Abstract

Purpose: To formulate Cannabis sativa-based syrup and investigate its anti-inflammatory potential and the stability of the formulation under stress conditions.Methods: The syrup was prepared using different combinations of crude C. sativa resin, propylene glycol, aspartame, sucrose, sodium metabisulphite (SMBs) and ethylenediaminetetraacetic acid (EDTA). The stability of the formulations was determined under accelerated temperature conditions. The anti-inflammatory activity of the resin and different formulations were evaluated by the egg albumin induced paw edema model in rats. Biochemical assay was determined by Reitman and Frankel colorimetric assay method while hematological assay was evaluated by standard protocols.Results: EDTA-containing syrup (CE) was the most stable with estimated shelf-life of 2204 days (K25ºC, 4.78 x 10-5/day). Higher propylene glycol levels significantly improved anti-inflammatory activity compared to those containing a lower amount. All the formulations showed anti-inflammatory activity higher than the crude resin with a dose-dependent inhibition of paw edema compared with the control. There was no significant difference (p < 0.05) between the serum glutamate-oxaloacetate transaminase (SGOT, 13.821 ± 0.190 - 16.008 ± 1.012), serum glutamate-pyruvate transaminase (SGPT, 19.241 ± 1.027 - 22.901 ± 1.093) and urea (9.812 ± 0.252 - 10.054 ± 0.252) levels of the treated and 16.856 ± 1.053, 24.960 ± 0.101 and 10.654 ± 0.925 units/L of the control animals respectively. With the exception of eosinophil that disappeared from the blood in the third week, all the hematological parameters showed a gradual increase in lymphocytes, neutrophils, monocytes, packed cell volume (PCV), white and red blood cell counts in the third week compared to control.Conclusion: Formulation of C. sativa as syrup using efficient carriers improves the pharmacological activity of the crude extract. SMBs and EDTA significantly enhance the stability of the syrup with no observable biochemical and hematological changes in treated animalsKeywords: Cannabis sativa, Syrup, Anti-inflammatory, Stability, Hematological

Highlights

  • Cannabis sativa remains one of the most influential strictly controlled and multi-constituent plants with multiple medicinal uses [1], yet its place in therapy has remained highly controversial [2] due to strict legislation against its use [3], controversial moral implications on itsMany researchers are of the opinion that purified Cannabis and its preparation could find their way into the armamentarium of therapeutic agents while ensuring that illegal use or abuse is completely discouraged [6]

  • The crude Cannabis sativa resin and its various syrup formulations caused varying degrees of suppression of paw edema in rats compared to control with somewhat dose-dependent effects in most cases

  • The stability of syrups is important because their physicochemical properties depend on excipients employed in preparation and was assessed by determining the amount of initial concentration degraded after certain time under stressed conditions

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Summary

INTRODUCTION

Cannabis sativa remains one of the most influential strictly controlled and multi-constituent plants with multiple medicinal uses [1], yet its place in therapy has remained highly controversial [2] due to strict legislation against its use [3], controversial moral implications on its. Against the backdrop that pharmacological (antiinflammatory) activity of Cannabis could be controlled by complex pharmacodynamic systems as well as pharmacokinetics of the extract, we formulated crude Cannabis extract syrup using different vehicles, assessed the antiinflammatory performances and its biochemical and hematological parameters in experimental animals, and the stability of the formulations with a view to improving the anti-inflammatory activity of Cannabis extracts. CCR=crude Cannabis extract formulated at two different concentration levels 1 (5 mg/mL) and 2 (10 mg/mL) with sodium metabisulphite SMBs (CB) and//or EDTA (CE) or base formula (CS). The antiinflammatory activities (rat paw sizes in mm), biochemical parameters (SGOT, SGPT and urea in units/L) and hematological parameters (WBC in cells/μL, RBC, lymphocytes, monocytes, neutrophils, eosinophil in units/μL and PCV in %) were expressed as a mean ± standard deviation from the mean (SD) (n=5), Student’s t-test was done to test for the significant difference between the means of samples and control at p

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