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Methotrexate (MTX), a stoichiometric inhibitor of dihydrofolate reductase enzyme, is a chemotherapeutic agent for treating a diversity of neoplasms. In this study, we design and developed a new formulation of MTX that serves as drug carrier and examined its cytotoxic effect in vitro. This target drug delivery system is dependent on the release of the MTX within the lysosomal compartment. The iron oxide magnetic nanoparticles (IONPs) were first surface-coated with L-lysine and subsequently conjugated with MTX through amidation between the carboxylic acid end groups on MTX and the amine groups on the IONPs surface. MTX-conjugated L-lysine coated IONPs (F-Lys-MTX NPs) was characterized by X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, vibrating sample magnetometer, and transmission electron microscopy techniques. The cytotoxicity of the void of MTX and F-Lys-MTX NPs were compared to each other by MTT assay of the treated MCF-7 cell lines. The results showed that the ζ-potential of F-Lys-MTX NPs was about −5.49 mV and the average size was 43.72 ± 4.73 nm. Model studies exhibited the release of MTX via peptide bond cleavage in the presence of proteinase K and at low pH. These studies specify that F-Lys-MTX NPs have a very remarkable anticancer effect, for breast cancer cell lines. [ABSTRACT FROM AUTHOR]

Abstract: In this work we reported the synthesis of tamoxifen (TMX) loaded l-tyrosine natural amino acids (Tyr) modified Fe3O4 magnetic nanoparticles. Tyr, which was containing phenol groups was selected to study their effects on biocompatibility, loading capacity and release profile of TMX. TMX loaded Tyr modified Fe3O4 magnetic nanoparticles (F@Tyr@TMX NPs) were characterized by X-ray diffraction, thermo gravimetric analysis, Fourier transform infrared spectroscopy, vibrating sample magnetometer, dynamic light scattering and transmission electron microscopy techniques. The results showed that the ζ-potential of F@Tyr@TMX NPs was about − 12.8 mV and the average size was 22.19 ± 3.58 [mean ± SD (n = 50)] nm. The loading capacity of 11.34 ± 0.09% and encapsulation efficiency of 51.21 ± 0.41%. Additionally, hemolysis test and MTT assays on HEK-293 were performed for determination of biocompatibility of F@Tyr@TMX NPs. Finally, the anticancer activity of F@Tyr@TMX NPs studied on MCF-7 breast cancer cell lines. The results indicate that these as prepared magnetic nanoparticles are suitable for delivery of TMX and even other hydrophobic drugs.Graphical Abstract: [ABSTRACT FROM AUTHOR]

Co-delivery approach has been recommended to reduce the amount of each drug and to achieve the synergistic effect for cancer treatment. Curcumin (CUR) and sulforaphane (SF) have antitumor effects, but their application is limited because of their low water solubility and poor oral bioavailability. To improve the bioavailability and solubility of SF and CUR, we performed an innovative co-delivery of them with PEGylated gold coated Fe3O4 magnetic nanoparticles (PEGylated Fe3O4@Au NPs) to endorse SF and CUR maintenance as an effective and promising antitumor drugs. The structure of the synthesized nanocarriers evaluated by X-ray diffraction, transmission electron microscopy, scanning electron microscopy, vibrating sample magnetometer, dynamic light scattering and Fourier transform infrared spectroscopy. The results revealed that the zeta potential of CUR and SF-loaded NPs were about -15.4 mV and the average sizes were 80.57 nm. They were monodispersed (polydispersity index = 0.161 ± 0.016) in water with high drug-loading capacity and stability. CUR and SF were encapsulated into NPs with loading capacity of 17.32 ± 0.023% and 16.74 ± 0.015% and the entrapment efficiency of 83.72 ± 0.14% and 81.20 ± 0.18% respectively. The in-vitro study of SF and CUR loaded PEGylated Fe3O4@Au NPs on human breast adenocarcinoma cell line (MCF-7) confirmed that cytotoxicity of SF and CUR can enhance when they are loaded on PEGylated Fe3O4@Au NPs in comparison to free SF and CUR. The results of real-time PCR and flow cytometry shown that this combination can increase therapeutic effects of SF and CUR by apoptosis and necrosis induction as well as inhibiting of migration in MCF-7 cell line. [ABSTRACT FROM AUTHOR]

Statins have been shown to exert ‘pleiotropic effects’ independent of their cholesterol lowering actions that include anti-inflammatory properties. In this study we synthesized mono methoxy poly (ethylene glycol)–poly (ε-caprolactone) (mPEG-PCL) di block copolymers. The structure of the copolymers was characterized by H nuclear magnetic resonance, Fourier-transform infrared spectroscopy, differential scanning calorimetry and gel permeation chromatography techniques. In this method, atorvastatin was encapsulated within micelles through a single-step nano-precipitation method, leading to the formation of atorvastatin-loaded mPEG-PCL (atorvastatin/mPEG-PCL) micelles. The resulting micelles were characterized further by various techniques such as dynamic light scattering and atomic force microscopy. In this study the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles on acute models of inflammation are analyzed, to compare the effect of indometacin in rats. Carrageenan induces rat paw edema; six animals of each group (10 groups) received indometacin, atorvastatin, and atorvastatin/mPEG-PCL micelles orally 1, 6, 12 and 24 h before carrageenan injection in paw. The paw edema thickness measured at 1, 2, 3 and 4 h after injection and percentage inhibition of edema in various groups were calculated. The results showed that the zeta potential of micelles was about −16.6 mV and the average size was 81.7 nm. Atorvastatin was encapsulated into mPEG-PCL micelles with loading capacity of 14.60 ± 0.96% and encapsulation efficiency of 62.50 ± 0.84%. Atorvastatin and atorvastatin/mPEG-PCL micelles showed significant anti-inflammatory activity in the present study. The anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles was significant in comparison with indometacin. Atorvastatin/mPEG-PCL micelles showed more anti-inflammatory activity than atorvastatin. This study revealed the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles and suggested the statins have a potential inflammatory activity along with its lipid lowering properties. Contrary to anti-inflammatory effects, the pro-inflammatory responses are independent of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibition and can be mediated directly by atorvastatin. [ABSTRACT FROM AUTHOR]

