Formulation and optimization of zinc-pectinate beads for the controlled delivery of resveratrol.
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.
Das
Surajit
S
Department of Pharmacy, Faculty of Science, National University of Singapore, Block S4, 18 Science Drive 4, Singapore, 117543, Republic of Singapore.
Ng
Ka-Yun
KY
Ho
Paul C
PC
D000042:Absorption; D002214:Capsules; D003692:Delayed-Action Preparations / Q000138:chemical synthesis*; D004058:Diffusion; D004339:Drug Compounding / Q000379:methods; D010368:Pectins / Q000138:chemical synthesis*; D000077185:Resveratrol; D013267:Stilbenes / Q000008:administration & dosage / Q000737:chemistry*; D014665:Vasodilator Agents / Q000737:chemistry
D002214:Capsules; D003692:Delayed-Action Preparations; D013267:Stilbenes; D014665:Vasodilator Agents; D010368:Pectins; D000077185:Resveratrol