Maghemite/poly(<Emphasis Type="SmallCaps">d,l</Emphasis>-lactide-<Emphasis Type="Italic">co</Emphasis>-glycolyde) composite nanoplatform for therapeutic applications

A reproducible methodology is described for the synthesis, by following the double emulsion/solvent evaporation technique, of magnetic nanocomposites (average diameter ≈ 135 nm) consisting of maghemite nuclei and a biodegradable poly(d,l-lactide-co-glycolide) matrix. The heterogeneous structure of the nanoparticles can confer them the responsiveness to magnetic gradients, giving both the possibility of their use as a drug delivery system and adequate heating characteristics for a hyperthermia effect. The physical chemistry of the nanocomposites was extensively characterized, this establishing that their surface properties were similar to that of pure poly(d,l-lactide-co-glycolide). From an electrokinetic point of view, zeta potential determinations (as a function of the ionic strength, and pH) pointed out that the nanocomposites were almost indistinguishable from the copolymer. The surface thermodynamic analysis agreed with the electrophoretic one in suggesting that the coverage of the magnetic nuclei was complete, since the hydrophilic nature of maghemite was modified and the nanoparticles turned into hydrophobic, just like the copolymer, when they were embedded into poly(d,l-lactide-co-glycolide). The magnetic behaviours of the composite nanoparticles were also checked. Their heating properties were studied in vitro in a high-frequency alternating gradient of magnetic field: a stable maximum temperature of 47 °C was satisfactorily achieved within 45 min. Blood compatibility of the nanocomposites was also defined in vitro. To our knowledge, this is the first time that such kind of magnetic-sensitive nanoformulation with very promising characteristics (e.g. blood compatibility, magnetic drug targeting capabilities, and hyperthermia) has been developed for therapeutic purposes.     

Magnetic lipid nanoparticles loading doxorubicin for intracellular delivery: Preparation and characteristics

Tumor intracellular delivery is an effective route for targeting chemotherapy to enhance the curative effect and minimize the side effect of a drug. In this study, the magnetic lipid nanoparticles with an uptake ability by tumor cells were prepared dispersing ferroso-ferric oxide nanoparticles in aqueous phase using oleic acid (OA) as a dispersant, and following the solvent dispersion of lipid organic solution. The obtained nanoparticles with 200 nm volume average diameter and −30 mV surface zeta potential could be completely removed by external magnetic field from aqueous solution. Using doxorubicin (DOX) as a model drug, the drug-loaded magnetic lipid nanoparticles were investigated in detail, such as the effects of OA, drug and lipid content on volume average diameter, zeta potential, drug encapsulation efficiency, drug loading, and in vitro drug release. The drug loading capacity and encapsulation efficiency were enhanced with increasing drug or lipid content, reduced with increasing OA content. The in vitro drug release could be controlled by changing drug or lipid content. Cellular uptake by MCF-7 cells experiment presented the excellent internalization ability of the prepared magnetic lipid nanoparticles. These results evidenced that the present magnetic lipid nanoparticles have potential for targeting therapy of antitumor drugs.     

Biodegradable thermoresponsive polymeric magnetic nanoparticles: a new drug delivery platform for doxorubicin

The use of nanoparticles as drug delivery systems for anticancer therapeutics has great potential to revolutionize the future of cancer therapy. The aim of this study is to construct a novel drug delivery platform comprising a magnetic core and biodegradable thermoresponsive shell of tri-block-copolymer. Oleic acid-coated Fe₃O₄ nanoparticles and hydrophilic anticancer drug “doxorubicin” are encapsulated with PEO–PLGA–PEO (polyethylene oxide–poly d, l lactide-co-glycolide–polyethylene oxide) tri-block-copolymer. Structural, magnetic, and physical properties of Fe₃O₄ core are determined by X-ray diffraction, vibrating sample magnetometer, and transmission electron microscopy techniques, respectively. The hydrodynamic size of composite nanoparticles is determined by dynamic light scattering and is found to be ~36.4 nm at 25 °C. The functionalization of magnetic core with various polymeric chain molecules and their weight proportions are determined by Fourier transform infrared spectroscopy and thermogravimetric analysis, respectively. Encapsulation of doxorubicin into the polymeric magnetic nanoparticles, its loading efficiency, and kinetics of drug release are investigated by UV–vis spectroscopy. The loading efficiency of drug is 89% with a rapid release for the initial 7 h followed by the sustained release over a period of 36 h. The release of drug is envisaged to occur in response to the physiological temperature by deswelling of thermoresponsive PEO–PLGA–PEO block-copolymer. This study demonstrates that temperature can be exploited successfully as an external parameter to control the release of drug.     

