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polymer micelle

Xin-Yue Dong, Tian-Qun Lang, Qi Yin, Peng-Cheng Zhang, Ya-Ping Li
Breast cancer is the most vicious killer for women, and tumor metastasis is one of the leading causes of breast cancer therapy failure. In this study, a new pH-sensitive polymer (polyethylene glycol-block-poly[(1,4-butanediol)-diacrylate-β-N,N-diisopropylethylenediamine], BDP) was synthesized. Based on BDP, docetaxel/silibinin co-delivery micelles (DSMs) was constructed. DSM had a well-defined spherical shape under the transmission electron microscope with average hydrodynamic diameter of 85.3±0.4 nm, and were stable in the bloodstream but could dissociate to release the chemotherapeutic agents in the low pH environment of the endo/lysosomes in the tumor cells...
July 17, 2017: Acta Pharmacologica Sinica
Hira Choudhury, Bapi Gorain, Manisha Pandey, Santosh Ashok Kumbhar, Rakesh Kumar Tekade, Arun K Iyer, Prashant Kesharwani
Docetaxel (DTX) is one of the important antitumor drugs, being used in several common chemotherapies to control leading cancer types. Severe toxicities of the DTX are prominent due to sudden parenteral exposure of desired loading dose to maintain the therapeutic concentration. Field of nanotechnology is leading to resist sudden systemic exposure of DTX with more specific delivery to the site of cancer. Further nanometric size range of the formulation aid for prolonged circulation, thereby extensive exposure results better efficacy...
July 12, 2017: International Journal of Pharmaceutics
He-Lin Xu, Zi-Liang Fan, De-Li ZhuGe, Bi-Xin Shen, Bing-Hui Jin, Jian Xiao, Cui-Tao Lu, Ying-Zheng Zhao
Severe toxicity and poor tumour penetration are two intrinsic limited factors to hinder the broad clinical application for most of first-line chemotherapeutics. In this study, a novel vitamin E succinate-grafted ε-polylysine (VES-g-PLL) polymer was synthesized by using ε-polylysine as backbone. By adjusting VES graft ratio, VES-g-PLL (50) with a theoretic VES graft ratio of 50% could self-assemble into a supermolecular micelle with a hydrodynamic diameter (Dh) of ca.20nm, and Zeta potential of 19.6mV. VES-g-PLL micelles themselves displayed a strong anti-tumour effect on glioma...
July 12, 2017: Colloids and Surfaces. B, Biointerfaces
Mingwei Mu, Tomohiro Konno, Yuuki Inoue, Kazuhiko Ishihara
To achieve stable and effective solubilization of poorly water-soluble bioactive compounds, water-soluble and amphiphilic polymers composed of hydrophilic 2-methacryloyloxyethyl phosphorylcholine (MPC) units and hydrophobic n-butyl methacrylate (BMA) units were prepared. MPC polymers having different molecular architectures, such as random-type monomer unit sequences and block-type sequences, formed polymer aggregates when they were dissolved in aqueous media. The structure of the random-type polymer aggregate was loose and flexible...
June 29, 2017: Colloids and Surfaces. B, Biointerfaces
Jaleh Varshosaz, Somayeh Taymouri, Erfaneh Ghassami
Polymer micellar nanogels are a group of core-shell polymeric micelles with swelling properties in aqueous media. Nanogel systems have proven their potential in controlled, sustained and targetable drug delivery area with no immunological responses. This review includes a comprehensive wide range of self-assembly of polymeric nanogels as delivery systems for anticancer drugs. Nanogels are nanoparticulate drug delivery systems which are specially designed for enhanced target oriented and cellular uptake of drugs with emphasis on chemotherapeutic agents studied in this review...
July 10, 2017: Current Pharmaceutical Design
Tarun Ojha, Vertika Pathak, Yang Shi, Wim Hennink, Chrit Moonen, Gert Storm, Fabian Kiessling, Twan Lammers
The performance of nanomedicine formulations depends on the Enhanced Permeability and Retention (EPR) effect. Prototypic nanomedicine-based drug delivery systems, such as liposomes, polymers and micelles, aim to exploit the EPR effect to accumulate at pathological sites, to thereby improve the balance between drug efficacy and toxicity. Thus far, however, tumor-targeted nanomedicines have not yet managed to achieve convincing therapeutic results, at least not in large cohorts of patients. This is likely mostly due to high inter- and intra-patient heterogeneity in EPR...
July 8, 2017: Advanced Drug Delivery Reviews
Qingjing Tian, Jia Shi, Xiaoyun Zhao, Donghua Di, Yihui Deng, Yanzhi Song
Tocopheryl polyethylene glycol 1000 succinate (TPGS) is considered a promising surfactant, but its high critical micelle concentration (CMC) limits its application. Cholesterol is hydrophobic, can act as a tumor-targeting ligand, and has strong binding ability with taxoids. Based on this information, we coupled cholesterol with TPGS to synthesize cholesterol-coupled TPGS (TPGS-CHMC), which had a lower CMC than pure TPGS. The TPGS-CHMC was used to prepare micelles loading with docetaxel (DTX) by a self-assembly method...
