Loaded Alginate Nanoparticles Research Articles

3D printed tablets containing oxaliplatin loaded alginate nanoparticles for colon cancer targeted delivery. An in vitro/in vivo study.

This study aimed to develop a colon-targeted tablet of oxaliplatin (OP) using the combination of nanotechnology and fused deposition modeling (FDM) 3D printing to improve its antitumor activity, tumor targetability, and safety profile. Eudragit L100-55 filament containing OP loaded alginate nanoparticles (OP-NPs) were fabricated using hot-melt extrusion method and printed by an FDM printer to 3D printed tablets with good uniformity in the drug content and selective release of OP in the colonic environment. The antitumor effect of 3D printed tablets containing OP-NPs in CT-26 tumor-bearing mice was evaluated compared to intravenous and oral administration of OP solution, and compressed tablets containing OP-NPs, which were prepared by direct compression method with the same formulation. The antitumor effect of 3D printed tablets containing OP-NPs was remarkable and comparable with intravenous OP solution (p˃0.05) with a better safety profile, whereas compressed tablets did not show any significant antitumor effect, probably in terms of non-selective drug release in stomach and upper intestine environments. This study highlights the potential of the combination of nanotechnology and 3D printing in the preparation of colon-specific drug delivery systems of chemotherapeutic drugs with good antitumor activity, tumor targetability, and safety profile for colorectal cancer treatment.

Influence of nanoparticles surface coating on physicochemical properties for CRISPR gene delivery

CRISPR is a powerful gene editing tool, but its non-viral delivery approaches are still limited due to low efficacy. To improve the efficacy of plasmid loaded alginate nanoparticles, three different polymer coating, chitosan, gum Arabic and PEG were applied and studied in comparison. The surface coating highly affected physicochemical properties of the nanoparticles. Smaller size nanoparticles showed higher cellular uptake in terms of quantity and efficiency. The transfection efficiency was highly correlated with the plasmid DNA released from the nanoparticles and the nanoparticles ability to protect the plasmid DNA from degradation. The indel gene editing efficiency of the nanoparticles was related to their protection ability but not related to their transfection efficiency. These results indicated the importance of careful tuning of nanomaterial physicochemical properties as it plays the ultimate role of the carrier biological activities.

In vivo synergism of free miltefosine or in alginate-based nanocarrier combined with voriconazole on aspergillosis.

Aim: To evaluate the activity of miltefosine (MFS), in its free form or loaded-alginate nanoparticles (MFS-AN), alone or combined with voriconazole (VRC) on Aspergillus fumigatus and Aspergillus flavus. Materials & methods: A broth microdilution assay was used for the susceptibility testing of Aspergillus isolates, and the antifungal efficacy was assessed using the aspergillosis model in Galleria mellonella larvae. Results: The in vitro synergistic effect of MFS with VRC was observed only against A. fumigatus, whereasboth combined therapies (MFS+VRC and MFS-AN+VRC) showed synergism in reducing the larval mortality rate and fungal burden in the larvae infected by A. fumigatus and A. flavus. Conclusions: MFS and MFS-AN combined with VRC may be an important strategy for improving antifungal therapy against aspergillosis.

Preparation and evaluation of alginate nanoparticles prepared by green method for drug delivery applications

Nanosized natural polymers have attained considerable attention in drug delivery applications due to their high encapsulation efficiency, non-toxic nature, sustained and targeted drug delivery. Here we have synthesized Rifampicin loaded alginate nanoparticles by green method. Physicochemical characterization of the nanoparticles was assessed using Transmission electron microscopy, Fourier transform infrared spectroscopy, Dynamic light scattering and X-ray diffraction technique. The swelling and in vitro drug release showed that the framework experiences pH-dependent swelling and release of Rifampicin. Rifampicin has lower release in acid medium and higher release in intestinal condition. Moreover, in view of the drug release results, the release kinetics and transport mechanisms were investigated and discussed. In vitro cytotoxicity assay demonstrated that the nanoparticles were non-toxic in nature. The acute oral toxicity study of the synthesized nanoparticles was done in Wistar albino rats. No systemic toxicity was observed after oral administration of nanoparticles. The present study demonstrated the potential of using alginate nanoparticles synthesized by a green method for drug delivery applications.

Exemestane loaded alginate nanoparticles for cancer treatment: Formulation and in vitro evaluation

Alginate, a biopolymer is most useful for anticancer drug delivery, because of it is biocompatible, nontoxic, biodegradable and exploiting ligand-receptor interaction. Breast cancer is spreading very fast due to the changing food habits and environmental causes. Exemestane (EXE) an oral chemotherapeutic drug was used to treat breast cancer, while loading EXE in alginate nanoparticles, the side effects which was faced during administration are expected to be reduced and control the release of exemestane. Thus, in the present study, an anticancer drug EXE was loaded into the Alginate nanoparticles (ALG-NPs) through simple controlled gelation method and evaluated in vitro to study the performance of ALG-NPs in delivering the anticancer drug EXE. The unloaded and loaded formulation was characterized by FT-IR, XRD and SEM studies. The encapsulation of Exemestane was confirmed using FTIR and XRD analysis results. The surface morphology, shape and size of the formulation was studied using SEM analysis and result reveals that the size was in nano size range with rough surface morphology. Encapsulation of EXE was studied by using UV–vis spectrophotometer. In vitro drug release studies implies that ALG-NPs acts as a novel drug delivery system for the effective controlled delivery for cancer treatment.

