Fabrication of Sustainable Modified Fenugreek Gum Block Copolymer in Oral Controlled Drug Delivery System: Synthesis, Toxicity, in Vitro and in Vivo Pharmacokinetics

Background

Grafting of small molecules over carbohydrate polymeric chain afford new chemically modified substances which possess modified properties which are essential for drug release studies. Fenugreek seeds contain carbohydrate gum polymer as one of the constituent which was isolated and grafted with acryl amide. Such grafted polymer was explored for drug release studies here.

Methods

The objective of present invention was to develop acrylamide (Aam) grafted fenugreek gum (FG) based polymer in the presence of ceric ammonium nitrate under microwave conditions. The developed copolymer was characterized for the confirmation of grafting using elemental analysis, DSC, FTIR, NMR, Mass spectrometry data and toxicity studies along with surface morphology. The potential of grafted polymer was assessed by formulating nifedipine tables including pure gum, grafted copolymer and HPMC K100M.

Results

In vitro drug release studies of the F1-F5 batches reflected 92.24 to 94.72% release within 5 h, while, F6-F10 extended the release up to 12 h. The release was retarded with increase in concentration of grafted copolymer which was anticipated. The optimized batch F8, demonstrated 94.19% drug release in 12 h and this batch was further extended to in vivo study. The pharmacokinetics studies of optimized formulation in rabbits showed an area under the curve of 6050.45 (ng/mL)×h as compared with marketed nifedipine tablet (6723.88 (ng/mL)×h) which signified the release modulating property of the polymer.

Conclusion

The acrylamide grafted copolymer successfully retarded the drug release and hence can be explored for the extended-release formulations and can be further explored as high performing material.