Abstract

Objective: The primary goal of this study was to convert a natural catechin-rich extract into nanoparticles by using a biodegradable and non-toxic polymer Eudragit L 100 to address the various biopharmaceutical problems of catechin.Methods: Nanoparticles were prepared by emulsion solvent evaporation technique using Eudragit L 100 in increasing concentration. Optimization of processing conditions like a selection of organic solvents, diluent and surfactant concentrations, drug and polymer ratio and method of drying to increase the biological efficiency were duly attempted. Parameters such as dynamic light scattering, zeta potential, SEM and energy-dispersive X-ray spectroscopy were assessed for the evaluation of nanoparticles.Results: The entrapment efficiency was found to be between 35-45 % with methanol compared to other organic solvents. The zeta potential values of all the formulations were in the range of±30 mV to±60 mV) which confirms moderate to good stability. A rapid or ‘burst’ effect of the drug release in pH 6.8 buffer showing 92 % in the first 30 min which gradually decreased to 52 % by the end of 180 min but in the pH 7.4, the release was found to be moderate. SEM and DLS indicated particles were of spherical shape lying in a nanometer range of 100 to 200 nm with a proportional influence of polymer on the particles size.Conclusion: Nanoformulations were found to be more stable and confirmed the presence of major elements such as carbon and oxygen. The findings collectively indicate that it may be worthwhile to apply nanotechnology for the design of an advanced oral dosage form for an enhanced bioavailability and biological efficacy.

Highlights

  • One of the important plant secondary metabolite belonging to a group of flavonoids with diverse health benefits in humans is catechin

  • Size reduction resulted in smaller particles which were beneficial because of an increased surface area or unique shape, size, and number

  • The reduction mechanism consists of deforming the sample until it breaks or tears and such breaking may be achieved by applying diverse forces like trituration

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Summary

Introduction

One of the important plant secondary metabolite belonging to a group of flavonoids with diverse health benefits in humans is catechin. They are polyphenolic compounds having three hydrocarbon rings consisting of six hydroxyl groups at different positions, and the position of hydroxyl groups is important for their antioxidant activities other biological activities [1, 2]. The prominent sources of catechin include apples, oranges, pears, black grapes, blackberries, cherries, raspberries, red wine and dark chocolate. Catechin has gained an immense interest for researchers has it is known to have anti-proliferative, antimicrobial, antiinflammation, and antioxidant properties, it is shown to improve blood flow and has potential benefits in cardiac health [3,4,5,6,7]

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