Evaluation of Organogel Nanoparticles as Drug Delivery System for Lipophilic Compounds

Abstract : The purpose of the study was to evaluate organogel nanoparticles as a drug delivery system by investigating their stability, according to the formulation strategy, and their release profile. The gelled nanoparticles were prepared by hot emulsification (above the gelation temperature) of an organogel in water, and cooling at room temperature. In the first step, we used DLS and DSC to select the most suitable formulations by optimizing the proportion of ingredients (HSA, PVA, castor oil) to obtain particles of the smallest size and greatest stability. Then, two lipophilic drug models, indomethacin and ketoconazole were entrapped in the nanoparticles made of castor oil gelled by 12-hydroxystearic acid. Thermal studies (DSC) confirmed that there was no significant alteration of gelling due to the entrapped drugs, even at 3% w/w. Very stable dispersions were obtained (>3 months), with gelled oil nanoparticles presenting a mean diameter between 250 and 300 nm. High encapsulation efficiency (>98%) was measured for indomethacin and ketoconazole. The release profile determined by in vitro dialysis showed an immediate release of the drug from the organogel nanoparticles, due to rapid diffusion. The study demonstrates the interest of these gelled oil nanoparticles for the encapsulation and the delivery of lipophilic active compounds.
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Baptiste Martin, Fabien Brouillet, Sophie Franceschi, Emile Pérez. Evaluation of Organogel Nanoparticles as Drug Delivery System for Lipophilic Compounds. AAPS PharmSciTech, American Association of Pharmaceutical Scientists, 2017, 18 (4), pp.1261-1269. ⟨10.1208/s12249-016-0587-y⟩. ⟨hal-02195496⟩

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