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

Abstract

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 pH-Dependent Controlled Release of Encapsulated Vitamin B1 from Liposomal Nanocarrier

“…To analyze the registered drug release profiles, the relative concentrations (c t /c 0 ) of the released vitamin B 1 as a function of time were calculated. For the mathematical description of the in vitro dissolution, seven different kinetic models were chosen, which are the first- [ 27 ] and second-order [ 28 ], Higuchi [ 29 ], Weibull [ 30 ], Korsmeyer–Peppas [ 31 ], Hopfenberg [ 32 ] and Hixon–Crowell [ 33 , 38 ] models. The calculation was executed based on a previously published open access spreadsheet method [ 26 ] by nonlinear fitting.…”

Recent Reports on Polysaccharide-Based Materials for Drug Delivery

“…Additionally, the mechanical strength of composite beads was improved compared to pure PC ones. Further studies on the biopolymeric beads were conducted to investigate the material’s applicability as colon-targeted DDS [ 129 ]. The most promising formulation was the one with polyacrylic acid, as it was more stable and capable of overcoming variable conditions of the digestive tract during drug delivery to the colon.…”