Unimolecular Self-Assembled Hemicyanine-Oleic Acid Conjugate Acts as a Novel Succinate Dehydrogenase Inhibitor to Amplify Photodynamic Therapy and Eliminate Cancer Stem Cells.

Photodynamic therapy with reactive oxygen species production is a prospective treatment to combat cancer stem cells (CSCs). However, the innate drawbacks, including short lifetime and diffusion distance of reactive oxygen species and hypoxia within solid tumors, have become bottlenecks for clinical applications of photodynamic therapy. Here, we develop a mitochondria-targeting hemicyanine-oleic acid conjugate (CyOA), which can self-assemble into supramolecular nanoparticles (NPs) without any exogenous excipients.

A novel lonidamine derivative targeting mitochondria to eliminate cancer stem cells by blocking glutamine metabolism.

Cancer stem cells (CSCs) have been blamed as the main culprit of tumor initiation, progression, metastasis, chemoresistance, and recurrence. However, few anti-CSCs agents have achieved clinical success so far. Here we report a novel derivative of lonidamine (LND), namely HYL001, which selectively and potently inhibits CSCs by targeting mitochondria, with 380-fold and 340-fold lower IC values against breast cancer stem cells (BCSCs) and hepatocellular carcinoma stem cells (HCSCs), respectively, compared to LND.

Nature-inspired preparation of self-adhesive, frost-resistant, and ion-conductive hydrogels for flexible strain sensors.

A nature-inspired strategy has been developed to prepare polyvinyl alcohol (PVA)/catechol-modified quaternized chitosan (QCS-C)/MXene hydrogels with good self-adhesion, frost-resistance, and high ion-conductivity. The PVA/QCS-C/MXene hydrogel shows an ionic conductivity of 8.82 S m and a gauge factor of 33.

Graphene oxide-reinforced poly (ether-ether-ketone)/silica composites with improved mechanical performance and surface bioactivity.

The control of interfacial interaction between polymers and fillers is essential for the fabrication of high-performance polymer composites. In this work, poly(ether-ether-ketone)/silica (PEEK/SiO) and PEEK/SiO/graphene oxide (GO) composite were prepared by ball milling-ultrasonic dispersion combined with melt extrusion injection molding. GO nanosheets were introduced as the interfacial enhancer to improve interfacial binding between SiO and PEEK.

Fabrication of FeO@PVA microspheres by one-step electrospray for magnetic resonance imaging during transcatheter arterial embolization.

Magnetic resonance imaging (MRI) has attracted increasing attention as a feasible alternative or adjunctive imaging modality for X-ray digital subtraction angiography because of the high tissue resolution and non-ionization radiation. In this study, a one-step electrospray method was developed to fabricate PVA microspheres encapsulated with in situ synthesized FeO nanoparticles. FeO@PVA microspheres were mono-dispersed black spheres with a wide range of sizes (262-958 µm).

Preparation of carbon nanofibrous mats encapsulating zero-valent Fe nanoparticles as Fe reservoir for removal of organic pollutants.

Zero-valent iron nanoparticles (ZVI NPs) display promising potential in the removal of organic pollutants and heavy metal ions for environmental remediation. However, it is crucial to prevent the oxidation of ZVI NP and control the release of Fe ions under storage and working conditions. In this study, ZVI NPs are encapsulated in single-axial and co-axial carbon nanofibers by electrospinning polyacrylonitrile (PAN)/Fe nanofibrous mats with different structures and then annealing the PAN nanofibrous mats in reduction atmosphere.

Preparation of Poly(ether-ether-ketone)/Nanohydroxyapatite Composites with Improved Mechanical Performance and Biointerfacial Affinity.

Poly(ether-ether-ketone) (PEEK) displays promising potential in hard tissue repair and orthopedic surgery due to its adaptable mechanical performance, good chemical resistance, and bioinertness. However, the low biointerfacial affinity of pure PEEK implants and the decrease of mechanical strength after processing greatly limit their clinical applications. In this work, the influences on mechanical performance and biointerfacial affinity of the PEEK/nanohydroxyapatite (nHA) composites are systematically investigated.

Disulfide based prodrugs for cancer therapy.

Advances in the tumor microenvironment have facilitated the development of novel anticancer drugs and delivery vehicles for improved therapeutic efficacy and decreased side effects. Disulfide bonds with unique chemical and biophysical properties can be used as cleavable linkers for the delivery of chemotherapeutic drugs. Accordingly, small molecule-, peptide-, polymer- and protein-based multifunctional prodrugs bearing cleavable disulfide bonds are well accepted in clinical settings.