In this study, a kind of magnetic Fe3O4@mTiO2-GO (where m was shorted mesoporous) hybrids with core–shell nano-structure for controlled dual targeted drug delivery was synthesized using a facile sono-chemical method. The structure and chemical composition of the nanocarrier (NC), and its surface morphology, were studied by X-ray diffraction (XRD), scanning electron microscopy (SEM) with an energy dispersive X-ray (EDX), vibrating sample magnetometer (VSM) spectroscopy and Fourier transform infrared spectroscopy (FT-IR). Synthesis of Fe3O4@mTiO2-GO was proved by XRD and FT-IR. SEM showed that the particle size of this NC was in the range of ∼ 85–95 nm. EDX confirmed the presence of Ti, Fe, C and O in the nanocarrier. VSM analysis showed the magnetic behavior of the Fe3O4@mTiO2-GO nano-hybrids with saturation magnetization (MS) of 1.57 emu/g at room temperature. Curcumin (CUR) as a hydrophobic and an anti-tumor model drug was loaded on the NC. Drug loading capacity and encapsulation efficiency of this NC were as high as 17.85 and 72.45%, respectively. The drug release behavior was sustained and pH-responsive. MTT results demonstrated no significant cytotoxicity of the NC on Human Foreskin Fibroblast Normal cell line (HFF-2), indicating that this NC can be safe for use as a drug carrier for delivering anticancer drugs to tumor sites. The results of an MTT test on Caco-2 cancerous cells proved that CUR in nano-carriers has retained its anti-cancer properties. [ABSTRACT FROM AUTHOR]

In this project, TiO@ZnO nanoparticles core-shell nanostructured and titanium dioxide@ mesoporous zinc oxide-graphene oxide (TiO@ZnO-GO) hybrid nanocomposites as controlled targeted drug delivery systems were synthesized by a facile sono-chemical method. We prepared a novel mesoporous and core-shell structure as a drug nanocarrier (NCs) for the loading and pH-responsive characteristics of the chemotherapeutic curcumin. The structure, surface charge, and surface morphology of NCs were studied using with X-ray diffraction, Fourier transform infrared spectroscopy, dynamic light scattering, brunauer-emmett-teller, scanning electron microscopy (SEM), and transmission electron microscopy (TEM). The SEM and TEM images of NCs show the uniform hexagonal mesoporous morphology with average grain size of about ∼ 190 nm. The drug loading was very high about 16 and 19 for TiO@ZnO and TiO@ZnO-GO, respectively. The NCs showed pH-dependent drug release behavior. Drug release from TiO@ZnO-GO in neutral pH were higher than in acidic medium, due to anionic charge of GO nanosheet. MTT assay results showed that the curcumin-loaded NCs showed significant toxicity due to which cell viability reduced to below 50% at 140 μg/mL concentration, thereby confirming its anticancer effects. The goal of this study is the application of water-dispersed TiO@ZnO-GO with pH-dependent release properties for design a new drug delivery carrier. [ABSTRACT FROM AUTHOR]

We report the synthesis of iron oxide magnetic nanoparticles (IONPs) coated with various natural amino acids (AAs) using a one‐pot reaction in an aqueous medium. Several AAs, which contained hydrophilic and hydrophobic groups, were selected to study their effects on size, morphology and toxicity of IONPs. Functionalized IONPs were characterized using X‐ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy, and scanning and transmission electron microscopies. Furthermore, vibrating sample magnetometry analysis shows these nanoparticles have excellent magnetic properties. Cellular toxicity of IONPs was also investigated on HFF2 cell lines. The AA‐coated IONPs are non‐toxic and biocompatible. Natural AA‐coated IONPs show a potential for their development in in vitro and in vivo biomedical fields due to their non‐toxicity, good ζ‐potential and related small size and narrow size distribution. [ABSTRACT FROM AUTHOR]

A low cytotoxic metal-organic framework (MOF) UiO-66 (UiO stands for University of Oslo) and NH-UiO-66, that showed high cell viability of HFF-2 via 3-(4, 5-dimethylthiazol-2-yl) 2, 5-diphenyl tetrazolium assay, was reported as an effective adsorbent (antidotal) agents. The structure of MOFs was confirmed by Fourier transform infrared, Field emission scanning electron microscopy (FESEM) and X-ray diffraction. Thermal behavior of MOFs was investigated using with thermogravimetric analyzer in nitrogen atmosphere to check the thermal stability. FESEM showed NH-UiO-66 displayed symmetrical crystals with triangular base pyramid morphology, with the particle size around 100 nm and uniform size distribution. The specific surface areas were calculated using the Brunauer-Emmett-Teller method and surface area and total pore volume of NH-UiO-66 were calculated to be 1258 m/g and 0.51 cm/g, respectively. Methotrexate salt (MTX) was selected as the model drug which was adsorbed into inner pores and channels of MOFs by diffusion manner. The interaction between MOFs and MTX and the effect of pH on interaction between them in aqueous solution was investigated. The final results showed that UiO-66 have high adsorbing capacity and great affinity to MTX. [ABSTRACT FROM AUTHOR]

Purpose: Among the potent anticancer agents,d,l-sulforaphane (SF) is very effective against many different types of cancer cells. Its clinical application is restricted because of its hydrophobicity, low gastrointestinal absorption and poor bioavailability. In the present study, a reliable micellar delivery system using monomethoxypoly (ethylene glycol)–poly (ɛ-caprolactone) (mPEG–PCL) was established. The encapsulation of SF inside mPEG–PCL as a nano-carrier was established and the cytotoxicity assay against human breast cancer cell line was evaluated. Methods: In this study, SF was encapsulated within mPEG–PCL micelles through a single-step nano-precipitation method, leading to creation of SF-loaded mPEG–PCL (SF/mPEG–PCL) micelles. Di-block mPEG–PCL copolymers were synthesized and used to prepare micelles. MPEG-PCL copolymer was characterized by HNMR, FTIR, differential scanning calorimetry and gel permeation chromatography techniques. Characterization, stability of micelles, the particle size and morphology were determined. The release profile of the SF from the micelles which prepared by the drug-loaded copolymer, was evaluated. The cytotoxicity of free SF, mPEG–PCL and SF-loaded mPEG–PCL micelles was compared with each other by performing MTT assay of the treated MCF-7 cell line. Expression levels of BCL-2, MMP-9, BCL-XL, BAK, BAX and GAPDH (endogenous gene) as control were quantified by real time PCR. To evaluate the apoptotic effects of Free SF compared with SF-loaded mPEG–PCL micelles, flow cytometry analysis was done using the annexin V-FITC apoptosis detection kit. Results: Our studies resulted in a successful establishment of uniformity and spherical SF-loaded mPEG–PCL micelles. The encapsulation efficiency of SF was 86 ± 1.58%. The results of atomic force microscopy revealed that the micelles have spherical shapes with size of 107 nm.In vitrorelease of SF from SF-entrapped micelles was remarkably sustained. The mPEG–PCL micelle showed little cytotoxicity in the case of MCF-7 cell line with concentration up to 1.5 mg/ml, whereas the SF-loaded mPEG–PCL micelles at all concentrations significantly was cytotoxic in the case of MCF-7 cell line. Finally, real-time PCR and flow cytometry were used to demonstrate that the SF-loaded mPEG–PCL could be efficiently inducing apoptosis in MCF-7 cell line. Conclusion: We achieved to a successful formulation of SF-loaded m-PEG/PCL micelles in this study. Based on the cytotoxicity results of mPEG–PCL micelles against human breast cancer cell line (MCF-7) in this study, it suggested that SF/mPEG–PCL micelles can be an effective breast cancer treatment strategy in the future. [ABSTRACT FROM AUTHOR]

