An Investigation into the Suitability of Amidated Pectin Hydrogel Beads as a Delivery Matrix for Chloroquine

Abstract

The aim of the present study was to delay the release of chloroquine to distal parts of the gastrointestinal tract by using a multiparticulate hydrogel formulation. Amidated pectin chloroquine beads (PC) with varying pectin-to-chloroquine ratios (PC) w/w loadings of 4:1, 2:1, and 1:1 in the dried beads were prepared by the gelation of drug-loaded pectin solutions in the presence of calcium. In vitro release studies of chloroquine from pectin-chloroquine hydrogel beads and chloroquine diphosphate powder were carried out in simulated gastric and intestinal fluids. The total release of the entrapped chloroquine from the hydrogel beads was achieved between 4 and 7 h in simulated intestinal fluid, but total release was not achieved in simulated gastric fluid. However, total release from chloroquine diphosphate powder was achieved by 1.5 and 2 h in gastric and intestinal fluids, respectively. The plasma pharmacokinetics of chloroquine from pectin hydrogel beads and chloroquine diphosphate solution following single or repeated dosing were compared in male Sprague-Dawley rats over a period of 60 h. Oral administration of the hyrogel beads to rats produced maximum plasma concentrations by 7 h, but highest plasma concentrations following chloroquine solution administration were observed by 2 h. The dissolution data and appearance of significant plasma concentrations of chloroquine 2 to 4 h after oral administration suggests release in duodenum, jejunum, or ileum.

Transdermal Delivery of Insulin by Amidated Pectin Hydrogel Matrix Patch in Streptozotocin-Induced Diabetic Rats: Effects on Some Selected Metabolic Parameters

“…Reports suggest that pectin (polygalacturonic acid) not only delivers drugs to the colonic region of the gastrointestinal tract, but also sustains drug release in vitro [25]. More interestingly, Musabayane et al, succeeded in sustaining plasma insulin concentrations in diabetic rats using orally administered, insulin-loaded amidated pectin hydrogel beads [14].…”

TIS21 negatively regulates hepatocarcinogenesis by disruption of cyclin B1–Forkhead box M1 regulation loop

“…Measurement of resveratrol concentration in plasma will indirectly indicate their release from the formulation. In addition, pharmacokinetic study is a popular method to evaluate the efficiency of the colon‐specific formulations18–25 and ethically more acceptable (require less animal). Thus, the optimized beads were subjected to in vivo pharmacokinetic study in rats and compared with unmodified beads (beads prepared without Glu) and resveratrol suspension.…”

Development of pectin based hydrogel membranes for biomedical applications

“…Pectin beads were prepared by ionic gelation method. Amidated pectin hydrogel beads were also prepared as a delivery matrix for chloroquine [12]. But the pectin beads have several drawbacks such as fast breakdown of the beads and difficulty of the controlled release of drugs.…”