Emulsion Evaporation Research Articles

L-Threonine-Derived Biodegradable Polyurethane Nanoparticles for Sustained Carboplatin Release

Background and objectives: The use of polymeric nanoparticles (NPs) in drug delivery systems offers the advantages of enhancing drug efficacy and minimizing side effects; Methods: In this study, L-threonine polyurethane (LTPU) NPs have been fabricated by water-in-oil-in-water emulsion and solvent evaporation using biodegradable and biocompatible LTPU. This polymer was pre-synthesized through the use of an amino acid-based chain extender, desaminotyrosyl L-threonine hexyl ester (DLTHE), where urethane bonds are formed by poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) (PLA-PEG-PLA) triblock copolymer and 1,6-hexamethylene diisocyanate (HDI). LTPU is designed to be degraded by hydrolysis and enzymatic activity due to the presence of ester bonds and peptide bonds within the polymer backbone. LTPU NPs were fabricated by water-in-oil-in-water double emulsion solvent evaporation methods; Results: The polymerization of LTPU was confirmed by 1H-NMR, 13C-NMR, and FT-IR spectroscopies. The molecular weights and polydispersity, determined with GPC, were 28,800 g/mol and 1.46, respectively. The morphology and size of NPs, characterized by DLS, FE-SEM, TEM, and confocal microscopy, showed smooth and spherical particles with diameters less than 200 nm; Conclusions: In addition, the drug loading, encapsulation efficiency, and drug release profiles, using UV-Vis spectroscopy, showed the highest encapsulation efficiency with 2.5% carboplatin and sustained release profile.

PH and light-triggered shape transformation of block copolymer particles in emulsion droplets

Dual-responsive shape-transformable block copolymer (BCP) particles have arisen great attentions because of their tunable physical and chemical characteristics triggered by external stimuli. Herein, we developed a simple yet effective strategy to realize pH and light dual-triggered shape-switchable BCP particles through the co-assembly of BCPs with photo-responsive additive 4-hydroxyazobenzene (Azo-OH) within the evaporation emulsion droplets. The formation of hydrogen bonding interactions between the Azo-OH and 4-vinylpyridine (4VP) unit increases the volume fraction of P4VP domain, in turn leading to a morphological transition of the particles from onions to pupas by tuning the Azo-OH content. Subsequent light-induced trans–cis transition of the Azo unit induces the enhancement of the hydrophilicity of the P4VP domains, giving rise to internal shape transitions of the BCP particles from pupas to onions with P4VP at the outmost-layer. Furtherly, since the hydrogen bonds between Azo-OH and 4VP group are sensitive to pH, the interfacial properties of the emulsion droplets and the assembled structures are tuned through adjusting the environment pH of the aqueous solution, causing the formation of various particle shape, including pupas, raspberries, and onions. This work offers a promising method to engineer the microstructures of polymeric assemblies, which may attract more attention on the applications of the stimuli-responsive particles.

Investigation of biological membrane permeability of nanoemulsion, nanostructured lipid carriers and lipid polymer hybrid nanocarriers based nanogel as transdermal carvedilol delivery system

Carvedilol was antihypertensive and antioxidant properties. It was practically water insoluble. It undergoes extensive hepatic first pass metabolism. The aim of this research to study permeability coefficient for NE, NLCs and LPHNs based nanogel through biological membrane using carvedilol as transdermal drug delivery system (TDDS). Aqueous phase titration, ultrasonic emulsion evaporation and microwave-based methods were used to prepare NE1-NE3, NLC1-NLC3 and LPHN1- LPHN3 respectively then subject to various measurements. The formulated lipid-based nanoparticles NE1-LPHN3 were employed as base to prepare lipid base nanogel G1- G9 that was compare to already prepared conventional gel of carvedilol (G). It was found colloidal features associated with the carvedilol loaded lipid-based nanoparticles NE1- LPHN3. The biomembrane permeation evaluation of G1-G9 formulations was indicated that the permeability coefficient (cm/min) of drug was significantly higher (p-value <0.05) for G1 and was significantly lower (p-value < 0.05) for conventional carvedilol gel (G). The preparation and evaluation processes were emphasized that G1-G9 suitable to deliver across biomembrane. The drug that was contained in LPHN based nanoglobules had lower ability to pass through experimental skin that gave it more ability to control drug diffusion in comparison to NE and NLCs.

