Abstract
Poor circulation stability and inadequate cell membrane penetration are significant impediments in the implementation of nanocarriers as delivery systems for therapeutic agents with low bioavailability. This research discusses the fabrication of a biocompatible poly(lactide-co-glycolide) (PLGA) based nanocarrier with cationic and hydrophilic surface properties provided by natural polymer chitosan and coating polymer polyethylene glycol (PEG) for the entrapment of the hydrophobic drug disulfiram. The traditional emulsification solvent evaporation method was compared to a microfluidics-based method of fabrication, with the optimisation of the parameters for each method, and the PEGylation densities on the experimental nanoparticle formulations were varied. The size and surface properties of the intermediates and products were characterised and compared by dynamic light scattering, scanning electron microscopy and X-ray diffraction, while the thermal properties were investigated using thermogravimetric analysis and differential scanning calorimetry. Results showed optimal particle properties with an intermediate PEG density and a positive surface charge for greater biocompatibility, with nanoparticle surface characteristics shielding physical interaction of the entrapped drug with the exterior. The formulations prepared using the microfluidic method displayed superior surface charge, entrapment and drug release properties. The final system shows potential as a component of a biocompatible nanocarrier for poorly soluble drugs.
Highlights
Nanostructured materials have demonstrated efficiency at improving bioavailability and reducing toxicity of bio-actives when implemented in the design of drug delivery systems [1]
Four initial formulation sets were prepared varying the solvent, surfactant concentration and sonication parameters, with an unmodified, unloaded poly(lactic-co-glycolic) acid (PLGA) formulation, an unmodified PLGA formulation loaded with disulfiram, a drug loaded PLGA formulation coated with chitosan and a drug loaded PLGA formulation coated with chitosan and polyethylene glycol (PEG)
Even though the abnormal tumour vasculature allows the penetration of particles 200 nm have been shown to accumulate in the liver or spleen [34]. Both methods were used with the ultimate goal of fabricating nanoparticles
Summary
Nanostructured materials have demonstrated efficiency at improving bioavailability and reducing toxicity of bio-actives when implemented in the design of drug delivery systems [1]. Synthetic polymeric nanocarriers are the simplest delivery systems because of their facile preparation, their ability to efficiently incorporate bio-actives within their matrices, and thereafter provide controlled release either by erosion or diffusion mechanisms [1]. PLGA can be prepared via various routes [2] from the co-polymers glycolic acid and lactic acid, which is derived from green and renewable resources such as corn [3]. It is a material well suited to be implemented in the design of synthetic polymeric nanocarriers due to its malleable structure that can be optimized by tuning the ratios of its constituent co-polymers to suit various applications [4].
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