Background: A simple and sensitive high performance liquid chromatography-electrospray ionization mass spectrometry method has been evaluated for the assignment of clonidine hydrochloride in human plasma. Methods: The mobile phase composed of acetonitrile-water 60:40 (v/v) and 0.2% formic acid 20 μl of sample was chromatographically analyzed using a repacked ZORBAX-XDB-ODS C18 column (2.1 mm×30 mm, 3.5 μ). Detection of analytes was achieved by tandem mass spectrometry with Electrospray Ionization (ESI) interface in positive ion mode operated under the multiple-reaction monitoring mode (m/z 230.0 →213). Sample pretreatment consisted of a one-step Protein Precipitation (PPT) with methanol and perchloric acid (HClO4) of 0.10 ml plasma. Results: Standard curve was linear (r=0.998) over the concentration range of 0.01- 10.0 ng/ml and showed suitable accuracy and precision. The Limit of Quantification (LOQ) was 0.01 ng/ml. The mean (SD) Cmax, Tmax, AUC0–t and AUC0–∞ values after administration of the test and reference formulations, respectively, were in this manner: 6.16 (0.32) versus 6.21 (0.07) ng/ml, 30.12 (0.86) versus 30.13 (0.73) hr, 290.37 (1.13) versus 293.39 (1.22) ng/ml/hr, and 350.17 (1.98) versus 352.96 (1.67) ng/ml/hr. The mean (SD) t1/2 was 120.12 (1.90) hr for the test formulation and 120.96 (1.54) hr for the reference formulation. No statistical differences were showed for Cmax and the area under the plasma concentration-time curve for test and reference tablets. Conclusion: The method is rapid, simple, very steady and precise for the separation, assignment, pharmacokinetic and bioavailability evaluation of clonidine in healthy Iranian adult male volunteers. [ABSTRACT FROM AUTHOR]

[Display omitted] • Synthesis a biodegradable mPEG-PCL polymer. • Conjugation of methotrexate to the copolymer. • Characterization of MTX–mPEG-PCL. • Self-assembled of MTX–mPEG-PCL into micelles in the presence of curcumin by nano-precipitation method. • Determination of drug loading and drug encapsulation. • Study the effects of cytotoxicity of methotrexate and curcumin and conjugated nanoparticles methotrexate and curcumin were investigated by MTT assay on MCF7 cancer cell lines. Therapeutic strategies used to treat cancer are focused on cytotoxic drugs as the main form of chemotherapy. Recently nanocarrier-based chemotherapy has been widely used to treat cancer. Drugs covalently attached to a polymer chain, known as prodrugs, can significantly enhance drug incorporation efficiency. This study aimed to synthesis a biodegradable mPEG-PCL copolymers for effective and targeted drug delivery of the anticancer compounds curcumin and methotrexate and to investigate their physicochemical properties and effects on breast cancer cells. In this study, mPEG-PCL copolymer was synthesized by polymerization of ὲ-Caprolactone dehydrated monomer in the presence of dry methoxy polyethylene glycol as the initiator and Sn(Oct) 2 as catalyst. The mPEG-PCL copolymers were synthesized and their structure was evaluated using Fourier Transform Infrared Spectroscopy (FTIR). Then, methotrexate was conjugated to a copolymer. The methotrexate conjugated mPEG–PCL(MTX–mPEG-PCL) was self-assembled into micelles in the presence of curcumin by nano-precipitation method and the drug loading was assessed. Finally, the cytotoxicity of methotrexate, curcumin and conjugated nanoparticles with methotrexate and curcumin were investigated through 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on Michigan Cancer Foundation-7 (MCF-7) cancer cell lines. The size of mPEG-PCL-MTX and mPEG-PCL-MTX-CUR nanoparticles were evaluated by zeta sizer with an average size of 51.89 ± 0.46 nm (PDI = 0.127), and 88.21 ± 0.31 nm (PDI = 0.344), respectively. The zeta potential of nanoparticles was −4.22 mV. FTIR studies showed methotrexate was conjugated to the copolymer. The amount of drug released in nanoparticles at pH = 5.5 was higher than pH = 7.4. By increasing the drug concentration in the drug-carrying nanosystem, cell survival was further reduced. Among the treatment groups, mPEG-PCL-MTX-CUR group demonstrated the greatest impact, while, the MTX group showed the least impact on cancer cell mortality. These findings suggest that micelles conjugated with MTX and loading CUR appear to be promising systems for achieving Enhanced Permeability and Retention (EPR) effect, and pH sensitivity, which could improve the release and accumulation of drugs at tumor sites. [ABSTRACT FROM AUTHOR]

Purpose: Among the potent anticancer agents, curcumin is known as a very efficacious against many different types of cancer cells, but its clinical applications has been limited because of hydrophobicity, low gastrointestinal absorption, poor bioavailability and rapid metabolism. In this way, a novel micellar delivery system with mPEG-PCL was synthesized and the release profile of the curcumin from the drug-loaded micelles was evaluated. Methods: In this study, curcumin was encapsulated within monomethoxypoly(ethylene glycol)-poly(e-caprolactone) (mPEG-PCL) micelles through a single-step nano-precipitation method, leading to creation of curcumin-loaded mPEG-PCL (Cur/mPEG-PCL) micelles. Diblock mPEG-PCL copolymers were synthesized and used to prepare micelles. mPEG-PCL copolymer was characterized in vitro by HNMR, FTIR, DSC and GPC techniques. Then, mPEG-PCL copolymers with curcumin were self-assembled into micelles in aqueous solution. The resulting micelles were characterized further by various techniques such as dynamic light scattering (DLS) and atomic force microscopy (AFM). Results: The findings showed the successful formation of smooth and spherical curcuminloaded micelles. The encapsulation efficiency of curcumin was 88 ± 3.32%. The results of AFM revealed that the micelles have spherical shapes with size of 73.8 nm. The release behavior of curcumin from micelles was compared in different media. In vitro release of curcumin from curcumin-entrapped micelles was followed remarkably sustained profile. The sustained release of drug was hypothetically due to the entrapment of curcumin in core of micelles. Conclusion: The results indicate the successful formulation of curcumin loaded m- PEG/PCL micelles. From the results, iIt can be concluded that curcumin m-PEG-PCL micelles may be considered as an effective treatment strategy for cancer in the future. [ABSTRACT FROM AUTHOR]

