The Influence of the Hydrophobic Polymeric Coating on 5-ASA Release from the Bipolymeric Milibeads with Amidated Pectin

The industrial polymeric carriers for peroral mesalazine application exploit, i.a., cellulose or polyacrylic acid derivatives, polyvinylpyrrolidone, and modified starch. Pectins, as natural polymers, are interesting materials in pharmaceutical applications due to properties such as non-toxicity, biocompatibility, and biodegradability. The aim of the study was the evaluation of the release of the drug from coated pectin beads doped with synthetic polymers as drug carriers to the colon, as well as interactions between ingredients. The drug release was carried out using basket apparatus. The amount of 5-ASA (5-aminosalicylic acid, mesalazine) released to the pH = 7.4 buffer with pectinase was measured at selected time intervals using UV-Vis spectroscopy. The zero-, first-, and second-order kinetics, as well as Higuchi, Korsmeyer–Peppas, and Hixon–Crowell equations, were used to analyze the release pattern. The interactions between beads components were investigated employing FTIR spectrophotometry and DSC study. The dissolution of the drug was divided into two parts. It was found that the release of 5-ASA followed mainly the Higuchi equation. The mass transport in the first stage of the release followed a non-Fickian model and the parameter n was in the range of 0.74 ± 0.2–0.99 ± 0.2. The formulation doped with PA (polyacrylic acid) was the most appropriate and capable of overcoming the variable conditions of the gastrointestinal tract

The Interactions and Release Kinetics of Sodium Hyaluronate Implemented in Nonionic and Anionic Polymeric Hydrogels, Studied by Immunoenzymatic ELISA Test

Hyaluronan is a natural polymer that was introduced to wound therapy. Formulations based on synthetic polymers such as methylcellulose (MC) and polyacrylic acid (PA) containing hyaluronan (HA) were proposed for the development of prospective wound-healing preparations. The formulations of different carrier concentrations containing a fixed amount of HA were prepared, and their viscosity was measured. The HA release was evaluated by employing the apparatus paddle over a disc. The hydrogels were introduced to the donor chamber, and HA was released to the pH = 7.4 buffer. The amount of HA released was obtained using the ELISA test. The release was analyzed on the basis of different kinetic models: zero-, first-, and second-order kinetics, as well as Higuchi and Korsmeyer–Peppas equations. The release rate constants and the half release time were calculated from these equations. According to the value of the coefficient of the determination, the best model describing the observed process was selected. The comparison between the dissolution profiles was carried out by calculating the difference factor f1 and the similarity factor f2. The interaction between the hydrogel components was investigated by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) measurements. The study revealed that the zero-order equation best described the release of HA from the formulations studied. The FTIR research and the DSC study showed the intermolecular interaction between HA chains in MC-based compositions, as well as between HA and the synthetic polymer in the PA-based formulations. The study revealed that the formulation with a higher concentration of synthetic polymer may prolong the release of HA. The obtained results indicated that the proposed hydrogels have potential for wound healing and may accelerate skin regeneration

Bipolymeric Pectin Millibeads Doped with Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine

Targeted drug delivery systems are a very convenient method of treating inflammatory bowel disease. The properties of pectin make this biopolymer a suitable drug carrier. These properties allow pectin to overcome the diverse environment of the digestive tract and deliver the drug to the large intestine. This investigation proposed bipolymeric formulations consisting of the natural polymer pectin and a synthetic polymer containing the drug 5-aminosalicylic acid. Pectin beads were prepared via ionotropic gelation involving the interaction between the hydrophilic gel and calcium ions. The obtained formulations consisted of natural polymer, 5-aminosalicylic acid (5-ASA) and one of the synthetic polymers, such as polyacrylic acid, polyvinylpyrrolidone, polyethylene glycol or aristoflex. The release of the drug was carried out employing a basket apparatus (USP 1). The acceptor fluid was pH = 7.4 buffer with added enzyme pectinase to reflect the colon environment. The amount of the released drug was determined using UV-Vis spectrophotometry at a wavelength of λ = 330 nm. The kinetics of the drug dissolution revealed that none of the employed models was appropriate to describe the release process. A kinetic analysis of the release profile during two release stages was carried out. The fastest drug release occurred during the first stage from a formulation containing pectin and polyethylene glycol. However, according to the applied kinetic models, the dissolution of 5-ASA was rather high in the formulation without the synthetic polymer during the second stage. Depending on the formulation, 68–77% of 5-ASA was released in an 8-hour time period. The FTIR and DSC results showed that there was no interaction between the drug and the polymers, but interactions between pectin and synthetic polymers were found