Cytotoxicity Of Nanoparticles Research Articles

Targeted delivery of 5-fluorouracil and shikonin by blended and coated chitosan/pectin nanoparticles for treatment of colon cancer

Herein, 5-fluorouracil and shikonin (extracted from Fusarium tricinctum) were loaded in chitosan/pectin nanoparticle (CS/PEC-NPs), prepared by blending (B-CS/PEC-NPs) and coating (C-CS/PEC-NPs) methods. The nanoparticles characterized by Fourier Transform Infrared (FTIR), X-ray diffraction (XRD), Energy-dispersive X-ray (EDX), Scanning Electron Microscope (SEM) and Differential Light Scattering (DLS). Then, some properties of the nanoparticles such as drug release rate and the nanoparticles cytotoxicity were studied. The FTIR, XRD, EDX, SEM and DLS results showed that the nanoparticles synthesized properly with an almost spherical morphology, an average size of 82–93 nm for B-CS/PEC-NPs, an average diameter of below 100 nm (mostly 66–89 nm) for C-CS/PEC-NPs, and hydrodynamic diameter of 310–817 nm. The drug release results indicated the lower release rate of drugs for B-CS/PEC-NPs relative to C-CS/PEC-NPs at different pHs, high release rate of drugs for the nanoparticles in the simulated large intestinal fluids containing pectinase, and Korsmeyer-Peppas model for release of the drugs. The results showed more cytotoxicity of B-CS/PEC-NPs containing drugs, especially B-CS/PEC-NPs containing both drugs (B-CS/PEC/5-FU/SHK-NPs) after treating with pectinase (IC50 of 18.6 μg/mL). In conclusion, despite the limitation of C-CS/PEC-NPs for simultaneous loading of hydrophilic and hydrophobic drugs, B-CS/PEC-NPs showed suitable potency for loading and targeted delivery of the drugs.

Antioxidant activity and cytotoxicity of greigite nanoparticles synthesized by hydrothermal technique.

The effects of 180, 210, and 230°C reaction temperatures on the structural and magnetic properties of synthesized iron sulfide nanoparticles were studied. The Rietveld refinement analysis result of the X-ray diffraction data indicated that greigite was the dominant phase in all samples. The sample was prepared at 210°C for 18h and had a greater wt% ratio of the greigite phase. The crystallite and particle sizes increased with increasing reaction temperatures. Scanning electron microscope images confirmed the presence of aggregation of synthesized rod-shaped nanoparticles. The magnetic hysteresis curves of all samples showed ferromagnetic behavior at room temperature. The magnetic saturation of three samples increases with increased reaction temperature, but the coercive force has the opposite behavior. Antioxidant activity and cytotoxicity of the sample synthesized at 210°C were investigated. This sample killed cancer cells at relatively moderate and high concentrations with high viability of normal cells, demonstrating the sample's suitability for use in killing cancer cells while avoiding normal cells.

Synthesis, modifications, and applications of iron-based nanoparticles.

Magnetic nanoparticles (MNPs) are appealing materials as assistant to resolve environmental pollution issues and as recyclable catalysts for the oxidative degradation of resistant contaminants. Moreover, they can significantly influence the advancement of medical applications for imaging, diagnostics, medication administration, and biosensing. On the other hand, due to unique features, excellent biocompatibility, high curie temperatures and low cytotoxicity of the Iron-based nanoparticles, they have received increasing attention in recent years. Using an external magnetic field, in which the ferrite magnetic nanoparticles (FMNPs) in the reaction mixtures can be easily removed, make them more efficient approach than the conventional method for separating the catalyst particles by centrifugation or filtration. Ferrite magnetic nanoparticles (FMNPs) provide various advantages in food processing, environmental issues, pharmaceutical industry, sample preparation, wastewater management, water purification, illness therapy, identification of disease, tissue engineering, and biosensor creation for healthcare monitoring. Modification of FMNPs with the proper functional groups and surface modification techniques play a significant role in boosting their capability. Due to flexibility of FMNPs in functionalization and synthesis, it is possible to make customized FMNPs that can be utilized in variety of applications. This review focuses on synthesis, modifications, and applications of Iron-based nanoparticles.

