Cyanoacrylate Nanoparticles Research Articles

Blood-Nanoparticle Interactions Create a Brain Delivery Superhighway for Doxorubicin.

This study investigated the brain targeting mechanism of doxorubicin-loaded polybutyl cyanoacrylate (PBCA) nanoparticles, particularly their interactions with the blood-brain barrier (BBB). The BBB protects the brain from drugs in the bloodstream and represents a crucial obstacle in the treatment of brain cancer. An advanced computer model analyzed the brain delivery of two distinct formulations, Doxil® and surfactant-coated PBCA nanoparticles. Computational learning was combined with in vitro release and cell interaction studies to comprehend the underlying brain delivery pathways. Our analysis yielded a surprising discovery regarding the brain delivery mechanism of PBCA nanoparticles. While Doxil® exhibited the expected behavior, accumulating in the brain through extravasation in tumor tissue, PBCA nanoparticles employed a unique and previously uncharacterized mechanism. They underwent cell hitchhiking, resulting in a remarkable more than 1000-fold increase in brain permeation rate compared to Doxil® (2.59 × 10-4 vs 0.32 h-1). The nonspecific binding to blood cells facilitated and intensified interactions of surfactant-coated PBCA nanoparticles with the vascular endothelium, leading to enhanced transcytosis. Consequently, the significant increase in circulation time in the bloodstream, coupled with improved receptor interactions, contributes to this remarkable uptake of doxorubicin into the brain.

In Vitro Efficacy of Isobutyl Cyanoacrylate Nanoparticles against Fish Bacterial Pathogens and Selection Preference by Rainbow Trout (Oncorhynchus mykiss).

The upsurge in havoc being wreaked by antibiotic-resistant bacteria has led to an urgent need for efficacious alternatives to antibiotics. This study assessed the antibacterial efficacy of two isobutyl cyanoacrylate nanoparticles (iBCA-NPs), D6O and NP30, against major bacterial pathogens of fish. In vivo tests on rainbow trout were preceded by in vitro tests of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). NP30 exhibited higher efficacy than D60, but both iBCA-NPs demonstrated dose-dependent and species-specific in vitro antibacterial properties against the bacterial isolates. Generally, Gram-negative bacteria were more resistant to the iBCA-NPs. Streptococcus iniae, Tenacibaculum maritimum, and Photobacterium damselae were particularly sensitive to both iBCA-NPs. Administered to rainbow trout at 3571.4 mg (iBCA-NP)/kg feed, the iBCA-NPs produced a relative gain rate and survival rates comparable to the control (p > 0.05). The condition factor and the hepatosomatic and viscerosomatic indices of fish were indifferentiable (p > 0.05) between the iBCA-NP groups and the control. The iBCA-NPs caused no alteration in stress, oxidative stress (superoxide dismutase, SOD), plasma complement titer, or lysozyme activity. This study presents the first report of antibacterial activity of iBCA-NPs against Gram-negative bacteria. The results of this study suggest that D60 and NP30 may contribute to reducing the amounts of antibiotics and chemotherapeutic agents used in aquaculture.

Development of levan-coated PIBCA nanoparticles and their antiproliferative activity against MDA-MB-231 and B16F10 cells

Polysaccharides have been described as a successful alternative in developing nanosystems to reach specific sites. Levan is an exopolysaccharide with several biological activities, including immunostimulant, blood plasma substitute, and drug action prolonging agent. The present work aimed to develop poly-isobutyl cyanoacrylate (PIBCA) nanoparticles coated levan (Np-Lev) and to verify its cytotoxicity in two cancer cell lines. Levan was obtained through the fermentation of ZAG 12 Zymomonas mobilis. The nanoparticles were prepared using the anionic emulsion polymerization technique and characterized in size, zeta potential, morphological analysis, X-ray diffraction, infrared spectroscopy, and thermogravimetric analysis. The cell lines MDA-MB-231 (metastatic breast cancer cells) and B16F10 (melanoma cells) were used to evaluate the antiproliferative activity and cellular uptake of Np-Lev. The technique of obtaining the levan allowed a higher yield than the reference methodology, achieving 71.4% more. The novel nanoparticles (Np-Lev) presented spherical shapes, size of 244 ± 2 nm with homogeneous distribution and zeta potential of −12 ± 1 mV. Characterization techniques, such as infrared spectroscopy and X-ray diffraction, confirmed the presence of levan in the nanoparticles. The thermogravimetric analysis results showed greater thermal resistance when compared to free levan. In addition, Np-Lev were more cytotoxic than levan in both cell lines. This toxicity may be related to the internalization of nanoparticles inside the cells since Np-Lev were captured by the cells, which could increase the activity of levan cytotoxicity. Thus, it was verified a substantial increase in levan yield, also that the levan produced could be used to prepare PIBCA nanoparticles, and finally these Np-Lev showed antiproliferative activity against breast cancer and melanoma cell lines. The results exposed here are of interest to explore levan potential, in addition to nanotechnology, as a promising nanosystem with various biological applications. Further studies are needed to understand the biological behavior of nanoparticles and assess their stability for future therapeutic application.

