Solid lipid nanoparticles for Anle 138b administration in Parkinson disease: towards an industrial scale up with nutraceutical formulations

INTRODUCTION Anle 138b, a novel drug for geriatric application in Parkinson's disease (PD), suffers from low water solubility and, hence, low bioavailability (1-2). Therefore, the research on novel water-soluble products as a vehicle for Anle 138b still represents a challenge for the neurological disorder of PD. The current study focused on some formulations consisting of solid lipid nanoparticles (SLNs) allowing the administration of Anle 138b combined with nutraceutical components, evaluated in vitro for their stability under storage in different conditions (3).

METHODS Via dynamic light scattering apparatus, the particle size evolution of the SLNs over 2 months was monitored during the storage time. Furthermore, via spectrophotometric quantification, drug content analysis allowed us to monitor the changes in the Anle 138b concentrations in order to identify the most promising formulation among the tested ones. For cytocompatibility assessment, by using the MTT test, differentiated SH-SY5Y cells were treated for 24 hours with SLN-Anle 138b in the presence of a multicomponent nutraceutical formulation.

RESULTS Viscous vegetal extract combined with SLN-Anle 138b was difficult to handle after seven days, whereas a less dense tested formulation was flocculated after one month of storage at 4 °C. In differentiated SH-SY5Y cells, a multicomponent nutraceutical formulation was well tolerated for 24 h, when combined with SLN-Anle 138b in the range of 1 and 10 µM.

CONCLUSIONS Candidate industrial products combining nutraceuticals and SLN-Anle 138b were evaluated for administration via the nasal route in PD patients, indicating the potential of a multicomponent preparation for non-invasive treatments.

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