Development of Microparticle-based Antioxidants for Diabetes
Diabetes mellitus is one of the major global public health problems. A large body of recent evidence suggests that cytoreductive-oxidative (redox) imbalance contributes to oxidative stress and the subsequent development and progression of diabetes and related complications by regulating certain signaling pathways associated with beta-cell dysfunction and insulin resistance.
Novel antioxidant delivery systems can overcome pharmacokinetic and stability issues and improve the selectivity of ROS scavenging. As an expert in the field of cellular stress, Creative Bioarray provides solutions for the development of antioxidants based on particle-based delivery systems and characterizes microspheres in terms of micromorphology, drug loading, encapsulation rate, particle size, and in vitro release characteristics, laying the foundation for the development of antioxidants based on microparticle-based delivery systems.
Why Choose Microparticle Delivery System
- Microparticle delivery systems can facilitate the entry of antioxidants with poor membrane permeability (e.g., SOD) into cells.
- Poly(cyclohexane-1,4-diyl acetone dimethylene ketal) (PCADK) degrades to acetone, a compound recognized as safe by the FDA, and 1,4-cyclohexanedimethanol, which has an excellent toxicity profile, has been used to encapsulate SOD and form SOD-PCADK particles.
- The hydrolysis products of polycondensate are non-toxic, readily metabolizable and excreted, and biocompatible.
- The degradation products of polycondensate are neutral small molecules, which are more suitable for encapsulating peptides, proteins, antigens, vaccines, gene drugs and other biological macromolecules.
Antioxidant PCADK Preparation and Characterization Solutions
- Synthesis and characterization scheme of PCADK
PCADK was synthesized on a multigram scale using an acetal exchange reaction between 1,4-cyclohexanedimethanol and 2,2-dimethoxypropane. 1HNMR spectra of PCADK were measured to confirm its chemical structure. PCADK has acetal bonds in its backbone and thus should degrade in the acidic environment of the phagosome after phagocytosis.
We measured the hydrolysis kinetics of PCADK in ground powder form at a certain acidic pH to estimate the behavior of PCADK-based delivery carriers after phagocytosis.
- Preparation and evaluation scheme of antioxidant PCADK microspheres
The antioxidants were encapsulated into PCADK microparticles using appropriate methods (e.g. W/O/W double emulsion procedure, S/O/W method and in-situ S/O/W method).
A. Determination of drug loading and encapsulation rate
Drug loading= drug content of the microspheres/total weight of the microspheres × 100%
Encapsulation rate= drug content in the microspheres / drug delivery volume × 100%
B. Determination of microsphere morphology and particle size
The morphology of the microspheres was observed by electron scanning microscopy, and the freeze-dried microspheres were fixed on conductive adhesive and gold sprayed to make scanning electron microscope specimens to observe the shape of the microspheres. The particle size and size distribution of the microspheres were determined by Malvern 2000 laser particle size meter.
C. Evaluation of in vitro release of antioxidants
A certain amount of drug-loaded microspheres was placed in a centrifuge tube, release medium was added, and the tube was placed in a constant temperature water bath shaker and removed at 1, 3, 5, 7, 12, 24, 36, 48, 60, 72, 96, 120, 144 and 168 h. The supernatant was collected. The mass concentration of antioxidants in the filtrate was measured after passing through the microporous filter membrane, and the cumulative release rate was calculated while replenishing an equal volume of fresh medium at the same temperature to continue the release. The cumulative release curves of the microspheres were plotted with time as the horizontal coordinate and cumulative release rate as the vertical coordinate.
D. Assessing the ability of micro-antioxidants to clear superoxide
The ability of antioxidant-PCADK microspheres to clear superoxide from target cells was assessed in cell culture.
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