Cannabinoid Formulations and Delivery Systems: Current and Future Options to Treat Pain

Abstract

The field of Cannabis sativa L. research for medical purposes has been rapidly advancing in recent decades and a growing body of evidence suggests that phytocannabinoids are beneficial for a range of conditions. At the same time impressing development has been observed for formulations and delivery systems expanding the potential use of cannabinoids as an effective medical therapy. The objective of this review is to present the most recent results from pharmaceutical companies and research groups investigating methods to improve cannabinoid bioavailability and to clearly establish its therapeutic efficacy, dose ranges, safety and also improve the patient compliance. Particular focus is the application of cannabinoids in pain treatment, describing the principal cannabinoids employed, the most promising delivery systems for each administration routes and updating the clinical evaluations. To offer the reader a wider view, this review discusses the formulation starting from galenic preparation up to nanotechnology approaches, showing advantages, limits, requirements needed. Furthermore, the most recent clinical data and meta-analysis for cannabinoids used in different pain management are summarized, evaluating their real effectiveness, in order also to spare opioids and improve patients’ quality of life. Promising evidence for pain treatments and for other important pathologies are also reviewed as likely future directions for cannabinoids formulations.

A Comprehensive Review on the Techniques for Extraction of Bioactive Compounds from Medicinal Cannabis

“…THCs are the primary psychoactive lipids with an incredibly low water solubility (0.003 mgmL −1 ) [ 32 ]. Therefore, various solubilizers or emulsifiers and advanced nanosized drug delivery systems have been applied to increase their bioavailability [ 33 , 34 , 35 , 36 , 37 , 38 ]. In addition, some formulations are employed to minimise the pharmacokinetic and pharmacodynamic variabilities of cannabinoids [ 39 ].…”

The Transdermal Delivery of Therapeutic Cannabinoids

“…Other methods of cannabinoid administration include intranasal, rectal, and intravenous [15,70]. The rectal administration of THC demonstrated approximately doubled rates of bioavailability compared to oral routes.…”

Cannabis-Based Oral Emulsion for Medical Purposes to Meet the Needs of Patients: Formulation, Quality and Stability

“…Moreover, in recent years, a large part of the literature and research funding has centred on its potentially harmful effects, rather than its use for medical purposes. However, the interest that this latter topic has stimulated is evident when reviewing the growing number of articles published and patents deposited that aim to evaluate the actual medical efficacy of this plant and its components [ 5 , 6 ].…”

“…The molecules of greatest pharmaceutical interest are, however, those in the decarboxylated form, as these are most easily absorbed in the intestine [ 9 ]. The inflorescences, which may be sold in the raw state or prior to grinding, can be vaporised in specifically designed devices, or can undergo extraction to obtain compounds suitable for oral administration [ 2 , 5 , 10 ].…”

“…This variability stems from the application of differing operating protocols during the preparation phase, but also because of the natural variability of Cannabis inflorescences. To minimise the former factor, it is to be hoped that there will soon be a standard production protocol for Cannabis extracts [ 5 , 15 , 16 , 17 , 18 ].…”