Development and Preclinical Evaluation of Nanoparticle-based Antioxidants for Diabetes
Redox imbalance leads to beta-cell dysfunction and activation of certain signaling pathways associated with insulin resistance, leading to oxidative stress and the subsequent development and progression of diabetes and related complications.
Several dietary antioxidants have shown therapeutic effects in diabetes. However, these antioxidants have poor solubility, permeability and stability in conventional delivery systems, ultimately leading to their poor oral bioavailability.
As experts in the field of cellular stress, Creative Bioarray offers development and preclinical evaluation programs for polymeric nanoparticle (PLGA) based antioxidants for diabetes. Nanoparticles are a novel antioxidant delivery system (NDDS) that can increase the bioavailability of antioxidants, overcome pharmacokinetic and stability issues, and improve the selectivity of scavenging ROS.
Curcumin, the active ingredient in the yellow spice turmeric, has shown a variety of pharmacological effects, such as antioxidant, anti-inflammatory, antibacterial and anticancer activities. We have successfully provided our customers with curcumin-PLGA nanoparticles for diabetes treatment in preclinical evaluation.
Preparation and Characterization of Diabetes Antioxidants Encapsulated PLGA Nanoparticles
- Preparation of antioxidant PLGA nanoparticles
The antioxidants were encapsulated into PLGA nanoparticles using appropriate methods (e.g. emulsion-diffusion-evaporation method, emulsion volatilization method, thin film dispersion method).
- Determination of particle size and surface zeta potential of antioxidant PLGA nanoparticles
Determination of particle size, polydispersity coefficient and zeta potential of nanoparticles, morphology determination of nanoparticles (transmission electron microscopy).
- Determination of drug loading and encapsulation rate
Drug loading rate/ 100% = measured antioxidant content / weight of drug loaded nanoparticles after lyophilization × 100
Encapsulation rate / 100% = measured antioxidant content / antioxidant dosage × 100
- In vitro release behavior of antioxidants
A certain amount of drug-laden-PLGA nanoparticles was sealed in a dialysis bag, placed in PBS solution, and 1 mL of PBS solution was taken out at different time points to determine the content of target antioxidants and plot the in vitro drug release curve.
Preclinical Experiments on the in vivo Bioavailability of Antioxidant-laden PLGA Nanoparticles
- Synthesis and characterization scheme of PCADK
To establish mouse models of diabetes or other related diseases. Oral antioxidant/ drug-laden-PLGA nanoparticle administration was performed in groups to assess.
- Diabetic antioxidant concentrations in blood.
- Blood glucose and insulin levels after administration.
- Ability of antioxidant-loaded-PLGA nanoparticles to scavenge superoxide.
- Effect of antioxidant-laden-PLGA nanoparticles on oxidative stress and antioxidant system in animals.
- Effect of antioxidant-loaded PLGA nanoparticles on protein glycation, polyol pathway in diabetic mice.
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