Comparable antibacterial effects and action mechanisms of ethyl cyanoacrylate nanoparticles on Bacillus subtilis and Escherichia coli evaluated by transcriptome and morphological changes

We previously demonstrated that ethyl cyanoacrylate nanoparticles (ECA-NPs) inhibit the growth specific rate of B. subtilis and E. coli under culture conditions, indicating their antibacterial effect.

Evaluation of the Growth-Inhibitory Spectrum of Three Types of Cyanoacrylate Nanoparticles on Gram-Positive and Gram-Negative Bacteria.

The development of novel effective antibacterial agents is crucial due to increasing antibiotic resistance in various bacteria. Poly (alkyl cyanoacrylate) nanoparticles (PACA-NPs) are promising novel antibacterial agents as they have shown antibacterial activity against several Gram-positive and Gram-negative bacteria. However, the antibacterial mechanism remains unclear. Here, we compared the antibacterial efficacy of ethyl cyanoacrylate nanoparticles (ECA-NPs), isobutyl cyanoacrylate NPs (iBCA-NPs), and ethoxyethyl cyanoacrylate NPs (EECA-NPs) using five Gram-positive and five Gram-negative bacteria. Among these resin nanoparticles, ECA-NPs showed the highest growth inhibitory effect against all the examined bacterial species, and this effect was higher against Gram-positive bacteria than Gram-negative. While iBCA-NP could inhibit the cell growth only in two Gram-positive bacteria, i.e., Bacillus subtilis and Staphylococcus aureus, it had negligible inhibitory effect against all five Gram-negative bacteria examined. Irrespective of the differences in growth inhibition induced by these three NPs, N-acetyl-L-cysteine (NAC), a well-known reactive oxygen species (ROS) scavenger, efficiently restored growth in all the bacterial strains to that similar to untreated cells. This strongly suggests that the exposure to NPs generates ROS, which mainly induces cell growth inhibition irrespective of the difference in bacterial species and cyanoacrylate NPs used.

Targeted Propolis-Loaded Poly (Butyl) Cyanoacrylate Nanoparticles: An Alternative Drug Delivery Tool for the Treatment of Cryptococcal Meningitis.

In this study, we describe a nano-carrier system for propolis that is able to cross an in vitro model of the blood-brain barrier (BBB) and effectively reduce the virulence of Cryptococcus neoformans in animal models. Antimicrobial properties of propolis have been widely studied. However, propolis applications are limited by its low water solubility and poor bioavailability. Therefore, we recently formulated novel poly (n-butyl cyanoacrylate) nanoparticles (PBCA-NP) containing propolis. PBCA-NP are biocompatible, biodegradable and have been shown to effectively cross the BBB using apolipoprotein E (ApoE) as a ligand. Prepared nanoparticles were characterized for particle size, zeta potential, propolis entrapment efficiency and in vitro release. Additionally, the PBCA-NP were functionalized with polysorbate 80, which then specifically adsorbs ApoE. Using an in vitro BBB model of human brain microvascular endothelial cells hCMEC/D3, it was shown that fluorescence labelled ApoE-functionalized PBCA-NP were internalized by the cells and translocated across the cell monolayer. Propolis-loaded PBCA-NP had in vitro, antifungal activity against C. neoformans, which causes meningitis. To utilize the invertebrate model, Galleria mellonella larvae were infected with C. neoformans and treated with propolis-loaded PBCA-NP. The larvae exhibited normal behavior in toxicity testing, and treatment with propolis-loaded PBCA-NP increased survival in the C. neoformans-infected larvae group. In addition, following cryptococcal infection and then 7 days of treatment, the tissue fungal burden of mice treated with propolis-loaded PBCA-NP was significantly lower than control groups. Therefore, our ApoE-functionalized propolis-loaded PBCA-NP can be deemed as a potential targeted nanoparticle in the therapeutic treatment of cerebral cryptococcosis.