This document is a correction notice for an article titled "Multi-wall carbon Nanotube surface-based functional nanoparticles for stimuli-responsive dual pharmaceutical compound delivery" published in Scientific Reports. The correction addresses an error in Figure 4 of the original article, where the drug release chart had incorrect labeling. Additionally, there was an error in the affiliation of one of the authors, which has been corrected. The corrected version of the article is now available. [Extracted from the article]

In recent years, various types of radiosensitizers have been developed to address the challenges of cancer radiotherapy. Here, platinum-functionalized oxygenated single-walled carbon nanotubes (O-SWCNTs-Pt) coated with folic acid (FA) and bovine serum albumin (BSA) (O-SWCNTs-Pt-BSA-FA) were synthesized, characterized, and used as radiosensitizers to improve the therapeutic efficacy of X-rays in a mouse model of breast cancer (4T1) in vitro. The nanosensitizer was characterized by different techniques, such as transmission electron microscopy (TEM), selected area electron diffraction (SAED), dynamic light scattering (DLS), zeta potential, X-ray diffraction (XRD), ultraviolet–visible (UV-visible), and Fourier transform infrared (FTIR) spectrometry. The evaluation of cell viability with nanocarriers O-SWCNTs-BSA, O-SWCNTs-Pt-BSA, Pt-BSA-FA, and O-SWCNTs-Pt-BSA-FA is reported at the concentrations of 10, 30, and 90 μg/mL by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay in the presence and absence of X-rays at 4 and 8 Gy. The results showed that administration of O-SWCNTs-BSA, O-SWCNTs-Pt-BSA, Pt-BSA-FA, and O-SWCNTs-Pt-BSA-FA + 8 Gy at a concentration of 90 μg/mL reduced survival by 75.31, 65.32, 67.35, and 60.35%, respectively. O-SWCNTs-Pt-BSA-FA has a hydrodynamic size of 88.57 nm and a surface charge of −29 mV, which indicates special stability. Compared with O-SWCNTs-BSA, O-SWCNTs-Pt-BSA, and Pt-BSA-FA, it has very strong cell-killing activity in the 4T1 cell line. It is also noteworthy that SWCNTs can act as a controlled release and delivery system for PtNPs due to their unique properties and easy penetration into biological membranes. As a result, the new nanosensitizer may play a role in cancer treatment in conjunction with radiotherapy technology. [ABSTRACT FROM AUTHOR]

A selective and highly sensitive high performance liquid chromatography-electrospray ionization mass spectrometry method has been developed for determination of ezetimibe concentrations in human plasma. Ezetimibe was extracted from plasma with ethyl acetate followed by evaporation of the organic layer and, then, reconstitution of the residue in mobile phase before injection to chromatograph. The mobile phase consisted of acetonitrile-ammonium acetate (10 mM, pH 3.0), 75:25 ( v/v). An aliquot of 10 μL was chromatographically analyzed on a prepacked Zorbax XDB-ODS C 18 column (2.1 × 100 mm, 3.5 micron). Detection of analytes was achieved by mass spectrometry with atmospheric pressure chemical ionization (APCI) interface in the negative ion mode operated under the multiple-reaction monitoring mode ( m/z transition: ezetimibe 408–271). Standard curves were linear ( r = 0.998) over the wide ezetimibe concentration range of 0.05–30.0 ng mL −1 with acceptable accuracy and precision. The limit of detection was 0.02 ng mL −1. The validated LC–APCI–MS method has been used successfully throughout a bioequivalence study on an ezetimibe generic product in 24 healthy male volunteers. [ABSTRACT FROM AUTHOR]

There was an incorrect labeling of the samples during the VSM experiment by the operator, which caused us to present an incorrect Ms for F@Tyr@TMX NPs in Fig. 6 revised below. Since the presented result is related to iron oxide nanoparticles, replacement of the image does not influence the main conclusions of the paper. In order to present valid results, we repeated the VSM experiments. [ABSTRACT FROM AUTHOR]

• Preparation of Pt@BSA nanoparticles. • Characterization of Pt@BSA nanoparticles. • Preparation Ag-Pt@BSA nanoradiosensitizers. • Characterization of Ag-Pt@BSA nanoradiosensitizers. • In vitro radio-enhancement of Ag-Pt@BSA. • Clonogenic assay. • Apoptosis assay. • Intracellular ROS generation. Cancer has traditionally been treated with surgery and chemotherapy. Radiation therapy (RT) is a branch of oncology based on radiation therapy that can be used alone or in combination with surgery and chemotherapy to achieve local control of breast cancer. Radiosensitizers make tumor cells more responsive and sensitive to ionizing radiation, consequently facilitating production of free radicals and hastening DNA damages. Stages I to III of breast cancer is managed with curative intent with multimodality treatment including radiotherapy. The current cancer therapies in particular radiotherapy have a high risk of serious side effects to the healthy tissues and do not guarantee remission. In response to this challenge, the present study developed bovine serum albumin capped platinum and silver nanoparticles (Ag-Pt@BSA NPs), a bimetallic radiosensitizer, which is a remedy to the aforementioned issue. This research makes use of a nanoplatform that contains two high-Z nanoparticles— Pt and Ag. A variety of methods were used to fully characterize the developed Ag-Pt@BSA NPs. Fourier-transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), dynamic light scattering (DLS), UV–Vis, X-ray diffractometery (XRD) and energy-dispersive X-ray spectroscopy (EDS) techniques were used to investigate the physical and chemical features of designed bimetallic nanoradiosensitizer. The Ag-Pt@BSA naoradiosensitizer was proven to have successfully prepared by FTIR, XRD and EDX. According to the DLS result, the hydrodynamic size of the NPs is 35.42 nm, and the average diameter in the TEM image is around 7.8 ± 2.6 nm. The initial hydrodynamic size Ag-Pt@BSA was around 35 nm and within the storage time its size remained below 40 nm which indicating the unique colloidal stability of fabricated nanoradiosensitizers. The zeta potential of Ag-Pt@BSA radio-enhancement was determined to be approximately −17.9 mV, providing additional support for the nanoparticles' colloidal stability. The results showed that the utilization of Ag-Pt@BSA NPs in conjunction with X-ray irradiation could substantially enhance the effectiveness of cancer therapy. This is supported by research, examining a series of in vitro tests including reactive oxygen species generation (ROS), cell viability, apoptosis and colony formation assay. Furthermore, the dosage-dependent radiosensitizing ability of the Ag-Pt@BSA NPs was also observed in the apoptosis and MTT assay against 4 T1 cells by increasing the localized radiation dosage. Ag-Pt@BSA NPs could be a potential radio-enhancer agent against breast cancers and, by extension, other cancers, since it multiplies the therapeutic effect of low-dose radiation while reducing the damage to normal tissues compared to high-dose radiation therapy. Increasing the concentration of Ag-Pt@BSA NPs and the dosage of X-ray irradiation boosted the radiosensitizing capacity in a dose-dependent way. [ABSTRACT FROM AUTHOR]