Multifunctional hierarchical mesoporous silica and black phosphorus nanohybrids as chemo-photothermal synergistic agents for enhanced cancer therapy.

Synergistic therapy with high efficacy and low side effects is of great significance in cancer treatment, and therefore the elaborate design of advanced nanocarriers to benefit diverse loading requirements of size-varied therapy agents is of critical importance. Herein, we demonstrate a multifunctional drug carrier platform based on a hierarchical porous and -NH2-modified silica nanocarrier (FMSN) with a super high specific surface area and a large pore volume, which not only improves the loading capacity of both doxorubicin, a chemotherapeutic drug, and black phosphorus quantum dots (BPQDs), a kind of biocompatible photothermal agent, but also enhances the photothermal stability and biostability of the degradable BPQDs. The unique structure and surface design enable our multimodal platform with heat-stimulative, pH-responsive and sustained-release properties for chemo-photothermal synergistic cancer therapy.

Coadministration with Tea Polyphenols Enhances the Neuroprotective Effect of Defatted Walnut Meal Hydrolysate against Scopolamine-Induced Learning and Memory Deficits in Mice.

The present study aimed to investigate the combined effects of defatted walnut meal hydrolysate (DWMH) and tea polyphenols (TP) on learning improvement and to explain mechanistically why the combined treatments were more effective than either subject alone. In the step-down avoidance test and the Morris water maze test, codelivery of DWMH and TP was more effective than either individual supplement in reversing memory impairment in scopolamine-treated mice. Mixing with TP significantly facilitated the protective effects of DWMH or DWMH-derived peptides (cationic peptide P1 and anionic peptide P2) on HO-injured SH-SY5Y cells.

A Simple Glutathione-Responsive Turn-On Theranostic Nanoparticle for Dual-Modal Imaging and Chemo-Photothermal Combination Therapy.

Constructing a tumor microenvironment stimuli activatable theranostic nanoparticle with simple components and preparation procedures for multimodality imaging and therapy remains a major challenge for current theranostic systems. Here we report a novel and simple glutathione (GSH)-responsive turn-on theranostic nanoparticle for dual-modal imaging and combination therapy. The theranostic nanoparticle, DHP, consisting of a disulfide-bond-linked hydroxyethyl starch paclitaxel conjugate (HES-SS-PTX) and a near-infrared (NIR) cyanine fluorophore DiR, is prepared with a simple one-step dialysis method.

Antioxidative Effects and Mechanism Study of Bioactive Peptides from Defatted Walnut ( Juglans regia L.) Meal Hydrolysate.

The peptide components of defatted walnut ( Juglans regia L.) meal hydrolysate (DWMH) remain unclear, hindering the investigation of biological mechanisms and exploitation of bioactive peptides. The present study aims to identify the peptide composition of DWMH, followed by to evaluate in vitro antioxidant effects of selected peptides and investigate mechanisms of antioxidative effect.

iRGD-decorated reduction-responsive nanoclusters for targeted drug delivery.

Herein, reduction-responsive disintegratable nanoclusters (NCs) were prepared as a novel nanovehicle for targeted drug delivery. The NCs, with a diameter of ∼170 nm, were self-assembled from hydrophobically modified and iRGD decorated hydroxyethyl starch (iRGD-HES-SS-C18). DOX was loaded into the NCs as a model drug.

Preparation of poly(lactic acid)/graphene oxide nanofiber membranes with different structures by electrospinning for drug delivery.

Nanofiber membranes display promising potential in biomedical fields, especially as scaffolds for drug delivery and tissue engineering. The structures and components of nanofibers play crucial roles in improving the mechanical properties and drug-releasing performance of nanofiber membranes. In this work, poly(lactic acid) (PLA)/graphene oxide (GO) nanofiber membranes with different structures (single-axial and co-axial structure) were prepared by electrospinning.

α-Amylase- and Redox-Responsive Nanoparticles for Tumor-Targeted Drug Delivery.

Paclitaxel (PTX) is an effective antineoplastic agent and shows potent antitumor activity against a wide spectrum of cancers. Yet, the wide clinical use of PTX is limited by its poor aqueous solubility and the side effects associated with its current therapeutic formulation. To tackle these obstacles, we report, for the first time, α-amylase- and redox-responsive nanoparticles based on hydroxyethyl starch (HES) for the tumor-targeted delivery of PTX.

Nanostructured lipid carriers as a novel oral delivery system for triptolide: induced changes in pharmacokinetics profile associated with reduced toxicity in male rats.

