4.3 Article

Solubility Enhancement and Antioxidation Maintenance of CBD Encapsulated in the P407-RUB Nano-micelle System

Journal

CURRENT DRUG DELIVERY
Volume 21, Issue 2, Pages 271-282

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1567201820666230330090025

Keywords

Nano-micelle system; solubilizer; rubusoside; cannabidiol; Sativex; Epidiolex

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This study aimed to improve the water solubility and stability of cannabidiol (CBD) using micelle technology. CBD-loaded mixed micelles (CBD-M) composed of Poloxamer 407 (P407) and rubusoside (RUB) were successfully prepared and showed significant improvement in solubility and encapsulation efficiency. The CBD-M solution remained stable and maintained the antioxidant activity of CBD after dilution and centrifugation. These findings suggest that CBD-M could serve as a promising formulation for enhanced CBD delivery.
Aim: The aim of this study is to improve the water solubility and stability of cannabidiol (CBD) utilizing micelle technology. Materials and Methods: Mixing of rubusoside (RUB) with Poloxamer 407 (P407) was explored as the wall material for the preparation of CBD micelles. In this study, CBD-loaded mixed micelles (CBD-M) composed of P407 and RUB was successfully formed by self-assembly then solid were prepared by solvent evaporation. The saturated solubility of CBD-loaded micelles in water increased to 15.60 mg/mL, 1560-fold compared with its intrinsic solubility (0.01 mg/mL). The average size of CBD-M was 103 +/- 2.66 nm and the encapsulation efficiency for CBD was 92.8 +/- 4.7%, and 18.6 +/- 0.94% for drug-loading. Results: The morphology and encapsulation of CBD-M were characterized by TEM, FI-IR, DSC and TG. The CBD-M solution was stable and CBD-M did not precipitate or leak after being diluted and centrifugated. Besides, CBD-M solution was stable for 6 months at 4 degrees C and room temperature. In vitro antioxidant studies found that the antioxidant activity of CBD remained at the same level after micellization. Conclusion: These results suggest that CBD-M may be a promising and competitive formulation for the delivery of CBD, laying a foundation for improving the bioavailability in the future.

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