Silver nanoparticle-induced cell damage via impaired mtROS-JNK/MnSOD signaling pathway

This study investigated the mechanism of silver nanoparticle (AgNP) cytotoxicity from a mitochondrial perspective. The effect of AgNP on manganese superoxide dismutase (MnSOD), a mitochondrial antioxidant enzyme, against oxidative stress has not been studied in detail. We demonstrated that AgNP decreased MnSOD mRNA level, protein expression, and activity in human Chang liver cells in a time-dependent manner. AgNP induced the production of mitochondrial reactive oxygen species (mtROS), particularly superoxide anion. AgNP was found to increase mitochondrial calcium level and disrupt mitochondrial function, leading to reduced ATP level, succinate dehydrogenase activity, and mitochondrial permeability. AgNP induced cytochrome c release from the mitochondria into the cytoplasm, attenuated the expression of the anti-apoptotic proteins phospho Bcl-2 and Mcl-1, and induced the expression of the pro-apoptotic proteins Bim and Bax. In addition, c-Jun N-terminal kinase (JNK) phosphorylation was significantly increased by AgNP. Treatment with elamipretide (a mitochondria-targeted antioxidant) and SP600125 (a JNK inhibitor) showed the involvement of MnSOD and JNK in these processes. These results indicated that AgNP damaged human Chang liver cells by destroying mitochondrial function through the accumulation of mtROS.

Evaluating antimicrobial activity and cytotoxicity of silver nanoparticles incorporated into reinforced zinc oxide eugenol: an in vitro study.

This study aimed to evaluate the antibacterial and cytotoxic effects of reinforced zinc oxide-eugenol (rZOE) incorporated with different concentrations of silver nanoparticles (AgNPs). The pastes of rZOE alone or mixed with AgNPs at concentrations of 1%, 2%, and 5% of weight were prepared. In vitro antimicrobial activity of prepared materials against Streptococcus (S.) mutans and Lactobacillus (L.) acidophilus were evaluated after 2, 4, and 6h of contact times using direct contact test (DCT) and also following 24h incubation by well-diffusion test (WDT). The cytotoxicity of the tested materials on human dental pulp stem cells was also determined by MTT assay. The DCT demonstrated that the time-dependent reductions of the colony numbers of both bacteria by three different concentrations of AgNPs incorporated into rZOE were equal but steeper than the rZOE alone (P < 0.05). The increases in growth inhibition zones of S. mutans and L. acidophilus were associated with the increasing concentration of AgNPs mixed with rZOE in the WDT; however, statistical analysis did not show any significant differences (P = 0.092). The MTT assay revealed a significantly lower percentage of cell viability after 1day of culture only with the rZOE + AgNP5% in comparison to the rZOE alone (P = 0.011) and the control medium (P = 0.001). Since the antimicrobial activities of three different concentrations of AgNPs incorporated into rZOE were equal and AgNPs had lower toxicity at lower concentrations, using AgNPs at 1% concentration is suggested to be mixed with rZOE.

Phytosynthesis of silver nanoparticles using aqueous sandalwood (Santalum album L.) leaf extract: Divergent effects of SW-AgNPs on proliferating plant and cancer cells.

