Novel prolonged release particulate system for transdermal delivery of water-insoluble antifungal drug
Mariia Saveleva,1, Ekaterina Lengert,1, Roman Verkhovskii,1, Anatolii Abalymov,1, Anton Pavlov,1, Sergei Shtykov,1, and Yulia Svenskaya,1
1 Saratov State University, Saratov, Russia
Abstract
A novel particulate system based on the submicron CaCO3 vaterite particles for the transdermal delivery of antifungal drug "Griseofulvin" (GF) was developed. The spherical mesoporous CaCO3 carriers with size of 1.1 μm were synthesized with the GF loading efficiency of 25 % w/w. The cytotoxic effect of the developed carriers was evaluated with fibroblasts and revealed no influence on the cell viability.
In order to inhibit the degradation of CaCO3 carriers and prolong the GF release inside the skin, the carriers’ surface was modified with the biocompatible polyelectrolytes multilayered coating. It was demonstrated, that the formation of polyelectrolyte shell on the carrier surface allowed for the efficient prolongation of drug release kinetics.
The efficiency of the developed particulate system for GF delivery was assessed by the topical application on white rats in vivo. The study of GF urinary excretion profiles in the course of 2 weeks was monitored in vivo in rats. It was revealed, that the polyelectrolyte shell on the carrier surface provided the prolongation of GF therapeutic intervention in vivo up to 244 h, as compared to the uncoated CaCO3 carriers. Thus, the proposed drug delivery system demonstrates the promising perspectives for improving efficiency and safety of topical treatment of dermal diseases.
This study was supported by Russian Science Foundation (project № 17-73-20172).
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Mariia Saveleva
Science Medical Center, Saratov State University
Russia
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