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.

Biodegradable poly(ethylene glycol)–poly(ε-carprolactone) polymeric micelles with different tailored topological amphiphilies for doxorubicin (DOX) drug delivery

RSC Advances ◽  
2016 ◽  
Vol 6 (63) ◽  
pp. 58160-58172 ◽  
Author(s):  
Y. Chen ◽  
Y. X. Zhang ◽  
Z. F. Wu ◽  
X. Y. Peng ◽  
T. Su ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ethylene Glycol ◽  
Self Assembly ◽  
Polymeric Micelles ◽  
The Self ◽  
Molar Ratio ◽  
Poly Ethylene Glycol ◽  
Biodegradable Poly ◽  
Poly Ethylene

The self-assembly and drug release of the three PEG–PCL copolymers with different topologies but identical molar ratio between PEG to PCL.

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.

Fabrication of Mixed Polymeric Micelles Based on Stimuli-Responsive Amphiphilic Copolymers for Drug Delivery and Controlled Release

NANO ◽  
2020 ◽  
Vol 15 (03) ◽  
pp. 2050040 ◽  
Author(s):  
Jia Liu ◽  
Juan Li ◽  
Tingting Liu
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Block Copolymers ◽  
Drug Release ◽  
Ethylene Glycol ◽  
Polymeric Micelles ◽  
Poly Ethylene Glycol ◽  
Mixed Polymeric Micelles ◽  
Poly Ethylene ◽  
Glycol Methyl Ether

In this report, mixed polymeric micelles (MPMs) system self-assembled from two kinds of cholesterol-grafted amphiphilic block copolymers cholesterol modified poly ([Formula: see text]-amino esters)-grafted disulfide poly (ethylene glycol) methyl ether (PAE(-ss-mPEG)-[Formula: see text]-Chol) and poly([Formula: see text]-amino ester)-g-poly(ethylene glycol) methyl ether-cholesterol (PAE-[Formula: see text]-mPEG-Chol) were prepared for drug delivery and controlled release with pH and redox-responsibilities. The self-assembly of two block copolymers was evaluated by measurement of critical micelle concentration (CMC) values using fluorescence spectroscopy. The hydrodynamic diameter, polydispersity index (PDI) and zeta-potential of MPMs in aqueous were recorded by dynamic light scattering (DLS) at different conditions. Doxorubicin (DOX) was efficiently encapsulated in the micellar core by the hydrophobic interaction. The drug loading content (LC) and encapsulation efficacy (EE) of MPMs with different formulations were evaluated. The DOX was released due to the swelling and disassembly of MPMs induced by low pH and high glutathione (GSH) concentrations. The in vitro results demonstrated that drug release rate and cumulative release were obviously dependent on pH values and reducing agents. The results showed that the MPMs could be the potential anticancer drug delivery carriers with pH/redox-triggered drug release profile.

Evaluation of bio-compatible poly(ethylene glycol)-based solid-phase microextraction fiber for in vivo pharmacokinetic studies of diazepam in dogs

The Analyst ◽  
2007 ◽  
Vol 132 (7) ◽  
pp. 672 ◽  
Author(s):  
Ali Es-haghi ◽  
Xu Zhang ◽  
Florin Marcel Musteata ◽  
Habib Bagheri ◽  
Janusz Pawliszyn
Keyword(s):  
Ethylene Glycol ◽  
Solid Phase Microextraction ◽  
Solid Phase ◽  
Pharmacokinetic Studies ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene

Tissue Distribution and Systemic Toxicity Evaluation of Raloxifene Targeted Polymeric Micelles of Poly (Styrene-Maleic Acid)-Poly (Amide- Ether-Ester-Imide)-Poly (Ethylene Glycol) Loaded With Docetaxel in Breast Cancer Bearing Mice

2019 ◽  
Vol 14 (3) ◽  
pp. 280-291 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Farshid Hassanzadeh ◽  
Batool Hashemi-Beni ◽  
Mohsen Minaiyan ◽  
Saeedeh Enteshari
Keyword(s):  
Side Effects ◽  
Antitumor Activity ◽  
Ethylene Glycol ◽  
Tissue Distribution ◽  
Tumor Cells ◽  
Maleic Acid ◽  
Polymeric Micelles ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Ether Ester

Background: Due to the low water solubility of Docetaxel (DTX), it is formulated with ethanol and Tween 80 with lots of side effects. For this reason, special attention has been paid to formulate it in new drug nano-carriers. Objective: The goal of this study was to evaluate the safety, antitumor activity and tissue distribution of the novel synthesized Raloxifene (RA) targeted polymeric micelles. Methods: DTX-loaded RA-targeted polymeric micelles composed of poly(styrene-maleic acid)- poly(amide-ether-ester-imide)-poly(ethylene glycol) (SMA-PAEE-PEG) were prepared and their antitumor activity was studied in MC4-L2 tumor-bearing mice compared with non-targeted micelles and free DTX. Safety of the micelles was studied by Hematoxylin and Eosin (H&E) staining of tumors and major organs of the mice. The drug accumulation in the tumor and major organs was measured by HPLC method. Results: The results showed better tumor growth inhibition and increased survival of mice treated with DTX-loaded in targeted micelles compared to the non-targeted micelles and free DTX. Histopathological studies, H&E staining of tumors and immunohistochemical examination showed the potential of DTX-loaded RA-targeted micelles to inhibit tumor cells proliferation. The higher accumulation of the DTX in the tumor tissue after injection of the micelles compared to the free DTX may indicate the higher uptake of the targeted micelles by the G-Protein-Coupled Estrogen Receptors (GPER). Conclusion: The results indicate that RA-conjugated polymeric micelles may be a strong and effective drug delivery system for DTX therapy and uptake of the drug into tumor cells, and overcome the disadvantages and side effects of conventional DTX.

scholarly journals Poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) Amphiphilic Copolymers for Long-Acting Injectables: Synthesis, Non-Acylating Performance and In Vivo Degradation

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1438
Author(s):  
Silvio Curia ◽  
Feifei Ng ◽  
Marie-Emérentienne Cagnon ◽  
Victor Nicoulin ◽  
Adolfo Lopez-Noriega
Keyword(s):  
Ethylene Glycol ◽  
Ring Opening ◽  
Gel Chromatography ◽  
Amphiphilic Copolymers ◽  
Trimethylene Carbonate ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Long Acting ◽  
In Vivo Degradation

This article presents the evaluation of diblock and triblock poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) amphiphilic copolymers (PEG-PTMCs) as excipients for the formulation of long-acting injectables (LAIs). Copolymers were successfully synthesised through bulk ring-opening polymerisation. The concomitant formation of PTMC homopolymer could not be avoided irrespective of the catalyst amount, but the by-product could easily be removed by gel chromatography. Pure PEG-PTMCs undergo faster erosion in vivo than their corresponding homopolymer. Furthermore, these copolymers show outstanding stability compared to their polyester analogues when formulated with amine-containing reactive drugs, which makes them particularly suitable as LAIs for the sustained release of drugs susceptible to acylation.

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