Abstract
Low water solubility frequently compromises the therapeutic efficacy of drugs and other biologically active molecules. Here, we report on coacervate polysaccharide nanoparticles (CPNs) that can transport and release a model hydrophobic drug, piroxicam, to the cells in response to changes in temperature. The proposed, temperature-responsive drug delivery system is based on ionic derivatives of natural polysaccharides—curdlan and hydroxypropyl cellulose. Curdlan was modified with trimethylammonium groups, while the anionic derivative of hydroxypropyl cellulose was obtained by the introduction of styrenesulfonate groups. Thermally responsive nanoparticles of spherical shape and average hydrodynamic diameter in the range of 250–300 nm were spontaneously formed in water from the obtained ionic polysaccharides as a result of the coacervation process. Their morphology was visualized using SEM and AFM. The size and the surface charge of the obtained objects could be tailored by adjusting the polycation/polyanion ratio. Piroxicam (PIX) was effectively entrapped inside the nanoparticles. The release profile of the drug from the CPNs-PIX was found to be temperature-dependent in the range relevant for biomedical applications.
Highlights
Nanoparticulate systems display many advantages as carriers in drug delivery applications [1,2]
The purpose of the current study was to obtain and characterize the coacervate nanoparticulate system based on the formation of polyion complex between two polysaccharide derivatives: cationic curdlan (C-CUR) and anionic hydroxypropyl cellulose (A-Hydroxypropyl cellulose (HPC)), and to evaluate its usefulness in the delivery of a poorly soluble drug, piroxicam
cationic derivative of curdlan (C-CUR) was mixed with an anionic derivative of hydroxypropylcellulose, A-HPC, to synthesize a series of coacervate nanoparticulate systems which were formed by a spontaneous and immediate self-assembly process in water
Summary
Nanoparticulate systems display many advantages as carriers in drug delivery applications [1,2] When applied parenterally, they increase the bioavailability of the compounds, which are either poorly soluble in aqueous media or characterized by low stability. They increase the bioavailability of the compounds, which are either poorly soluble in aqueous media or characterized by low stability This allows for the reduction of a necessary dose, increasing both the efficiency and safety of the therapy [3]. The nanocarrier may allow for controlled release of the active compound or for its targeted delivery Such systems are often applied in ophthalmic delivery, as they offer longer residence times at the site of the cul-de-sac. Nanoparticles are less irritant to the eye than larger particles and may improve the saturation and inherent solubility of hydrophobic drugs in lachrymal fluids [5]
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