The biogenic approach for the synthesis of metal nanoparticles provides an efficient eco-friendly alternative to chemical synthesis. This study presents a novel route for the biosynthesis of silver nanoparticles using aqueous sandalwood (SW) leaf extract as a source of reducing and capping agents under mild, room temperature synthesis conditions. The bioreduction of Ag+ to Ago nanoparticles (SW-AgNPs) was accompanied by the appearance of brown color, with surface plasmon resonance peak at 340-360 nm. SEM, TEM and AFM imaging confirm SW-AgNP's spherical shape with size range of 10-32 nm. DLS indicates a hydrodynamic size of 49.53 nm with predominant negative Zeta potential, which can contribute to the stability of the nanoparticles. FTIR analysis indicates involvement of sandalwood leaf derived polyphenols, proteins and lipids in the reduction and capping of SW-AgNPs. XRD determines the face-centered-cubic crystalline structure of SW-AgNPs, which is a key factor affecting biological functions of nanoparticles. This study is novel in using cell culture methodologies to evaluate effects of SW-AgNPs on proliferating cells originating from plants and human cancer. Exposure of groundnut calli cells to SW-AgNPs, resulted in enhanced proliferation leading to over 70% higher calli biomass over control, enhanced defense enzyme activities, and secretion of metabolites implicated in biotic stress resistance (Crotonyl isothiocyanate, Butyrolactone, 2-Hydroxy-gamma-butyrolactone, Maltol) and plant cell proliferation (dl-Threitol). MTT and NRU were performed to determine the cytotoxicity of nanoparticles on human cervical cancer cells. SW-AgNPs specifically inhibited cervical cell lines SiHa (IC50-2.65 ppm) and CaSki (IC50-9.49 ppm), indicating potential use in cancer treatment. The opposing effect of SW-AgNPs on cell proliferation of plant calli (enhanced cell proliferation) and human cancer cell lines (inhibition) are both beneficial and point to potential safe application of SW-AgNPs in plant cell culture, agriculture and in cancer treatment.

Surface Modification of Mesoporous Silica Nanoparticles for Application in Targeted Delivery Systems of Antitumour Drugs.

The problem of tumour therapy has attracted the attention of many researchers for many decades. One of the promising strategies for the development of new dosage forms to improve oncology treatment efficacy and minimise side effects is the development of nanoparticle-based targeted transport systems for anticancer drugs. Among inorganic nanoparticles, mesoporous silica deserves special attention due to its outstanding surface properties and drug-loading capability. This review analyses the various factors affecting the cytotoxicity, cellular uptake, and biocompatibility of mesoporous silica nanoparticles (MSNs), constituting a key aspect in the development of safe and effective drug delivery systems. Special attention is paid to technological approaches to chemically modifying MSNs to alter their surface properties. The stimuli that regulate drug release from nanoparticles are also discussed, contributing to the effective control of the delivery process in the body. The findings emphasise the importance of modifying MSNs with different surface functional groups, bio-recognisable molecules, and polymers for their potential use in anticancer drug delivery systems.

Volatile carbonyl metabolites analysis of nanoparticle exposed lung cells in an organ-on-a-chip system

The evaluation of nanoparticles (NPs) cytotoxicity is crucial for advancing nanotechnology and assessing environmental pollution. However, existing methods for NPs cytotoxicity evaluation suffer from limited accuracy and inadequate information content. In the study, we developed a novel detection platform that enables the identification of cellular carbonyl metabolites at the organ level. The platform is integrated with a cell co-culture lung organ chip (LOC) and a micropillar concentrator. Notably, our work represents the successful measurement of the amounts of cellular metabolites on LOC system. The volatile carbonyl metabolites (VCMs) generated by cells exposure to various types of NPs with different concentrations were captured and detected by high-resolution mass spectrometry (MS). Compared with conventional cell viability and reactive oxygen species (ROS) analysis, our method discerns the toxicological impact of NPs at low concentrations by analyzed VCM at levels as low as ppb level. The LOC system based metabolic gas detection confirmed that low concentrations of NPs have a toxic effect on the cell model, which was not reflected in the fluorescence detection, and the effect of NP material is more significant than the size effect. Furthermore, this method can distinguish different NPs acting on cell models through cluster analysis of multiple VCMs.