2-AG-loaded and bone marrow-targeted PCL nanoparticles as nanoplatforms for hematopoietic cell line mobilization

BackgroundThe use of mobilizing agents for hematopoietic stem cell (HSC) transplantation is insufficient for an increasing number of patients. We previously reported lipid made endocannabinoid (eCB) ligands act on the human bone marrow (hBM) HSC migration in vitro, lacking long term stability to be therapeutic candidate. In this study, we hypothesized if a novel 2-AG-loaded polycaprolactone (PCL)-based nanoparticle delivery system that actively targets BM via phosphatidylserine (Ps) can be generated and validated.MethodsPCL nanoparticles were prepared by using the emulsion evaporation method and characterized by Zetasizer and scanning electron microscopy (SEM). The encapsulation efficiency and release profile of 2-AG were determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The presence of cannabinoid receptors (CBRs) in HSCs and monocytes was detected by flow cytometry. Cell morphology and viability were assessed using transmission electron microscopy (TEM), SEM, and the WST-1 viability assay. The migration efficacy of the 2-AG and 2-AG-loaded nanoparticle delivery system on HSCs and HPSCs (TF-1a and TF-1) and monocytes (THP-1) was evaluated using a transwell migration assay.ResultsThe 140–225 nm PCL nanoparticles exhibited an increasing polydispersity index (PDI) after the addition of Ps and 2-AG, with a surface charge ranging from − 25 to -50 mV. The nanoparticles released up to 36% of 2-AG within the first 8 h. The 2-AG-Ps-PCL did not affect cellular viability compared to control on days 5 and 10. The HSCs and monocytes expressed CB1R and CB2R and revealed increased migration to media containing 1 µM 2-AG-Ps-PCL compared to control. The migration rate of the HSCs toward monocytes incubated with 1 µM 2-AG-Ps-PCL was higher than that of the monocytes of control. The 2-AG-Ps-PCL formulation provided a real time mobilization efficacy at 1 µM dose and 8 h time window via a specific CBR agonism.ConclusionThe newly generated and validated 2-AG-loaded PCL nanoparticle delivery system can serve as a stable, long lasting, targeted mobilization agent for HSCs and as a candidate therapeutic to be included in HSC transplantation (HSCT) protocols following scale-up in vivo preclinical and subsequent clinical trials.Graphical

Rapid and Facile Synthesis of Homoporous Colorimetric Films Using Leaf Vein-Mediated Emulsion Evaporation Method for Visual Monitoring of Food Freshness.

A new method for rapid and facile fabrication of homoporous films with high volatile amine sensitivity was developed. First, red cabbage anthocyanin was encapsulated in ethyl cellulose to form water-in-organic (W/O) emulsion. Afterward, the W/O emulsion was rapidly dried using the supporting matrix Magnolia Grandiflora Linn leaf vein at 60% relative humidity and 50 °C to form a colorimetric film with regular hexagonal pores with an average side length of about 23 μm. The films exhibited good sensitivity to ammonia (NH3), dimethylamine, and trimethylamine, with limit of detection of 0.26, 0.24, and 0.38 μM, respectively, and high stability when stored in high humid environments. An obvious color change of the films from pink to green was clearly observed during the freshness monitoring of pork, chicken, salmon, and shrimp. Thus, this work offered a novel and reliable method for the development of porous films for food freshness monitoring.

