Chitosan nanoparticles for the transport of APIs against diabetes mellitus

Diabetes mellitus can have serious consequences such as blindness, heart disease, strokes or amputations. In this publication, chitosan nanoparticles will be synthesized to improve the transport of APIs.

New Chitosan-Based Co-Delivery Nanosystem for Diabetes Mellitus Therapy

Lupascu, F.G.; Sava, A.; Tătărușanu, S.-M.; Iacob, A.-T.; Dascălu, A.; Profire, B.-Ș.; Vasincu, I.-M.; Apotrosoaei, M.; Gîscă, T.-C.; Turin-Moleavin, I.-A.; et al. New Chitosan-Based Co-Delivery Nanosystem for Diabetes Mellitus Therapy. Polymers 2024, 16, 1825. https://doi.org/10.3390/polym16131825

Diabetes mellitus is a chronic metabolic disorder characterized by persistent hyperglycemia, resulting from decreased insulin secretion, insulin resistance, or both. It is mainly represented by type 2 diabetes, which accounts for more than 90% of all cases. Chronic hyperglycemia associated with diabetes mellitus can lead to severe complications such as blindness, kidney failure, heart disease, stroke, and gangrene, often requiring foot amputation.

New therapeutic approaches are needed because the global prevalence of diabetes mellitus is increasing, partly due to lifestyle factors. Current treatments may not adequately address the associated risk factors, including oxidative stress, dyslipidemia, mitochondrial dysfunction, and micro/macrovascular complications. Therefore, there is a need for therapies that can provide optimal glycemic control and manage these associated risk factors effectively.

Pioglitazone (Pio) is an antidiabetic drug that works primarily by reducing insulin resistance. Curcumin (Cur) is a powerful antioxidant with significant blood sugar-lowering effects. However, both drugs have their limitations when used alone. Pio has lower bioavailability and a short half-life, while Cur is unstable and poorly soluble in water, which limits its therapeutic use.

This can be improved by encapsulation in e.g. chitosan-based nanoparticles. Nanoparticles can improve the solubility, bioavailability and stability of drugs, particularly in connection with the treatment of diabetes mellitus. Chitosan is particularly well suited for this purpose due to its excellent biocompatibility and biodegradability. It is also non-toxic and has an antibacterial effect.

For these reasons, chitosan nanoparticles for the co-transport of pioglitazone and curcumin were developed and characterized in the following study. A low molecular weight chitosan (MW = 50-190 kDa, 75-85% degree of deacetylation and 20-300 cP viscosity) was used. Comparable and also more narrowly specified chitosan can be found in our shop.

Results

• Amorphous State of APIs: The XRD study demonstrated that the active pharmaceutical ingredients (APIs), Curcumin (Cur) and Pioglitazone (Pio), loaded into the chitosan nanoparticles (CTS NPs) were in an amorphous state, which could improve their solubility and bioavailability compared to their crystalline state
• Successful Loading and Interaction: FT-IR spectroscopy confirmed the successful loading of the APIs into the CTS matrix, with observed shifts in characteristic peaks indicating interactions between the APIs and CTS in the CTS-Pio-Cur NPs
• In Vitro Release and Absorption: The in vitro release studies in different simulated fluids (SGF, SIF, and SCF) indicated that the developed CTS-APIs NPs are suitable for oral administration, showing good absorption in the gastrointestinal tract

Summary: The study concluded that the developed chitosan-based nanoparticles (CTS-Pio-Cur NPs) for co-delivery of Pioglitazone and Curcumin showed improved solubility, bioavailability, and controlled release of the APIs, making them suitable candidates for multitarget antidiabetic therapy.

Link to article: https://www.mdpi.com/2073-4360/16/13/1825