Enhanced bioavailability and biosafety of cannabidiol nanomicelles for effective anti-inflammatory therapy
Source abstract
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.
Source: expertdata · Quality: candidate unverified · Source record ↗
Research context
OpenAlex topics: Cannabis and Cannabinoid Research
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
References (32)
Show source-provided references
1. Amphiphilic block copolymers for drug delivery10.1002/jps.10397 ↗
2. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability10.1023/A:1016212804288 ↗
3. Cannabidiol reduces host immune response and prevents cognitive impairments in Wistar rats submitted to pneumococcal meningitis10.1016/j.ejphar.2012.09.053 ↗
4. Bioactive glass/poloxamer 407 hydrogel composite as a drug delivery system: The interplay between glass dissolution and drug release kinetics10.1016/j.colsurfb.2021.111934 ↗
5. The oxidation of phytocannabinoids to cannabinoquinoids10.1021/acs.jnatprod.9b01284 ↗
6. The neuroprotective effect of cannabidiol in an in vitro model of newborn hypoxic-ischemic brain damage in mice is mediated by CB(2) and adenosine receptors10.1016/j.nbd.2009.10.023 ↗
7. Pre-treatment twice with liposomal clodronate protects against acetaminophen hepatotoxicity through a pre-conditioning effect10.1016/j.livres.2020.07.002 ↗
8. ATP and adenosine: Role in the immunopathogenesis of rheumatoid arthritis10.1016/j.imlet.2019.08.009 ↗
9. A review of poloxamer 407 pharmaceutical and pharmacological characteristics10.1007/s11095-006-9104-4 ↗
10. In vitro and in vivo models for the study of oral delivery of nanoparticles10.1016/j.addr.2013.01.003 ↗
11. Impact of differential particle size of fenofibrate nanosuspensions on biopharmaceutical performance using physiologically based absorption modeling in rats10.1016/j.jddst.2020.102040 ↗
12. Nevirapine loaded Poloxamer 407/Pluronic P123 mixed micelles: Optimization of formulation and in vitro evaluation10.1016/j.colsurfb.2015.03.030 ↗
13. Effect of particle size reduction on dissolution and oral absorption of a poorly water-soluble drug, cilostazol, in beagle dogs10.1016/j.jconrel.2005.11.013 ↗
14. The profile of immune modulation by cannabidiol (CBD) involves deregulation of nuclear factor of activated T cells (NFAT)10.1016/j.bcp.2008.06.022 ↗
15. Preparation and characterization of Syringic acid-loaded TPGS liposome with enhanced oral bioavailability and in vivo antioxidant efficiency10.1208/s12249-019-1290-6 ↗
16. Polymeric micelles and alternative nanonized delivery vehicles for poorly soluble drugs10.1016/j.ijpharm.2012.08.042 ↗
17. Uniform nano-sized valsartan for dissolution and bioavailability enhancement: Influence of particle size and crystalline state10.1016/j.ijpharm.2012.12.025 ↗
18. The nonpsychoactive cannabis constituent cannabidiol is an oral anti-arthritic therapeutic in murine collagen-induced arthritis10.1073/pnas.160105897 ↗
19. Role of pharmacokinetic and pharmacodynamic parameters in neuroadaptations induced by drugs of abuse, with a focus on opioids and psychostimulants10.1016/j.neubiorev.2018.06.006 ↗
20. Mucoadhesive nanostructured lipid carriers as a cannabidiol nasal delivery system for the treatment of neuropathic pain10.1016/j.ejps.2020.105698 ↗
21. Cannabidiol—recent advances10.1002/cbdv.200790147 ↗
22. Molecular characterization of a peripheral receptor for cannabinoids10.1038/365061a0 ↗
23. RNA nanotechnology to solubilize hydrophobic antitumor drug for targeted delivery
24. Increases in drug and opioid overdose deaths—United States, 2000–201410.15585/mmwr.mm6450a3 ↗
25. Design, optimization, characterization and in-vivo evaluation of Quercetin enveloped Soluplus(R)/P407 micelles in diabetes treatment10.1080/21691401.2018.1501379 ↗
26. The proposed multimodal mechanism of action of cannabidiol (CBD) in epilepsy: Modulation of intracellular calcium and adenosine-mediated signalling10.1016/j.yebeh.2019.08.009 ↗
27. Effect of size and pegylation of liposomes and peptide-based synthetic lipoproteins on tumor targeting10.1016/j.nano.2017.04.009 ↗
28. Cannabidiol displays unexpectedly high potency as an antagonist of CB1 and CB2 receptor agonists in vitro10.1038/sj.bjp.0707133 ↗
29. Formulation development, stability and anticancer efficacy of core-shell cyclodextrin nanocapsules for oral chemotherapy with camptothecin10.3762/bjoc.11.22 ↗
30. Luteolin alters macrophage polarization to inhibit10.1007/s10753-019-01099-7 ↗
31. Predicting drug disposition via application of BCS: Transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system10.1007/s11095-004-9004-4 ↗
32. Asperosaponin VI inhibits LPS-induced inflammatory response by activating PPAR-gamma pathway in primary microglia10.1016/j.sjbs.2020.07.013 ↗