GLUT1-Targeting and GSH-Responsive DOX/L61 Nanodrug Particles for Enhancing MDR Breast Cancer Therapy

Efficient targeting to tumor tissues and subsequent rapid drug release in cancer cells remains a major challenge for nanodrug delivery systems. Herein, smart nanodrug particles with reduction-sensitive and active tumor-targeting ability are constructed based on the nanoprecipitation of glucosamine-grafted pluronic L61 (GA-L61) and disulphide-linked doxorubicin dimer (DOX SS DOX) to overcome tumor multidrug resistance (MDR). These nanoparticles show proper size and excellent stability under neutral conditions, while quickly release DOX due to the breakage of disulfide bonds under reductive medium. In vitro cellular uptake and drug efflux demonstrate that L61 can efficiently increase DOX concentration in MCF/ADR resistant cells by inhibiting the function of drug resistance proteins. In vivo biodistribution reveals that glucose transporter 1 (GLUT1)-mediated tumor-targeting significantly improves tumor accumulation of the glucosamine-contained nanoparticles. Finally, the combination of GLUT1-targeting, glutathione (GSH)-responsive, and MDR-reversal effects in nanoparticles achieve superior antitumor effects, which can provide an efficient, safe, and economic approach for drug delivery and cancer chemotherapy.     

Low‐Magnetization Magnetic Microcapsules: A Synergistic Theranostic Platform for Remote Cancer Cells Therapy and Imaging

Multifunctional magnetic microcapsules (MMCs) for the combined cancer cells hyperthermia and chemotherapy in addition to MR imaging are successfully developed. A classical layer‐by‐layer technique of oppositely charged polyelectrolytes (poly(allylamine hydrochloride) (PAH) and poly(4‐styrene sulfonate sodium) (PSS)) is used as it affords great controllability over the preparation together with enhanced loading of the chemotherapeutic drug (doxorubicin, DOX) in the microcapsules. Superparamagnetic iron oxide (SPIOs) nanoparticles are layered in the system to afford MMC1 (one SPIOs layer) and MMC2 (two SPIOs layers). Most interestingly, MMC1 and MMC2 show efficient hyperthermia cell death and controlled DOX release although their magnetic saturation value falls below 2.5 emu g^?1, which is lower than the 7–22 emu g^?1 reported to be the minimum value needed for biomedical applications. Moreover, MMCs are pH responsive where a pH 5.5 (often reported for cancer cells) combined with hyperthermia increases DOX release predictably. Both systems prove viable when used as T2 contrast agents for MR imaging in HeLa cells with high biocompatibility. Thus, MMCs hold a great promise to be used commercially as a theranostic platform as they are controllably prepared, reproducibly enhanced, and serve as drug delivery, hyperthermia, and MRI contrast agents at the same time.     

Synthesis and characterization of tat-mediated O-CMC magnetic nanoparticles having anticancer function

This paper describes a new formulation of magnetic nanoparticles coated by a novel polymer matrix—O-carboxylmethylated chitosan (O-CMC) as drug/gene carrier. The O-CMC magnetic nanoparticles were derivatized with a peptide sequence from the HIV-tat protein to improve the translocational property and cellar uptake of the nanoparticles. To evaluate the O-MNPs-tat as drug carriers, MTX was incorporated as a model drug and MTX-loaded O-MNPs-tat with an average diameter of 45–60 nm were prepared and characterized by TEM, AFM and VSM. The cytotoxicity of MTX-loaded O-MNPs-tat was investigated with U-937 tumor cells. The results showed that the MTX-loaded O-MNPs-tat retained significant antitumor toxicity; additionally, sustained release of MTX from O-CMC nanoparticles was observed in vitro, suggesting that the tat-O-MNPs could be a novel magnetic targeting carrier.     

