scholarly journals Construction of Dimeric Drug-Loaded Polymeric Micelles with High Loading Efficiency for Cancer Therapy

2019 ◽  
Vol 20 (8) ◽  
pp. 1961 ◽  
Author(s):  
Bing Yu ◽  
Qingye Meng ◽  
Hao Hu ◽  
Tao Xu ◽  
Youqing Shen ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Poly Ethylene Glycol ◽  
The Core ◽  
Loading Efficiency ◽  
Low Load ◽  
Poly Ethylene ◽  
Phosphate Buffered Saline ◽  
Hydrophilic Shell

Polymeric micelles (PMs) have been applied widely to transport hydrophobic drugs to tumor sites for cancer treatment. However, the low load efficiency of the drug in the PMs significantly reduces the therapeutic efficiency. We report here that disulfide-linked camptothecin (CPT) as a kind of dimeric drug can be effectively embedded in the core of poly(ε-caprolactone)–poly(ethylene glycol)–poly(ε-caprolactone) (PCL–PEG–PCL) PMs for improving drug-loading efficiency, and PEG can be used as a hydrophilic shell. Moreover, the dimeric CPT-loaded PCL–PEG–PCL PMs exhibited excellent solubility in phosphate-buffered saline (PBS) media and significant cytotoxicity to cancer cells.

scholarly journals Impact of Core-Forming Segment Structure on Drug Loading in Biodegradable Polymeric Micelles Using PEG-b-Poly(lactide-co-depsipeptide) Block Copolymers

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Akihiro Takahashi ◽  
Yuta Ozaki ◽  
Akinori Kuzuya ◽  
Yuichi Ohya
Keyword(s):  
Block Copolymers ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Polymeric Micelle ◽  
Molecular Weights ◽  
The Core ◽  
Drug Delivery Carrier ◽  
Loading Efficiency ◽  
Drug Loading Efficiency ◽  
Model Drug

We synthesized series of amphiphilic AB-type block copolymers having systematic variation in the core-forming segments using poly(lactide-co-depsipeptide)s as a hydrophobic segment and prepared polymeric micelles using the block copolymers, PEG-b-poly(lactide-co-depsipeptide). We then discussed the relationship between the core-forming segment structure and drug loading efficiency for the polymeric micelles. PEG-b-poly(lactide-co-depsipeptide)s, PEG-b-PLGL containingl-leucine (Leu), and PEG-b-PLGF containingl-phenylalanine (Phe), with similar molecular weights and various mole fractions of depsipeptide units, were synthesized. Polymeric micelles entrapping model drug (fluorescein, FL) were prepared using these copolymers. As a result, PEG-b-poly(lactide-co-depsipeptide) micelles showed higher drug loading compared with PEG-b-PLLA and PEG-b-PDLLA as controls. The drug loading increased with increase in the mole fraction of depsipeptide unit in the hydrophobic segments. The introduction of aliphatic and aromatic depsipeptide units was effective to achieve higher FL loading into the micelles. PEG-b-PLGL micelle showed higher drug loading than PEG-b-PLGF micelle when the amount of FL in feed was high. These results obtained in this study should be useful for strategic design of polymeric micelle-type drug delivery carrier with high drug loading efficiency.

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 Fabrication of Hybrid Polymeric Micelles Containing AuNPs and Metalloporphyrin in the Core

Polymers ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 390 ◽  
Author(s):  
Yanxia Wang ◽  
Heng Yang ◽  
Si Chen ◽  
Hua Chen ◽  
Zhihua Chai
Keyword(s):  
Polymeric Micelles ◽  
Laser Light ◽  
Poly Ethylene Glycol ◽  
Axial Coordination ◽  
The Core ◽  
Novel Approach ◽  
Transmission Electron ◽  
Uv Visible ◽  
Poly Ethylene ◽  
Copolymer Poly