511 Iron Oxide Nanoplatform HMC-FMX for Targeted Chemotherapeutic Treatment of Glioblastoma

INTRODUCTION: Glioblastoma multiforme (GBM), is the most common and aggressive form of primary brain tumors in adults with a high mortality rate. Despite the emergence of potent chemotherapies, clinical efficacy has been limited in part due to the blood-brain barrier (BBB). Therefore, recurrence rate is high, limiting life expectancy. Our nanoplatform is based on ferumoxytol (FMX), an FDA-approved MRI-sensitive supramagnetic iron oxide nanoparticle conjugated to heptamethine cyanine (HMC), a near infrared-flourescent ligand that specifically targets organic anion transporter polypeptides (OATP) expressed in GBM and endothelial cells. METHODS: To show the specificity of OATP-targeting by HMC-FMX nanoplatform, cells were pre-incubated with OATP inhibitors and then incubated with HMC-FMX. Fluorescent intensity and HMC uptake were assesed by flow cytometry. Cytotoxicity of the drug-loaded nanoparticles, HMC-FMX(SN38) and HMC-FMX(CPT) compared to SN38 and Camptothecin (CPT) in U87 cells was assessed by flow cytometry following cell staining with Annexin and 7-AAD. RESULTS: The HMC-FMX nanoplatform is successfully taken up by both U87 and endothelial cells. OATP inhibition significantly decreased HMC uptake (10%-30%) in comparison to control in U87 and endothelial cells. In addition, HMC-FMX(SN38) and HMC-FMX(CPT) exerted increased cytotoxic effect on U87 cells compared with SN38 and CPT alone. Furthermore, majority of apoptotic cells were observed in the HMC-positive cells in contrast to HMC-negative cells. CONCLUSIONS: HMC-FMX can encapsulate chemotherapeutic drugs, such as SN38 and CPT. HMC-FMX as a nanoplatform demonstrates specific, safe and efficient drug delivery through the BBB into GBM cells in vitro.

Enhanced efficacy of β-carotene loaded solid lipid nanoparticles optimized and developed via central composite design on breast cancer cell lines

β-carotene is obtained from both plants and animals and has been the subject of intense research because of its provitamin-A, antioxidant, and anticancer effects. Its limited absorption and oxidative degradation significantly reduce its antitumor efficacy when taken orally. In our study, we utilize a central composite design to develop “bio-safe and highly bio-compatible” solid lipid nanoparticles (SLNs) by using only the combination of palmitic acid and poloxamer-407, a block co-polymer as a surfactant. The current research aim to develop and characterize SLNs loaded with β-carotene to improve their bioavailability and therapeutic efficacy. In addition, the improved cytotoxicity of solid lipid nanoparticles loaded with β-carotene was screened in-vitro in human breast cancer cell lines (MCF-7). The nanoparticles exhibits good stability, as indicated by their mean zeta potential of −26.3 ± 1.3 mV. The particles demonstrated high drug loading and entrapment capabilities. The fabricated nanoparticle's prolonged release potential was shown by the in-vitro release kinetics, which showed a first-order release pattern that adhered to the Higuchi model and showed a slow, linear, and steady release over 48 h. Moreover, a diffusion-type release mechanism was used to liberate β-carotene from the nanoparticles. For six months, the nanoparticles also showed a notable degree of physical stability. Lastly, using the MTT assay, the anti-cancer properties of β-carotene-loaded solid lipid nanoparticles were compared with intact β-carotene on MCF-7 cell lines. The cytotoxicity tests have shown that the encapsulation of β-carotene in the lipid bilayers of the optimized formulation does not interfere with the anti-cancer activity of the drug. When compared to standard β-carotene, β-carotene loaded SLNs showed enhanced anticancer efficacy and it is a plausible therapeutic candidate for enhancing the solubility of water-insoluble and degradation-sensitive biotherapeutics like β-carotene.

