Combined synergetic potential of metformin loaded pectin-chitosan biohybrids nanoparticle for NIDDM.

RATIONALE: Combined therapy is a promising approach over its preference to minimize the dose, adverse effects and enhanced therapeutic efficiency in a various diseases including diabetes. AIM: The present research work is to explore combined synergistic anti-diabetic potential of chitosan and pectin with Metformin (CPM) nano-formulation, with special emphasis on effect of Metformin when integrated with bio polymers. METHODS: The biohybrid nanoparticles (CPMNP) were formulated by ionic gelation process. The optimized formulation was examined for various in vitro characterizations, in vivo anti-diabetic potential, biodistribution and targeting efficiency. RESULTS: The optimized biohybrid showed higher content of Metformin 92.1 ±â€¯3.3% and extended release. The pectin coated nanoparticles had smooth spherical morphology with 581.8 nm size and positive surface charge (+41.76 mV). The biohybrid regulated blood glucose, improved the glucose utilization in vital organs, control the dyslipdimea and renal impairment in diabetic rats. CPMNP-4 significantly enhanced the up regulation of IRA, GLUT-2 and GK receptor gene expression and down regulate the TNF-α and IL-6 in pancreas. Also, nanoparticles showed healthier biodistribution simultaneously capability to penetrate in vital organs. CONCLUSION: The combined synergistic effects of Metformin and biopolymers are due their corresponding mechanism to enhance glucose uptake, minimized the adverse effects during diabetic therapy.

Development and Characterization of Metformin Loaded Pectin Nanoparticles for T2 Diabetes Mellitus.

AIM: The present investigation was aimed to formulate and evaluate Metformin loaded pectin (PCM) nanoparticles (NPs) for sustained action for management of Type 2 Diabetes Mellitus (T2DM). METHOD: The nanoparticles were formulated by ionic gelation technique. The nano-formulations were subjected for the analyses of entrapment efficiency and drug release stud for 12h. The optimized formulation examined various in vitro characterizations such as particle size, zeta potential, surface morphology and FTIR studies. The in vitro heamocomptability, protein binding stability and glucose uptake studies were performed with nanoparticles. RESULTS: The PCMNP-4 showed drug entrapment efficiency, 68 ± 4.2 % and demonstrated favourable in vitro prolonged release characteristics. The mean particles diameter of optimized formulation was 482.7 nm and 0.270 poly dispersity index (PI), had spherical shape and zeta potential of (+38.85 mV). In addition, the nanoparticles were reasonably stable in the presence of excess bovine serum albumin, which suggested that the nanoparticles may also be stable in the blood stream. The percentage of haemolysis induced by Metformin and placebo PCNPs were less than 5%. The results indicated that the PCMNPs are hemocompatible and therefore, safe for oral administration. The glucose uptake was increased 1.5 fold in RBCs and L6 skeleton muscle cell line compared with Metformin. CONCLUSION: Hence, the designed nanoparticle system could possibly be advantageous in terms of prolonged release, to achieve reduced dose frequency and improve patient compliance.