Tumor-Targeted Delivery of Bufalin-Loaded Modified Albumin-Polymer Hybrid for Enhanced Antitumor Therapy and Attenuated Hemolysis Toxicity and Cardiotoxicity.

A novel albumin polymer hybrid with a core-shell structure was designed to target delivery of bufalin, which is an antineoplastic monomer with serious cardiotoxicity. The sheath layer was composed of ursodeoxycholic acid (UA)-modified bovine serum albumin (UA-BSA), while the stable core consisted of poly n-butyl cyanoacrylate (PBCA) nanoparticles. The UA-BSA was synthetized, and the substitution degree was characterized. The physical properties of bufalin-loaded UA-modified protein-PBCA nanocomplexes (BF-uPPNCs), such as morphology, particle size, and encapsulation efficiency, were evaluated. FTIR and DSC revealed the bufalin to be in an amorphous state. Furthermore, the in vitro release study indicated a sustained release profile of BF-uPPNCs. The MTT and cellular uptake study demonstrated that BF-uPPNCs significantly improved the inhibitory effect of the bufalin accompanied with an enhanced cell uptake capacity on HepG2 cells. In addition, in vivo research demonstrated that BF-uPPNCs had a better antitumor effect coupled with improved therapeutic effect, and reduced hemolysis, vascular irritation, and cardiotoxicity. This work therefore presented a novel albumin polymer hybrid with favorable stability, efficient tumor-targeted delivery potential, and side effect reduction ability, which can be a potential vehicle for an anticancer drug.

Docetaxel-Loaded Cholesterol-PEG Co-Modified Poly (n-Butyl) Cyanoacrylate Nanoparticles for Antitumor Drug Pulmonary Delivery: Preparation, Characterization, and in vivo Evaluation.

Background and AimPolymeric nanoparticles (NPs) have received much attention as promising carrier systems in lung cancer and brain metastases.MethodsHere, for the first time, we investigated the feasibility of using inhaled cholesterol-PEG co-modified poly (n-butyl) cyanoacrylate NPs (CLS-PEG NPs) of docetaxel (DTX) for sustained pulmonary drug delivery in cancer metastasis.ResultsSpray-dried or freeze-dried NPs yielded sustained drug release in vitro. In vitro inhalation evaluation data indicated that the inhalation formulation had better inhalability. Compared with intravenous (IV) administration, pharmacokinetic data suggested that the inhalation formulation prolonged plasma concentration of DTX for greater than 24 h and is more quickly and completely absorbed into the rat lung after intratracheal (IT) administration. Furthermore, freeze-dried powders were found to increase the t1/2 and area under curve (AUC) by 2.3 and 6.5 fold compared to the free drug after IT administration, and spray-dried powders were found to increase the t1/2 and AUC by 3.4 and 8.8 fold, respectively. After pulmonary administration of the inhalation formulation, DTX appeared to prolong the pulmonary absorption time. In addition, the inhalation formulation was distributed to the brain in a sustained release manner.ConclusionThese experimental results demonstrated that freeze- and spray-dried powders have the potential for pulmonary sustained release, and they also have the potential to be used as a novel treatment for the delivery of drugs that pass through the air–blood barrier and enter the brain and are efficient carriers for the treatment of brain metastasis.