Investigation of Antimicrobial Activity and Cytotoxicity of Silver Nanoparticle Synthesized using Dopamine as a Reducing and Capping Agent

AbstractWe present a study focused on the controlled fabrication of silver nanoparticles (AgNPs) through colloidal synthesis, employing dopamine as a reducing and capping agent. By manipulating the concentration of silver nitrate, the production of spherical AgNPs with distinct particle diameters (16, 24, 48, and 74 nm) was achieved. The investigation extended to the evaluation of AgNPs′ impact on human embryonic kidney cells, revealing a concentration‐dependent response. At lower AgNPs concentrations, cell viability remained nearly 100 %, progressively declining with rising AgNPs concentrations. Importantly, the cytotoxic thresholds observed were notably elevated, underscoring the relatively mild to moderate toxicity profile of the nanoparticles. Furthermore, the antimicrobial efficacy of these synthesized AgNPs was probed against E. coli and S. aureus bacterial strains. Notably, the AgNPs exhibited robust antimicrobial activity, with superior performance exhibited by smaller‐sized particles compared to larger ones. Impressively, the minimum inhibitory concentration reached as low as 3.5 μg/mL, indicating their potent antimicrobial potential. The achieved distinct particle diameters, concentration‐dependent cytotoxic responses, and potent antimicrobial efficacy against bacterial strains underscore the multifaceted potential of these nanoparticles. These findings contribute valuable insights for their application in diverse fields, from biomedicine to antimicrobial solutions.

Polymeric Propranolol Nanoparticles for Intraocular Delivery: Formulation, Characterization, and Vitreous Pharmacokinetics.

Recent studies have reported the promising effect of intravitreal propranolol on retinal neovascularization. However, rapid clearance and short half-life of the drug in the vitreous are the main drawbacks of this therapeutic approach. This study investigates the extension of the residence time of propranolol in the vitreous by polymeric nanoparticles (NPs) with the prospect of improving choroidal neovascularization treatment. The poly (lactic-co-glycolic) acid (PLGA) NPs were fabricated by a modified double emulsion solvent evaporation method and the obtained NPs were characterized for their size, poly dispersity index (PDI), and surface image. The in vitro release, cell cytotoxicity, and uptake of NPs were also evaluated. To investigate the effect of the vitreous pharmacokinetic drug loaded NPs versus that of the free propranolol, they were intravitreally injected into the rabbits' eyes and the drug vitreous concentrations in defined intervals were analyzed by high performance liquid chromatography (HPLC). The spherical NPs with about 230 nm size, and almost 10% drug loading were obtained. Based on the 3-(4, 5-Dimethylthiazol-2-Yl)-2, 5-Diphenyltetrazolium Bromide (MTT) outcomes, 30 µg/ml of propranolol was considered as the guide dosage in the intravitreal injection. Confocal microscopy images verified the presence of labeled NPs in the posterior segment after five days of receiving the injection. In vivo assay revealed that the vanishing rate of propranolol in rabbits treated with propranolol NPs was reduced at twice the rate as compared to that of the vanishing rate experienced with only the free drug. PLGA NPs can prolong the existence of propranolol in both vitreous and posterior ocular tissues, and thus, may provide an effective approach in treatment of posterior segment neovascularization.

Low-Toxicity Self-Photosensitized Biohybrid Systems for Enhanced Light-Driven H2 Production.

Nanoparticles (NPs) represent a potential optoelectronic source capable of significantly boosting hydrogen production; however, their inevitable cytotoxicity may lead to oxidative damage of bacterial cell membranes. In this study, we employed non-photosynthetic Escherichia coli K-12 as a model organism and utilized self-assembled cadmium sulfide (CdS) nanoparticles to construct a low-toxicity and hydrogen-production-enhancing self-photosensitive hybrid system. To mitigate the cytotoxicity of CdS NPs and synthesize biocompatible CdS NPs on the cell surface, we employed engineered E. coli (efeB/OE) for bioremediation, achieving this goal through the overexpression of the peroxidase enzyme (EfeB). A comparative analysis with E. coli-CdS revealed a significant downregulation of genes encoding oxidative stress proteins in efeB/OE-CdS post-irradiation. Atomic force microscopy (AFM) confirmed the stability of bacterial cell membranes. Due to the enhanced stability of the cell membrane, the hydrogen yield of the efeB/OE-CdS system increased by 1.3 times compared to the control, accompanied by a 49.1% reduction in malondialdehyde (MDA) content. This study proposes an effective strategy to alleviate the toxicity of mixed biological nanoparticle systems and efficiently harness optoelectronic electrons, thereby achieving higher hydrogen production in bioremediation.

