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 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.

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.

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.

Extrudable salicylic acid-based poly(anhydride-esters) for injectable drug releasing applications

2019 ◽  
Vol 34 (2) ◽  
pp. 178-189 ◽  
Author(s):  
Sabrina S Snyder ◽  
Yue Cao ◽  
Kathryn E Uhrich
Keyword(s):  
Salicylic Acid ◽  
Ethylene Glycol ◽  
Drug Loading ◽  
Invasive Procedure ◽  
Minimal Invasive ◽  
Poly Ethylene Glycol ◽  
Barrier Materials ◽  
Injectable Drug ◽  
Poly Ethylene

Injectable biomaterials have attracted more and more interest owing to their advantages over traditional open surgeries: minimal invasive procedure and ease of handling. Commonly used synthetic injectable polymers exhibited low drug loading and poor biodegradability. In this work, we describe a novel series of degradable copolymers comprising salicylic acid–based poly(anhydride-esters) and poly(ethylene glycol) subunits suitable for injectable drug releasing applications. By tuning the rheology properties, these salicylic acid–based poly(anhydride-esters) and poly(ethylene glycol) copolymers may function as injectable drug delivery vehicles that deliver salicylic acid at the injury site. These copolymers were designed to have glass transition temperatures (Tg) below 0ºC, resulting in extrudable polymers that behave like viscous fluids at room temperature. Salicylic acid–based poly(anhydride-esters) and poly(ethylene glycol) copolymers of different ratios (2:1, 1:1, and 1:2 salicylic acid–based poly(anhydride-esters) and poly(ethylene glycol)) were synthesized and characterized by nuclear magnetic resonance and Fourier-transform infrared spectroscopies. Their shear viscosities were determined both at room and physiological temperatures. The in vitro drug release profiles, cytotoxicity, and anti-inflammatory activities were assessed. The shear viscosities were found to compare favorably with current injectable barrier materials on the market.

scholarly journals Tailoring Atomoxetine Release Rate from DLP 3D-Printed Tablets Using Artificial Neural Networks: Influence of Tablet Thickness and Drug Loading

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 111
Author(s):  
Gordana Stanojević ◽  
Djordje Medarević ◽  
Ivana Adamov ◽  
Nikola Pešić ◽  
Jovana Kovačević ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Release Rate ◽  
Drug Loading ◽  
Prolonged Release ◽  
Cylindrical Shape ◽  
Poly Ethylene Glycol ◽  
Scanning Calorimetry ◽  
3D Printed ◽  
Artificial Neural ◽  
Poly Ethylene

Various three-dimensional printing (3DP) technologies have been investigated so far in relation to their potential to produce customizable medicines and medical devices. The aim of this study was to examine the possibility of tailoring drug release rates from immediate to prolonged release by varying the tablet thickness and the drug loading, as well as to develop artificial neural network (ANN) predictive models for atomoxetine (ATH) release rate from DLP 3D-printed tablets. Photoreactive mixtures were comprised of poly(ethylene glycol) diacrylate (PEGDA) and poly(ethylene glycol) 400 in a constant ratio of 3:1, water, photoinitiator and ATH as a model drug whose content was varied from 5% to 20% (w/w). Designed 3D models of cylindrical shape tablets were of constant diameter, but different thickness. A series of tablets with doses ranging from 2.06 mg to 37.48 mg, exhibiting immediate- and modified-release profiles were successfully fabricated, confirming the potential of this technology in manufacturing dosage forms on demand, with the possibility to adjust the dose and release behavior by varying drug loading and dimensions of tablets. DSC (differential scanning calorimetry), XRPD (X-ray powder diffraction) and microscopic analysis showed that ATH remained in a crystalline form in tablets, while FTIR spectroscopy confirmed that no interactions occurred between ATH and polymers.

Thermally Cross-Linked Oligo(poly(ethylene glycol) fumarate) Hydrogels Support Osteogenic Differentiation of Encapsulated Marrow Stromal Cells In Vitro

2004 ◽  
Vol 5 (1) ◽  
pp. 5-10 ◽  
Author(s):  
Johnna S. Temenoff ◽  
Hansoo Park ◽  
Esmaiel Jabbari ◽  
Daniel E. Conway ◽  
Tiffany L. Sheffield ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Osteogenic Differentiation ◽  
Stromal Cells ◽  
Marrow Stromal Cells ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene

scholarly journals Local Toxicity of Topically Administrated Thermoresponsive Systems: In Vitro Studies with In Vivo Correlation

2018 ◽  
Vol 47 (3) ◽  
pp. 426-432 ◽  
Author(s):  
Sivan Yogev ◽  
Ayelet Shabtay-Orbach ◽  
Abraham Nyska ◽  
Boaz Mizrahi
Keyword(s):  
Block Copolymer ◽  
Ethylene Glycol ◽  
Medical Devices ◽  
Poly Lactic Acid ◽  
Poly Ethylene Glycol ◽  
Thermoresponsive Polymers ◽  
Wide Range ◽  
Poly Ethylene

Thermoresponsive materials have the ability to respond to a small change in temperature—a property that makes them useful in a wide range of applications and medical devices. Although very promising, there is only little conclusive data about the cytotoxicity and tissue toxicity of these materials. This work studied the biocompatibility of three Food and Drug Administration approved thermoresponsive polymers: poly( N-isopropyl acrylamide), poly(ethylene glycol)-poly(propylene glycol)-poly(ethylene glycol) tri-block copolymer, and poly(lactic acid-co-glycolic acid) and poly(ethylene glycol) tri-block copolymer. Fibroblast NIH 3T3 and HaCaT keratinocyte cells were used for the cytotoxicity testing and a mouse model for the in vivo evaluation. In vivo results generally showed similar trends as the results seen in vitro, with all tested materials presenting a satisfactory biocompatibility in vivo. pNIPAM, however, showed the highest toxicity both in vitro and in vivo, which was explained by the release of harmful monomers and impurities. More data focusing on the biocompatibility of novel thermoresponsive biomaterials will facilitate the use of existing and future medical devices.

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