July 10, 2017: Drug Delivery and Translational Research
Christoph Göbel, Ottokar Klimm, Florian Puchtler, Sabine Rosenfeldt, Stephan Förster, Birgit Weber
Spin-crossover compounds are a class of materials that can change their spin state from high spin (HS) to low spin (LS) by external stimuli such as light, pressure or temperature. Applications demand compounds with defined properties concerning the size and switchability that are maintained when the compound is integrated into composite materials. Here, we report the synthesis of [Fe(Leq)(Lax)]n coordination polymer (CP) nanoparticles using self-assembled polystyrene-block-poly(4-vinylpyridine) (PS-b-P4VP) block copolymer (BCP) micelles as template...
2017: Beilstein Journal of Nanotechnology
Maikel Herbrink, Jan H M Schellens, Jos H Beijnen, Bastiaan Nuijen
The tyrosine kinase inhibitor nilotinib has a very low aqueous solubility and a low and variable oral bioavailability. A pharmaceutical formulation with an improved solubility may enhance the bioavailability and reduce the variability thereof and of the pharmacokinetics. The aim of this study was to enhance the solubility of nilotinib by developing a spray dried solid dispersion. A broad selection of polymer excipients were tested for solubilizing properties. The spray drying technique was used to produce solid dispersions of nilotinib hydrochloride (NH) in matrices of the best performing polymers...
July 8, 2017: International Journal of Pharmaceutics
Weiping Ji, Bo Wang, Qiuping Fan, Chao Xu, Youwu He, Youfen Chen
Multidrug resistance (MDR) against chemotherapeutic agents has become the major obstacle to successful cancer therapy and multidrug resistance-associated proteins (MRPs) mediated drug efflux is the key factor for MDR. Indomethacin (IND), one of the non-steroidal anti-inflammatory agents, has been demonstrated to increase cytotoxic effects of anti-tumor agents as MRP substrates. In this study, dextran-g-indomethacin (DEX-IND) polymeric micelles were designed to delivery paclitaxel (PTX) for the treatment of MDR tumors...
2017: PloS One
Seema Upadhyay, Iliyas Khan, Avinash Gothwal, Praveen K Pachouri, N Bhaskar, Umesh D Gupta, Devendra S Chauhan, Umesh Gupta
PURPOSE: First line antiTB drugs have several physical and toxic manifestations which limit their applications. RIF is a hydrophobic drug and has low water solubility and INH is hepatotoxic. The main objective of the study was to synthesize, characterize HPMA-PLA co-polymeric micelles for the effective dual delivery of INH and RIF. METHODS: HPMA-PLA co-polymer and HPMA-PLA-INH (HPI) conjugates were synthesized and characterized by FT-IR and (1)H-NMR spectroscopy...
July 6, 2017: Pharmaceutical Research
Robert J Ono, Ashlynn L Z Lee, Zhi Xiang Voo, Shrinivas Venkataraman, Bei Wei Koh, Yi Yan Yang, James L Hedrick
Biodegradable polycarbonate-based ABA triblock copolymers were synthesized via organocatalyzed ring-opening polymerization, and successfully formulated into chemically crosslinked hydrogels by strain-promoted alkyne-azide cycloaddition (SPAAC). The synthesis and crosslinking of these polymers is copper-free, thereby eliminating the concern over metallic contaminants for biomedical applications. Gelation occurs rapidly within a span of 60 seconds by simple mixing of the azide- and cyclooctyne-functionalized polymer solutions...
July 6, 2017: Biomacromolecules
Jos W H Wennink, Yanna Liu, Petri I Mäkinen, Francesca Setaro, Andrès de la Escosura, Meriem Bourajjaj, Jari P Lappalainen, Lari P Holappa, Joep B van den Dikkenberg, Mina Al Fartousi, Panagiotis N Trohopoulos, Seppo Ylä-Herttuala, Tomas Torres, Wim E Hennink, Cornelus F van Nostrum
Selective elimination of macrophages by photodynamic therapy (PDT) is a new and promising therapeutic modality for the reduction of atherosclerotic plaques. m-Tetra(hydroxyphenyl)chlorin (mTHPC, or Temoporfin) may be suitable as photosensitizer for this application, as it is currently used in the clinic for cancer PDT. In the present study, mTHPC was encapsulated in polymeric micelles based on benzyl-poly(ε-caprolactone)-b-methoxy poly(ethylene glycol) (Ben-PCL-mPEG) using a film hydration method, with loading capacity of 17%...