Resource utilization of emulsion evaporation modified aluminum industrial refractory waste in the preparation of composite modified asphalt

AbstractAluminum industrial refractory waste pose a huge risk to the environment, and hence a safe resource utilization is mandatory to build a green industrial construction industry. Herein, a thermoplastic polyester elastomers‐spent refractory material (TPEE‐SRM) modifier having a two‐layer structure of “protective layer‐functional layer” was developed. Scanning electron microscopy and surface area analysis revealed that Eps used in the protective layer formed a dense film layer (50% decrease in specific surface) with a 97.7% sequestration of fluoride. As the reaction occurred in an organic solution, fluoride posed no risk to the environment. TPEE functional layer itself melted and dissolved with asphalt under high‐temperature conditions, and hence it established a strong interfacial interaction with asphalt. This led to an increase of 99.73% in the complex modulus (G*) and 41.75% in the rutting‐resistance performance (Jnr) of the TPEE‐SRM composite modified asphalt than that of the pristine styrene‐butadiene‐styrene (SBS) modified asphalt. The performance of the TPEE‐SRM/SBS composite modified asphalt after 10 years of use was also evaluated by conducting high pressure aging simulation tests. The linear amplitude scanning test results showed a 27.1‐fold increase in Nf 5.0%. Owing to the efficient and green modification method, the newly designed TPEE‐SRM modifier poses great application prospects and feasibility for designing advanced functional modified asphalt for construction and highway industries alongside a suitable disposal aspect for SRM.

In vitro evaluation of PLGA loaded hesperidin on colorectal cancer cell lines: an insight into nano delivery system

BackgroundColorectal cancer is a common disease worldwide with non-specific symptoms such as blood in the stool, bowel movements, weight loss and fatigue. Chemotherapy drugs can cause side effects such as nausea, vomiting and a weakened immune system. The use of antioxidants such as hesperidin could reduce the side effects, but its low bioavailability is a major problem. In this research, we aimed to explore the drug delivery and efficiency of this antioxidant on the HCT116 colorectal cancer cell line by loading hesperidin into PLGA nanoparticles.Materials and methodsHesperidin loaded PLGA nanoparticles were produced by single emulsion evaporation method. The physicochemical properties of the synthesized hesperidin-loaded nanoparticles were determined using SEM, AFM, FT-IR, DLS and UV-Vis. Subsequently, the effect of the PLGA loaded hesperidin nanoparticles on the HCT116 cell line after 48 h was investigated by MTT assay at three different concentrations of the nanoparticles.ResultThe study showed that 90% of hesperidin were loaded in PLGA nanoparticles by UV-Vis spectrophotometry and FT-IR spectrum. The nanoparticles were found to be spherical and uniform with a hydrodynamic diameter of 76.2 nm in water. The release rate of the drug was about 93% after 144 h. The lowest percentage of cell viability of cancer cells was observed at a concentration of 10 µg/ml of PLGA nanoparticles loaded with hesperidin.ConclusionThe results indicate that PLGA nanoparticles loaded with hesperidin effectively reduce the survival rate of HCT116 colorectal cancer cells. However, further studies are needed to determine the appropriate therapeutic dosage and to conduct animal and clinical studies.

Study on the adsorption properties of lysozyme by cellulose microspheres modified with reactive red 120

Microspheres of cellulose acetate, characterized by a multi-layered, uniform, and continuous porous structure, were synthesized through the process of emulsion evaporation. Subsequent deacetylation facilitated the modification of the cellulose microspheres’ surface, which was functionalized with Reactive Red 120, serving as an affinity dye ligand. This modification yielded a cationic adsorbent. The adsorptive behavior of lysozyme from aqueous solutions, with lysozyme designated as the target protein, was examined in relation to the effects of pH and ionic strength. The adsorptive capacity of the cellulose microspheres, modified with Reactive Red 120, for lysozyme was determined to be 106.57 mg g−1, exhibiting rapid equilibration within 40 min. The adsorption kinetics and thermodynamics were accurately described by the pseudo-second-order kinetic model and the Langmuir model, respectively, with correlation coefficients (R2) of 0.98 and 0.97. Furthermore, dynamic adsorption experiments revealed an enhanced adsorption capacity of 36.5 mg g−1, significantly surpassing that of the unmodified microspheres. The cellulose microspheres, derived from cellulose acetate and modified accordingly, are environmentally benign and sustainable, thereby holding significant promise for various biological applications.

Fluorescent Lateral Flow Immunoassay Based on Quantum Dots Nanobeads.

