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A Nano-QSAR Model for the Cytotoxicity of Doxorubicin Prodrug Micelles in Multidrug-Resistant Cancer Cells.

Nano-QSAR modeling provides a cost-effective approach for predicting the toxic effects of nanoparticles by reducing the experimental effort and improving the predictive accuracy. Cytotoxicity is the degree of toxicity of the particles toward the cells. In this study, a nano-QSAR model was developed for estimating the cytotoxicity (pIC50) of doxorubicin prodrug micelles on MCF-7/ADR cells by using degree-based topological indices and physicochemical properties such as particle size and polydispersity index. Doxorubicin is a leading anticancer drug, and using it as a nanomedicine, doxorubicin pr…

Polymeric micelle loaded with lapachol for topical treatment of mice infected with Leishmania (Leishmania) major.

Cutaneous leishmaniasis (CL) is a neglected tropical disease. The treatment is restricted to a handful number of drugs that exhibit toxic effects and limited efficacy. The development of new alternative therapies, including the identification of effective drugs for topical treatment of CL, is of utmost interest. The aim of this study was to prepare, characterize and evaluate the efficacy of topical therapy with lapachol-micelle in the experimental treatment of CL. The lapachol-micelle was prepared using polaxamer 407. A preliminary stability study was conducted for 15 days at room temperature.

Development of a reverse-phase HPLC method for the simultaneous determination of curcumin and dexamethasone in polymeric micelles.

BACKGROUND: A rapid, simple, accurate, and robust reverse-phase high-performance liquid chromatography (RP-HPLC) method was developed to quantify curcumin and dexamethasone in polymeric micelle nanoparticle formulations simultaneously. METHODS: The optimized chromatographic conditions involved a Universal HS C18 column, isocratic elution with a methanol: acidic water (pH 3.5, 80:20, v/v) mobile phase, and detection wavelengths of 425 nm for curcumin and 254 nm for dexamethasone. The developed method was subsequently validated according to ICH guidelines, and demonstrated excellent linearity (

Effects of hydrophobic chain lengths on the structure and properties of polymeric micelles: experimental and simulation studies.

Amphiphilic block copolymers with polyester-based hydrophobic segments, particularly PEG-PLA, exhibit considerable potential as carrier materials for delivering water-insoluble small-molecule drugs via self-assembled micelles. A comprehensive understanding of relationship between carrier material structures and micelle properties is critical for optimizing the drug-loading capacities, drug release behaviors and tumor cell inhibitory properties of micelle formulations. This study aims to elucidate the influences of different hydrophobic chain lengths of mPEG-PLLA on self-assembling to micelles …

Polymeric micelle gel with luliconazole: in vivo efficacy against cutaneous candidiasis in Wistar rats.

The objective of this research was focused on the design and development of luliconazole-loaded polymeric micelle hydrogel (LUL-PM-CHG) usin … e size, micellar incorporation efficiency, and polydispersity index. The LUL-loaded P123/F127 mixed micelles involved the thin film hydration method for thin preparation. The characteristics of optimized formulation include a particle size of 226 ± 8.52 nm, a polydispersity index (PDI) of 0.153 ± 0.002, a zeta potential (ZP) of 30.15 ± 2.32 mV, and a micel …

Influence of calcium concentration on the re-assembly of sodium caseinate into casein micelles and on their renneting behavior.

Inducing the spontaneous aggregation from casein molecules (i.e. αs1, αs2, β, and κ-casein) into re-assembled casein micelles (RCMs) through the addition of salts as an alternative to native casein micelles, has garnered increasing attention in recent years. In this investigation, re-assembled casein micelles were generated by adding varying amounts of calcium, phosphate, and citrate ions to a sodium caseinate dispersion. The formed micelles were further characterized in terms of particle size, optical density, and partitioning of calcium ions and caseins. Besides, their small-angle X-ray scat…

A tumor targeted nano micelle carrying astragaloside IV for combination treatment of bladder cancer.

Immune checkpoint inhibitors (ICIs) are effective agents for tumor immunotherapy. However, their clinical effectiveness is unsatisfactory due to off-target effects and a suppressive immune microenvironment. This study developed a nanodrug delivery system for bladder cancer (BCa) using PCL-MPEG and PCL-PEG-CHO to synthesize internal hydrophobic and external hydrophilic micelles (PP) that encapsulated water-insoluble astragaloside IV (PPA). The aldehyde group on the surface of PPA reacted with the amino group of aPD-L1, allowing the decoration of this antibody on the surface of the micelles. The…

Micelle-mediated synthesis of quinoxaline, 1,4-benzoxazine and 1,4-benzothiazine scaffolds from styrenes.

