Abstract
Chitosan (CS) is a polymer extensively used in drug delivery formulations mainly due to its biocompatibility and low toxicity. In the present study, chitosan was used for nanoencapsulation of a budesonide (BUD) drug via the well-established ionic gelation technique and a slight modification of it, using also poly(vinyl alcohol) (PVA) as a surfactant. Scanning electron microscopy (SEM) micrographs revealed that spherical nanoparticles were successfully prepared with average sizes range between 363 and 543 nm, as were measured by dynamic light scattering (DLS), while zeta potential verified their positive charged surface. X-ray diffraction (XRD) patterns revealed that BUD was encapsulated in crystalline state in nanoparticles but with a lower degree of crystallinity than the neat drug, which was also proven by differential scanning calorimetry (DSC) and melting peak measurements. This could be attributed to interactions that take place between BUD and CS, which were revealed by FTIR and by an extended computational study. An in vitro release study of budesonide showed a slight enhancement in the BUD dissolution profile, compared to the neat drug. However, drug release was substantially increased by introducing PVA during the nanoencapsulation procedure, which is attributed to the higher amorphization of BUD on these nanoparticles. The release curves were analyzed using a diffusion model that allows estimation of BUD diffusivity in the nanoparticles.
Highlights
Chronic obstructive pulmonary disease (COPD) is characterized by chronic airflow limitation and airways inflammation [1]
Due to the fact that budesonide is mainly used in inhalable systems, the proper ratio was selected in order to eliminate the factor of the size that could affect its delivery through the respiratory tract [51]
BUD loaded CS nanoparticles were successfully prepared via an ionic gelation technique in different ratios and poly(vinyl alcohol) (PVA) was used as an emulsifier in order to enhance
Summary
Chronic obstructive pulmonary disease (COPD) is characterized by chronic airflow limitation and airways inflammation [1]. It is a progressive life-threatening lung disease that was responsible for the death of 5% of the population globally in the year 2015, according to World Health Organization data. The main causes of the disease are smoking and environmental pollutants. It affects men and women and the most susceptible groups among them are mainly smokers and the elderly. The major symptoms of COPD are dyspnea, breathlessness, chronic cough and sputum production. The above-mentioned symptoms provoke serious long-term disability in patients’
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