Development of Core-Crosslinked Micelles for Drug Delivery System

2012 ◽  
Vol 486 ◽  
pp. 449-454 ◽  
Author(s):  
Yue Zhao ◽  
Ming Tao Liang ◽  
Yoseop Kim ◽  
Xin Tan ◽  
Ling Zhang ◽  
...  

A polymer drug delivery system was developed using crosslinked self-assembled micelles, which form stable coreshell particles. The block copolymer, composed of poly [poly (ethylene glycol) methyl ether methacrylat-block-[poly (methyl methacrylate-p-nitrophenyl acrylate)] [P(PEGMEMA)-b-P(MMA-NPA)], was synthesized via reversible addition fragmentation chain transfer (RAFT) polymerization. The self-assembled micelles were stabilized by core crosslinking through the reaction of p-nitrophenyl acrylate with 1,8-octandiamine forming stable coreshell particles.

Nanomedicine ◽  
2019 ◽  
Vol 14 (15) ◽  
pp. 2011-2025 ◽  
Author(s):  
Zhen Li ◽  
Jialong Fan ◽  
Chunyi Tong ◽  
Hongyan Zhou ◽  
Wenmiao Wang ◽  
...  

Aim: Constructing a new drug-delivery system using carboxylated graphene quantum dots (cGQDs) for tumor chemotherapy in vivo. Materials & methods: A drug-delivery system was synthesized through a crosslink reaction of cGQDs, NH2-poly(ethylene glycol)-NH2 and folic acid. Results: A drug delivery system of folic acid-poly(ethylene glycol)-cGQDs was successfully constructed with ideal entrapment efficiency (97.5%) and drug-loading capacity (40.1%). Cell image indicated that the nanosystem entered into human cervical cancer cells mainly through macropinocytosis-dependent pathway. In vivo experiments showed the outstanding antitumor ability and low systemic toxicity of this nanodrug-delivery system. Conclusion: The newly developed drug-delivery system provides an important alternative for tumor therapy without causing systemic adverse effects.


Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5147
Author(s):  
Wanting Hou ◽  
Ruiqi Liu ◽  
Siwei Bi ◽  
Qian He ◽  
Haibo Wang ◽  
...  

Due to a strong retardation effect of o-nitrobenzyl ester on polymerization, it is still a great challenge to prepare amphiphilic block copolymers for polymersomes with a o-nitrobenzyl ester-based hydrophobic block. Herein, we present one such solution to prepare amphiphilic block copolymers with pure poly (o-nitrobenzyl acrylate) (PNBA) as the hydrophobic block and poly (N,N’-dimethylacrylamide) (PDMA) as the hydrophilic block using bulk reversible addition-fragmentation chain transfer (RAFT) polymerization of o-nitrobenzyl acrylate using a PDMA macro-RAFT agent. The developed amphiphilic block copolymers have a suitable hydrophobic/hydrophilic ratio and can self-assemble into photoresponsive polymersomes for co-loading hydrophobic and hydrophilic cargos into hydrophobic membranes and aqueous compartments of the polymersomes. The polymersomes demonstrate a clear photo-responsive characteristic. Exposure to light irradiation at 365 nm can trigger a photocleavage reaction of o-nitrobenzyl groups, which results in dissociation of the polymersomes with simultaneous co-release of hydrophilic and hydrophobic cargoes on demand. Therefore, these polymersomes have great potential as a smart drug delivery nanocarrier for controllable loading and releasing of hydrophilic and hydrophobic drug molecules. Moreover, taking advantage of the conditional releasing of hydrophilic and hydrophobic drugs, the drug delivery system has potential use in medical applications such as cancer therapy.


2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Tabinda Riaz ◽  
Nabyl Khenoussi ◽  
Delia Mihaela Rata ◽  
Leonard Ionut Atanase ◽  
Dominique C. Adolphe ◽  
...  

Abstract Electrospinning (ES) is a versatile and diverse technique to fabricate nano and micro fibers that could be utilized as drug delivery systems. The aim of this research was the fabrication and characterization of drug loaded nanofibrous scaffold produced by single-needle ES using poly(Ɛ-caprolactone) (PCL) and poly(ethylene glycol-400) (PEG) and to investigate the potential of this material as a drug delivery system. A model drug, Ibuprofen (IBU), was used. Ibuprofen is a medicine that is a non-steroidal, anti-inflammatory drug (NSAID). Two concentrations of IBU, 5 wt% and 7 wt%, were incorporated for the ES of PCL and PCL/PEG nanofibers. Characterization of nanofibers was done by using Scanning Electron Microscopy (SEM), Differential Scanning Calorimeter (DSC), Thermogravimetric Analysis (TGA), and Water Contact Angle Measurements. The impact of IBU on nanofibers’ properties such as morphology, diameters, hydrophilicity, and tensile strength was investigated. Finally, the drug release kinetics of IBU from nanofibers was analyzed and their percentage release efficiency of IBU (RE%) was determined by UV-vis spectroscopy during 24 h.