A Comparative Study of Aspirin Loaded Alginate Nanoparticles Prepared by Desolvation Technique Using Acetone and Ethanol as Desolvating Agents

In this present study Aspirin loaded alginate nanoparticles were prepared by desolvation technique using acetone and ethanol as desolvating agents. Continuous and intermittent addition methods were adapted for the addition of desolvating agent to the aqueous solution. Two formulations were prepared by using each desolvating agent. F1 and F3 were prepared by continuous addition of acetone and ethanol as desolvating agents. F2 and F4 were prepared by intermittent addition of acetone and ethanol as desolvating agents. In all the Formulations, particles were found to be nanometric in size. Comparative study was made among these four Formulations for particle size, Mean particle diameter, Product yield, Drug content,Electrophoretic mobility, Zetapotential, Entrapment efficiency, Loading capacity. Dissolution studies were performed for all the four formulations and compared for better dissolution profile. Comparative study was made to determine the most appropriate desolvating agent and best method for the preparation of alginate nanoparticles. Among all Formulations Intermittent addition of ethanol was showing better result with Mean particle diameter of 237.4 nm, Entrapment efficiency of 37.4 %, Loading capacity of 10.22 %. The Zeta potential value (-52.3) was higher than all other Formulations. Based on these results it was concluded that intermittent addition method was the best method and ethanol was the better desolvating agent for the preparation of aspirin nanoparticles. Keywords: Aspirin loaded, alginate nanoparticles, desolvation technique, acetone, ethanol, desolvating agents.

Alginate nanoparticles protect ferrous from oxidation: Potential iron delivery system

A novel, efficient delivery system for iron (Fe2+) was developed using the alginate biopolymer. Iron loaded alginate nanoparticles were synthesized by a controlled ionic gelation method and was characterized with respect to particle size, zeta potential, morphology and encapsulation efficiency. Successful loading was confirmed with Fourier Transform Infrared spectroscopy and Thermogravimetric Analysis. Electron energy loss spectroscopy study corroborated the loading of ferrous into the alginate nanoparticles. Iron encapsulation (70%) was optimized at 0.06% Fe (w/v) leading to the formation of iron loaded alginate nanoparticles with a size range of 15–30nm and with a negative zeta potential (−38mV). The in vitro release studies showed a prolonged release profile for 96h. Release of iron was around 65–70% at pH of 6 and 7.4 whereas it was less than 20% at pH 2.The initial burst release upto 8h followed zero order kinetics at all three pH values. All the release profiles beyond 8h best fitted the Korsmeyer-Peppas model of diffusion. Non Fickian diffusion was observed at pH 6 and 7.4 while at pH 2 Fickian diffusion was observed.

Silk sericin loaded alginate nanoparticles: Preparation and anti-inflammatory efficacy

In this study, silk sericin loaded alginate nanoparticles were prepared by the emulsification method followed by internal crosslinking. The effects of various silk sericin loading concentration on particle size, shape, thermal properties, and release characteristics were investigated. The initial silk sericin loadings of 20, 40, and 80% w/w to polymer were incorporated into these alginate nanoparticles. SEM images showed a spherical shape and small particles of about 71.30–89.50nm. TGA analysis showed that thermal stability slightly increased with increasing silk sericin loadings. FTIR analysis suggested interactions between alginate and silk sericin in the nanoparticles. The release study was performed in acetate buffer at normal skin conditions (pH 5.5; 32°C). The release profiles of silk sericin exhibited initial rapid release, consequently with sustained release. These silk sericin loaded alginate nanoparticles were further incorporated into topical hydrogel and their anti-inflammatory properties were studied using carrageenan-induced paw edema assay. The current study confirms the hypothesis that the application of silk sericin loaded alginate nanoparticle gel can inhibit inflammation induced by carrageenan.

Development and evaluation of brain targeted intranasal alginate nanoparticles for treatment of depression

The purpose of the present study was to investigate the potential of Venlafaxine loaded alginate nanoparticles (VLF AG-NPs) for treatment of depression via intranasal (i.n.) nose to brain delivery route. The VLF AG-NPs were prepared and optimized on the basis of various physio-chemical characteristics. Pharmacodynamic studies of the VLF AG-NPs for antidepressant activity were carried in-vivo by forced swimming test and locomotor activity test on albino Wistar rats. VLF AG-NPsi.n. treatment significantly improved the behavioural analysis parameters i.e. swimming, climbing, and immobility in comparison to the VLF solutioni.n. and VLF tabletoral. The intranasal VLF AG-NPs also improved locomotor activity when compared with VLF solutioni.n. and VLF tabletoral. Confocal laser scanning fluorescence microscopy studies were performed on isolated organs of rats after intravenous and intranasal administrations of Rodamine-123 loaded alginate nanoparticles to determine its efficacy for nose to brain delivery and also for its qualitative distribution to other organs. Brain uptake and pharmacokinetic studies were performed by determination of VLF concentration in blood and brain respectively for VLF AG-NPsi.n., VLF solutioni.n. and VLF solutioni.v. The greater brain/blood ratios for VLF AG-NPsi.n. in comparison to VLF solutioni.n. and VLF solutioni.v. respectively at 30 min are indicative of superiority of alginate nanoparticles for direct nose to brain transport of VLF. Thus, VLF AG-NPsi.n. delivered greater VLF to the brain in comparison to VLF solution which indicates that VLF AG-NPs could be a promising approach for the treatment of depression.