Effects of surfactants on properties of polymer-coated magnetic nanoparticles for drug delivery application

The objective of this research was to compare the effects of two different surfactants on the physicochemical properties of thermo-responsive poly(N-isopropylacrylamide-acrylamide-allylamine) (PNIPAAm-AAm-AH)-coated magnetic nanoparticles (MNPs). Sodium dodecyl sulfate (SDS) as a commonly used surfactant in nanoparticle formulation process and Pluronic F127 as an FDA approved material were used as surfactants to synthesize PNIPAAm-AAm-AH-coated MNPs (PMNPs). The properties of PMNPs synthesized using SDS (PMNPs-SDS) and PF127 (PMNPs-PF127) were compared in terms of size, polydispersity, surface charge, drug loading efficiency, drug release profile, biocompatibility, cellular uptake, and ligand conjugation efficiency. These nanoparticles had a stable core–shell structure with about a 100-nm diameter and were superparamagnetic in behavior with no difference in the magnetic properties in both types of nanoparticles. In vitro cell studies showed that PMNPs-PF127 were more cytocompatible and taken up more by prostate cancer cells than that of PMNPs-SDS. Cells internalized with these nanoparticles generated a dark negative contrast in agarose phantoms for magnetic resonance imaging. Furthermore, a higher doxorubicin release at 40 °C was observed from PMNPs-PF127, and the released drugs were pharmacologically active in killing cancer cells. Finally, surfactant type did not affect the conjugation efficiency to the nanoparticles when folic acid was used as a targeting ligand model. These results indicate that PF127 might be a better surfactant to form polymer-coated magnetic nanoparticles for targeted and controlled drug delivery.     

Carbon Dots‐Cluster‐DOX Nanocomposites Fabricated by a Co‐Self‐Assembly Strategy for Tumor‐Targeted Bioimaging and Therapy

Carbon‐based nanomaterials could afford versatile potential applications in biomedical optical imaging and as nanoparticle drug carriers, owing to their promising optical and biocompatible capabilities. In this paper, it is first found that amphipathic cetylpyridinium chloride (CPC)‐stabilized oil‐soluble carbon dots (CDs) could self‐assemble into hydrophilic CDs clusters with hydrophobic core under ultrasound, in which CPC acts as carbon source, stabilizer, and phase transfer agent. Next, the size‐control (for size‐dependent passive tumor targeting) and doxorubicin (DOX) uploading of aqueous CDs clusters, and subsequent surface charge modification via overcoating with cRGD‐ and octylamine‐modified polyacrylic acid (cRGD‐PAA‐OA) (reversing their surface charges into negative and introducing active tumor‐targeting ability) are explored systematically. Based on this sequential administration mode, CDs‐cluster‐DOX/cRGD‐PAA‐OA nanocomposites exhibit selective human malignant glioma cell line (U87MG) tumor targeting. In in vitro drug release experiments, the nanocomposites could release DOX timely. Owning to the dual tumor targeting effects and seasonable drug release, CDs‐cluster‐DOX/cRGD‐PAA‐OA show remarkably tumor targetability and enhanced antitumor efficacy (and reduced adverse reaction), comparing to free DOX in animal models. These results indicate that fabricating nanocomposite via co‐self‐assembly strategy is efficient toward drug delivery system for tumor‐targeting theranostic.     

Core–Shell Bi2Se3@mSiO2‐PEG as a Multifunctional Drug‐Delivery Nanoplatform for Synergistic Thermo‐Chemotherapy with Infrared Thermal Imaging of Cancer Cells

