SMART CHITOSAN-BASED MICROBEAD FORMULATION FOR COLON-TARGETED DELIVERY OF LACTOFERRIN

Abstract

Objective: This study aims to develop a novel smart formulation based on dual-responsive Polyethylene Glycol Methacrylate-Grafted-Chitosan (PEGMA-g-Cs) copolymers for the controlled delivery of Lactoferrin. The goal is to enhance the bioavailability and therapeutic efficacy of Lactoferrin in treating colorectal cancer, addressing its rapid degradation in a highly acidic gastric environment. Methods: Gold-coated Superparamagnetic Iron Oxide Nanoparticles (Au-SPIONs) were synthesized and loaded into PEGMA-g-Cs microspheres. Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), Proton Nuclear Magnetic Resonance (HNMR), X-Ray Diffraction (XRD), Infrared Spectroscopy (IR), UV-visible spectrophotometry (UV-Vis), optical microscopy, and Dynamic Light Scattering (DLS) were used to characterise the synthesized materials. Drug loading and release studies of lactoferrin-loaded microbead formulations were conducted to evaluate encapsulation efficiency, loading capacity, and release profiles. Results: The lactoferrin-loaded microbead formulations demonstrated excellent encapsulation efficiency and loading capacity. Specifically, Encapsulation Efficiency (EE) was 77% and Loading Capacity (LC) was 4.99% for the homogenizer batch, while the magnetic stirring batch achieved 86% EE and 3.12% LC. The formulation exhibited minimal release (<20%) in Simulated Gastric Fluid (SGF) and almost complete release in Simulated Colonic Fluid (SCF). The 3-[4,5-Dimethylthiazol-2-Yl]-2,5-Diphenyl Tetrazolium Bromide (MTT) cell cytotoxicity assay in human CaCo-2 colon cancer cells revealed a significant reduction in cell proliferation following treatment with the new formulations. Conclusion: The findings suggest that the new formulation can be a promising approach for the targeted delivery of Lactoferrin, thereby improving the efficacy of colorectal cancer treatment by enhancing the bioavailability of lactoferrin.