Lipid nanoparticles as an emerging platform for cannabinoid delivery: physicochemical optimization and biocompatibility

Abstract

This work aims at developing and optimizing a valuable oral delivery carrier for the cannabinoid derivative CB13, which presents a high therapeutic potential in chronic pain states that respond poorly to conventional analgesics, but also shows highly unfavorable physicochemical properties. CB13-loaded lipid nanoparticles (LNP) formulations were developed through solvent-emulsion evaporation and optimized in terms of physicochemical properties, long-term stability, integrity under gastric simulated conditions and in vitro interaction with NIH 3T3, HEK 293T and Caco-2 cells. An optimized formulation of LNP containing CB13 was obtained from a wide range of conditions assayed and analyzed. The selection of the lipid core, production conditions and the inclusion of lecithin proved to be key factors for the final properties of encapsulation, integrity and performance of the carriers. The LNP formulation proposed proved to be a promising carrier for the oral delivery of CB13, a cannabinoid with high therapeutic potential in chronic pain states that currently lack a valid oral treatment.

• Lipid carriers
• nanoparticle formulation
• neuropathic pain
• oral delivery
• poor soluble drugs

Acknowledgements

The authors specially thank the Microscopy services of CITIUS (University of Seville) for technical assistance.

Declaration of interest

This work was supported by Junta Andalucía, Spain (Project Nr. P09-CTS5029) and Fundação para a Ciência e Tecnologia, Portugal (PEst-OE/SAU/UI4013/2011) and the PhD grants of M. Durán-Lobato (USE-09090-M) and R. Lopes (SFRH/BD/44218/2008).