Deregulation of BCL2 family genes in glioblastoma cells consequent to poly(butyl cyanoacrylate) nanoparticles treatment

Brain tumours develop resistance to chemotherapy mainly due to the presence of the blood brain barrier which partially blocks the penetration of drugs into the brain. Poly(butyl cyanoacrylate) nanoparticles have been extensively proposed for delivering drugs into the brain and have shown their ability to cross the blood brain barrier in vitro and in vivo. However, the application of nanoparticles could be limited by their potential side effects. In this study, two glioblastoma cell lines with the poly(butyl cyanoacrylate) nanoparticles were treated at different concentrations. Through MTT assay, the viability of treated cells was quantified. Induction of apoptosis was analysed by flowcytometry as well as quantitative PCR assay for the expression of BCL2 family genes. The results of this study showed that the treatment with poly(butyl cyanoacrylate) nanoparticles induced neither apoptosis nor necrosis in these cells. The quantitative real-time PCR results showed that poly(butyl cyanoacrylate) nanoparticles treatment caused significant changes in the expression of some BCL2 family members. In conclusion, it seems that poly(butyl cyanoacrylate) nanoparticles treatment at non-toxic dose can change the expression of some apoptosis-related genes in glioblastoma cells while has no significant effect on their viability.

Preparation, intestinal segment stability, and mucoadhesion properties of novel thymopentin-loaded chitosan derivatives coated with poly (n-butyl) cyanoacrylate nanoparticles.

BackgroundIn order to develop a promising carrier for the oral delivery of proteins and peptide drugs, a novel bioadhesive nanocarrier of chitosan (CTS) derivatives coated with poly (n-butyl) cyanoacrylate nanoparticles (PBCA-NPs) was prepared in this study.MethodsThree different thymopentin (TP5)-loaded nanoparticles were prepared in the present study. TP5-PBCA-NPs were developed by modifying an emulsion polymerization method, and CTS and chitosan–glutathione (CG) derivative-coated PBCA nanoparticles were obtained from the electrostatic interactions between CTS or CG with negatively charged PBCA nanoparticles.ResultsThe particle sizes of TP5-PBCA-NPs, TP5-CTS-PBCA-NPs, and TP5-CG-PBCA-NPs were 212.3±6.9, 274.6±8.2, and 310.4±7.5 nm, respectively, while the respective zeta potentials were −22.6±0.76, 23.3±1.2, and 34.6±1.6 mV with encapsulation efficiencies of 79.37%±2.15%, 74.21%±2.13%, and 72.65%±1.48%, respectively. An everted intestinal ring method indicated that drug stability was remarkably improved after incorporation into the nanoparticles, especially the CG-coated nanoparticles. The mucus layer retention rates for CTS- and CG-coated nanoparticles were 1.43 and 1.83 times that of the uncoated nanoparticles, respectively, using ex vivo mucosa. The in vivo mucoadhesion study illustrated that the transfer of uncoated PBCA-NPs from the stomach to the intestine was faster than that of CTS-PBCA-NPs and CG-PBCA-NPs, while the CG-PBCA-NPs presented the best intestinal retentive characteristic.ConclusionIn summary, this study demonstrated the feasibility and benefit of orally delivering peptide drugs using novel CTS derivative-coated nanoparticles with optimal stability and bioadhesive properties.

Research and development of 2-ethyl-6-methyl-3-oxypyridine succinate nano-form for the treatment of epilepsy

The aimis to develop an antiepileptic drug based on polymer nanoparticles with 2-ethyl-6-methyl-3-oxypyridine succinate to facilitate the drug transport through the blood-brain barrier.Materials and methods.The nano-drug was created using the biologically active substance 2-ethyl-6-methyl-3-hydroxypyridine succinate and polybutyl cyanoacrylate (PBCA) nanoparticles. The advantages of this nano-form over the active ingredient of the same drug were studied using experimental models: the maximum electroshock test (MES), the antagonism test with corazol, models with a cobaltinduced epileptic focus and secondary generalized convulsions, and models of status epilepticus.Results.The antiseizure effects of the nanoform on the experimental models of epilepsy are identified.Conclusion.The nano-drug reduces the number of secondary generalized clonic-tonic seizures by 7.8 times; it also reduces 10-fold the animal mortality and diminishes the seizure manifestations that occur in the interictal period of the epileptic status.

Effects of phospholipid and polyethylene glycol monostearate (100) on the in vitro and in vivo physico-chemical characterization of poly(n-butyl cyanoacrylate) nanoparticles.