Characterization, cytotoxicity and anti-human renal cell carcinoma efficacies of copper nanoparticles green-synthesized by Panax ginseng

A recent study was undertaken to investigate the possible cytotoxic effects of copper nanoparticles (CuNPs) that include an aqueous extract of Panax ginseng on various human renal cell carcinoma cell lines, namely HEK293, CaKi-2, RCC-GH, and RCC-JW (KTCTL-195) for the first time. The identification of these nanoparticles was carried out using different techniques. To evaluate the potential anti-human renal cell carcinoma properties of the synthesized NPs, a 2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was conducted. Additionally, the 2,2-Diphenyl-1-picrylhydrazyl (DPPH) assay was conducted to investigate the antioxidant efficacy. The peaks observed at 3398, 2918, 1617, and 1015 cm−1 in the secondary metabolites of the P. ginseng extract corresponded to the functional groups of O–H, C–H, C = O, C = C, and C-O, respectively. The X-ray powder diffraction (XRD) results revealed that the CuNPs had a CuO formula and exhibited a spherical morphology with a size of less than 80 nm, as observed in the FE-SEM image. To assess the anti-renal cell carcinoma efficacy of CuNPs, an MTT assay was performed on HUVEC, HEK293, CaKi-2, RCC-GH, and RCC-JW (KTCTL-195) cells. Notably, CuNPs exhibited high anti-renal cell carcinoma efficacy on the aforementioned tumor cells. The IC50 values of CuNPs were found to be 102, 149, 178 and 191 µg/mL on HEK293, CaKi-2, RCC-GH, and RCC-JW (KTCTL-195) cells, respectively. The results of this study revealed significant anti-renal cell carcinoma and antioxidant efficacies of CuNPs.

The efficacy of ZnO-NPs prepared via green route against colon and breast cancer cells

This study is an attempt to utilize green tea [GT] extract and pomegranate peel [PP] for the synthesis of zinc oxide nanoparticles. The selected plants are rich in phenols therefore are awaited to successfully synthesize ZnO nanoparticles without the need for an alkylating agent. In addition, these extracts contain various functional groups that confer colloidal stability for nanoparticles and ameliorate their biocompatibility via a one pot synthesis route. X-ray diffraction analysis (XRD), and transmission electron microscopy (TEM) techniques are used to investigate both structural and morphological properties of the obtained nanoparticles [Zn-GT and Zn-PP]. To confirm the presence of functional groups adsorbed on the surface of biogenic-NPs, Fourier transform infrared spectroscopy (FTIR) and thermogravimetric analysis (TGA) were employed. The outcomes demonstrated that only the use of green tea extract was successful in synthesizing zinc oxide from the zinc acetate dihydrate precursor, producing particles with an average size of approximately 25 nm. Anticancer activity and cytotoxicity of the biosynthesized Zn-GT nanoparticles were assessed against human breast cancer [MCF7] and colorectal carcinoma [HCT116] cell lines. The cytotoxicity of ZnO nanoparticles is presented with reference to normal skin [BJ1] cell line subjected to similar concentrations of the NPs. The obtained results verified a discriminative inhibition of both MCF7 and HCT116 cancer cell growth upon using Zn-GT, which completely succeeded in preventing cancer cell growth.