A range of heterocycles based on quinoxalines, 1,4-benzoxazines and 1,4-benzothiazines have been accessed from styrenes by reacting them with benzene-1,2-diamine, 2-aminophenol and 2-aminothiophenol respectively in micellar medium. This reaction occurring in a less explored cetylpyridinium bromide (CPB) micellar medium operates in the presence of NBS through a tandem hydrobromination-oxidation cascade, converting styrenes to phenacyl bromides. Its subsequent nucleophilic addition with aromatic 1,2-dinucleophiles and further transformations led to the formation of heterocyclic constructs. The l

Harnessing Competitive Interactions to Regulate Supramolecular "Micelle-Droplet-Fiber" Transition and Reversibility in Water.

The supramolecular assembly of proteins into irreversible fibrils is often associated with diseases in which aberrant phase transitions occur. Due to the complexity of biological systems and their surrounding environments, the mechanism underlying phase separation-mediated supramolecular assembly is poorly understood, making the reversal of so-called irreversible fibrillization a significant challenge. Therefore, it is crucial to develop simple model systems that provide insights into the mechanistic process of monomers to phase-separated droplets and ordered supramolecular assemblies. Such mo

Solubility Enhancement and Antioxidation Maintenance of CBD Encapsulated in the P407-RUB Nano-micelle System.

AIM: The aim of this study is to improve the water solubility and stability of cannabidiol (CBD) utilizing micelle technology. MATERIALS AND METHODS: Mixing of rubusoside (RUB) with Poloxamer 407 (P407) was explored as the wall material for the preparation of CBD micelles. In this study, CBD-loaded mixed micelles (CBD-M) composed of P407 and RUB was successfully formed by self-assembly then solid were prepared by solvent evaporation. The saturated solubility of CBD-loaded micelles in water increased to 15.60 mg/mL, 1560-fold compared with its intrinsic solubility (0.01 mg/mL). The average siz…

Self-Tumor Antigens in Solid Tumors Turned into Vaccines by α-gal Micelle Immunotherapy.

A major reason for the failure of the immune system to detect tumor antigens (TAs) is the insufficient uptake, processing, and presentation of TAs by antigen-presenting cells (APCs). The immunogenicity of TAs in the individual patient can be markedly increased by the in situ targeting of tumor cells for robust uptake by APCs, without the need to identify and characterize the TAs. This is feasible by the intra-tumoral injection of α-gal micelles comprised of glycolipids presenting the carbohydrate-antigen "α-gal epitope" (Galα1-3Galβ1-4GlcNAc-R). Humans produce a natural antibody called "anti-G…

Терапевтический эффект циклоспорина А, загружающего микроэлементы TPGS на модель мыши, вызванную нейроинфламмацией.

Нейроинфламмация является несомненной отличительной чертой нейродегенеративных процессов, характеризующихся повреждением памяти, потерей координации и мышечной силы в таких заболеваниях, как болезнь Альцгеймера, болезнь Паркинсона и множественный склероз, а также депрессивные расстройства. Циклоспорина А (КСА) уже была идентифицирована как перспективный нейрозащитный песптид в силу его хорошо известных антивоспалительных свойств. В этом случае CSA был инкапсулирован в α-токоперол полиэтилен гликол 1000 сучканатов (TPGS) и внутринационально утилизирован липополизакхаридом (LPS) модели нейроинфл

Совпадение в аннотации оригинала
Neuroinflammation is an undoubted hallmark of neurodegenerative processes characterized by memory impairment, loss of coordination and muscl … roperties. Herein, CSA was encapsulated into α-tocopherol polyethylene glycol 1000 succinate (TPGS) micelles and intranasally administered to a lipopolysaccharide (LPS) induced mouse model of neuroinflammation. After the treatment, mice were subjected to behavioral tests to assess cognitive and motor skills, while the biodistribution of CSA in plasma and o …

Binding of Ca2+ Ions to Alkylbenzene Sulfonates: Micelle Formation, Second Critical Concentration and Precipitation.

Anionic surfactants, such as sodium linear alkylbenzene sulfonates (NaLAS), are utilized in various fields, including industry, household, and agriculture. The efficiency of their use in aqueous environments is significantly affected by the presence of cations, Ca2+ and Mg2+ in particular, as they can decrease the concentration of the surfactant due to precipitation. To understand cation-sulfonate interactions better, we study both NaLAS colloidal solutions in the presence of CaCl2 and precipitates forming at higher salt concentrations. Upon addition of CaCl2, we find the surface tension and c

Electro-responsive micelle-based universal drug delivery system for on-demand therapy in epilepsy.