In this study, poly(n-butyl cyanoacrylate) nanoparticles (PBCA-NPs) modified with various amounts of soybean phospholipid (PC) and polyethylene glycol monostearate (S100) were prepared in order to investigate the effects of PC and S100 on the nanoparticles' physico-chemical properties, cytological properties and in vivo gastrointestinal absorption. Coumarin-6 (C6) was used as a fluorescent probe; C6-loaded PBCA-NPs modified with both PC and S100 (C6-PS-PBCA-NPs) were prepared using miniemulsion polymerization, and C6-loaded PBCA-NPs modified with either S100 (C6-S-PBCA-NPs) or PC (C6-P-PBCA-NPs) were used as references. All of the different NPs were shown to be stably dispersed and to have a small particle size. A cytotoxicity study indicated that all of the blank PBCA-NPs were safe and nontoxic. The uptake of NPs by Caco-2 cells was shown to be increased when the amount of PC was increased from 0% to 1.25% and the amount of S100 was increased from 0% to 0.725%. The use of a ligated intestinal loop model demonstrated that C6-PS-PBCA-NPs could rapidly penetrate a highly viscoelastic mucous layer, leading to an improvement in the absorption efficiency. During a pharmacokinetic study, C6-PS-PBCA-NPs improved the absorption of C6, as indicated by their higher Cmax and AUC0-t values compared with those of C6-S-PBCA-NPs or C6-P-PBCA-NPs. Overall, the results of this study indicate that PBCA-NPs modified with PC and S100 can enhance the absorption of orally administered drugs.

Ibuprofen Release from Poly(ethyl cyanoacrylate) Nanoparticles Prepared by Semicontinuous Heterophase Polymerization

Ibuprofen-loaded poly(ethyl cyanoacrylate) nanoparticles were prepared by semicontinuous heterophase polymerization of ethyl cyanoacrylate in the presence of ibuprofen; different surfactant concentration, pH, and temperature were used. Particle size was measured by quasi-light scattering and transmission electron microscopy, while the amount of drug released was determined by UV spectroscopy. Nanoparticles with diameters between 10 and 58 nm, loaded with ibuprofen, were obtained. The smallest particles and the higher drug loading were obtained at the highest pH tested. The analysis of the release data showed that the drug release profiles correspond to the Weibull model. Moreover, it was found that most of the ibuprofen is released within the first 80–120 min; initially the release rate is slow, but then it increases to finally decrease. This behavior contrasts with the reported burst of drug concentration in the plasma after oral administration of IB.

Toxicity of Cisplatin-Loaded Poly Butyl Cyanoacrylate Nanoparticles in a Brain Cancer Cell Line: Anionic Polymerization Results

Cancer is one of the most important issues in modern medicine and the most common cause of death after cardiovascular diseases in many countries. Brain cancer is one of the most common causes of cancer death among men and women, ranking third. Chemotherapeutic drugs that aim to prevent uncontrolled proliferation of cells in tissues of the body and induce apoptosis of tumor cells are prominent candidates for development. Since cisplatin has an apoptosis-inducing role, it is widely used as an anticancer agent. In this research, toxicity of cisplatin was studied with the C6 rat glioma cell lined using the MTT method. In addition, nanoparticles underwent SEM microscopic imaging. Particle average size, size distribution, polydispersity index (PDI) and zeta potential of poly butyl cyanoacrylate nanoparticles were found to be 222 nm, 0.470 ± 0.04 and 5.1 ± 0.2 mV, respectively. The results showed that nanoconjugates of cisplatin have more cytotoxic effects on C6 cells than the free drug (P<0.05), pointing to an enhanced potential of the synthesized nano-particles as a new nanocarrier for chemotherapy.