Quantum dots, also known as semiconductor nanocrystals, are novel fluorescent labels for biological imaging and sensing. However, quantum dot-antibody conjugates with small dimensions (~10 nm), prepared through laborious purification procedures, exhibit limited sensitivity in detecting certain trace disease markers using lateral flow immunoassay strips. Herein, we present a method for the preparation of quantum dot nanobeads (QDNB) using a one-step emulsion evaporation method. Using the as-prepared QDNB, a fluorescent lateral flow immunoassay was fabricated to detect disease biomarkers using C-reactive protein (CRP) as an example. Unlike single quantum dot nanoparticles, quantum dot nanobead-antibody conjugates are more sensitive as immunoassay labels due to signal amplification by encapsulating hundreds of quantum dots in one polymer composite nanobead. Moreover, the larger size of QDNBs facilitates easier centrifugation separation when conjugating QDNBs with antibodies. The fluorescent lateral flow immunoassay based on QDNBs was fabricated, and the CRP concentration in the sample was measured in 15 min. The test results can be qualitatively assessed under UV light illumination and quantitatively measured using a fluorescent reader within 15 min.

Monodisperse polyhydroxyalkanoate nanoparticles as self-sticky and bio-resorbable tissue adhesives

Monodisperse nanoparticles of biodegradable polyhydroxyalkanoates (PHAs) polymers, copolymers of 3-hydroxybutyrate (3HB) and 4-hydroxybutyrate (4HB), are synthesized using a membrane-assisted emulsion encapsulation and evaporation process for biomedical resorbable adhesives. The precise control over the diameter of these PHA particles, ranging from 100 nm to 8 μm, is achieved by adjusting the diameter of emulsion or the PHA concentration. Mechanical properties of the particles can be tailored based on the 3HB to 4HB ratio and molecular weight, primarily influenced by the level of crystallinity. These monodisperse PHA particles in solution serve as adhesives for hydrogel systems, specifically those based on poly(N, N-dimethylacrylamide) (PDMA). Semi-crystalline PHA nanoparticles exhibit stronger adhesion energy than their amorphous counterparts. Due to their self-adhesiveness, adhesion energy increases even when those PHA nanoparticles form multilayers between hydrogels. Furthermore, as they degrade and are resorbed into the body, the PHA nanoparticles demonstrate efficacy in in vivo wound closure, underscoring their considerable impact on biomedical applications.

Surface modified PLGA nanoparticles of gabapentin: Biodistribution and pharmacodynamic investigation via intranasal route

Epilepsy is a chronic condition and is caused by abnormal electrical conduction by nerve cells. It can affect people from different age groups. The prime objective of epilepsy therapeutics is the targeted and sustained release of drugs at the site of action i.e. in the brain. In the present study, PLGA nanoparticles of gabapentin, coated with Polysorbate 80 were prepared with the aim of delivering the drug to the brain through the nasal route. The said nanoparticles were formulated by the method of double emulsion and solvent evaporation. Thereafter, the prepared nanoparticles were characterized for particle size, Zeta potential, and Surface morphology of the nanoparticles was evaluated by SEM &TEM In vitro release in PBS (pH 7.4) and SNF (pH 5.5). In addition, FTIR and DSC techniques were used to confirm the P80 coating around the nanoparticle's surface. In vitro, cell assays like Cytotoxicity studies, and quantitative and qualitative cell uptake studies were studied on Neuro-2a cells. The nasal mucosa of the goat was used to perform histopathological studies to evaluate the toxicity of nanoparticles. A biodistribution study was performed on Swiss albino mice and the results showed that the concentration of the drug reaching the brain in the case of P80 modified nanoparticles was maximum as compared to Plain PLGA nanoparticle, and aqueous solution of the drug. Pharmacodynamic studies were performed to assess the delay in different phases of convulsion and the results showed that the modified nanoparticles of gabapentin were able to significantly delay the episodes of convulsion. Overall, results demonstrate that modified nanoparticles are potential drug carriers in the brain for the management of epilepsy.

