Formulation and Optimization of Zinc-Pectinate Beads for the Controlled Delivery of Resveratrol

Abstract

Preventive and therapeutic efficacies of resveratrol on several lower gastrointestinal (GI) diseases (e.g., colorectal cancer, colitis) are well documented. To overcome the problems due to its rapid absorption and metabolism at the upper GI tract, a delayed release formulation of resveratrol was designed to treat these lower GI diseases. The current study aimed to develop a delayed release formulation of resveratrol as multiparticulate pectinate beads by varying different formulation parameters. Zinc-pectinate (Zn-pectinate) beads exhibited better delayed drug release pattern than calcium-pectinate (Ca-pectinate) beads. The effects of the formulation parameters were investigated on shape, size, Zn content, moisture content, drug encapsulation efficiency, swelling-erosion, and resveratrol retention pattern of the formulated beads. Upon optimization of the formulation parameters in relative to the drug release profiles, the optimized beads were further subjected to morphological, chemical interaction, enzymatic degradation, and stability studies. Almost all prepared beads were spherical with approximately 1 mm diameter and efficiently encapsulated resveratrol. The formulation parameters revealed great influence on resveratrol retention and swelling-erosion behavior. In most of the cases, the drug release data more appropriately fitted with zero-order equation. This study demonstrates that the optimized Zn-pectinate beads can encapsulate very high amount of resveratrol and can be used as delayed release formulation of resveratrol.

Hesperidin Hydrogel Formulation Using Pectin-Chitosan Polymer Combination

“…. (7) hour the swelling percentage in pH 6.8 and 7.4 medium decreases [11,28]. The result shows that the distribution of pH 5.0 SI data that is analyzed is distributed normally.…”

“…Pectin, with its characteristic as a weak acid (pKa 3-4) with the carboxylic group (-COO-) tends to ionize at higher pH. This causes a repelling force among the carboxylate group in pectin leading to the increase of hydrogel swelling power [11]. The highest swelling percentage was achieved in pH 6.8 medium after 5 h, at the 6 ) in chitosan will occur, while pectin is unionized, so repelling force takes place inside the chitosan structure which causes significant swelling in formula with higher chitosan concentration (formula 2 and 4) [2].…”

“…Other research showed that hydrogel beads of pectin-zein protects indomethacin from upper gastrointestinal tract conditions and its release was controlled by pectin degradation with pectinase; however, pectin is highly soluble in water, which leads to the development of another polymer with low solubility in water, to produce a strong and effective gel for carrying drug which is entrapped in gastric fluid and small intestine [9][10]. One of the polymers that can be used to overcome this problem is chitosan, which its carboxylic group binds ionically with the chitosan amine group [11].…”

Formulation of Mulberry Leaf (Morus Alba L.) Extract Hydrogel Beads Using Cross-Linked Pectin

“…With the great number of hydrogen bonds, the ability to bind with water and the ability to swell in water become greater [9]. When compared with the research from Das et al, the swelling ability of Surini and Diandra Int J App Pharm, Vol 9, Suppl 1, 2017, hydrogel beads is <100%, whereas the swelling ability of mulberry leaf extract was better, at more than 200% [8].…”

“…Zinc is a cation divalent that is cross linked with the carboxyl group of pectin to create hydrogel beads. A study reported that zinc possesses a high ability to bind with pectin, which can form beads with a greater gel strength [8]. This research aims to make and evaluate mulberry leaf extract hydrogel beads with pectin as a polymer and zinc acetate as a cross linker to produce a nutraceutical product in a bead dosage form.…”