Thermo‐chemotherapy combining photothermal therapy (PTT) with chemotherapy has become a potent approach for antitumor treatment. In this study, a multifunctional drug‐delivery nanoplatform based on polyethylene glycol (PEG)‐modified mesoporous silica‐coated bismuth selenide nanoparticles (referred to as Bi₂Se₃@mSiO₂‐PEG NPs) is developed for synergistic PTT and chemotherapy with infrared thermal (IRT) imaging of cancer cells. The product shows no/low cytotoxicity, strong near‐infrared (NIR) optical absorption, high photothermal conversion capacity, and stability. Utilizing the prominent photothermal effect, high‐contrast IRT imaging and efficient photothermal killing effect on cancer cells are achieved upon NIR laser irradiation. Moreover, the successful mesoporous silica coating of the Bi₂Se₃@mSiO₂‐PEG NPs cannot only largely improve the stability but also endow the NPs high drug loading capacity. As a proof‐of‐concept model, doxorubicin (DOX) is successfully loaded into the NPs with rather high loading capacity (≈50.0%) via the nanoprecipitation method. It is found that the DOX‐loaded NPs exhibit a bimodal on‐demand pH‐ and NIR‐responsive drug release property, and can realize effective intracellular drug delivery for chemotherapy. The synergistic thermo‐chemotherapy results in a significantly higher antitumor efficacy than either PTT or chemotherapy alone. The work reveals the great potential of such core–shell NPs as a multifunctional drug‐delivery nanosystem for thermo‐chemotherapy.     

Theranostic Iron@Gold Core–Shell Nanoparticles for Simultaneous Hyperthermia‐Chemotherapy upon Photo‐Stimulation

The challenges of nanoparticles, such as size‐dependent toxicity, nonbiocompatibility, or inability to undergo functionalization for drug conjugation, limit their biomedical application in more than one domain. Oval‐shaped iron@gold core–shell (oFe@Au) magnetic nanoparticles are engineered and their applications in magnetic resonance imaging (MRI), optical coherence tomography (OCT), and controlled drug release, are explored via photo stimulation‐generated hyperthermia. The oFe@Au nanoparticles have a size of 42.57 ± 5.99 nm and consist of 10.76 and 89.24 atomic % of Fe and Au, respectively. Upon photo‐stimulation for 10 and 15 minutes, the levels of cancer cell death induced by methotrexate‐conjugated oFe@Au nanoparticles are sixfold and fourfold higher, respectively, than oFe@Au nanoparticles alone. MRI and OCT confirm the application of these nanoparticles as a contrast agent. Finally, results of in vivo experiments reveal that the temperature is elevated by 13.2 °C, when oFe@Au nanoparticles are irradiated with a 167 mW cm^?2 808 nm laser, which results in a significant reduction in tumor volume and scab formation after 7 days, followed by complete disappearance after 14 days. The ability of these nanoparticles to generate heat upon photo‐stimulation also opens new doors for studying hyperthermia‐mediated controlled drug release for cancer therapy. Applications include biomedical engineering, cancer therapy, and theranostics fields.     

A novel magnetic fluid based on starch-coated magnetite nanoparticles functionalized with homing peptide

Preparation and characterization in vitro and in vivo of a novel magnetic fluid based on starch-coated magnetite nanoparticles functionalized with homing peptide is reported in this paper. Precursory magnetic fluids stabilized with starch were prepared, in a polymeric starch matrix, by controlled chemical coprecipitation of magnetite phase from aqueous solutions. The average hydrodynamic diameter of starch-coated iron oxide nanoparticles (SIONs) was 46 nm. As a homing peptide, A54 is the most effective peptide specific to the human hepatocellular carcinoma cell line BEL-7402. Final magnetic fluids were obtained through chemical coupling of homing peptide labeled with 5-carboxyl-fluorescein (FAM-A54) and SIONs. Magnetic measurements showed the saturation magnetization value of SIONs amounted to 45 emu/g and the FAM-A54-coupled SIONs showed a good magnetic response in magnetic field. The results of experiments in vitro and in vivo showed that SIONs were endowed with specific affinity to corresponding tumor cells after coupling with FAM-A54 and the FAM-A54-coupled SIONs could be accumulated in the tumor tissue with more efficiency than individual magnetic targeting or biomolecular targeting. This novel magnetic fluid with dual function has great potential applications in diagnostics and therapeutics of human tumor such as drug targeting, magnetic hyperthermia, and magnetic resonance imaging.     