Synthesis of innovative epoxy resin and polyamine hardener microcapsules and their age monitoring by confocal Raman imaging

AbstractWe present an innovative breakthrough encompassing synthesis, characterization, and age monitoring of epoxy resin and polyamine hardener microcapsules to form a dual‐component system for self‐healing anticorrosion coatings. The epoxy resin microcapsules (ER‐MC) are fabricated through oil–water emulsion and in situ polymerization, with poly (urea‐formaldehyde‐melamine) as shell material and a mixture of epoxy resin and n‐butyl glycidyl ether as core material. Modified aliphatic fast reactive polyamine hardener is microencapsulated with polymethylmethacrylate as shell using double emulsion and solvent evaporation method (PAH‐MC). Characterization includes optical microscopy, scanning electron microscopy, and particle size analyzer utilizing laser diffraction. The resulting microcapsules exhibited spherical shape with smooth surface devoid of porosity. Fourier transform infrared spectroscopy‐attenuated total reflection is utilized to confirm encapsulation by identifying the chemical structures of both microcapsule constituents. The thermogravimetric analysis further confirms the core content of microcapsules obtained from solvent extraction. ER‐MC contains approximately 66 wt %, while PAH‐MC stands 40 wt %, both showcasing remarkable thermal stability below 200°C. A ten‐month storage period fails to diminish the presence of the healing agents encapsulated within the polymeric walls, which is revealed by Raman spectroscopy utilizing 2D compositional mapping. This research demonstrates the viability of creating dual microcapsules and exemplify their potential for developing self‐healing coatings with dual‐component film‐forming healing agents.

Oral delivery of the amylin receptor agonist pramlintide

AbstractAmylin receptor agonism safely benefit diabetic patients, reducing the insulin requirements and glycemic excursions. Pramlintide is the triple proline human amylin analogue first used as injectable drug, but lacking physico‐chemical compatibility when co‐formulated with insulin. Here, we report the design and characterization of polymeric microparticles for oral delivery of pramlintide. Eudragit S100, a gastric‐resistant polymer, was used in preparation of pramlintide‐loaded spherical microcapsules by double emulsion and solvent evaporation technique, with approximately 66 μm ± 11 particle size, with 83.2% ± 2.7 efficiency for pramlintide entrapment and 67.6% ± 2.1 yield. Intra‐venous pramlintide free in solution showed a plasmatic half‐life of 6.8 min in mice. In contrast, oral delivery of acid‐resistant pramlintide‐loaded microparticles in mice showed a protracted release for 120 min compared to 30 min obtained for pramlintide in solution. Our data provide evidences for the potential use of the oral route in the therapeutic development of pramlintide formulations.

Prediction model of asphalt emulsion evaporation rate based on CFD simulation and genetic programming-based symbolic regression

The evaporation rate of asphalt emulsion is critical to the strength development of asphalt emulsion materials. Its value is dependent on environmental factors, i.e. relative humidity, temperature, and wind speed. However, the quantitative relation of evaporation rate with these environmental factors are unclear. To quantificationally study the effect of environmental factors on the water evaporation rate of asphalt emulsion, a computational fluid dynamics (CFD) simulation model of water evaporation is firstly proposed and validated by experiment. Then, wide range of environmental factors are studied in the CFD simulation model, and genetic programming-based symbolic regression is used to train the simulation results of CFD samples. Finally, a relatively accurate prediction equation of the evaporation rate of asphalt emulsion versus environmental factor is proposed, and the sensitivity of the water evaporation rate under the three environmental factors is analyzed. Results show that the evaporation rate can be accurately simulated by CFD. All the three environmental factors can greatly affect the evaporation rate of asphalt emulsion, while their effect on the sensitivity of the water evaporation rate is ranked as: temperature > relative humidity > wind speed. To ensure an acceptable curing period, asphalt emulsion-based materials should be avoided to be paved in the conditions of low temperature and high relative humidity.

Nanogel: Types, Methods of Preparation, Limitation, Evaluation and Application – A Systematic Review

Nanogels combine the characteristics of nanomaterials with hydrogels. To meet the expanding demands from various areas, a sizable number of nanogels have been designed and manufactured using the emulsion solvent diffusion nano precipitated method, emulsion evaporation of the solvent method, reverse micellar method and modified diffusion emulsification method. Thermosensitive nanogel, pH-sensitive nanogel, ultrasound-sensitive magnetic response, response to multiple stimuli, chain transfer polymerization, photo-induced crosslinking polymerization and modifications for active targeting are the types of nanogels based on response towards stimuli and polysaccharide, chitosan, pullulan, hyaluronic acid, alginate, cyclodextrin, gum acacia, protein are used to prepare nanogel. Nanogels have considerable potential and novelty within the biomedical sector due to their uniformity, adjustable dimensions, little toxicity, resilience in the presence of serum, and capacity for responsive behavior with a comparatively high drug encapsulation capacity. Nanogels have considerable potential in bioactive substance delivery, organ targeting, and chemotherapy. The article highlighted the preparation, types, evaluation and applicability of nanogel as a targeted delivery system.

