An Alternative Excipient from Vegetable Source for Oral Drug Dosage Forms to Regulate Drug Delivery

Abstract:

Introduction: Tablet is the preferred drug dosage form. Cellulose fiber (Micro Crystalline Cellulose) is the major excipient used. For chronic diseases, frequent dosage is required resulting in cumulative excipient load and tachyphylaxis due to drug. We intent to invent excipients from vegetable sources to mitigate above challenges and reduce dosage as chronic sufferers (Diabetes mellitus) requires lifelong treatment. Aims and Objectives: To develop an excipient from Brassica oleracea and Vigna radiata sprouting which can regulate drug delivery, avoid excipient led toxicity and tachyphylaxis. Materials and Methods: Alkali and acid based depolymerization method was followed and cellulose fibers were studied for safety, physical, chemical and molecular parameters. With the developed cellulose fibers two drugs were formulated using Active Pharmaceutical Ingredient- Metformin and Miglitol. Efficacy was assayed using cell lines-Neuroblastoma, Kidney HK-2, L6 Myoblasts, 3T3-L1 Preadipocytes, INS-1 and HEPG 2 hepatocytes and compared with conventional micro crystalline cellulose- based formulations. Results: Characterization of developed excipients was done in comparison with conventional cellulose, invented excipients had long fibers, higher bulk density, flow, even particle size compared to conventional cellulose. Dissolution and disintegration of Metformin from Brassica oleracea fiber was slow and Miglitol showed quick release from Vigna radiata compared to conventional excipient. Therapeutic effect of both drugs from developed excipients was higher compared to conventional excipient-based drug by cell culture assay. Both developed excipients did not show mutagenic effect. Conclusion: Brassica oleracea fiber slows release of metformin; may reduce drug dosage, tachyphylaxis, release of Miglitol from Vigna radiata was rapid, may compliment metformin therapy.

Keywords: Herbal excipients, Cellulose fibers, Microcrystalline cellulose, Tachyphylaxis, Vegetable source excipient, Brassica oleracea, Vigna radiata, Metformin, Miglitol.