Multi-structure assemblies consisting of gold nanoparticles and porphyrin were fabricated by using diblock copolymer, poly(ethylene glycol)-block-poly(4-vinylpyridine) (PEG-b-P4VP). The copolymer of PEG-b-P4VP was used in the formation of core-shell micelles in water, in which the P4VP block serves as the core, while the PEG block forms the shell. In the micellar core, gold nanoparticle and metalloporphyrin were dispersed through the axial coordination. Structural and morphological characterizations of the complex micelle were carried out by transmission electron microscopy, laser light scatting, and UV-visible spectroscopy. Metalloporphyrin in the complex micelle exhibited excellent photostability by reducing the generation of the singlet oxygen. This strategy may provide a novel approach to design photocatalysts that have target applications in photocatalysis and solar cells.

scholarly journals Optimization of self-assembling properties of fatty acids grafted to methoxy poly(ethylene glycol) as nanocarriers for etoposide

2012 ◽  
Vol 62 (1) ◽  
pp. 31-44 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Farshid Hasanzadeh ◽  
Mojtaba Eslamdoost
Keyword(s):  
Fatty Acids ◽  
Ethylene Glycol ◽  
Chain Length ◽  
Drug Loading ◽  
Poly Ethylene Glycol ◽  
Self Assembling ◽  
Loading Efficiency ◽  
Drug Loading Efficiency ◽  
Poly Ethylene ◽  
Polymer Ratio

Optimization of self-assembling properties of fatty acids grafted to methoxy poly(ethylene glycol) as nanocarriers for etoposide The objective of this work was to study the effect of fatty acid chain length grafted to methoxy poly(ethylene glycol) (mPEG) on self assembling properties of micelles for etoposide delivery. Three amphiphilic copolymers were synthesized using mPEG, myristic acid, stearic acid and behenic acid through an esteric linkage. The particle size and zeta potential of the micelles were determined by the dynamic light scattering method. Etoposide was loaded into micelles by film casting using various drug/polymer ratios. Drug release was studied by the dialysis method. The structure of copolymers was confirmed by 1H NMR and FTIR. Central micellar concentration (CMC) measurements showed that the longer hydrophobic chains formed more thermodynamically stable micelles. Among the prepared copolymers, etoposide showed the highest solubility in the mPEG-behenic copolymer. Drug loading efficiency depended on the hydrophobic chain length and drug/polymer ratio. The highest drug loading efficiency was found in mPEG-myristic micelles with 1:20 drug/polymer ratio. Micelles released 80 % of loaded drug within about 5 h.

scholarly journals Reduction-Triggered Breakable Micelles of Amphiphilic Polyamide Amine-g-Polyethylene Glycol for Methotrexate Delivery

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Yihang Huang ◽  
Jun Liu ◽  
Yani Cui ◽  
Huanan Li ◽  
Yong Sun ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Chemical Structure ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Hydrophobic Core ◽  
The Core ◽  
Loading Efficiency ◽  
Normal Circumstance ◽  
Intracellular Compartments ◽  
Drug Loading Efficiency

Reduction-triggered breakable polymeric micelles incorporated with MTX were prepared using amphiphilic PAA-g-PEG copolymers having S–S bonds in the backbone. The micelles were spherical with diameters less than 70 nm. The micelles could encapsulate the hydrophobic MTX in the hydrophobic core. The drug loading content and drug loading efficiency of the micelles were highly dependent on the copolymer chemical structure, ranging from 2.9 to 7.5% and 31.9 to 82.5%, respectively. Both the drug loading content and drug loading efficiency increased along with more hydrophobic segments in the copolymers. In normal circumstance, these micelles were capable of keeping stable and hold most of the MTX in the core, stabilizing the incorporated MTX through theπ-πstacking with the phenyl groups in the backbone of the copolymers. In reductive environments that mimicked the intracellular compartments, the entire MTX payload could be quickly released due to the reduction-triggered breakage of the micelles. These micelles showed good antiproliferative activity against several cancer cell lines, including KB, 4T-1 and HepG2, especially within the low drug concentration scope.

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