Anti-cancer activity of microbubble conjugated with Sorafenib containing liposome and IL4R-targeting peptide in kidney cancer cells.

Microbubble-based cancer treatment is a promising new approach that utilizes tiny gas-filled bubbles to deliver cancer drugs directly to tumor sites. This study aims to investigate the anti-cancer effect of the novel microbubble (MB) complex conjugated with sorafenib containing liposome and interleukin 4 receptor (IL4R) targeting peptide in kidney cancer cells. MBs were synthesized by using a solvent with an emulsion evaporation technique. To target kidney tumor cells, the produced MBs were conjugated with sorafenib (SOR) loaded liposomes and peptide ligands for (IL4RTP). The anti-cancer effect of the MB complex was accessed by WST-1 assay, confocal microscopy analysis, and western blotting analysis. The finally prepared IL4RTP (MB-Lipo(SOR)-IL4RTP) showed an average size of 1,600 nm. A498, a kidney cancer cell line that expresses IL4Rα strongly, had an uptake of the MB-Lipo(SOR)-IL4RTP when exposed to frequency ultrasonic energy. Additionally, MB-Lipo(SOR)-IL4RTP suppressed the growth of A498 cells in an IL4R-dependent manner. This cell proliferation assay results were validated by western blotting analysis of the signal transduction proteins such as FOXO3, phosphorylated Erk, total Erk, and p27. Taken together, these findings show that MB-Lipo(SOR)-IL4RTP exerts the effective targeting capacity for A498 kidney cancer cells via regulation of Erk phosphorylation as a promising ultrasound contrast and therapeutic agent for treating kidney cancers.

Modification of solid form of drug in oil-in-water emulsion: Effect of self-assembly of the emulsifier glycyrrhizic acid

The encapsulation and solid form control of a hydrophobic drug in oral administration remains a persistent challenge. Here, an oil-in-water emulsion evaporation approach was developed to simultaneously control solid form and release profile of hydrophobic and amphiphilic drugs in solid dose. Hydrophobic drugs treating cardiovascular and cerebrovascular diseases (CCVD) were selected as drugs for the oil phase. A saponin with hepatoprotective effect, glycyrrhizic acid (GA), was employed as emulsifier due to its amphiphilic structure, and on the other hand, its excellent hepatoprotective effects can reduce the risk of liver disease caused by CCVD medication. By adjusting the composition of the emulsion, various GA self-assemblies were triggered including crystal, micelle and fiber. The emulsions with different GA forms at the interface subsequently act as evaporation crystallizers for CCVD-drugs. Consequently, solid form of CCVD-drugs was influenced either kinetically or thermodynamically by the GA concentration, the GA-drug miscibility and slow migration of GA fibers. Moreover, immediate and sustained release for both GA and CCVD-drugs were achieved, respectively. The emulsion evaporation approach in this work represents a strategy enabling formulation of hydrophobic and amphiphilic drugs with controlled solid forms and release profiles.

Development of Gefitinib-Loaded Solid Lipid Nanoparticles for the Treatment of Breast Cancer: Physicochemical Evaluation, Stability, and Anticancer Activity in Breast Cancer (MCF-7) Cells.

