Ruth Harris

Functional Characterization of Chitin and Chitosan

Chitin and its deacetylated derivative chitosan are natural polymers composed of randomly distributed � -(1-4)- linked D-glucosamine (deacetylated unit) and N-acetyl-D-glucosamine (acetylated unit). Chitin is insoluble in aqueous media while chitosan is soluble in acidic conditions due to the free protonable amino groups present in the D-glucosamine units. Due to their natural origin, both chitin and chitosan can not be defined as a unique chemical structure but as a fam- ily of polymers which present a high variability in their chemical and physical properties. This variability is related not only to the origin of the samples but also to their method of preparation. Chitin and chitosan are used in fields as different as food, biomedicine and agriculture, among others. The success of chitin and chitosan in each of these specific applica- tions is directly related to deep research into their physicochemical properties. In recent years, several reviews covering different aspects of the applications of chitin and chitosan have been published. However, these reviews have not taken into account the key role of the physicochemical properties of chitin and chitosan in their possible applications. The aim of this review is to highlight the relationship between the physicochemical properties of the polymers and their behaviour. A functional characterization of chitin and chitosan regarding some biological properties and some specific applications (drug delivery, tissue engineering, functional food, food preservative, biocatalyst immobilization, wastewater treatment, molecular imprinting and metal nanocomposites) is presented. The molecular mechanism of the biological properties such as biocompatibility, mucoadhesion, permeation enhancing effect, anticholesterolemic, and antimicrobial has been up- dated.

Chitosan Amphiphilic Derivatives. Chemistry and Applications

Chitosan is a natural polymer composed of randomly distributed -(1-4)-linked D-glucosamine (deacetylated unit) and Nacetyl-D-glucosamine (acetylated unit). It has been described as a non-toxic, biodegradable and biocompatible polymer with very interesting biological properties, such as permeation-enhancing and mucoadhesive properties, anticoagulant and antimicrobial activity and so on. Chitosan has been used in several areas such as biomedical, pharmaceutical and biotechnological fields as well as in the food industry. Recently, there has been a growing interest in the modification of chitosan to improve its solubility in physiological conditions, to introduce new applications or to improve chitosan biological properties. Research and development on a variety of amphiphilic copolymers containing hydrophobic and hydrophilic segments, have been very active due to their spontaneous self-assembly behaviour in aqueous media These smart transitions often lead to diverse functional compartment structures like micelles, vesicles and gels, which represent promising applications in the field of biotechnology and pharmaceutics. The aim of the present paper is to review the latest advances in the synthesis of chitosan amphiphilic derivatives with a special emphasis in their applications.

Chitosan-genipin microspheres for the controlled release of drugs: clarithromycin, tramadol and heparin.

The aim of this study was to first evaluate whether the chitosan hydrochloride-genipin crosslinking reaction is influenced by factors such as time, and polymer/genipin concentration, and second, to develop crosslinked drug loaded microspheres to improve the control over drug release. Once the crosslinking process was characterized as a function of the factors mentioned above, drug loaded hydrochloride chitosan microspheres with different degrees of crosslinking were obtained. Microspheres were characterized in terms of size, morphology, drug content, surface charge and capacity to control in vitro drug release. Clarithromycin, tramadol hydrochloride, and low molecular weight heparin (LMWH) were used as model drugs. The obtained particles were spherical, positively charged, with a diameter of 1–10 μm. X-Ray diffraction showed that there was an interaction of genipin and each drug with chitosan in the microspheres. In relation to the release profiles, a higher degree of crosslinking led to more control of drug release in the case of clarithromycin and tramadol. For these drugs, optimal release profiles were obtained for microspheres crosslinked with 1 mM genipin at 50 ºC for 5 h and with 5 mM genipin at 50 ºC for 5 h, respectively. In LMWH microspheres, the best release profile corresponded to 0.5 mM genipin, 50 ºC, 5 h. In conclusion, genipin showed to be eligible as a chemical-crosslinking agent delaying the outflow of drugs from the microspheres. However, more studies in vitro and in vivo must be carried out to determine adequate crosslinking conditions for different drugs.

Suitability of a colorimetric method for the selective determination of chitosan in dietary supplements

A colorimetric method previously described for the determination of chitosan has been evaluated because lack of linearity had been observed at certain concentrations. Calibration curves of varied-characteristic chitosans, recovery studies and chitosan quantification in seven commercial dietary supplements have been performed. Some analysis conditions including the solvent of the samples have been studied and optimised. Different data combinations have been checked in order to select the widest range of concentrations where no serial correlation was found. With the selected conditions the method is linear, reproducible and provides reliable results in the analysis of the chitosan content in capsules. Its selectivity has been proved by the lack of interference with other compounds present in the dietary supplements. But in the case of tablet products, the presence of cellulose and magnesium stearate may produce an underestimation of the chitosan content.

Chitosan and inhalers: a bioadhesive polymer for pulmonary drug delivery

Abstract: Pulmonary drug delivery routes present several advantages compared to conventional drug administration, such as fewer systemic side effects than oral or parenteral administration. Many studies show drug delivery systems that are intended for pulmonary administration. However, the time that these systems stay at the mucose surfaces is limited. Mucoadhesive polymers are needed to increase residence time of drugs and therefore to promote absorption through the mucose. Chitosan, a polysaccharide obtained by chitin deacetylation, is used in drug release systems and has mucoadhesion and absorption-promoting properties. There are numerous studies on the use of chitosan drug delivery systems to increase the bioavailability of drugs at the lung mucose. This chapter is a review of literature reports detailing chitosan-based drug delivery systems intended for use in inhalers. The effect of different types of chitosan particulate systems on aerosolization properties will be compared.