Mesoporous silicates prepared using food-grade surfactants and their application as drugs delivery systems.

Résumé

One of the biggest concerns facing pharmaceutical companies these days is that most of the new drugs candidates suffers from insufficient dissolution rate in biorelevant media, leading to a poor bioavailability. This is one of the major reasons for failure of new drugs in preclinical development. Crystalline form of the drug is usually the main cause of this poorly dissolution rate. To overcome this difficulty, one of the possibilities is to reach a stable amorphized form of the drug for which the solubilization rate was proven to be much more efficient. Since 2001, silica nanostructured particles emerged as an ingenious solution to remedy to the kinetics release issues by stabilization of the amorphized form of the active pharmaceutical ingredient (API). In this work, synthesis of a new silica-based materials was performed by combining the use of a natural structuring agent (saponin) with the innovative aerosol assisted sol-gel process. Saponin from Quillaja Saponaria was selected as structure directing agent because it is a wildly available bio-sourced and biocompatible molecules. Its use could lead to a mesoporous silica material with a nano-structured texture like the materials synthesized with petrochemical (such as Pluronic) sourced surfactants. Hence, it will then be possible to bypass those petrochemical compounds and therefore to have a sustainable synthesis. In the context of API release, the pore size distribution is known to strongly influence the drug release kinetics. To tune the textural properties of materials, a naturally sourced swelling agent was employed as well. The chosen API (itraconazole) was loaded in the synthetized materials. All solids were extensively characterized. In particular, the amorphous state of the API was proven by X-ray diffraction (XRD) coupled with differential scanning calorimetry (DSC) characterization. The most promising materials were tested in vitro under simulated gastric fluid (SGF) conditions with good results in terms of dissolution profile of the selected API.

la date de réponse	18 janv. 2023
langue originale	Anglais
L'institution diplômante	Universite de Namur
Superviseur	Carmela Aprile (Promoteur)