Plant mediated biosynthesis of Mn3O4 nanostructures and their biomedical applications

Nanomaterials have drawn significant attention for their biomedical and pharmaceutical applications. In the present study, manganese tetra oxide (Mn3O4) nanoparticles were prepared greenly, and their physicochemical properties were studied. Taxus baccata acetone extract was used as a safely novel precursor for reducing and stabilizing nanoparticles. The synthesized nanoparticles were characterized by transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDS), Brunauer–Emmett–Teller (BET), and Barrett-Joyner-Halenda (BJH) and X-ray diffraction (XRD). The cytotoxicity of Mn3O4 (hausmannite) nanostructures was evaluated against murine macrophage cell line J774-A1 and U87 glioblastoma cancer cells for approximately 72 h. Spherical Mn3O4 nanoparticles with tetragonal spinel structures demonstrated minimal toxicity against normal body cells with CC50 around 876.38 μg mL−1. Moreover, Mn3O4 nanoparticles as well as the combination of antimoniate meglumine and Mn3O4 nanoparticles exhibited maximum mortality in Leishmania major. The synthesized nanominerals displayed a significant inhibitory effect against glioblastoma cancer cells at 100 μg mL−1. The selective cytotoxicity of Mn3O4 nanoparticles indicates that these biogenic agents can be employed simultaneously for diagnostic and therapeutic applications in medical applications.

Influence of Different Ratios of DSPE-PEG2k on Ester Prodrug Self-Assembly Nanoparticles for Cell Migration and Proliferation Suppression.

Bufalin (BFL, an active anti-tumor compound derived from toad venom) is limited in its application due to high toxicity and rapid metabolism of the cardiotonic steroid. Ester prodrug self-assembly nanoparticles have shown significant improved effects in addressing the above-mentioned issues. An ester bond was formed between linoleic acid and bufalin to synthesize linoleic acid-bufalin prodrug (LeB). The self-assembly nanoparticles (LeB-PSNs) containing different mass ratios of DSPE-PEG2k and prodrug (6:4, 7:3, 8:2, 9:1 and 10:0) were prepared via co-precipitation method and defined as 6:4-PSNs, 7:3-PSNs, 8:2-PSNs, 9:1-PSNs and LeB-PSNs, respectively. Further, the characterization (particle size, zeta potential, surface morphology and stability) of the nanoparticles was carried out. Finally, we evaluated the impact of different ratios of DSPE-PEG2k on the hydrolysis rate, cytotoxicity, cellular uptake, cell migration and proliferation suppression potential of the prodrug nanoparticles. The linoleic acid-bufalin prodrug (LeB) was successfully synthesized. Upon the addition of DSPE-PEG2k at different weight ratios, both particle size and polydispersity index (PDI) significantly decreased, while the zeta potential increased remarkably. No significant differences in particle size, PDI and Zeta potential were observed among the 9:1, 8:2 and 7:3 PSNs. Notably, the 8:2 (w/w) DSPE-PEG2k nanoparticles exhibited superior stability, hydrolysis and cellular uptake rates, along with efficient cell cytotoxicity, cell migration and proliferation suppression. These findings indicate that DSPE-PEG2k could improve the performance of BFL prodrug nanoparticles, namely enhancing stability and achieving adaptive drug release by modulating the hydrolysis rate of esterase. This study therefore provides more opportunities for the development of BFL application.

Assessment of Anti-inflammatory, Antimicrobial and Cytotoxicity of Chitosan-Moringa Composite and Calcium Hydroxide Nanoparticles as an intra-canal medicament in vitro

In this study Chitosan nanoparticles was characterized usingUV spectrophotometry, FT-IR, Transmission electron microscopy, and X-Ray diffraction. The composition of Moringa oleifera of ethanolic extract was analyzed using GC-Mass.The antimicrobial, anti-inflammatory, and cytotoxicity of Chitosan-Moringa composite, H2CaO2 nanoparticles, Ca(OH)2, and Moringa oleifera of ethanol extract as an intra-canal medicament in vitro were also investigated. Results of our research summarized that; The UV of chitosan nanoparticles range from 280 to 300 nm. The FT-IR results confirm the presence of a broad and powerful band at 3442 cm1, 1636 cm1, and 1052 cm1 all band confirm the presence of the native chitosan. The X-Ray diffraction proved three strong characteristic peaks indicating crystallinity of chitosan nanoparticles chains. The TEM of Chitosan nanoparticles size was between 76.61 – 126.91nm and the shape was less spherical with slightly wrinkled surface. The major chemical compounds in Moringa ethanol extract by GC-Mass were detected. Also, the antimicrobial activity of Moringa extracts proved that ethanol extract had the highest zone of inhibition. The antimicrobial activity of Moringa-chitosan composite had the highest antimicrobial activity followed by H2CaO2 nanoparticles against dental pathogens. The anti-inflammatory effects on HRBC hemolysis at concentration 100μg/mL Ca (OH)2 gave the best lower production than the positive control Stander Indo meth followed by H2CaO2 nanoparticles, Moringa ethanol extract, and finally Chitosan-Moringa composite. The MTT assay against OEC have been showed that, Ca (OH)2 is the most cytotoxic with the lowest IC50 followed by Moringa ethanol extract, Chitosan-Moringa composite, and finally H2CaO2 nanoparticles.

