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1.
Int J Pharm ; 660: 124370, 2024 Jul 20.
Article de Anglais | MEDLINE | ID: mdl-38906498

RÉSUMÉ

Limited attempts have been made previously to develop high-loading CBD inhalable powders, which are essential for high dose delivery. Therefore, this study aimed to develop and characterise inhalable powders with ≥ 95 % w/w CBD by wet ball milling. The effects of magnesium stearate (2 % and 5 %) and inhaler resistance (low-resistance and high-resistance RS01 inhalers) on aerosol performance were also compared. Wet ball milling produced CBD powders with > 50 % production yield. The milled particles showed irregular shapes. The powders were crystalline with minimal amorphous content, low residual solvent level (<1%), and low moisture sorption (<4%). Magnesium stearate improved both the emitted and fine particle fractions. The aerodynamic particle size distribution of the formulations differed between the low-resistance and high-resistance RS01 inhalers. The latter decreased throat deposition but increased inhaler retention. The dissolution profiles showed that all three formulations released CBD steadily and plateaued at 30 min. The best scenario was CBD with 5 % magnesium stearate dispersed from the high resistance RS01 inhaler, showing the highest FPF with the lowest throat deposition. This combination may be tested in vivo in the future to investigate its pharmacokinetic profile.


Sujet(s)
Cannabidiol , Taille de particule , Poudres , Acides stéariques , Administration par inhalation , Acides stéariques/composition chimique , Cannabidiol/administration et posologie , Cannabidiol/composition chimique , Cannabidiol/pharmacocinétique , Aérosols , Inhalateurs à poudre sèche , Excipients/composition chimique , Chimie pharmaceutique/méthodes , Libération de médicament , Nébuliseurs et vaporisateurs , Préparation de médicament/méthodes , Solubilité
2.
Pharm Res ; 40(5): 1087-1114, 2023 May.
Article de Anglais | MEDLINE | ID: mdl-36635488

RÉSUMÉ

The use of cannabidiol (CBD) for treating brain disorders has gained increasing interest. While the mechanism of action of CBD in these conditions is still under investigation, CBD has been shown to affect numerous different drug targets in the brain that are involved in brain disorders. Here we review the preclinical and clinical evidence on the potential therapeutic use of CBD in treating various brain disorders. Moreover, we also examine various drug delivery approaches that have been applied to CBD. Due to the slow absorption and low bioavailability with the current oral CBD therapy, more efficient routes of administration to bypass hepatic metabolism, particularly pulmonary delivery, should be considered. Comparison of pharmacokinetic studies of different delivery routes highlight the advantages of intranasal and inhalation drug delivery over other routes of administration (oral, injection, sublingual, buccal, and transdermal) for treating brain disorders. These two routes of delivery, being non-invasive and able to achieve fast absorption and increase bioavailability, are attracting increasing interest for CBD applications, with more research and development expected in the near future.


Sujet(s)
Encéphalopathies , Cannabidiol , Voies d'administration de substances chimiques et des médicaments , Humains , Encéphale , Encéphalopathies/traitement médicamenteux , Cannabidiol/administration et posologie , Cannabidiol/pharmacocinétique , Cannabidiol/usage thérapeutique
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