Development, Characterization and In Vitro Gastrointestinal Release of PLGA Nanoparticles Loaded with Full-Spectrum Cannabis Extracts

• Published in: AAPS PharmSciTech 2024-05, Vol.25 (5), p.120, Article 120
• Main Authors: Villate, Aitor, Barreto, Gastón Pablo, Nicolás, Markel San, Aizpurua-Olaizola, Oier, Olivares, Maitane, Usobiaga, Aresatz
• Format: Article
• Language: English
• Subjects: Alginates - chemistry; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Cannabidiol - chemistry; Cannabinoids - chemistry; Cannabis - chemistry; Chemistry, Pharmaceutical - methods; Chitosan - chemistry; Drug Carriers - chemistry; Drug Liberation; Gastrointestinal Tract - metabolism; Lactic Acid - chemistry; Nanocapsules - chemistry; Nanoparticles - chemistry; Particle Size; Pectins - chemistry; Pharmacology/Toxicology; Pharmacy; Plant Extracts - chemistry; Polyglycolic Acid - chemistry; Polylactic Acid-Polyglycolic Acid Copolymer - chemistry; Research Article
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-024-02836-4

Cannabinoids, such as ∆ 9 -tetrahydrocannabinol (THC) and cannabidiol (CBD), are effective bioactive compounds that improve the quality of life of patients with certain chronic conditions. The copolymer poly(lactic-co-glycolic acid) (PLGA) has been used to encapsulate such compounds separately, providing pharmaceutical grade edible products with unique features. In this work, a variety of PLGA based nanoformulations that maintain the natural cannabinoid profile found in the plant (known as full-spectrum) are proposed and evaluated. Three different cannabis sources were used, representing the three most relevant cannabis chemotypes. PLGA nanocapsules loaded with different amounts of cannabinoids were prepared by nanoemulsion, and were then functionalized with three of the most common coating polymers: pectin, alginate and chitosan. In order to evaluate the suitability of the proposed formulations, all the synthesized nanocapsules were characterized, and their cannabinoid content, size, zeta-potential, morphology and in vitro bioaccessibility was determined. Regardless of the employed cannabis source, its load and the functionalization, high cannabinoid content PLGA nanocapsules with suitable particle size and zeta-potential were obtained. Study of nanocapsules’ morphology and in vitro release assays in gastro-intestinal media suggested that high cannabis source load may compromise the structure of nanocapsules and their release properties, and hence, the use of lower content of cannabis source is recommended. Graphical Abstract