Targeted co-delivery of methotrexate and chloroquine via a pH/enzyme-responsive biocompatible polymeric nanohydrogel for colorectal cancer treatment.

Application of conventional chemotherapy regardless of its unique effectiveness have been gradually being edged aside due to limited targeting capability, lack of selectivity and chemotherapy-associated side effects. To this end, colon-targeted nanoparticles combination therapy have shown great therapeutic potential against cancer. Herein, pH/enzyme-responsive biocompatible polymeric nanohydrogels based on poly(methacrylic acid) (PMAA) containing methotrexate (MTX) and chloroquine (CQ) were fabricated.

evaluation of anti-angiogenesis property of anti-VEGFR2 nanobody-conjugated H40-PEG carrier loaded with methotrexate.

Objectives: In this study, Boltorn® H40-PEG-MTX-anti-VEGFR2 nanobody was fabricated in which nanobody was selected for blocking the receptor, H40 as a nanocarrier for delivery of methotrexate (MTX) to the tumor cells, and polyethylene glycol (PEG) moieties for improving the blood circulation time and safety.

Materials And Methods: The synthesis process of the nanosystem has been characterized by different analytical methods.

Results: The prepared nanoplatform exhibited high drug loading capacity, excellent colloidal stability, and an average particle size of around 105 nm.

Recent advances in targeting malaria with nanotechnology-based drug carriers.

Malaria, as one of the most common human infectious diseases, remains the greatest global health concern, since approximately 3.5 billion people around the world, especially those in subtropical areas, are at the risk of being infected by malaria. Due to the emergence and spread of drug resistance to the current antimalarials, malaria-related mortality and incidence rates have recently increased.

A robust polyfunctional Pd(II)-based magnetic amphiphilic nanocatalyst for the Suzuki-Miyaura coupling reaction.

Herein, a robust Pd(II)-based polyfunctional magnetic amphiphilic artificial metalloenzyme was prepared by anchoring a Pd(2,2'-dipyridylamine)Cl bearing hydrophilic monomethyl ether poly(ethylene glycol) (mPEG) chains on the surface of amino-functionalized silica-coated magnetic nanoparticles. The 2,2'-dipyridylamine (dpa) has shown excellent complexation properties for Pd(II) and it could be easily anchored onto functionalized magnetic support by the bridging nitrogen atom. Moreover, the bridging nitrogen atom at the proximity of Pd(II) catalytic center could play an important role in dynamic suppramolecular interactions with substrates.

pH-sensitive curcumin conjugated micelles for tumor triggered drug delivery.

Development of new drugs are confronted with some barriers and challenges, since these projects are mainly expensive, complex, time consuming with lack of success, there is an urgent need to reformulate the current poorly water soluble anti-cancer drugs. In this study, a new type of polymer-curcumin conjugates based on glycidyl azide polymer (GAP) was developed for cancer therapy. The copolymer was used for delivery of curcumin (CUR) as an anticancer drug to cancer cells.

pH-Sensitive Magnetite Nanoparticles Modified with Hyperbranched Polymers and Folic Acid for Targeted Imaging and Therapy.

Objective: A novel pH-sensitive superparamagnetic drug delivery system was developed based on quercetin loaded hyperbranched polyamidoamine-b-polyethylene glycol-folic acid-modified Fe3O4 nanoparticles (Fe3O4@PAMAM-b-PEG-FA).

Methods: The nanoparticles exhibit excellent water dispersity with well-defined size distribution (around 51.8 nm) and strong magnetisability.

Synthesis and evaluation of injectable thermosensitive penta-block copolymer hydrogel (PNIPAAm-PCL-PEG-PCL-PNIPAAm) and star-shaped poly(CL─CO─LA)-b-PEG for wound healing applications.

Background: Loss of skin integrity due to injury, burning, or illness makes the development of new treatment options necessary. Skin tissue engineering provides some solutions for these problems.

Objective: The potential of a biodegradable star-shaped copolymer [Poly(CL─CO─LA)-b-PEG] and penta-block copolymer hydrogel (PNIPAAm-PCL-PEG-PCL-PNIPAAm) was assessed for skin tissue engineering applications.