• Various methods and nanomaterials used to deliver the CRISPR/Cas9 discussed. • Recent progress in the delivery of CRISPR/Cas9 system via nanomaterials presented. • Three different forms of CRISPR/Cas9 discussed in more detail point by point. • Both biological aspect and the structure of nanomaterials discussed. • Outline future challenges in the field of CRISPR/Cas9 components delivery summarized. Exploiting bacterial DNA-acting enzymes and expanding their repertoire for genome engineering have been major technological and conceptual advances in molecular biology over the last decade. The CRISPR-Cas9 system offers many attractive superiorities, such as multiplexing, high precision, low cost, and simplicity compared to other strategies/systems/approaches known to date for gene editing. The efficient co-delivery of Cas9 and single guide RNA(s) into a desired cell and subsequent correct targeting of selected genomic fragment(s) are among the most critical and determining issues for CRISPR-Cas9-based genome engineering. CRISPR/Cas9 components can be transported into target cells via various delivery methods, including physical methods (such as electroporation and microinjection) as well as viral and non-viral methods. Physical and viral methods, with all their privileges, still suffer from disadvantages including induction of immune responses, cell damage, lack of high specificity, etc. We are witnessing a remarkable increase in the employment of nanomaterials as non-viral carriers for the delivery of the CRISPR/Cas9 system. Nanoparticles have so far presented numerous advantages such as ease of synthesis, high efficiency, low cost, size tunability, non-mutagenicity, non-immunogenicity, etc. with regard to the delivery of CRISPR/Cas9. Here, we will review the recent progress in the delivery of CRISPR/Cas9 system components via nanomaterials and outline future challenges. [ABSTRACT FROM AUTHOR]

In this study, Bi2S3@BSA–Bio–MTX nanoparticles (NPs) were synthesized for the first time by bovine serum albumin (BSA)‐mediated biomineralization (Bi2S3@BSA NPs) followed by covalent bonding of biotin (Bio) and methotrexate (MTX) on the surface of the Bi2S3@BSA NPs via carbodiimide chemistry. The synthesized NPs were globular and exhibited uniform morphology with a hydrodynamic diameter of 107.6 ± 6.81 nm (mean ± standard deviation) and zeta potential of −20.9 ± 2.18 mV. Drug release from Bi2S3@BSA–Bio–MTX NPs indicated an enzyme‐dependent release pattern. The in vitro biocompatibility of NPs was confirmed by investigating their cytotoxicity against the HEK‐293 cell line and hemolysis assay test, whereas the in vivo biocompatibility of the NPs was evaluated and confirmed by the lethal dose 50 (LD50) test. To evaluate the in vitro anticancer activity of the functionalized NPs and MTX, their cytotoxic effects was assessed against 4T1 cancer cells by 5‐dimethylthiazol‐z‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assay with and without X‐ray radiation. Results showed that Bi2S3@BSA–Bio–MTX NPs have excellent anticancer activity, especially following X‐ray radiation. [ABSTRACT FROM AUTHOR]

Among the potent anticancer agents, methotrexate (MTX) is very effective against many different types of cancer cells. Implementation of chemotherapy along with radiotherapy, known as synchronous chemoradiotherapy, can augment the treatment efficacy. In the present study self‐assembled MTX conjugated mPEG‐PCL copolymer encapsulating gold nanoparticles (AuNPs) hybrid (mPEG‐PCL‐MTX@Au) was developed as both drug carrier and radiosensitizer. After successful synthesis and characterization of hybrids with different techniques such as hydrogen nuclear magnetic resonance (HNMR), Fourier transform infrared spectroscopy (FTIR), ultraviolet–visible (UV‐Vis), x‐ray diffraction analysis (XRD), dynamic light scattering (DLS), and transmission electron microscopy (TEM). The anticancer activity of designed system was evaluated with a series of biological assays. TEM image indicate that AuNPs encapsulated by self‐assembled mPEG‐PCL‐MTX NPs. It was found that the micelle of that shown in the TEM image contains nine gold nanoparticles (NPs). The hydrodynamic diameter of mPEG‐PCL‐MTX@Au was 81.40 ± 8 nm. As a result, at acidic pH, which simulates tumor tissue, the most drug release is done compared to neutral pH conditions, which are the physiological conditions of the body. About 70% of the drug was released in acidic pH, while in alkaline pH, it was about 35%. The effectiveness of cancer treatment was significantly improved by using developed NPs, which introduces simultaneous chemotherapy and radiotherapy. MTT and apoptosis assays show that the mPEG‐PCL‐MTX@Au as the final formulation improves the radiosensitivity of the 4T1 breast cancer cells and also remarkably kills breast cancer. Furthermore, the result revealed that designed hybrid system extremely able to produce reactive oxygen species (ROS) within cancer cells. These results offer powerful evidence for the potential capability of mPEG‐PCL‐MTX@Au in radiosensitization of malignant tumors and opens up a new avenue of research in this area. [ABSTRACT FROM AUTHOR]

In this article, Fe3O4/GO and Fe3O4/ZnO/GO nanocomposites (NPs) synthesized by thermal treatment at 823 K, and their drug delivery properties for curcumin (CUR) as an anticancer drug were investigated. The structural, morphological, and magnetic properties of these Nps were studied. The results of XRD, FTIR and EDX analyses indicated the synthesis of pure and crystalline structures of GO, Fe3O4/GO and Fe3O4/ZnO/GO NPs. Moreover, the mean size of spherical shape in Fe3O4/GO and Fe3O4/ZnO/GO nanoparticles was 42.36 and 53.21 nm, respectively. Based on the results of release and loading at different pHs, the drug is well loaded on the NPs and released at the tumor site. Based on these studies, the drug loading percentage on Fe3O4/GO is higher than Fe3O4/ZnO/GO. Also, the results showed that 41.65% of the drug is released from Fe3O4/GO and 23.43% from Fe3O4/ZnO/GO in the first ten hours after being in the cancer cell site. The Hemolysis test of prepared NPs and the cytotoxicity of NCs and CUR-loaded on NCs against U87 cancer cells and fibroblast human cells were investigated using the MTT assay. The toxic effect of Fe3O4/GO and of Fe3O4/ZnO/GO was more in U87 cancer cells compared to normal fibroblast cells. The results of anticancer activity of Nano-carriers on brain cancer cell lines revealed that CUR-loaded nanocrystals (NCs) have significant cytotoxicity activity on U87. Therefore, these NCs are capable of acting as drug delivery systems for anti-cancer drugs like CUR. [ABSTRACT FROM AUTHOR]

