Preliminary Evaluation of Novel Triglyceride-Based Nanocomposites for Biomedical Applications

Abstract

This work describes the development and characterization of triglyceride-based magnetic nanocomposites for application in magnetic hyperthermia and controlled drug delivery. The magnetic solid lipid nanocomposites (MSLN) constituted by mixtures of trilaurin-tricaprylin and trilaurin-tricaprin have been successfully obtained by emulsification-solvent evaporation method. The developed MSLNs were subjected to an external oscillating magnetic field and showed significant hyperthermia. The samples were exposed to frequencies of 688 and 869 kHz causing, respectively, a temperature increase of 15.5 and 22.7 °C (trilaurin-tricaprylin) and 17.3 and 26.1 °C (trilaurin-tricaprin). Also, in vitro assays in the absence of magnetic field showed that the triglyceride-based formulations were able first to encapsulate and then to sustained release an antitumoural hydrophobic drug. After 72 h of assay trilaurin-tricaprylin and trilaurin-tricaprin released 73 and 55% of their cargo, respectively. In addition, MSLN exhibited low in vitro cytotoxic activity against human neutrophils.Keywords: lipid mixture, magnetic hyperthermia, drug delivery, oncocalyxone-A IntroductionNanotechnology is an expanding sector and the use of superparamagnetic iron oxide nanoparticles (SPIONs) is attracting increasing attention in several areas. SPIONs are widely employed for biotechnological applications through the development of magnetic systems for use in: cell separation, as contrast agents for magnetic resonance imaging (MRI), magnetic hyperthermia, targeted bioactive compounds delivery and biosensors. [1][2][3][4] Such applications explore the biggest advantages of using SPIONs: biocompatibility and satisfactory magnetic response at applied magnetic field (superparamagnetic character). 5,6 The surface of the magnetic nanoparticles should be modified, not only in order to prevent oxidation and aggregation, but also to provide colloidal stability, reduced magnetic susceptibility, as well as to expand the effectiveness of cellular uptake and biodistribution. The hydroxyl groups present on the surface of nanoparticles can function as an anchor point for various types of compounds such as oleic acid, which is commonly used in the synthesis of magnetic ferrofluids. The criteria adopted to select the appropriate coating of magnetic nanoparticles depends mainly on the intended application. In the case of this research, magnetic nanoparticles made of iron oxide were coated with oleic acid (Fe 3 O 4 @OA) for subsequent incorporation into lipid carriers. 7-9The lipid carriers have been widely used as they also possess excellent characteristics such as biocompatibility Preliminary Evaluation of Novel Triglyceride-Based Nanocomposites for Biomedical Applications J. Braz. Chem. Soc. 1548 and versatility, and they have been proposed for the delivery of bioactive compounds by oral, intravenous, topical and parenteral routes. 10,11The solid lipid nanoparticles (SLNs) emerged in the early 90's and currently are alternative encapsulation systems and carriers o...

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“…The nanocomposites object of this study (Scheme 1) were prepared in one step following a modified melt emulsification method according to our published procedure [20,23]. Basically, an organic phase composed of the wax, drug (DOX), magnetic nanoparticles and fluorescent dye (DiO) was sonicated at temperatures above the melting point of the wax in the presence of a water phase composed of water and a surfactant (Tween80).…”