Temperature and Redox Dual‐Responsive Biodegradable Nanogels for Optimizing Antitumor Drug Delivery

The strategy to efficiently deliver antitumor drugs via nanocarriers to targeted tumor sites and achieve controllable drug release is attracting great research interest in cancer therapy. In this study, a novel type of disulfide‐bonded poly(vinylcaprolactam) (PVCL)‐based nanogels with tunable volume phase transition temperature and excellent redox‐labile property are prepared. The nanogels are hydrophilic and swell at 37 °C, whereas under hyperthermia (e.g., 41 °C), the nanogels undergo sharp hydrophilic/hydrophobic transition and volume collapse, which enhances the cellular uptake and drug release. The incorporation of disulfide bond linkers endows the nanogels with an excellent disassembly property in reducing environments, which greatly facilitates drug release in tumor cells. Nanogels loaded with doxorubicin (DOX) (DOX‐NGs) (DOX‐NGs) are stable in physiological conditions with low drug leakage (15% in 48 h), while burst release of DOX (92% in 12 h) can be achieved in the presence of 10 × 10^?3 m glutathione and under hyperthermia. The DOX‐NGs possess improved cell killing efficiency under hyperthermia (IC₅₀ decreased from 1.58 μg mL^?1 under normothermia to 0.5 μg mL^?1). Further, the DOX‐NGs show a pronounced tumor inhibition rate of 46.6% compared with free DOX, demonstrating that this new dual‐responsive nanogels have great potential as drug delivery carriers for cancer therapy in vivo.     

Tuneable magnetic properties of hydrothermally synthesised core/shell CoFe2O4/NiFe2O4 and NiFe2O4/CoFe2O4 nanoparticles

The aim of this study was to prepare a novel targeting nano drug delivery system of 2-methoxyestradiol (2-ME) based on the folic acid-modified bovine serum albumin, in order to improve the clinical application disadvantages and antitumor effect of 2-ME. In this study, 2-methoxyestradiol-loaded albumin nanoparticles (2-ME-BSANPs) were prepared by desolvation method, and then the activated folic acid was conjugated to 2-ME-BSANPs by covalent attachment (2-ME-FA-BSANPs). The size and zeta potential of 2-ME-FA-BSANPs were about 208.8 ± 5.1 nm and ?32.70 ± 1.01 mV, respectively. 2-ME loading efficiency and loading amount of the nanoparticles were 80.49 ± 3.80 and 10.25 ± 1.59 %, respectively. SEM images indicated that 2-ME-FA-BSANPs were of a round shape, similar uniform size, and smooth surface. Studies on drug release indicated that 2-ME-FA-BSANPs had the properties of sustained and controlled release, which provided them with the ability to fight continually against cancer cells. Internalization analysis demonstrated that 2-ME-FA-BSANPs-targeting drug delivery system could get efficiently transferred into the cells through the folic acid-mediated endocytosis, leading to higher apoptosis and affording higher antitumor efficacy against SMMC-7721 cells in vitro compared with 2-ME alone. Furthermore, the cell-cycle arrest of 2-ME-FA-BSANPs on the SMMC-7721 cells occurred at G2/M phase, and 2-ME-FA-BSANPs did not change the inhibition of the tumor mechanisms of 2-ME. Based on these results, it was concluded that albumin nanoparticles could be the promising nano carrier for 2-ME, and 2-ME-FA-BSANPs-targeting drug delivery system may be promising candidate for providing high treatment efficacy with minimal side effects in future cancer therapy.     

Folate-decorated chitosan/doxorubicin poly(butyl)cyanoacrylate nanoparticles for tumor-targeted drug delivery

A novel chitosan coated poly(butyl cyanoacrylate) (PBCA) nanoparticles loaded doxorubicin (DOX) were synthesized and then conjugated with folic acid to produce a folate-targeted drug carrier for tumor-specific drug delivery. Prepared nanoparticles were surface modified by folate for targeting cancer cells, which is confirmed by FTIR spectroscopy and characterized for shape, size, and zeta potential measurements. The size and zeta potential of prepared DOX-PBCA nanoparticles (DOX-PBCA NPs) were almost 174 ± 8.23 nm and +23.14 ± 4.25 mV, respectively with 46.8 ± 3.32% encapsulation capacity. The transmission electron microscopy study revealed that preparation allowed the formation of spherical nanometric and homogeneous. Fluorescent microscopy imaging and flow cytometry analysis revealed that DOX-PBCA NPs were endocytosed into MCF-7 cells through the interaction with overexpressed folate receptors on the surface of the cancer cells. The results demonstrate that folate-conjugated DOX-PBCA NPs drug delivery system could provide increased therapeutic benefit by delivering the encapsulated drug to the folate receptor positive cancer cells.     

