Up to 8%5 of the European population and approximately 3.8 million individuals in the United States6 are affected by Neuropathic pain (NP). NP is generally chronic and disabling and challenging to treat with only 40-60% of patients achieving partial relief7 . Neuropathic pain may arise as a consequence of a lesion or disease affecting the somatosensory system and could be CNS or PNS related8 . The management of patients with chronic NP is complex and response to existing treatments often inadequate9 . Common therapeutics include antidepressants, antiepileptic, opioids and tramadol. The therapeutic potential of cannabinoids has recently been investigated following the discovery of the endocannabinoid system and is gaining clinical acceptance to improve NP outcomes, particularly for CB2 receptors agonists which have shown to produce antinociception without psychotropic effect10-14. Synthetic and natural cannabinoids compounds are generally lipophilic in nature and evidence indicates that lipophilicity may be of importance for potentializing their therapeutic activity15-16. Furthermore, pharmacological activity of a drug is the result of affinity and interaction with its biological target but also optimum and reliable exposure at the target site. Appropriate drug delivery system (DDS) are thereby required to deliver the drug at a sufficient concentration to the site of action. The goals of this research project were 1) to design, develop and study an early drug delivery system allowing in vivo PK and PD studies of a selective CB2 agonist recently synthesized in our laboratory, 2) to design and elaborate a DDS based on cationic nanocapsules for a highly lipophilic natural CB2 agonist for future theragnostic applications.