2018 ◽  
Vol 33 (2) ◽  
pp. 119-133 ◽  
Author(s):  
Jing Xu ◽  
Benkai Qin ◽  
Shujuan Luan ◽  
Peilan Qi ◽  
Yingying Wang ◽  
...  

Biodegradable pH-sensitive amphiphilic block polymer (mPEG-Hyde-PLGA) was synthesized via ring-opening polymerization, initiated from a hydrazone-containing macro-initiator. In this way, a pH-sensitive hydrazone bond was inserted into the backbone of block copolymer, linking hydrophilic poly(ethylene glycol) segment and hydrophobic poly(lactic-co-glycolic acid) segment. The copolymer self-assembled to form stable micelles with mean diameters below 100 nm and served as a drug delivery system for doxorubicin, with drug loading content of 5.3%. pH sensitivity of the hydrazone-containing micelles was investigated by changes in diameter and size distribution observed by dynamic light scattering measurements when the micelles were encountered to acidic medium. Small pieces and larger aggregates were found by transmission electron microscopy resulting from the disassociation of the micelles in acidic conditions. It was also noted that doxorubicin release from the pH-sensitive micelles is significantly faster at pH 4.0 and pH 5.0 compared to pH 7.4, while almost no difference was detected in the case of pH non-sensitive micelles. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays on HepG-2 and MCF-7 cells revealed that doxorubicin-loaded pH-sensitive micelles had higher antitumor activity than pH-insensitive ones. This pH-sensitive drug delivery system based on hydrazone-containing block copolymer has been proved as a promising drug formulation for cancer therapy.


Polymers ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 1181
Author(s):  
Lan Yao ◽  
Haihui Li ◽  
Kai Tu ◽  
Lifen Zhang ◽  
Zhenping Cheng ◽  
...  

Polymeric nanomaterials made from amphiphilic block copolymers are increasingly used in the treatment of tumor tissues. In this work, we firstly synthesized the amphiphilic block copolymer PBnMA-b-P(BAPMA-co-PEGMA) via reversible addition-fragmentation chain transfer (RAFT) polymerization using benzyl methacrylate (BnMA), poly (ethylene glycol) methyl ether methacrylate (PEGMA), and 3-((tert-butoxycarbonyl)amino)propyl methacrylate (BAPMA) as the monomers. Subsequently, PBnMA-b-P(APMA-co-PEGMA)@NIR 800 with photothermal conversion property was obtained by deprotection of the tert-butoxycarbonyl (BOC) groups of PBAPMA chains with trifluoroacetic acid (TFA) and post-modification with carboxyl functionalized ketocyanine dye (NIR 800), and it could self-assemble into micelles in CH3OH/water mixed solvent. The NIR photothermal conversion property of the post-modified micelles were investigated. Under irradiation with NIR light (λmax = 810 nm, 0.028 W/cm2) for 1 h, the temperature of the modified micelles aqueous solution increased to 53 °C from 20 °C, which showed the excellent NIR photothermal conversion property.


2011 ◽  
Vol 322 ◽  
pp. 219-223
Author(s):  
Lian Lai Cui ◽  
Tao Yu ◽  
Xin Tan ◽  
Yue Zhao ◽  
Jian Ping Li ◽  
...  

Block copolymers D,L-Polylactide-b-poly(poly(ethylene glycol) methyl ether acrylate) (D,L- P(LA)-b-P(PEGMA)) were prepared via ring-opening polymerization and reversible addition fragmentation chain transfer (RAFT) polymerization. The block polymers generated in the reaction reveal the living behavior with the molecular weight increasing with time. The copolymer D,L-P(LA)200-b-P(PEGMA)225 was synthesized successfully with D,L-P(LA) macro-RAFT agent, and was self-assembled in an aqueous environment, leading to the formation of self-assembly micelles. A distinct critical micelle concentration (CMC) was observed of the self-assembly system. The size of it was characterized by both DLS and TEM.


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