In the current study, the toxic effects of gefitinib-loaded solid lipid nanoparticles (GFT-loaded SLNs) upon human breast cancer cell lines (MCF-7) were investigated. GFT-loaded SLNs were prepared through a single emulsification-evaporation technique using glyceryl tristearate (Dynasan™ 114) along with lipoid® 90H (lipid surfactant) and Kolliphore® 188 (water-soluble surfactant). Four formulae were developed by varying the weight of the lipoid™ 90H (100-250 mg), and the GFT-loaded SLN (F4) formulation was optimized in terms of particle size (472 ± 7.5 nm), PDI (0.249), ZP (-15.2 ± 2.3), and EE (83.18 ± 4.7%). The optimized formulation was further subjected for in vitro release, stability studies, and MTT assay against MCF-7 cell lines. GFT from SLNs exhibited sustained release of the drug for 48 h, and release kinetics followed the Korsmeyer-Peppas model, which indicates the mechanism of drug release by swelling and/or erosion from a lipid matrix. When pure GFT and GFT-SLNs were exposed to MCF-7 cells, the activities of p53 (3.4 and 3.7 times), caspase-3 (5.61 and 7.7 times), and caspase-9 (1.48 and 1.69 times) were enhanced, respectively, over those in control cells. The results suggest that GFT-loaded SLNs (F4) may represent a promising therapeutic alternative for breast cancer.

Nanoscale celecoxib prodrugs: As efficient anti-inflammatory principles

We have synthesized lipidic prodrugs of celecoxib by grafting aliphatic chains to celecoxib through acyl sulfonamide (1), aryl sulfonyl carbamate (2) and aryl sulfonyl urea (3) chemical linkages. Their molecular formulas were confirmed through HR-MS and the formation of ester bond by FTIR and NMR spectroscopy. Nanoparticles of the different prodrugs 1-3 were successfully formulated using emulsion evaporation method and DSPE-PEG2000 as the only excipient. All nanoparticles depicted size between 130 and 160 nm, PdI ≤0.2 and negative zeta potential values from −25 to −35 mV. In addition, they were stable upon storage at 4 °C and/or at room temperature for about a month (in shelf). Morphology of all nanoparticles were spherical-type as observed in transmission electron microscopy (TEM) and scanning electron microscopy (SEM). The encapsulation efficiency of the prodrug was as high as 99% for all three corresponding prodrugs NPs. The nanoscale prodrugs 1–3, are reported for the first time. Moreover, all the characterization data (physicochemical and biological) regarding NPs are also unique. In addition, all prodrug nanoparticles have preserved in vitro anti-inflammatory activity when incubated with the THP-1 cell line activated with lipopolysaccharide (LPS). In vivo studies on a collagen induced arthritis murine model showed results: Prodrug 3 NPs showed activity but were not as efficient as celecoxib in its free form, this might be due to no or very slow release of celecoxib from the prodrug 3 NPs. To promote the reduction of inflammation using NPs would require to explore the possible administration (in vivo) of other prodrugs 1 and 2 NPs in the future.

Morphological Evolution of Hybrid Block Copolymer Particles: Toward Magnetic Responsive Particles.

The co-assembly of block copolymers (BCPs) and inorganic nanoparticles (NPs) under emulsion confinement allows facile access to hybrid polymeric colloids with controlled hierarchical structures. Here, the effect of inorganic NPs on the structure of the hybrid BCP particles and the local distribution of NPs are studied, with a particular focus on comparing Au and Fe3O4 NPs. To focus on the effect of the NP core, Au and Fe3O4 NPs stabilized with oleyl ligands were synthesized, having a comparable diameter and grafting density. The confined co-assembly of symmetric polystyrene-b-poly(1,4-butadiene) (PS-b-PB) BCPs and NPs in evaporative emulsions resulted in particles with various morphologies including striped ellipsoids, onion-like particles, and their intermediates. The major difference in PS-b-PB/Au and PS-b-PB/Fe3O4 particles was found in the distribution of NPs inside the particles that affected the overall particle morphology. Au NPs were selectively localized inside PB domains with random distributions regardless of the particle morphology. Above the critical volume fraction, however, Au NPs induced the morphological transition of onion-like particles into ellipsoids by acting as an NP surfactant. For PS-b-PB/Fe3O4 ellipsoids, Fe3O4 NPs clustered and segregated to the particle/surrounding interface of the ellipsoids even at a low volume fraction, while Fe3O4 NPs were selectively localized in the middle of PB domains in a string-like pattern for PS-b-PB/Fe3O4 onion-like particles.