poly(ε-caprolactone)-block-poly(quaternary-amino-ester) was synthesized and self-assembled with poly(ethylene glycol)-block-poly(ε-caprolactone) to form zwitterionic, mixed-shell polymeric micelles (ZW-MSPMs). In the acidic environment of staphylococcal biofilms, ZW-MSPMs became positively charged because of conversion of the zwitterionic poly(quaternary-amino-ester) to a cationic lactone ring. This allowed ZW-MSPMs to self-target, penetrate, and accumulate in staphylococcal biofilms in vitro. In vivo biofilm targeting by ZW-MSPMs was confirmed for staphylococcal biofilms grown underneath an implanted abdominal imaging window through direct imaging in living mice. ZW-MSPMs interacted strongly with important EPS components such as eDNA and protein to disperse biofilm and enhance ciprofloxacin efficacy toward remaining biofilm, both in vitro and in vivo. Zwitterionic micellar dispersants may aid infection control and enhance efficacy of existing antibiotics against remaining biofilm.

Multifunctional periodontal membrane for treatment and regeneration purposes

2020 ◽  
Vol 35 (2) ◽  
pp. 117-138 ◽  
Author(s):  
Gulhan Isik ◽  
Nesrin Hasirci ◽  
Aysen Tezcaner ◽  
Aysel Kiziltay
Keyword(s):  
Stem Cells ◽  
Vitamin E ◽  
Ethylene Glycol ◽  
Dental Pulp ◽  
Drug Loading ◽  
Dental Pulp Stem Cells ◽  
Poly Ethylene Glycol ◽  
E Coli ◽  
Poly Ethylene

Periodontitis is a chronic inflammatory disease that causes gum tissue degeneration and alveolar bone and tooth loss. The aim of this study is to develop a multifunctional matrix for the treatment of periodontitis and enhancement of regeneration of the periodontal tissue. The matrix was prepared from vitamin E containing hydrogel made of alginate and gelatin, and doxycycline HCl containing methoxy poly(ethylene glycol)-block-polycaprolactone micelles. Methoxy poly(ethylene glycol)-block-polycaprolactone was synthesized with ring-opening polymerization technique and characterized by proton nuclear magnetic resonance (1H NMR), Fourier-transform infrared spectroscopy, differential scanning calorimetry, and gel permeation chromatography. Micelles were characterized by measuring zeta potential, hydrodynamic diameter, drug encapsulation efficiency, drug loading capacity, and in vitro drug-release kinetics. Micelles were obtained with an average size of 164 nm and drug loading amount of 5.8%. The activity of doxycycline HCl–loaded micelles and vitamin E containing hydrogels was determined against Escherichia coli ( E. coli) and Staphylococcus aureus ( S. aureus) with disk diffusion method. Bio-efficacy of micelle-loaded alginate–gelatin hydrogels were tested in vitro using L929 fibroblasts and dental pulp stem cells. Doxycycline HCl–loaded micelles and vitamin E containing hydrogels showed a sustained release and exhibited inhibition zone against E. coli and S. aureus. Hydrogels with vitamin E and doxycycline HCl–loaded micelles promoted osteogenic differentiation of dental pulp stem cells. Results suggest that alginate–gelatin hydrogels containing doxycycline HCl–loaded micelles and vitamin E can be good candidates for the treatment of periodontitis and tissue regeneration.

Synthesis of pH-sensitive amphotericin B–poly(ethylene glycol) conjugates and study of their controlled release in vitro

2007 ◽  
Vol 15 (12) ◽  
pp. 4069-4076 ◽  
Author(s):  
Miloš Sedlák ◽  
Martin Pravda ◽  
Frantisek Staud ◽  
Lenka Kubicová ◽  
Kateřina Týčová ◽  
...  
Keyword(s):  
Controlled Release ◽  
Ethylene Glycol ◽  
Amphotericin B ◽  
Ph Sensitive ◽  
Poly Ethylene Glycol ◽  
Release In Vitro ◽  
Poly Ethylene

Preparation and characterization of hydrogels based on acryloyl end-capped four-arm star-shaped poly(ethylene glycol)-branched-oligo(l-lactide) via Michael-type addition reaction

2010 ◽  
Vol 64 (5) ◽  
Author(s):  
Huai-Qing Yu ◽  
Rimin Cong
Keyword(s):  
Ethylene Glycol ◽  
Addition Reaction ◽  
Gelation Time ◽  
Precursor Solution ◽  
Poly Ethylene Glycol ◽  
Biomedical Material ◽  
Michael Type Addition ◽  
Degradation Behaviors ◽  
Poly Ethylene

AbstractAn acryloyl end-capped four-arm star-shaped poly(ethylene glycol)-branched-oligo(l-lactide) (4A-PEG-PLA) macromer was firstly prepared. A novel kind of hydrogels was synthesized via the Michael-type addition reaction between (2S,3S)-1,4-bis-sulfanylbutane-2,3-diol (dithiothreitol) and this macromer. Gelation time was determined visually as the time when the precursor solution did not flow on inverting the vials. Hydrogel structure was characterized by FTIR analysis, swelling and degradation tests. It was found that colorless and transparent hydrogels were quickly generated in situ. The gelation time, swelling and degradation behaviors of this kind of hydrogels could be adjusted by changing the concentration of the macromer solution in PBS buffer (pH 7.4). This novel hydrogel is expected to be used as a biomedical material.

Amphotericin B-Loaded Poly(Lactide)-Poly(Ethylene Glycol)-Blend Nanoparticles: Characterization and In Vitro Efficacy and Toxicity

2013 ◽  
Vol 9 (5) ◽  
pp. 594-598 ◽  
Author(s):  
Caroline Rodrigues ◽  
Diani Casa ◽  
Luciana Dalmolin ◽  
Luciana Camargo ◽  
Najeh Khalil ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Amphotericin B ◽  
Poly Ethylene Glycol ◽  
Nanoparticles Characterization ◽  
Poly Ethylene
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