Chitosan–pectin polyelectrolyte complex as a carrier for colon targeted drug delivery

Abstract

a b s t r a c tObjective: The objective of present work was to prepare a polyelectrolyte complex (PEC) between chitosan (polycation) & pectin (polyanion) and to develop enteric coated tablets for colon delivery using the PEC. Methodology: The PECs were prepared using different concentrations of chitosan and pectin. Drug loaded enteric coated tablets were prepared by wet granulation method using PEC to sustain the release at colon and coating was done with Eudragit S 100 to prevent the early release of the drug in stomach and intestine. Two independent variable, % PEC (chitosan/pectin) and % coating were optimized by 3 2 full factorial design. Statistical model were also used to supplement the optimization. DSC was performed to confirm the interaction between the polyions. Developed formulations were evaluated for physical appearance, weight variation, thickness, hardness, friability, % swelling, assay, in-vitro and ex-vivo drug release studies to investigate the PEC's ability to deliver the drug to colon. Ex-vivo release study using rat caecal content was also carried out on optimized formulation. Results and discussion: DSC results confirmed chitosan/pectin interaction and subsequent formation of PEC. The optimized formulation containing 1.1% of PEC and 3% of coating showed highest swelling and release in alkaline pH mechanism of which was found to be microbial enzyme dependent degradation established by ex-vivo study using rat caecal content.

Three‐dimensional plotted alginate fibers embedded with diclofenac and bone cells coated with chitosan for bone regeneration during inflammation

“…Chitosan molecules carry a positive group ( ) and are able to form ionic crosslinking with the negative group (COO − ) on the alginate molecules. The amount of chitosan coated or the use of chitosan crosslinking agents such as pectin or genipin may be used to change drug retention and release efficacy …”

Pectin and Pectin-Based Composite Materials: Beyond Food Texture

“…These polyelectrolyte complexes have many uses in diverse fields like food industry [ 233 ], biomedicine [ 234 , 235 ], and pharmaceutical industry, especially as a drug delivery vehicle [ 231 , 236 ] and colon-specific drug delivery [ 237 , 238 , 239 ]; these drug carriers include hydrogel, films, tablets, pellets and beads. The interest on this system for controlled release of drugs lies in the fact that both polymers have the capacity to protect the drug from being released in the upper intestinal tract and deliver it in the colon [ 238 ].…”

Unsuccessful Delivery of Tetrandrine From Colon-Targeted Dosage Forms Comprising Alginate/Hydroxypropyl Methylcellulose and Alginate–chitosan Beads

“…Supernatants were then collected and diluted again to 50 ml in HCl (pH 1.2), and tetrandrine contents were determined using a ultraviolet-visible (UV-Vis) spectrophotometer (Shimadzu UV-1800, Japan) at 280 nm. Entrapment efficiencies and drug contents were calculated using the following formulas [18]:…”