Abstract 2073: Focused ultrasound-mediated transport of poly(alkyl) cyanoacrylate nanoparticles across the blood-brain barrier in a melanoma brain metastasis model

Abstract Drug delivery into the brain is impeded by the blood-brain barrier (BBB) - a dynamic interface that protects brain homeostasis, but also screens the brain from the vast majority of large and/or hydrophilic drug molecules. Focused ultrasound (FUS) has emerged as one of the promising methods to open the BBB safely and reversibly. We have previously reported FUS-mediated BBB opening using a novel platform consisting of microbubbles surrounded by poly(alkyl cyanoacrylate) nanoparticles that could prospectively be used for FUS- and nanoparticle-mediated drug delivery into the brain (1,2). Here, we have been investigating FUS-mediated BBB opening using a novel ultrasound system capable of generating FUS at two frequencies, 1.1 MHz and 7.8 MHz during the same experiment. This system allows a very precise selection of the exposure area. We used FUS exposure at 1 MHz to open the BBB by cavitation, while exposure at 7.8 MHz was employed to enable the action of acoustic radiation force. This force is caused by a transfer of momentum from acoustic waves to the tissues in which they propagate, and can facilitate nanoparticle transport in the extracellular matrix. FUS-mediated BBB opening was performed in NOD/SCID mice with melanoma brain metastases developed after intracardiac injection of human melanoma brain metastasis cells (3). The cells were fluorescently labeled, which enabled their detection in the brain. Poly(isohexyl) cyanoacrylate (PIHCA) nanoparticle-microbubbles similar to those reported in our earlier works (1,2) were injected immediately before the FUS exposure. Successful opening of the BBB was verified by MRI using a gadolinium-based contrast agent. An optimal window of exposure intensities that allow BBB disruption was found to be close a mechanical index of 0.3. Location of fluorescently labeled nanoparticles relative to blood vessels and tumor cells was determined in frozen sections using confocal microscopy. Tissue damage and FUS-induced changes at the cellular and molecular level were studied using histological and molecular techniques. In conclusion, the dual-frequency ultrasound transducer setup and our novel nanoparticle-microbubble platform showed promising results which will be used to develop a novel treatment of brain metastasis combining dual-frequency FUS with drug delivery using microbubbles. 1. Nanoparticle-stabilized microbubbles for multimodal imaging and drug delivery. Mørch Ý et al. Contrast Media Mol Imaging. 2015 Sep;10(5):356-66 2. Nanoparticle delivery to the brain - By focused ultrasound and self-assembled nanoparticle-stabilized microbubbles. Åslund AK et al. J Control Release. 2015 Oct 28;220(Pt A):287-294 3. Automated tracking of nanoparticle-labeled melanoma cells improves the predicted power of a brain metastasis model. Sundstrøm T et al. Cancer Res. 2013 Feb;73(8):2445-2456. Citation Format: Habib Baghirov, Andreas Åslund, Sofie Snipstad, Sigrid Berg, Rune Hansen, Frits Thorsen, Yrr Mørch, Catharina de Lange Davies. Focused ultrasound-mediated transport of poly(alkyl) cyanoacrylate nanoparticles across the blood-brain barrier in a melanoma brain metastasis model. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 2073.

Preparation and Loading with Rifampicin of Sub-50 nm Poly(ethyl cyanoacrylate) Nanoparticles by Semicontinuous Heterophase Polymerization

We report the preparation of poly(ethyl cyanoacrylate) (PECA) nanoparticles by semicontinuous heterophase polymerization carried out at monomer starved conditions at three monomer addition rates. Particles in the nanometer range were obtained, the size of which diminishes with decreasing monomer addition rate as shown by the fact that particles with mean diameters of ca. 42 and 30 nm were obtained at the faster and intermediate dosing rates, respectively, whereas two populations of particles, one of 15.5 and the other of 36 nm in mean diameters, were produced at the slower dosing rate. The obtained molecular weights were from 2,200 to 3,500 g/mol, depending on the addition rate, which are typical of the anionic polymerizations of cyanoacrylates in aqueous dispersions at low pHs. The rifampicin (RIF) loading into the nanoparticles was successful since the entire drug added was incorporated. The drug release study carried out at pH of 7.2 indicated a faster release from the free RIF at intermediate and larger release times as expected since, in the nanoparticles, first the drug has to diffuse through the nanoparticle structure. The comparison of several drug release models indicates that the RIF release from PECA nanoparticles follows that of Higuchi.

Synthesis and In vitro Cytotoxicity of a Novel Efficient Cisplatin-loaded poly N-butyl cyanoacrylate.