Synthesis and Characterization of Biodegradable Semi-Interpenetrating Polymer Networks Based on Star-Shaped Copolymers of ɛ-Caprolactone and Lactide.

In this paper, the focus is on a new kind of biodegradable semi-interpenetrating polymer networks, which is derived from ɛ-caprolactone, lactide, 1,4-butane diisocyanate and ethylenediamine and also its potential has been investigated in soft tissue engineering applications. The polymers were characterized by nuclear magnetic resonance (NMR) spectrometry, Fourier transform infrared spectroscopy (FT-IR), differential thermal analysis (DTA), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). These experiments show that the polymers with the right composition and the expected molecular weight were achieved.

Design and construction of multifunctional hyperbranched polymers coated magnetite nanoparticles for both targeting magnetic resonance imaging and cancer therapy.

Magnetic drug targeting is a drug delivery strategy that can be used to improve the therapeutic efficiency on tumor cells and reduce the side effects on normal cells and tissues. The aim in this study is designing a novel multifunctional drug delivery system based on superparamagnetic nanoparticles for cancer therapy. Magnetic nanoparticles were synthesized by coprecipitation of iron oxide followed by coating with poly citric acid (PCA) dendritic macromolecules via bulk polymerization strategy.

pH-responsive unimolecular micelles self-assembled from amphiphilic hyperbranched block copolymer for efficient intracellular release of poorly water-soluble anticancer drugs.

Novel unimolecular micelles from amphiphilic hyperbranched block copolymer H40-poly(ε-caprolactone)-b-poly(acrylic acid)-b'-methoxy poly(ethylene glycol)/poly(ethylene glycol)-folate (i.e., H40-PCL-b-PAA-b'-MPEG/PEG-FA (HCAE-FA)) as new multifunctional nanocarriers to pH-induced accelerated release and tumor-targeted delivery of poorly water-soluble anticancer drugs were developed.

Folate-decorated thermoresponsive micelles based on star-shaped amphiphilic block copolymers for efficient intracellular release of anticancer drugs.

In this study, a new type of folate-decorated thermoresponsive micelles based on the star-shaped amphiphilic block copolymer 4s[poly(ε-caprolactone)-b-2s(poly(N-isopropylacrylamide-co-acrylamide)-b'-methoxy poly(ethylene glycol)/poly(ethylene glycol)-folate)] (i.e., 4s[PCL-b-2s(P(NIPAAm-co-AAm)-b'-MPEG/PEG-FA)] (PCIAE-FA)), were developed for the tumor-targeted delivery and temperature-induced controlled release of hydrophobic anticancer drugs.

Ultrasound-promoted synthesis of novel spirooxindolo/spiroacenaphthen dicyano pyrrolidines and pyrrolizidines through regioselective azomethine ylide cycloaddition reaction.

Novel dicyano functionalised spiropyrrolidine and spiropyrrolizidine were synthesized from the reaction of various arylidenemalononitrile Knöevenagel adducts with non-stabilized azomethine ylides generated from isatin/acenaphthenequinone and sarcosine/N-phenylglycine/proline. The reactions were carried out under both conventional heating and ultrasonic irradiation conditions. In general, improvement in rates and yields were observed when the reactions were carried out under sonication compared with classical conditions.

Ultrasound-assisted one-pot, three-component synthesis of 1H-pyrazolo[1,2-b]phthalazine-5,10-diones.

Triethylamine was found to be an efficient catalyst for the synthesis of 1H-pyrazolo[1,2-b]phthalazine-5,10-diones by one-pot reaction of phthalhydrazide, aromatic aldehydes, and malononitrile or ethyl cyanoacetate in ethanol under ultrasonic irradiation. The advantages of this method are the use of an inexpensive and readily available catalyst, easy workup, improved yields, and the use of ethanol as a solvent that is considered to be relatively environmentally benign.

1'-Methyl-2-oxo-5'-phenyl-spiro-[indoline-3,3'-pyrrolidine]-4',4'-dicarbo-nitrile.

The title spiro-compound, C(20)H(16)N(4)O, crystallizes with four independent mol-ecules in the asymmetric unit. In all of them, the oxindole unit is planar, the r.m.