Abstract
Chitosan (CS) is a natural polysaccharide, widely studied in the past due to its unique properties such as biocompatibility, biodegradability and non-toxicity. Chemical modification of CS is an effective pathway to prepare new matrices with additional functional groups and improved properties, such as increment of hydrophilicity and swelling rate, for drug delivery purposes. In the present study, four derivatives of CS with trans-aconitic acid (t-Acon), succinic anhydride (Succ), 2-hydroxyethyl acrylate (2-HEA) and acrylic acid (AA) were prepared, and their successful grafting was confirmed by FTIR and 1H-NMR spectroscopies. Neat chitosan and its grafted derivatives were fabricated for the encapsulation of fluticasone propionate (FLU) and salmeterol xinafoate (SX) drugs, used for chronic obstructive pulmonary disease (COPD), via the ionotropic gelation technique. Scanning electron microscopy (SEM) micrographs demonstrated that round-shaped microparticles (MPs) were effectively prepared with average sizes ranging between 0.4 and 2.2 μm, as were measured by dynamic light scattering (DLS), while zeta potential verified in all cases their positive charged surface. FTIR spectroscopy showed that some interactions take place between the drugs and the polymeric matrices, while X-ray diffraction (XRD) patterns exhibited that both drugs were encapsulated in MPs’ interior with a lower degree of crystallinity than the neat drugs. In vitro release studies of FLU and SX exposed a great amelioration in the drugs’ dissolution profile from all modified CS’s MPs, in comparison to those of neat drugs. The latter fact is attributed to the reduction in crystallinity of the active substances in the MPs’ interior.
Highlights
Lung drug delivery is a significant field of research in the handling of chronic inflammatory pulmonary diseases, such as asthma and chronic obstructive pulmonary disease (COPD) [1]
The first part focuses on the synthesis and characterization of chitosan derivatives as well as on the investigation of the evolved interactions between the used monomers and the chitosan backbone
Four different derivates of CS were synthesized after the modification of its backbone with trans-aconitic acid (t-Acon), succinic anhydride (Succ), 2-hydroxyethyl acrylate (2-HEA)
Summary
Lung drug delivery is a significant field of research in the handling of chronic inflammatory pulmonary diseases, such as asthma and chronic obstructive pulmonary disease (COPD) [1]. COPD is a life-threatening lung disease characterized by progressive, persistent airflow limitation and airways inflammation leading to excessive production of mucus as well as progressive decline in lung function [2]. It is a multi-system condition comprising, among others, systemic inflammation, oxidative stress, bony muscle malfunction and cardiovascular symptoms [3]. The principal factors causing the appearance of the aforementioned disease include the continual inhalation of toxic particles and fumes among with tobacco smoking, while the polluted atmosphere, age and genetic predisposition illustrate a catalytic role [4,5].
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