To conquer the low water solubility and bioavailability of curcumin (CUR), to corroborate its functional qualities and to broaden its applicability in the pharmaceutical sector, numerous nanoscale methods have been widely exploited for its administration. Because of its polycystic, biodegradable, biocompatibility, non-toxicity, and non-allergenic properties, bovine serum albumin (BSA) and glycine (Gly) have been actively investigated as natural biopolymers for decades. Various BSA and Gly-based nanocarriers with unique features for CUR delivery, such as magnetic ferrite nanoparticles, are being developed (MNPs). In this work, magnesium ferrite (MgFe2O4)/BSA and nickel ferrite (NiFe2O4)/Gly nanocomposites loaded with CUR (drug model) were manufactured for the first time using a chemical co-precipitation approach to create biocompatible drug nanocarriers. It was found that the synthesized MgFe2O4/BSA and NiFe2O4/Gly nanoparticles have a uniform particle distribution and their size is much less than 100 nm. Saturation magnetization in MgFe2O4 and NiFe2O4 reaches 13.07 and 33.4 emu/g the remarkable peak of magnetization decreases to 10.99 and 32.36 emu/g after the addition of polymers. These analyses also showed the presence of chemical bonds in the structure of the nanocomposite. The curcumin diffusion process in NPs were determined using a mathematical modeling. The yielding of the product for MgFe2O4/BSA and NiFe2O4/Gly in 200 h is about 72 and 63%, respectively. Also, regressed relative diffusivities (D/R2), including effective steric hindrance, were determined as 5.75 × 10-4 and 2.72 × 10-4 h-1 for MgFe2O4/BSA and NiFe2O4/Gly, respectively. It shows that there is a significant steric barrier that significantly deviates from the molecular diffusion of the liquid. As a result, the low effective release of curcumin in the particles is more noticeable. Our study demonstrated the effective relationship between the polymer architecture and the biophysical properties of the resulting nanoparticles and shed light on new approaches for the design of efficient NP-based drug carriers. [ABSTRACT FROM AUTHOR]

To solve the traditional radiotherapy obstacles, and also to enhance the radiation therapy efficacy various radiosensitizers have been developed. Radiosensitizers are promising agents that under X-ray irradiation enhance injury to tumor tissue by accelerating DNA damage. In this report, silver-silver sulfide nanoparticles (Ag-Ag2S NPs) were synthesized via a facile, one-pot and environmentally friendly biomineralization method. Ag-Ag2S was coated with bovine serum albumin (BSA) in situ and applied as an X-ray sensitizer to enhance the efficiency of radiotherapy. Also, folic acid (FA) was conjugated to Ag-Ag2S@BSA to impart active targeting capability to the final formulation (Ag-Ag2S@BSA-FA). Prepared NPs were characterized by transmission electron microscopes (TEM), scanning electron microscope (SEM), dynamic light scattering (DLS), ultraviolet–visible spectroscopy (UV–Vis), X-ray diffraction analysis (XRD), and X-ray photoelectron spectroscopy (XPS) techniques. Results show that most of the NPs have well-defined uniform Janus structures. The biocompatibility of the NPs was then evaluated both in vitro and in vivo. A series of in vitro assays were performed on 4T1 cancer cells to evaluate the therapeutic efficacy of the designed NPs. In addition, the radio-enhancing ability of the NPs was tested on the 4T1 breast cancer murine model. MTT, live and dead cell staining, apoptosis, ROS generation, and clonogenic in vitro assays demonstrated the efficacy of NPs as radiosensitizers in radiotherapy. In vivo results as well as H&E staining tumor tissues confirmed tumor destruction in the group that received Ag-Ag2S@BSA-FA NPs and exposed to X-ray. The results showed that prepared tumor-targeted Ag-Ag2S@BSA-FA NPs could be potential candidates as radiosensitizers for enhanced radiotherapy. [ABSTRACT FROM AUTHOR]

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 via 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. PMAA-MTX-CQ exhibited high drug loading capacity of which MTX was 4.99% and was CQ 25.01% and displayed pH/enzyme-triggered drug release behavior. Higher CQ release rate (76%) under simulated acidic microenvironment of tumor tissue whereas 39% of CQ was released under normal physiological conditions. Intestinally, MTX release was facilitated in the presence of proteinase K enzyme. TEM image demonstrated spherical morphology with particle size of less than 50 nm. In vitro and in vivo toxicity assessments indicated that developed nanoplatforms possessed great biocompatibility. These nanohydrogels did not cause any adverse effects against Artemia Salina and HFF2 cells (around 100% cell viability) which highlight the safety of prepared nanohydrogels. There was no death in mice received different concentrations of nanohydrogel through oral administration and less than 5% hemolysis was found in red blood cells incubated with PMAA nanohydrogels. In vitro anti-cancer results showed that combination therapy based on PMAA-MTX-CQ can effectively suppress the growth of SW480 colon cancer cells (29% cell viability) compared to monotherapy. Altogether, these findings suggest that pH/enzyme-responsive PMAA-MTX-CQ could effectively inhibit cancer cell growth and progression via site-specific delivery of its cargo in a safe and controlled manner. [ABSTRACT FROM AUTHOR]

Multifunctional nanoplatforms based on novel bimetallic nanoparticles have emerged as effective radiosensitizers owing to their potential capability in cancer cells radiosensitization. Implementation of chemotherapy along with radiotherapy, known as synchronous chemoradiotherapy, can augment the treatment efficacy. Herein, a tumor targeted nanoradiosensitizer with synchronous chemoradiotion properties, termed as CuFe 2 O 4 @BSA-FA-CUR, loaded with curcumin (CUR) and modified by bovine serum albumin (BSA) and folic acid (FA) was developed to enhance tumor accumulation and promote the anti-cancer activity while attenuating adverse effects. Both copper (Cu) and iron (Fe) were utilized in the construction of these submicron scale entities, therefore strong radiosensitization effect is anticipated by implementation of these two metals. The structure–function relationships between constituents of nanomaterials and their function led to the development of nanoscale materials with great radiosensitizing capacity and biosafety. BSA was used to anchor Fe and Cu ions but also to improve colloidal stability, blood circulation time, biocompatibility, and further functionalization. Moreover, to specifically target tumor sites and enhance cellular uptake, FA was conjugated onto the surface of hybrid bimetallic nanoparticles. Finally, CUR as a natural chemotherapeutic agent was encapsulated into the developed bimetallic nanoparticles. With incorporation of all abovementioned stages into one multifunctional nanoplatform, CuFe 2 O 4 @BSA-FA-CUR is produced for synergistic chemoradiotherapy with positive outcomes. In vitro investigation revealed that these nanoplatforms bear excellent biosafety, great tumor cell killing ability and radiosensitizing capacity. In addition, high cancer-suppression efficiency was observed through in vivo studies. It is worth mentioning that co-use of CuFe 2 O 4 @BSA-FA-CUR nanoplatforms and X-ray radiation led to complete tumor ablation in almost all of the treated mice. No mortality or radiation-induced normal tissue toxicity were observed following administration of CuFe 2 O 4 @BSA-FA-CUR nanoparticles which highlights the biosafety of these submicron scale entities. These results offer powerful evidence for the potential capability of CuFe 2 O 4 @BSA-FA-CUR in radiosensitization of malignant tumors and opens up a new avenue of research in this area. [Display omitted] [ABSTRACT FROM AUTHOR]