Cyclodextrin-conjugated nanocarrier for magnetically guided delivery of hydrophobic drugs

A magnetic nanosystem that simultaneously implements the cyclodextrin–drug complexation power, bioadhesive property of gum arabic (GA) and inherent magnetic properties of Fe₃O₄ nanoparticles, has recently been reported. In this study, a magnetic nanocarrier was fabricated by conjugating 2-hydroxypropyl-cyclodextrin (HCD) onto the gum arabic modified magnetic nanoparticles (GAMNP). The analyses of transmission electron microscopy (TEM) and dynamic light scattering (DLS) revealed that the product had a mean diameter of 14.8 nm and a mean hydrodynamic diameter of 29.3 nm. This nanocarrier showed good loading efficiency for ketoprofen. In addition, the in vitro release profile of ketoprofen from HCD-GAMNP was characterized by an initial fast release followed by a delayed release phase. In view of the better biocompatibility and the combined properties like specific targeting, complexation ability with hydrophobic drugs makes the nanosystem an exciting prospect for drug delivery.     

Antimicrobial and antitumor activities of 1,2,4‐triazoles/polypyrrole chitosan core shell nanoparticles

Combination of natural biodegradable polymer with a synthetic polymer offers excellent properties for the support in drug delivery system. For this purpose, biodegradable conductive nanoparticle polypyrrole based on chitosan (PPC) has been prepared via oxidative polymerization of pyrrole in presence of chitosan using FeCl₃ as oxidant in acidic medium and used as a carrier for 1,2,4‐triazoles. The resultant nanoparticles were characterized by X‐ray diffraction, Fourier transform infrared analysis, transmission electron microscopy, scanning electron microscopy, and thermal gravimetric analysis. The results indicate that spherical nanoparticle of average diameter 52 ± 8 nm was successfully prepared. The spherical particles were composed of dark sphere surrounded by grey shell. A circumferential dark ring is observed in the shell after loading 1,2,4‐triazoles into PPC nanoparticles. The loaded triazoles were released almost linearly against time in a sustained fashion into different pH media. The mechanism of triazoles release was determined using different kinetics equations. The antibacterial activities against the gram‐negative and gram‐positive bacteria were examined. Furthermore, the antitumor activity of PPC nanoparticles loaded 1,2,4‐triazoles was also examined against Ehrlich ascites carcinoma cells and breast cancer cell line (MCF7). Polypyrrole chitosan loaded nanoparticles exhibited higher antitumor activity than 1,2,4‐triazoles.     

Amphiphilic Drug Delivery Microcapsules via Layer-by-Layer Self-Assembly

A strategy to incorporate and release the amphiphilic drugs of doxorubicin (DOX) and ibuprofen (IBU) in the same microcapsules is introduced, A layer-by-layer (LbL) assembly of microcapsules with doxorubicin hydrochloride (DOX) or green fluorescent agent, hydrophilic fluorescein isothiocyanate (FITC), encapsulated in CaCO₃ microparticle templates, was conducted via alternatively depositing sodium carboxymethyl cellulose (CMC) and chitosan (CHI) onto IBU or red fluorescent agent (hydrophobic Nile Red) preloaded poly-L-lactide (PLLA) coated magnetic Fe₃O₄-DOX-loaded CaCO₃ (or FITC-loaded) templates. The structure, morphology, composition, magnetic properties and drugs distribution of the obtained microcapsules were characterized by nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), zeta potential analysis, thermogravimetric analysis (TGA), vibrating sample magnetometry (VSM) and confocal laser scanning microscopy. The fluorescent agents loading of FITC and Nile Red were confirmed by observations using confocal laser scanning microscopy. Fluorescence observations showed that the DOX was distributed both in the walls and in the cavities of the microcapsules, while IBU was present in the capsule wall. The in–vitro release of the dual drugs, DOX and IBU, from the microcapsules with different numbers of CHI and CMC layers was characterized. A tunable amount of drug release was achieved by changing the number of layers. The release study indicated that the LBL microcapsules exhibited better sustained release capacity compared to the uncoated microcapsules. The microcapsules inherited a strong magnetic property from the Fe₃O₄ nanoparticles, sufficient for targeting and magnetic hyperthermia drug delivery systems.     

