Enhanced bioavailability and biosafety of cannabidiol nanomicelles for effective anti-inflammatory therapy--颗粒学报PARTICUOLOGY

Rao, Y., Li, R., Liu, S., Meng, L., Wu, Q., Yuan, Q., . . . Qin, M. (2022). Enhanced bioavailability and biosafety of cannabidiol nanomicelles for effective anti-inflammatory therapy. Particuology, 69, 1-9. https://doi.org/10.1016/j.partic.2021.11.010

Enhanced bioavailability and biosafety of cannabidiol nanomicelles for effective anti-inflammatory therapy

Yuan Rao ^a, Runwei Li ^a, Saixing Liu ^a, Linchao Meng ^b, Qilin Wu ^b, Qipeng Yuan^a *, Hao Liang ^a *, Meng Qin ^a *

a College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, China
b StarHealth Botanical Technology Corporation, Beijing 100005, China

10.1016/j.partic.2021.11.010

Volume 69, October 2022, Pages 1-9

Received 18 October 2021, Revised 11 November 2021, Accepted 23 November 2021, Available online 6 December 2021, Version of Record 11 December 2021.

E-mail: yuanqp@mail.buct.edu.cn; lianghao@mail.buct.edu.cn; qinmeng550@163.com

Highlights

• Cannabidiol (CBD) nanomicelles with a drug loading of 14.29% were prepared using P407.

• Anti-inflammatory effect of CBD nanomicelles was better than that of CBD.

• No obvious evidence indicated toxicity to the liver and kidney.

• Solubility of CBD was improved.

Abstract

Cannabidiol (CBD) shows great anti-inflammatory potential; however, the hydrophobicity and strong first-pass effect of CBD leads to its extremely low oral bioavailability. Poloxamer 407 (P407) is a triblock copolymer composed of (poly)ethylene oxide (PEO) and (poly)propylene oxide (PPO) sections. It has a PEO-PPO-PEO structure, which is widely used in the preparation of drug delivery systems that are highly biocompatible. When it reaches a certain concentration in water, P407 can self-assemble into a micelle structure containing a hydrophobic core and a hydrophilic shell. A potential approach to enhancing the oral bioavailability of hydrophobic drugs incorporating them into the hydrophilic carrier. We prepared CBD nanomicelles with a drug loading of 14.29% by a cosolvent evaporation method using P407 with appropriate antioxidants. Cell experiments indicated that anti-inflammatory markers (IL-4 and IL-10) increased, while inflammatory markers (TNF-α and IL-6) decreased. Moreover, animal experiments showed that inflammatory cells were inhibited by CBD nanomicelles, and the anti-inflammatory effect of micelles was better than that of CBD, while no obvious evidence indicated toxicity to the liver and kidney.

Graphical abstract

Keywords

CBD; Poloxamer 407; Polymeric micelle; Anti-inflammatory; Cytotoxicity

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