Objective: The current research was based on developing CS-PLGA nanoparticles (NPs) drug delivery system (DDS) for improving the bio-availability of metformin HCl, an anti-diabetic drug. Methods: Nanoprecipitation method was utilized to prepare the metformin HCl-loaded CS-PLGA NPs DDS. The metformin HCl-loaded NPs were validated using an analytical method and characterization of NPs was also done. These polymers release the drug in a controlled manner. Results: The correlation coefficient (R2) value for the metformin HCl calibration curve was 0.9971 in phosphate buffer pH 6.8 at a concentration range of 0-12 μg/ml. Metformin HCl-loaded NPs release the drug at 144 h, approximately 90%. DSC tests were carried out for 50 mg and 75 mg of MET HCl incorporated NPs and FT-IR for 50 mg of MET HCl incorporated NPs, it was clear from the FT-IR and DSC spectra that there were no interactions between the metformin HCl and the polymer. Conclusion: It was proven that metformin HCl-loaded NPs act as a prominent DDS by exhibiting extensive drug release and an increase in its bioavailability.