A universal drug delivery system (DDS) with brain-targeted ability is demanded to enhance antiepileptic therapeutic efficacy and reduce side … eability across the blood-brain barrier. Based on the hydrophobic-hydrophilic transition of Fc, the micelles can respond to epileptiform discharges and thus release the loaded AEDs. Improved antiepileptic efficacy of the micelles has been demonstrated in acute, continuous, and chronic epilepsy models. In summary, we have developed a universal micelle-based …

The in-vitro study of novel phospholipid micelles loaded with amphotericin B on plasmodium falciparum protozoan.

Malaria is one of the most challenging parasitic infectious diseases in tropical and subtropical regions all over the world. The increasing drug resistance of plasmodium falciparum even makes the treatment procedure of malaria challenging and more problematic. Therefore, it is essential to develop new antimalarial drugs for effective treatments. In this study, the encapsulated amphotericin B (Constantinides et al.) in DSPC/DSPE-PEG2000 micelles was investigated as an antimalarial drug against P. falciparum 3D7 strain. The mean particle size, morphological and microstructural properties of drug…

Biomedical Applications of polymeric micelles in the treatment of diabetes mellitus: Current success and future approaches.

INTRODUCTION: Diabetes mellitus (DM) is the most common metabolic disease and multifactorial, harming patients worldwide. Extensive research has been carried out in the search for novel drug delivery systems offering reliable control of glucose levels for diabetics, aiming at efficient management of DM. AREAS COVERED: Polymeric micelles (PMs) as smart drug delivery nanocarriers are discussed, focusing on oral drug delivery applications for the management of hyperglycemia. The most recent approaches used for the preparation of smart PMs employ molecular features of amphiphilic block copolymers…

Hydration of bromide at reverse micelle interfaces studied by X-ray absorption fine structure.

Nanoconfined water exhibits various interesting properties, which are not only of fundamental importance but also of practical use. Because reverse micelles (RMs) provide versatile ways to prepare nanoconfined water, the understanding of their physicochemical properties is essential for developing efficient applications. Although the water properties in the RMs could be affected by its interaction with the RM interface, the details have not been well understood. This study focuses on the local structures of Br- in hexadecyltrimethylammonium bromide (HTAB) RMs formed in chloroform and 10% hexan…

Safety assessment of polymeric micelles as an ophthalmic drug delivery system for intravitreal administration of dasatinib.

BACKGROUND AND AIMS: Ocular safety/biocompatibility is an essential element of ophthalmic drug delivery. We previously applied poly(ethylene glycol)-block-poly(ɛ-caprolactone) (PEG-b-PCL) micelles to deliver dasatinib for the management of proliferative vitreoretinopathy (PVR) in vitro. Herein, we seek to ascertain the ocular safety/compatibility of blank and dasatinib loaded PEG-b-PCL micelles, which will set the stage for the future in vivo efficacy evaluations and/or clinical translation for PVR or other eye diseases. METHODS: To access the safety of blank and dasatinib loaded micelles, in…

A polymeric micelle with an endosomal pH-sensitivity for intracellular delivery and enhanced antitumor efficacy of hydroxycamptothecin.

Amphiphilic poly(ethylene glycol)-imino-poly(benzyl-l-aspartate) (PIPA) and poly(ethylene glycol)-poly(benzyl-l-aspartate) (PPA) block copolymers were synthesized as pH-responsive and pH-nonresponsive copolymers, respectively. Polymer micelles were fabricated by the film dispersion method, and hydroxycamptothecin (HCPT) was physically encapsulated into the micelles. The average diameter of the HCPT-loaded PIPA micelles (PIPAH micelles) was approximately 230 nm, which was slightly smaller than that of the HCPT-loaded PPA micelles (PPAH micelles, approximately 260 nm). The drug-loading content a…

Chitosan based micelle with zeta potential changing property for effective mucosal drug delivery.

Mucus permeation, mucoadhesion and cell membrane interaction are properties that a drug carrier needs to deliver macromolecule compounds through the mucus barrier and inside epithelial cells effectively. Herein, we prepared micelles from phosphorylated chitosan-stearic acid conjugates (CSSAP) possessing those properties. Their zeta potential can be shifted from negative to neutral once contacting with alkaline phosphatase (ALP). CSSAP micelles showed effective mucus permeation and cell association, thus could be used as a promising platform for mucosal drug delivery. CSSAP was obtained via two…