Evaluation of the antibacterial activity of poly-(<Emphasis Type="SmallCaps">d</Emphasis>,<Emphasis Type="SmallCaps">l</Emphasis>-lactide-co-glycolide) nanoparticles containing violacein

Since violacein—an antibiotic, antiviral, and antiparasitic compound—exhibits poor solubility in water, polymeric poly-(d,l-lactide-co-glycolide) nanoparticles containing this compound improved its solubility and biological activity. The nanoparticles were prepared by the nanoprecipitation method and characterized in terms of average diameter, zeta potential, drug loading, polymer recovery, in vitro release kinetic, and in vitro antibacterial activity. Nanoparticles with diameters between 116 and 139 nm and negative-charged outer surfaces were obtained. Drug-loading efficiency and polymer recovery were 87 and 93%, respectively. In vitro release kinetics assays showed that violacein loaded in these nanoparticles has sustained release behavior until 5 days. Both free and nanoparticles-loaded violacein exhibited in vitro antibacterial activity against Staphylococcus aureus ATCC 29213 and ATCC 25923 strains and exhibiting around two to five times lower minimum inhibitory concentration (MIC) than free violacein, respectively. The encapsulated violacein was efficient against methicilin-resistant Staphylococcus aureus (MRSA) strains. No significant activity against Escherichia coli and Salmonella enterica was found.     

Cellular uptake and radiosensitization of SR-2508 loaded PLGA nanoparticles

SR-2508 (etanidazole), a hypoxic radiosensitizer, has potential applications in radiotherapy. The poly(d,l-lactide-co-glycolide)(PLGA) nanoparticles containing SR-2508 were prepared by w/o/w emulsification-solvent evaporation method. The physicochemical characteristics of the nanoparticles (i.e. encapsulation efficiency, particle size distribution, morphology, in vitro release) were studied. The cellular uptake of the nanoparticles for the two human tumor cell lines: human breast carcinoma cells (MCF-7) and human carcinoma cervices cells (HeLa), was evaluated by fluorescence microscopy and transmission electronic microscopy. Cell viability was measured by the ability of single cell to form colonies in vitro. The prepared nanoparticles were spherical in shape with size between 90 nm and 190 nm. The encapsulation efficiency was 20.06%. The drug release pattern exhibited an initial burst followed by a plateau for over 24 h. The cellular uptake of nanoparticles was observed. Co-culture of MCF-7 and HeLa cells with SR-2508 loaded nanoparticles showed that released SR-2508 retained its bioactivity and effectively sensitized two hypoxic tumor cell lines to radiation. The radiosensitization of SR-2508 loaded nanoparticles was more significant than that of free drug.     

Silica-modified Fe-doped calcium sulfide nanoparticles for in vitro and in vivo cancer hyperthermia

In this study, sulfide-based magnetic Fe-doped CaS nanoparticles modified with a silica layer were investigated for cancer hyperthermia. A polyvinyl pyrrolidone polymer was used as the coupling agent. The developed nanoparticles contained 11.6 wt% iron concentration, and their X-ray diffraction pattern was similar to those of CaS and Fe–CaS nanoparticles. The average particle size was approximately 47.5 nm and homogeneously dispersed in aqueous solutions. The major absorption bands of silica were observed from the FTIR spectrum. The magnetic properties and heating efficiency were also examined. The specific absorption ratio of nanoparticles at a concentration of 10 mg/mL at 37 °C in an ethanol carrier fluid was 37.92 W/g, and the nanoparticles would raise the temperature to over 45 °C within 15 min. A cytotoxicity analysis revealed that the nanoparticles had good biocompatibility, which indicated that the nanoparticles did not affect cell viability. The therapeutic effects of the nanoparticles were investigated using in vitro and animal studies. Cells seeded with nanoparticles and treated under an AC magnetic field revealed a percentage of cytotoxicity (60%) that was significantly higher from that in other groups. In the animal study, during a hyperthermia period of 15 days, tumor-bearing Balb/c mice that were subcutaneously injected with nanoparticles and exposed to an AC magnetic field manifested a reduction in tumor volume. The newly developed silica-modified Fe–CaS nanoparticles can thus be considered a promising and attractive hyperthermia thermoseed.