Due to the increased incidence and population growth that has been leading to growing number of cases worldwide, early diagnosis and treatment of cancer is crucial. Low density cancer tissue cannot be diagnosed before progressing toward a metastatic stage. Thus, theranostic systems play a significant role in assisting timely diagnosis and treatment. The combination of magnetic resonance imaging (MRI) and computed tomography (CT) contrast agents in a single probe is of high importance and necessity, where individual strengths of each approach can be merged while shortcomings of each modality could be compensated. With this motivation, we have developed and synthesized Bi2S3@BSA‐Fe3O4 nanoparticles as a dual MRI/CT contrast agent and carrier of curcumin (CUR) as natural anticancer drug. The nanoparticles shortened both the longitudinal (T1) and transverse (T2), MRI relaxation times, with a more distinct effect on producing negative contrast (T2) images with a relaxivity (r2) of 54.73 mM−1 s−1. The magnetite/bismuth hybrid nanoparticle also was capable of increasing CT image contrast. Further, in vitro cytotoxicity assay showed high biocompatibility of the synthesized nanoparticles. Furthermore, in vitro cytotoxicity assay on cancer cells showed high anticancer activity of the synthesized nanoparticles. [ABSTRACT FROM AUTHOR]

Background and purpose: Acinetobacter baumannii (A. baumannii) is known as a pathogen with antibiotic resistance, causing respiratory infections. PLGA has been approved for use in vaccines as well as drug delivery. This study was performed to evaluate PLGA nanoparticles containing the outer membrane proteins (OMPs) of A. baumannii in stimulating the mice's immune system and improving pneumonia. Experimental approach: Double emulsion solvent evaporation technique was used. The properties of the obtained nanospheres were determined using a zetasizer, FTIR, and AFM devices. Nanoparticles were administered to mice BALB/c by applying the intramuscular route. ELISA was used to measure the amounts of immunoglobulins produced; also, an opsonophagocytic killing assay was used to measure the effectiveness of immunoglobulins. Immunized mice were then challenged with live A. baumannii through the lungs; their internal organs were also removed for bacteriological studies. Findings/Results: The prepared particles were 550 nm in diameter with a negative surface charge. The production of the OMPs specific IgG was much higher in the group receiving nanoparticles containing antigen as compared to those getting pure antigen. The immunoglobulins produced against nanoparticles were superior to those developed against pure antigens. Mice that received the new nanovaccine were more resistant to pneumonia caused by this bacterium than those that received pure antigen. Conclusion and implication: Overall, it can be said that PLGA nanoparticles could deliver their internal antigens (OMPs) well to the immune system of mice and stimulate humoral immunity in these animals, thus protecting them against pneumonia caused by A. baumannii. [ABSTRACT FROM AUTHOR]

Insulin-like growth factor-1 receptor (IGF-1R) is expressed in malignant and normal breast tissue, and its intermittent activation by multiple IGF-1 signaling pathways leads to neoplasm cell proliferation, impaired apoptosis, increased survival, and resistance to cytotoxic therapeutic agents. Therefore, simultaneous suppression of the receptor and its cognate ligand would be a powerful promising strategy inhibiting malignant phenotypes of breast cancer cells. In the present study, Methoxypoly(ethylene glycol) - Poly(caprolactone) was hybridized with Dimethyldioctadecylammonium bromide (DDAB) cationic lipid (mPEG-PCL-DDAB) nanoparticles (NPs) and used as a carrier for simultaneous delivery of lycopene and insulin-like growth factor 1 receptor-specific lycopene encapsulated-mPEG-PCL-DDAB nanoparticle/siRNA to MCF-7 breast cancer cells. Then, the antitumor effects of this construct were evaluated in vitro. The results demonstrated that the synthesized mPEG-PCL-DDAB nanoparticle had suitable physicochemical properties. The use of mPEG-PCL-DDAB nanoparticle-loaded anti-insulin-like growth factor 1 receptor-siRNA and lycopene dramatically induced the process of apoptosis and arrested cell cycle in the MCF-7 tumor cell lines. In general, the findings of this study demonstrated the potency of mPEG-PCL-DDAB nanoparticles for dual delivery of siRNA, and lycopene in breast cancer cell lines followed the induction of apoptosis. [ABSTRACT FROM AUTHOR]

In the present study the effect of nanodiamond (ND) on the adsorption capacity of Drug has been investigated. Thermal oxidation nanodiamond (OND) was used as adsorbents for Methotrexate adsorption. The surface properties of NDs were studied by Fourier transform infrared spectroscopy and zeta potential. It was determined that thermal oxidation changed the surface properties of ND, including increase the amount of carboxylic acid groups and decreasing the zeta potential of ND by increasing the thermal oxidation time. The adsorption experiments showed that untreated ND (UND) has large adsorption capacity and fast adsorption kinetic for methotrexate (MTX). These results suggest that the adsorption behavior of UND with the MTX follows not only the charge but also the chemical interaction. Due to form the strong hydrogen bond between the carboxyl groups of MTX and the oxygen containing groups on the surface of NDs, Kinetic studies showed that the kinetic data are well fitted with the pseudo- second-order model for most of the adsorbents. MTT assay, Hemolysis assay and acute toxicity were used for determining biocompatibility of the adsorbents; MTT assay showed no significant toxicity up to near 300 µg/mL, OND showed neglectable hemolysis and acute toxicity result demonstrated OND was nontoxic. [ABSTRACT FROM AUTHOR]

The article discusses Thidiazuron induced efficient in vitro organogenesis and regeneration of Scutellaria bornmuelleri as an important medicinal plant. It is used in traditional Chinese medicine to treat bronchitis, hepatitis, diarrhea, tumors, infectious disease, inflammatory, and allergic diseases. The presence of flavones, such as baicalin, wogonoside, wogonin, baicalein, and luteolin, is responsible for pharmacological activities of S. baicalensis.

