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 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 Physicochemical, Pharmacokinetic, and Toxicity Evaluation of Methoxy Poly(ethylene glycol)-b-Poly(d,l-Lactide) Polymeric Micelles Encapsulating Alpinumisoflavone Extracted from Unripe Cudrania tricuspidata Fruit

Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 366 ◽  
Author(s):  
Min Jeong Jo ◽  
Yang Hee Jo ◽  
Yu Jin Lee ◽  
Chun-Woong Park ◽  
Jin-Seok Kim ◽  
...  
Keyword(s):  
Drug Release ◽  
Ethylene Glycol ◽  
Physicochemical Properties ◽  
Polymeric Micelles ◽  
Pharmacokinetic Studies ◽  
Severe Toxicity ◽  
Poly Ethylene Glycol ◽  
Cudrania Tricuspidata ◽  
Poly Ethylene

Alpinumisoflavone, a major compound in unripe Cudrania tricuspidata fruit is reported to exhibit numerous beneficial pharmacological activities, such as osteoprotective, antibacterial, estrogenic, anti-metastatic, atheroprotective, antioxidant, and anticancer effects. Despite its medicinal value, alpinumisoflavone is poorly soluble in water, which makes it difficult to formulate and administer intravenously (i.v.). To overcome these limitations, we used methoxy poly(ethylene glycol)-b-poly(d,l-lactide) (mPEG-b-PLA) polymeric micelles to solubilize alpinumisoflavone and increase its bioavailability, and evaluated their toxicity in vivo. Alpinumisoflavone-loaded polymeric micelles were prepared using thin-film hydration method, and their physicochemical properties were characterized for drug release, particle size, drug-loading (DL, %), and encapsulation efficiency (EE, %). The in vitro drug release profile was determined and the release rate of alpinumisoflavone from mPEG-b-PLA micelles was slower than that from drug solution, and sustained. Pharmacokinetic studies showed decreased total clearance and volume of distribution of alpinumisoflavone, whereas area under the curve (AUC) and bioavailability were significantly increased by incorporation in mPEG-b-PLA micelles. In vivo toxicity assay revealed that alpinumisoflavone-loaded mPEG-b-PLA micelles had no severe toxicity. In conclusion, we prepared an intravenous (i.v.) injectable alpinumisoflavone formulation, which was solubilized using mPEG-b-PLA micelles, and determined their physicochemical properties, pharmacokinetics, and toxicity profiles.

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.

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.

scholarly journals Preparation of Silymarin–quercetin Loaded Nanoparticles by Spontaneous Emulsification Solvent Diffusion Method Using D-alpha-tocopheryl Poly (Ethylene Glycol) 1000 Succinate

2021 ◽  
pp. 84-94
Author(s):  
S. Senthila ◽  
P. Manoj Kumar ◽  
P. Venkatesan
Keyword(s):  
Electron Microscopy ◽  
Drug Release ◽  
Ethylene Glycol ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Release Profile ◽  
Poly Ethylene Glycol ◽  
Drug Release Profile ◽  
Spontaneous Emulsification ◽  
Poly Ethylene

Silymarin, a flavonolignan, derived from Silybum marianum, family Asteraceae has long been used as a hepatoprotective remedy. Silymarin has cytoprotective activities due to its antioxidant property and free radical scavenging activity. The pharmacokinetic studies of past three decades revealed that silymarin has poor absorption, rapid metabolism especially by Phase II metabolism and ultimately poor oral bioavailability. Quercetin, a flavonoid present in edible vegetables and fruits, It is a potent antioxidant and shows a wide range of biological functions. Quercetin improves blood levels and efficacy of number of drugs since it is P-Glycoprotein inhibitor and also inhibits drug metabolizing enzymes. Both silymarin and quercetin were, poorly soluble in the water shows low bioavailability. The advanced type of formulation like polymeric nanoparticles (PNPs) can be successfully utilised for bioavailability enhancement and targeting the Silymarin-quercetin to hepatocytes. A controlled release PNPs of silymarin-quercetin were prepared by spontaneous emulsification solvent diffusion (SESD) method using Poly Lactic-co-Glycolic Acid (PLGA) as biodegradable polymer, D-alpha-tocopheryl poly (ethylene glycol) 1000 succinate (TPGS) used as a solubilizer, as an emulsifier. TPGS as an emulsifier and further as a matrix material blended with PLGA was used to enhance the encapsulation efficiency and improve the drug release profile of nanoparticles. Different formulations with various drug: polymer ratios and volume and concentration of surfactant, centrifugation time were evaluated. The effect of formulation parameters such as drug/polymer ratio, volume and surfactant content were evaluated. The surface morphology and size of the nanoparticles were studied by scanning electron microscopy (SEM) Transmission electron microscopy (TEM). Drug encapsulation efficiency and in vitro drug release profiles of nanoparticles were determined using UV spectrophotometry. The nanoparticles prepared with combination of both the drugs in this study were spherical with size range of 100–200 nm. It was shown that TPGS was a good emulsifier for producing nanoparticles of hydrophobic drugs and improving the encapsulation efficiency and drug loading and drug release profile of nanoparticles. Although the amount of the TPGS used had a significant effect on the nanoparticle size and morphology, the drug loading and release profile of nanoparticles

Poly(caprolactone)–poly(ethylene glycol)–poly(caprolactone) (PCL–PEG–PCL) nanoparticles: a valuable and efficient system for in vitro and in vivo delivery of curcumin

RSC Advances ◽  
2016 ◽  
Vol 6 (17) ◽  
pp. 14403-14415 ◽  
Author(s):  
Hamidreza Kheiri Manjili ◽  
Ali Sharafi ◽  
Hossein Danafar ◽  
Mirjamal Hosseini ◽  
Ali Ramazani ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Single Step ◽  
Precipitation Method ◽  
Poly Ethylene Glycol ◽  
Efficient System ◽  
Poly Ethylene ◽  
Poly Caprolactone ◽  
In Vivo Delivery

Curcumin was encapsulated within PCL–PEG–PCL micelles through a single-step nano-precipitation method, leading to the creation of CUR/PCL–PEG–PCL micelles..

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