Abstract
In order to improve the solubility properties of BCS class II drug itraconazole, fast dissolving oral polymeric film formulations based on itraconazole nanocrystals were produced. Drug nanocrystals were manufactured by the wet pearl milling technique. In polymeric film formulations, hydroxypropyl methyl cellulose (HPMC) was used as a film forming polymer, and glycerin was used as a plasticizer. For nanocrystal suspensions and film formulations, thorough physicochemical characterization was performed, including particle sizing and size deviation, film appearance, weight variation, thickness, folding endurance, drug content uniformity, disintegration time, and dissolution profile. After milling, the nanoparticles were 369 nm in size with a PI value of 0.20. Nanoparticles were stable and after redispersion from film formulations, the particle size remained almost the same (330 nm and PI 0.16). The produced films were flexible, homogeneous, fast disintegrating, and drug release rate from both the nanosuspension and film formulations showed immediate release behavior. Based on the study, the film casting method for production of itraconazole nanocrystal based immediate release formulations is a good option for improved solubility.
Highlights
Decreasing the particle size is a very efficient way to improve the solubility of poorly soluble drug materials [1,2]
hydroxypropyl methyl cellulose (HPMC) is well-known for its good film forming ability, and in an earlier study, drug release from HPMC films were found to be fast, due to low viscosity [21]
HPMC E5 LV was selected as a film forming polymer for this study
Summary
Decreasing the particle size is a very efficient way to improve the solubility of poorly soluble drug materials [1,2]. Formation of nanocrystals is just one way to manipulate the raw material, and after nanonization, the final formulation still needs to be made. Nanosuspensions can be used, for ocular drug delivery [3], for example, but, for solid dosage forms, the formulation process is typically a multistage process. Nanosuspensions are formulated to solid dosage forms, like tablets, capsules, granules [4], or more recently, oral polymeric films [5]. For nanocrystal-based drug delivery systems, polymeric films are especially beneficial, while no extra drying step is required—nanosuspensions can be added as such to the polymeric solution for the film casting or 3D printing
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