After oral administration in rodents, triptolide (TP), a diterpenoid triepoxide compound, active as anti-inflammatory, immunosuppressive, anti-fertility, anti-cystogenesis, and anticancer agent, is rapidly absorbed into the blood circulation (from 5.0 to 19.5 minutes after dosing, depending on the rodent species) followed by a short elimination half-life (from about 20 minutes to less than 1 hour).

A new strategy for enhancing the oral bioavailability of drugs with poor water-solubility and low liposolubility based on phospholipid complex and supersaturated SEDDS.

A novel supersaturated self-emulsifying drug delivery system (Super-SEDDS) loaded with scutellarin-phospholipid complex (SPC) was developed. The system aimed to address the limitations presented by conventional SEDDS as delivery carriers for drugs with poor water-solubility, low liposolubility and high dose. As an intermediate, SPC was first prepared based on the response surface design.

Preparation and optimization of triptolide-loaded solid lipid nanoparticles for oral delivery with reduced gastric irritation.

Triptolide (TP) often causes adverse reactions in the gastrointestinal tract when it is administered orally. This study aimed to prepare and optimize triptolide-loaded solid lipid nanoparticles (TP-SLN) with reduced gastric irritation. The microemulsion technique was used to formulate TP-SLN employing a five-level central composite design (CCD) that was developed for exploring the optimum levels of three independent variables on particle size, encapsulation efficiency (EE) and drug loading (DL).

Micelles assembled with carbocyanine dyes for theranostic near-infrared fluorescent cancer imaging and photothermal therapy.

It is an emerging focus to explore a theranostic nanocarrier for simultaneous cancer imaging and therapy. Herein, we demonstrate a theranostic micelle system for cancer near infrared fluorescent (NIRF) imaging with enhanced signal to noise ratio and superior photothermal therapy. The copolymers consisting of monomethoxy poly(ethylene glycol) and alkylamine-grafted poly(L-aspartic acid) are assembled with carbocyanine dyes into theranostic micelles, which exhibit small size, high loading capacity, good stability, sustained release behavior, and enhanced cellular uptake.

Preparation of Coenzyme Q10 nanostructured lipid carriers for epidermal targeting with high-pressure microfluidics technique.

Objective: The objective of this work was to prepare coenzyme Q10 loaded nanostructured lipid carriers (Q10-NLC) and evaluate its epidermal targeting effect.

Methods: Q10-NLC was prepared by high-pressure microfluidics technique. Formulations and preparation parameters were optimized with response surface design.

Cellular uptake and intracellular trafficking of PEG-b-PLA polymeric micelles.

Besides as an inert carrier for hydrophobic anticancer agents, polymeric micelles composed of di-block copolymer poly(ethylene glycol)-poly(lactic acid) (PEG-b-PLA) function as biological response modifiers including reversal of multidrug resistance in cancer. However, the uptake mechanisms and the subsequent intracellular trafficking remain to be elucidated. In this paper, we found that the uptake of PEG-b-PLA polymeric micelles incorporating nile red (M-NR) was significantly inhibited by both dynamin inhibitor dynasore and dynamin-2 dominant negative mutant (dynamin-2 K44A).

Prolongation of epidural analgesia using solid lipid nanoparticles as drug carrier for lidocaine.

Background And Objectives: Solid lipid nanoparticles (SLNs), as a drug carrier, are a very attractive strategy for sustained and controlled drug release. In this study, we investigated the feasibility of SLNs to prolong the action of lidocaine for potential application in epidural anesthesia and analgesia.

Methods: Lidocaine-loaded SLNs were prepared with different lipids, including monostearin (MS), glyceryl palmitostearate (GP), and stearic acid (SA).

Potent dried drug nanosuspensions for oral bioavailability enhancement of poorly soluble drugs with pH-dependent solubility.

The objective of this study was to enhance the oral bioavailability of itraconazole (ITZ) with dried drug nanosuspensions. The feasibility of using poloxamer 407 or HPMC (50 cp) as stabilizers for preparing ITZ nanosuspensions by facile acid-base neutralization was investigated. Dried ITZ nanosuspensions were prepared by spray drying.

Highly compressed assembly of deformable nanogels into nanoscale suprastructures and their application in nanomedicine.

Assembly of nanoparticles as interfacial stabilizers at oil-in-water (O/W) interfaces into microscopic suprastructures for stabilizing Pickering emulsions is an intriguing focus in the fields of chemical industry and material sciences. However, it is still a major challenge to assemble nanoscale suprastructures using nanoparticles as building blocks at O/W interfaces for fabricating nanoscale emulsion droplets with applicable potential in nanomedicine. Here, we show that it is possible to fabricate the nanodroplets by assembling highly deformable nanogels into the nanoscale suprastructures at spatially confined O/W interfaces.