Purpose: Typically, drug-loaded polymer colloidal carriers are synthesized by the drug entrapment during anionic emulsion polymerization. The purpose of this study was to trial the ability of Cisplatin-loaded Poly Butyl Cyanoacrylate (PBCA) nanoparticles. Methods: The cytotoxicity of Cisplatin-loaded PBCA nanoparticles was evaluated by MT assay. The Polymeric nanoparticles have been characterized using TEM, SEM, FTIR and DLS. Results: Polymeric nanoparticles with loaded and unloaded drug prepared by this method, have spherical structure with 350 and 230 nm in diameter and their zeta potentials were -3.2 and -10.7 mv respectively. The average amount of drug loaded on the nanoparticles was 70.88 ± 5.51%. MTT assay was carried out to evaluate the cytotoxicity property of the nanoparticles. Inhibition concentration values (IC 50 ) for Cisplatin-loaded Nanoparticles were 20.8 and 18.2 μM for 24 and 48 h respectively. Conclusion: It was shown that cisplatin-loaded nanoparticles strongly increased cytotoxicity in comparison to classic drug in the MCF-7 cell line.

A facile method of synthesizing size-controlled hollow cyanoacrylate nanoparticles for transparent superhydrophobic/oleophobic surfaces

A novel method to synthesize size-controllable hollow polymeric nanoparticles is reported. The synthesis process completes in a moment with tunable particle diameters. Coated surfaces show superhydrophobicity/oleophobicity with high transparency.

Sericin/Poly(ethylcyanoacrylate) Nanospheres by Interfacial Polymerization for Enhanced Bioefficacy of Fenofibrate: In Vitro and In Vivo Studies.

Fenofibrate is a lipophilic drug used in hypercholesterolemia and hypertriglyceridemia as a lipid-regulating agent; however, it is characterized by poor water solubility and low dissolution rate, which result in a low oral bioavailability. In the present study, sericin/poly(ethylcyanoacrylate) nanospheres are synthesized by interfacial polymerization in aqueous media and investigated as a novel sericin-based delivery system for improved and enhanced oral bioefficacy of fenofibrate. The incorporation of sericin into the prepared cyanoacrylate nanoparticles and their spherical shape are confirmed by Lowry assay and scanning electron microscopy, respectively. Hydrophilic and mucoadhesive properties of the synthesized nanospheres are also evaluated. Finally, both in vitro release and in vivo studies are performed and the oral absorbable amount of fenofibrate is calculated to be higher than 70% when incorporated into the polymeric material, reducing the levels of total cholesterol (TC), triacylglycerols (TG), very low-density lipoproteins (VLDL), and low-density lipoproteins (LDL) compared to fenofibrate alone.

Epirubicin loading in poly(butyl cyanoacrylate) nanoparticles manifests via altered intracellular localization and cellular response in cervical carcinoma (HeLa) cells

Objective: Drug loading into nanocarriers is used to facilitate drug delivery to target cells and organs. We have previously reported a change in cellular localization of epirubicin after loading to poly(butyl cyanoacrylate) (PBCA) nanoparticles. We aimed to further investigate the altered cellular localization and cellular responses to the described drug formulation.Materials and methods: HeLa cells were treated with epirubicin-loaded PBCA nanoparticles prepared by the pre-polymerization method. A systematic study was performed to evaluate the formulation cytotoxicity. Cellular localization and uptake of the formulation as well as cellular response to the treatment were evaluated.Results: Our studies revealed decreased cytotoxicity of the nanoparticle-formulated epirubicin compared to the free drug as well as a noticeable change in the drug’s intracellular localization. Epirubicin-loaded nanoparticles were internalized via endocytosis, accumulated inside endosomal vesicles and induced a two-fold stronger pro-apoptotic signal when compared to the free drug. The level of the tumor suppressor protein p53 in HeLa cells increased significantly upon treatment with free epirubicin, but remained relatively unchanged when cells were treated with equivalent dose of nanoparticle-loaded drug, suggesting a possible shift from p53-dependent DNA/RNA intercalation-based induction of cytotoxicity by free epirubicin to a caspase 3-induced cell death by the epirubicin-loaded PBCA formulation.