Environmentally benign preparation of copper oxide nanoparticles and its potential biological and photocatalytic activities

The study reports environment friendly facile preparation of multi-functional CuO nanoparticles using Kiwi fruit and assesses its photocatalytic and a variety of biological activities. The PXRD pattern demonstrates that the nanoparticles were members of the pure monoclinic structure with particles having sizes from 8 to 10 nm. They were found to exhibit a porous and sponge-like morphology with almost spherical shape, as seen by TEM and SEM pictures. The peak centered at 608 cm−1 was caused by stretching of Cu–O in FTIR spectrum. The nanoparticles found to possess high photocatalytic degradation activity towards model dye such as methylene blue. The nanoparticles exhibit various potential biological activities. It efficiently suppresses the 1,1-Dipheny-2-picrylhydrazyl (DPPH) free radical activity. It has antibacterial efficacy against pathogenic bacterial strains such as Escherichia coli and Staphylococcus aureus. CuO nanoparticles were investigated for anti-diabetic activity, and they demonstrated excellent α-glucosidase (IC50 of 183 ± 9 μg/ml) and α-amylase (IC50 of 124 ± 6 μg/ml) inhibition effects. The MTT test was used to examine the cytotoxicity of CuO nanoparticles on the HeLa cell line, which showed dose-dependent activity with IC50 value of 303 ± 15 μg/ml, which indicate that they were significantly cytotoxic. Copper oxide nanoparticles improved platelet aggregation and plasma coagulation without exhibiting hemolytic activity. This study demonstrates a quick, simple, low-cost, facile, environmentally benign green synthetic approach for large-scale synthesis of multifunctional CuO nanoparticles.

Coarse‐Grained Model‐Assisted Design of Polymer Prodrug Nanoparticles with Enhanced Cytotoxicity: A Combined Theoretical and Experimental Study

AbstractTo achieve drug release from polymer prodrug nanoparticles, the drug‐polymer linker must be accessible for cleavage to release the drug, which can occur under certain physiological conditions (e.g., presence of specific enzymes). Supramolecular organization of polymer prodrug nanoparticles is crucial as it greatly affects the location of the linker, its surface exposure/solvation and thus its cleavage to release the drug. Since experimental access to these data is not straightforward, new methodologies are critically needed to access this information and to accelerate the development of more effective polymer prodrug nanoparticles, and replace the time‐consuming and resource‐intensive traditional trial‐and‐error strategy. In this context, we reported here the use of a coarse‐grained model to assist the design of polymer prodrug nanoparticles with enhanced cytotoxicity. By choosing the solvent accessible surface area as the critical parameter for predicting drug release and hence cytotoxicity of polymer prodrug nanoparticles, we developed an optimized polymer‐drug linker with enhanced hydrophilicity and solvation. Our hypothesis was then experimentally validated by the synthesis of the corresponding polymer prodrugs based on two different drugs (gemcitabine and paclitaxel), which demonstrated greater performances in terms of drug release and cytotoxicity on two cancer cell lines. Interestingly, our methodology can be easily applied to other polymer prodrug structures, which would contribute to the development of more efficient drug delivery systems via in silico screening.