In this work, chitosan nanoparticles were prepared by ionotropic gelation of chitosan with tripolyphosphate (TPP). The effects of the ionic strength of the solvent employed in the particle preparation on the average size and compactness of the particles were investigated. In addition, the effects of the chitosan concentration and the crosslinker to polymer ratio on the particle characteristics were studied. The chitosan-TPP nanoparticles were characterized by dynamic light scattering, zeta potential, and turbidity measurements. The compactness of the nanoparticles was estimated with a method based on the size of the nanoparticles and the turbidity of the nanoparticle suspension. All the investigated preparation parameters, i.e., the ionic strength of the solvent, the chitosan concentration, and the TPP to chitosan ratio, affected the particle characteristics. For instance, smaller and more compact particles were formed in saline solvents, compared to particles formed in pure water. Further, the addition of monovalent salt rendered it possible to prepare particles in the nanometer size range at a higher polymer concentration. Solvent salinity is thus an important parameter to address in the preparation of chitosan nanoparticles crosslinked with TPP.
The physical stability of chitosan nanoparticles cross-linked with sodium tripolyphosphate (TPP) was investigated over a period of 1 month. Special emphasis was placed on changes in the particle size and the particle compactness, which are two important physicochemical parameters of nanoparticulate drug delivery systems. The chitosan-TPP particles were prepared at different ionic strengths, chitosan chloride concentrations, and TPP-to-chitosan ratios. In the presence of monovalent salt, the positive ζ potential of the particles was reduced. In spite of this, the particles were more stable when prepared and stored under saline conditions compared to water. This could be attributed to the smaller particle sizes found in the presence of sodium chloride. Most of the particles prepared in saline solvents were stable with respect to changes in the size and the compactness of the particles. However, instability was observed at the highest cross-linker-to-polymer ratios. Generally, a reduction in the ζ potential and an increase in the particle compactness were observed at increasing TPP-to-chitosan ratios. This combined with the size increase induced by a high concentration of chitosan, increased the aggregation and sedimentation tendency of the particles and reduced the colloidal stability of the particles.
The present review is aimed at elucidating relatively new aspects of mucoadhesion/mucus interaction and related phenomena that emerged from a Mucoadhesion workshop held in Munster on 2-3 September 2015 as a satellite event of the ICCC 13th-EUCHIS 12th. After a brief outline of the new issues, the focus is on mucus description, purification, and mucus/mucin characterization, all steps that are pivotal to the understanding of mucus related phenomena and the choice of the correct mucosal model for in vitro and ex vivo experiments, alternative bio/mucomimetic materials are also presented. Then a selection of preparative techniques and testing methods are described (at molecular as well as micro and macroscale) that may support the pharmaceutical development of mucus interactive systems and assist formulators in the scale-up and industrialization steps. Recent applications of mucoadhesive systems (including medical devices) intended for different routes of administration (oral, gastrointestinal, vaginal, nasal, ocular, and intravesical) and for the treatment of difficult to treat pathologies or the alleviation of symptoms are described.
Good oral health is of major importance for general health and well-being. Several innovative drug delivery systems have been developed for the local treatment and prevention of various diseases in the oral cavity. However, there are currently few optimal systems and many therapeutic challenges still remain, including low drug efficacy and retention at targeted site of action. The present review provides an insight into the latest drug delivery strategies for the local treatment and prevention of the four most common oral pathologies, namely, dental caries, periodontitis, oral mucosal infections and oral cancer. The potential of bioadhesive formulations, nanoparticulate platforms, multifunctional systems and photodynamic methodologies to improve therapy and prophylaxis in future local applications for the oral cavity will be discussed.
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