Enhanced cellular delivery of idarubicin by surface modification of propyl starch nanoparticles employing pteroic acid conjugated polyvinyl alcohol
ABSTRACT Enhanced intracellular internalization of the anti-cancer active idarubicin (IDA) was achieved through appropriate surface modification of IDA loaded propyl starch nanoparticles. This was conducted by synthesizing pteroic acid modified polyvinyl alcohol (ptPVA) and employing this stabilizer for formulating the said nanoparticles. Pteroic acid attached at the nanoparticles improved the surface protein adsorption of the nanoparticle, a condition which the nanoparticles would largely experience in vitro and in vivo and hence improve their cellular internalization. Spherical, homogenous IDA nanoparticles (214 ± 5 nm) with surface modified by ptPVA were formulated using the solvent emulsification-diffusion technique. The encapsulation efficiency and drug loading amounted around 85%. In vitro release studies indicated a controlled release of IDA. Safety and efficacy of the nanoparticles was confirmed by suitable cellular cytotoxicity assays. Protein binding studies indicated a higher adsorption of the model protein on nanoparticles formulated with ptPVA as compared to PVA. Cellular uptake studies by confocal laser scanning microscopy revealed a higher cellular uptake of ptPVA stabilized nanoparticles thus confirming the proposed hypothesis of higher protein adsorption being responsible for higher cellular internalization.
SourceAvailable from: David Julian Mcclements[Show abstract] [Hide abstract]
ABSTRACT: Natural and modified polysaccharides are promising vehicles for nano- and micro-encapsulation of active food ingredients. This article reviews the state of the art of carbohydrate-based delivery systems for utilization in the food, pharmaceutical and other industries. Initially, an overview of the different kinds of carbohydrates used to assemble delivery systems is given, including starch, cellulose, pectin, guar gum, chitosan, alginate, dextrin, cyclodextrins, new sources of native gums, and their combinations and chemically modified forms. Their molecular and physicochemical properties, functional performance, and advantages and disadvantages for encapsulation are given. Various approaches for fabrication of carbohydrate-based delivery systems are then discussed, including coacervation, spray drying, electrospinning, electrospray, supercritical fluid, emulsion-diffusion, reverse micelle, emulsion-droplet coalescence, emulsification/solvent evaporation, salting-out, ultrasonication and high pressure homogenization. The biological fate of carbohydrate nanocarriers during digestion, absorption, metabolism and excretion are discussed, and some notes about their bioavailability and potential toxicity are provided. Finally, the functional performances of different carbohydrate-based delivery systems are discussed, and future developments are highlighted.Trends in Food Science & Technology 09/2014; 39(1). DOI:10.1016/j.tifs.2014.06.007 · 4.65 Impact Factor
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ABSTRACT: Selective relaxation rate measurements effectively proved the affinity of dexamethasone 21-phosphate disodium salt for quaternary ammonium-chitosan conjugates, their thiolated derivatives and the corresponding nanostructured aggregates. Affinity was also probed by dynamic dialysis. The release profile of dexamethasone loaded nanoparticles was defined by quantitative NMR and interrupted dialysis experiments, and mucoadhesivity of empty nanoparticles was effectively probed by selective relaxation rate measurements.International Journal of Pharmaceutics 12/2013; DOI:10.1016/j.ijpharm.2013.12.018 · 3.79 Impact Factor
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ABSTRACT: Conventional cancer chemotherapies cannot differentiate between healthy and cancer cells, and lead to severe side effects and systemic toxicity. Another major problem is the drug resistance development before or during the treatment. In the last decades, different kinds of controlled drug delivery systems have been developed to overcome these shortcomings. The studies aim targeted drug delivery to tumor site. Magnetic nanoparticles (MNP) are potentially important in cancer treatment since they can be targeted to tumor site by an externally applied magnetic field. In this study, MNPs were synthesized, covered with biocompatible polyethylene glycol (PEG) and conjugated with folic acid. Then, anti-cancer drug idarubicin was loaded onto the nanoparticles. Shape, size, crystal and chemical structures, and magnetic properties of synthesized nanoparticles were characterized. The characterization of synthesized nanoparticles was performed by dynamic light scattering (DLS), Fourier transform–infrared spectroscopy (FT–IR), transmission electron microscopy (TEM), scanning electron microscopy (SEM) analyses. Internalization and accumulation of MNPs in MCF-7 cells were illustrated by light and confocal microscopy. Empty MNPs did not have any toxicity in the concentration ranges of 0––500 μg/mL on MCF-7 cells, while drug-loaded nanoparticles led to significant toxicity in a concentration-dependent manner. Besides, idarubicin-loaded MNPs exhibited higher toxicity compared to free idarubicin. The results are promising for improvement in cancer chemotherapy.Biomedecine [?] Pharmacotherapy 07/2014; 68(6). DOI:10.1016/j.biopha.2014.08.013 · 2.11 Impact Factor