Abstract The present paper aimed to synthesize, using thermal-treatment method, a variety of Co 1-X Zn x Fe 2 O 4 -based nanocarriers (NCs) as Dual-controlled and targeted drug delivery systems (DDS) and provide a new structure as NCs suitable for the loading and pH-responsive characteristics of the chemotherapeutic curcumin (CUR). To study the structure, surface morphology, surface charge and magnetic properties of NCs, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), Zetasizer and vibrating sample magnetometer (VSM) were applied here. TEM images of Co 0.2 Zn 0.8 Fe 2 O 4 (Co-0.2) showed that NCs had a uniform spherical mesoporous morphology with an average grain size of about ∼17 nm. Also, it was found that Drug loading was very high, about 22.70 and 21.99 for Co 0.6 Zn 0.4 Fe 2 O 4 (Co-0.6) and Co 0.4 Zn 0.6 Fe 2 O 4 (Co-0.4), respectively. As indicated, NCs had highly pH-dependent drug release behavior, although different and unique in every one of them, which could be related to zeta potential of Co-0.6. In fact, the neutral zeta potential of Co-0.6 became positive when the pH of releasing media changed from 7.4 to 5.5. Consequently, the hydrogen bond between the Co-0.6 and CUR brake. Therefore, as expected, drug releasing varied from Co-0.6 to about 54% at pH 5.5, rather 29% at pH 7.4. To determine the cytotoxicity of NCs, hemolysis assay, MTT assay and acute toxicity test were used. The tests showed that NCs had the least in vitro and in vivo cytotoxicity and NCs, as a result, could be regarded to be nontoxic. MTT results demonstrated that drug loaded NCs had the same cell viability as bare drugs. Then, it can be concluded that these NCs have the potential required to act as drug delivery systems for anti-cancer drugs delivery such as CUR. Highlights • Co 1−X Zn x Fe 2 O 4 based nanocarriers (NCs) as Dual controlled targeted drug delivery systems (DDS) were synthesized. • Zeta potential at different pH, could control the release of CUR from NCs. • We controlled the release of CUR from NCs with replacing appropriate ratio of Zn and Co instead of Fe. • NCs had great in vivo and in vitro biocompatibility. • Small size of drug loaded-NCs and their stability can help to accumulate drugs in tumor site. [ABSTRACT FROM AUTHOR]

Abstract This study manipulated a chrysin loaded bovine serum albumin nanoparticles (BSA NPs), which could solubilize the poorly water-soluble drug and increase the therapeutic efficacy of the drug. Chrysin (5, 7-dihydroxyflavone) is a natural flavonoid which have some significant biological effects on the processes of chemical defense. Chrysin loaded bovine serum albumin nanoparticles (Chrysin-BSA NPs) were synthesized by a simple desolvation procedure. The resultant Chrysin-BSA NPs showed a spherical shape, with a diameter of 97.5 ± 5.75 nm (mean ± SD) nm and a ζ-potential of - 11 mV. The in vitro drug release study of chrysin presented a sustained and controlled release pattern. Cellular toxicity of BSA NPs was also investigated on HFF2 cell lines. Additionally, a hemolysis test of as prepared NPs were performed. Hemolysis assay and cytotoxicity study results on HFF-2 cell line show that as prepared BSA NPs are biocompatible. The in vitro cytotoxicity of the nanoparticles was performed by MTT assay on MCF-7 cancer cells. These results suggest that Chrysin-BSA NPs are a new drug delivery system for cancer therapy. Graphical abstract Unlabelled Image Highlights • The bovine serum albumin nanoparticles were prepared through desolvation process. • The resultant Chrysin-BSA NPs showed a spherical shape, with a diameter of 97.5 ± 5.75 nm. • Hemolysis assay and cytotoxicity study results show that BSA NPs are biocompatible. Therefore, the prepared Chrysin-BSA NPs is a promising drug delivery system for chrysin. [ABSTRACT FROM AUTHOR]

Triblock poly(ε-caprolactone) - poly(ethylene glycol) - poly(ε-caprolactone) (PCL-PEG-PCL) copolymers were synthesized and used to prepare polymersomes for controlled release of lovastatin (LOV) as hydrophobic drug. Biodegradable PCL-PEG-PCL copolymer nanoparticles were prepared and the drug loading, release, release kinetics, and anti-cancer activity of these drugs was investigated. The PCL-PEG-PCL copolymer was synthesized by ring-opening polymerization of e-caprolactone in the presence of mPEG as the initiator and Sn(Oct)2 as the catalyst. The synthesized copolymers and nanoparticles were characterized by FTIR, 1H NMR, DLS, and AFM techniques. The efficiency of drug loading and release from nanoparticles in vitro was studied by UV-Vis spectrophotometry. Additionally, MTT assays on HFF-2 cell lines were performed for determining the biocompatibility of polymersomes. Finally, the antiproliferative activity of polymersomes was examined on MCF-7 breast cancer cell line. The obtained results showed that the average diameter of nanoparticles was less than 57 nm. The loading capacity and encapsulation efficiency of LOV was 16.1 ± 0.36% and 59.01 ± 0.78%, respectively. In vitro release study showed that the release rate of polymersomes depended on pH and was higher at lower pH than under neutral condition. The result of cell viability assay on the MCF-7 line proved that bare nanoparticles showed little inherent cytotoxicity whereas the LOV-loaded nanoparticles were cytotoxic. [ABSTRACT FROM AUTHOR]

[Display omitted] • Synthesis of Tetraphenylporphyrin and H2T(4-SO2Cl)PP. • Conjugation of functionalized porphyrin to albumin-metronidazole nanoparticles. • In vitro radiation/photodynamic therapy. Breast cancer is the second leading cause of cancer death in women after lung cancer. In the context of cancer therapy, chemotherapy regarded as the most common method of treatment, but besides this beneficial modality, radiation therapy (RT) is used as a supplementary or palliative treatments. In this regard, we aimed at preparing albumin- Tetraphenylporphyrin -metronidazole nanosystem (BSA-Met- H2T(4-SO2)PP NPs) as an effective photo/radiosensitizer along with RT to tackle breast cancer. Accordingly, the synthesized nanosystems were analyzed by various characterization techniques such as dynamic light scattering (DLS), fourier transform infrared spectroscopy (FT-IR), UV–vis, and proton nuclear magnetic resonance (1HNMR), also transmission electron microscopy (TEM) technique was used to determine the morphology and size of fabricated nanosystems. Moreover, the biosafety of developed nanosystems were ascertained using LD 50 and hemolysis assay. Based on DLS measurements the average size and polydispersity index of fabricated nanosystems were about 190 nm and 0.36, respectively. The BSA-Met-H2T(4-SO2)PP NPs showed pH-dependent drug release behavior. The results showed that the drug loading (DL) for metronidazole and Tetraphenylporphyrin were 3.406% and 13.586%, respectively. Both hemolysis and LD 50 confirmed the biosafety of the BSA-Met-H2T(4-SO2)PP NPs. Finally, MTT assay revealed that the prepared nanoparticles exhibited great anti-cancer activity upon radiation and light against 4 T1 cancer cells. Overall, our findings suggest that PPHN-MET NPs may be promising candidates for the effective radiation/or light-induced cancer therapy. [ABSTRACT FROM AUTHOR]