July 2, 2017: European Journal of Pharmaceutical Sciences
Leonardo Chiappisi, Stephen David Leach, Michael Gradzielski
The formation of water insoluble polyelectrolyte/surfactant complexes (PESCs) upon mixing two homogeneous polycation/anionic surfactant and polycation/nonionic surfactant solutions is reported here. This phase separation is unexpected and differs markedly from the commonly observed enhanced solubility of colloidal systems in mixed surfactant systems. The study was performed on mixtures of the cationic biopolysaccharide chitosan (poly d-glucosamine) and mixed micelles composed of an ethoxylated fatty alcohol and its carboxylic acid terminated equivalent...
July 5, 2017: Soft Matter
Roman Lehner, Kegang Liu, Xueya Wang, Patrick Hunziker
Novel, biocompatible polyplexes, based on the combination of cationic pentablock copolymers with folic acid functionalized copolymers were designed and developed for target-specific siRNA delivery. The resulting micelleplexes spontaneously formed polymeric micelles with a hydrophobic core surrounded directly by a cationic poly-2-(4-azidobutyl)-oxazole (PABOXA) and subsequently shielded by hydrophilic poly-2-methyl-oxazole (PMOXA) layer. The described micelleplexes form highly stable particles even in complete serum after 24 h compared with the highly cationic polymer PEI, which show aggregate formation in serum containing buffer solution...
July 4, 2017: Biomacromolecules
Ming-Xue Wu, Xin Wang, Ying-Wei Yang
Researches on cargo delivery systems have received burgeoning attention and advanced rapidly. For synthetic nanodevices, polymer nanoassemblies and their inorganic-organic hybrid materials, especially smart mesoporous silica nanoparticle (MSN)-polymer hybrids (e. g., MSN@PGMAs), have attracted increasing attention in recent years. Their superior characteristics and unique features such as dynamic transition of morphology endow them the ability to efficiently entrap cargo molecules and undergo smart cargo delivery and release in response to various external stimuli...
July 4, 2017: Chemical Record: An Official Publication of the Chemical Society of Japan ... [et Al.]
Wendong Ke, Zengshi Zha, Jean Felix Mukerabigwi, Weijian Chen, Yuheng Wang, Chuanxin He, Zhishen Ge
The amphiphilic block copolymer anticancer drug nanocarriers clinically used or in the progress of clinical trials frequently suffer from the modest final therapeutic efficacy due to lack of intelligent features. For example, the biodegradable amphiphilic block copolymer, poly(ethylene glycol)-b-poly(D,L-lactide) (PEG-PDLLA), has been approved for clinical applications as a paclitaxel (PTX) nanocarrier (Genexol-PM) due to the optimized pharmacokinetics and biodistribution, however, lack of intelligent features limits the intracellular delivery in tumor tissue...
June 29, 2017: Bioconjugate Chemistry
Claudia Dähling, Gudrun Lotze, Hideharu Mori, Dmitry V Pergushov, Felix A Plamper
The kinetics of interpolyelectrolyte complexation involving architecturally complex (star-like) polymeric components is addressed. Specifically, the spontaneous coupling of branched cationic star-shaped miktoarm polymers, i.e., quaternized poly(ethylene oxide)114-(poly(2-(dimethylamino)ethyl methacrylate)17)4 (PEO114-(qPDMAEMA17)4), and temperature-sensitive linear anionic diblock copolymers poly(vinyl sulfonate)31-b-poly(N-isopropylacrylamide)27 (PVS31-b-PNIPAM27) and further rearrangements of the formed complexes were investigated by means of stopped-flow small-angle X-ray scattering (SAXS)...
June 29, 2017: Journal of Physical Chemistry. B
Zhi Liu, Max Purro, Jing Qiao, May P Xiong
Multifunctional self-assembled micelles composed of Pluronics F127 polymer chains are developed and investigated for chelation and selective detection of iron(III) in vitro and in iron-overloaded cells. Tetraphenylethene (TPE) is encapsulated into the micelle core and the iron chelate drug deferoxamine (DFO) is conjugated to micelles to generate a fluorescence quenching detection system termed DFO-TFM for short, where T stands for TPE, F for F127, and M for micelle. The key to the successful formation of this fluorescence quenching system is due to the near-ideal overlap between the absorption spectrum of the DFO:iron(III) complex and fluorescence spectrum of TPE...
June 29, 2017: Advanced Healthcare Materials
Sang-Min Lee
An amphiphilic cholesterol-terminated poly[acrylic acid] (Chol-PAA) that can be self-aggregated into nanoscale micelles in aqueous media has been prepared via nitroxide-mediated radical polymerization for the facile postformation modification of lipid vesicles. By varying the amount of Chol-PAA addition, the incorporation of Chol-PAA on the liposome templates was verified with zeta potential while the dynamic light scattering measurements revealed the polymer length of Chol-PAA dictated the hydrodynamic diameter of the resulting polymer-grafted vesicles (PGVs)...
June 26, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
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