Diatomite as a potential drug carrier for Itraconazole and improvement in release control

Many obstacles associated with the use of conventional drug delivery systems have led to the development of new various micro/nano sized drug carriers, such as microcapsules and nanoparticles. These carriers are designed with the aim to improve therapeutic outcomes and/or reduce drug’s adverse effects, by providing protection of the entrapped drug against in vivo degradation, releasing drug in desired man­ner, improving drug solubility and/or reducing its immunogenicity. Additionally, their

small sizes make these carriers when loaded with the bioactive molecules suitable for different routes of administration allowing their vectorization to the target site.

In this work, Diatomite (DTM) was used as a support material for Itraconazole (ITZ) which is known for its fairly low side effects. The major drawback in the therapeutic application and efficacy of ITZ as oral dosage forms is its very low aqueous solubility which is related to its hydrophobic structure.

Three Binary systems were prepared using different proportions of the two components and where tested for the ability of DTM material to improve the solubility of ITZ in aqueous solvents and in organic media. The efficacy of encapsulation was demonstrated by standard methods such as extraction and UV analysis. The prepared systems were characterized using UV-Vis, FTIR, MEB, AFM and Optical microscopy. Moreover, the study of kinetics and mechanism of drug release in the gastric medium exhibit a sustained profile during a time of two hours.