Quinapyramine Sulfate-Loaded Sodium Alginate Nanoparticles Show Enhanced Trypanocidal Activity

Abstract

Aim: To reduce the dose, toxic effects and to ensure sustained release of quinapyramine sulfate (QS), a highly effective drug against Trypanosoma evansi. Materials & methods: QS-loaded sodium alginate nanoparticles (QS-NPs) were formed by emulsion-crosslinking technology using dioctyl-sodium-sulfosuccinate and sodium alginate. The formulation was characterized for size, stability, morphology and functional groups by a zetasizer, scanning electron microscopy, atomic force microscopy, transmission electron microscopy and Fourier transform infrared spectroscopy. In vitro safety and toxicity studies were performed by metabolic assay in Vero cell lines, and in vivo efficacy was evaluated in mice. Results: QS-NPs were <60 nm with 96.48% entrapment efficiency and 3.70% drug loading. The formulation showed an initial burst effect followed by slow drug release in accordance with quasi-Fickian Higuchi diffusion mechanism. QS-NPs were much less toxic and able to clear the parasite at a much lower concentration than QS. Conclusion: The QS-NPs synthesized are safe, less toxic and highly effective compared with QS.

Original submitted 18 December 2012; Revised submitted 18 July 2013

Keywords::

• nanoparticle
• quinapyramine sulfate
• sodium alginate
• Trypanosoma evansi

Financial & competing interests disclosure

The financial support from the Department of Science and Technology, Government of India, in the form of the research project ‘Synthesis, characterization and evaluation of drug-loaded nanoformulations against Trypanosoma evansi in animal model’ under nanomission programme is highly acknowledged. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

The authors state that they have obtained appropriate institutional review board approval or have followed the principles outlined in the Declaration of Helsinki for all human or animal experimental investigations.

Notes

In vitro release data were fitted into four different mathematical models for drug release kinetics. The Korsmeyer–Peppas equation is Mt/M∞ = ktⁿ, where Mt is the amount of drug release at time t, M∞ is the total amount of drug present in formulation, k is the release rate constant and n is the diffusion exponent indicating the mechanism of drug release.

Additional information

Funding

The financial support from the Department of Science and Technology, Government of India, in the form of the research project ‘Synthesis, characterization and evaluation of drug-loaded nanoformulations against Trypanosoma evansi in animal model’ under nanomission programme is highly acknowledged. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.