Metformin Hydrochloride Loaded Mucoadhesive Microspheres and Nanoparticles for Anti-Hyperglycemic and Anticancer Effects Using Factorial Experimental Design

Metformin Hydrochloride Loaded Mucoadhesive Microspheres and Nanoparticles for Anti-Hyperglycemic and Anticancer Effects Using Factorial Experimental Design

Metformin hydrochloride (HCl) microspheres and nanoparticles were formulated to enhance bioavailability and minimize side effects through sustained action and optimized drug-release characteristics. Initially, the same formulation design with different ratios of metformin HCl and Eudragit RSPO was u...

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Bibliographic Details
Published in:Drug design, development and therapy Vol. 17; pp. 3661 - 3684
Main Authors: Kotha, Amina Alam, Ahmad, Shihab Uddin, Dewan, Irin, Bhuiyan, Mohiuddin Ahmed, Rahman, Fahad Imtiaz, Naina Mohamed, Isa, Reza, Md Selim
Format: Journal Article
Language:English
Published: New Zealand Dove Medical Press Limited 01-01-2023
Dove
Dove Medical Press
Subjects:
Analysis
anti-hyperglycemic
anticancer
Calorimetry
Calorimetry, Differential Scanning
Cancer
Care and treatment
Chemistry, Pharmaceutical - methods
Delayed-Action Preparations
Diabetes therapy
Hypoglycemic Agents - pharmacology
Metformin
Metformin - chemistry
Metformin - pharmacology
microsphere
Microspheres
Nanoparticles
Original Research
Particle Size
Permeability
Pharmaceutical industry
Polymers
Research Design
Spectroscopy, Fourier Transform Infrared
Type 2 diabetes
United States
Germany
microsphere
anti-hyperglycemic
nanoparticles
anticancer
permeability
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Summary:Metformin hydrochloride (HCl) microspheres and nanoparticles were formulated to enhance bioavailability and minimize side effects through sustained action and optimized drug-release characteristics. Initially, the same formulation design with different ratios of metformin HCl and Eudragit RSPO was used to formulate four batches of microspheres and nanoparticles using solvent evaporation and nanoprecipitation methods, respectively. The produced formulations were evaluated based on particle size and shape (particle size distribution (PSD), scanning electron microscope (SEM)), incompatibility (differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR)), drug release pattern, permeation behavior, in vivo hypoglycemic effects, and in vitro anticancer potential. Compatibility studies concluded that there was minimal interaction between metformin HCl and the polymer, whereas SEM images revealed smoother, more spherical nanoparticles than microspheres. Drug release from the formulations was primarily controlled by the non-Fickian diffusion process, except for A1 and A4 by Fickian, and B3 by Super case II. Korsmeyer-Peppas was the best-fit model for the maximum formulations. The best formulations of microspheres and nanoparticles, based on greater drug release, drug entrapment, and compatibility characteristics, were attributed to the study of drug permeation by non-everted intestinal sacs, in vivo anti-hyperglycemic activity, and in vitro anticancer activity. This study suggests that the proposed metformin HCl formulation can dramatically reduce hyperglycemic conditions and may also have anticancer potential.
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These authors contributed equally to this work
ISSN:1177-8881
1177-8881
DOI:10.2147/DDDT.S432790