Delta-9-tetrahydrocannabinol (THC) is one of the most effective antinociceptive agents used in the treatment of peripheral neuropathy. THC is highly lipophilic and susceptible to thermal and oxidative degradation. Identifying appropriate solvents in which THC is stable as well as adequately solubilized is crucial in developing topical dosage forms. Lipid solvent systems are of utmost utility and relevance for formulating highly lipophilic drugs. Hence, the objective of this project was to screen the solubility of THC in lipidic excipients, monitor THC content in the selected vehicles during stability, and study the influence of these excipients on permeation of THC across skin. The solubility of THC in liquid lipid excipients was in the range of 421 to 500 mg/g. The solubility of THC in solid lipid excipients was in the range of 250 to 750 mg/g. THC in its neat form was poorly stable, but when dissolved in lipid-based excipients, its stability improved significantly. THC in lipid excipients was more stable at 4 ± 3°C compared to samples stored at 25 ± 2°C. The antioxidants (butylated hydroxytoluene and ascorbyl palmitate) used in the excipients further improved the stability of THC. The results demonstrated that the liquid and solid lipid excipients used in the study could solubilize THC freely and mitigate the degradation of THC significantly. The binary combination of lipid excipients enhanced THC skin permeation and retention, demonstrating the potential for topical formulation development of THC.
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http://dx.doi.org/10.1208/s12249-022-02385-8 | DOI Listing |
Sci Rep
January 2025
Department of Chemistry, Faculty of Science, Gonbad Kavous University, Gonbad Kavous, Iran.
A bright future lies ahead for the application of natural biocomposites in the food industry. In this research, edible biocomposite films were created using sodium caseinate (SC)-gum tragacanth (GT) and incorporating carum carvi seed essential oil (EO) as a nanoemulsion. Different ratios of oil were used as variables.
View Article and Find Full Text PDFAnal Chem
January 2025
School of Chemical Engineering, The University of Adelaide, North Terrace, Adelaide 5005, Australia.
The rise in the popularity of lipid nanoparticle (LNP)-based formulations necessitates the need for screening tools to quickly predict their colloidal stability in the presence of common excipients. Protein chemists have employed the diffusion interaction parameter () determined using dynamic light scattering as an indicator of formulation stability, yet this approach has not been applied to particulate systems. Herein, measurements of LNPs revealed behavior dissimilar to that of proteins.
View Article and Find Full Text PDFNat Nanotechnol
January 2025
Global Regulatory Affairs CMC, Sanofi, Marcy-l'Etoile, France.
Lipid nanoparticles (LNPs) for nucleic acid delivery often use novel lipids as functional excipients to modulate the biodistribution, pharmacokinetics, pharmacodynamics and efficacy of the nucleic acid. Novel excipients used in pharmaceutical products are subject to heightened regulatory scrutiny and often require data packages comparable to an active pharmaceutical ingredient. Although these regulatory requirements may help to ensure patient safety they also create economic and procedural barriers that can disincentivize innovation and delay clinical investigation.
View Article and Find Full Text PDFInt J Pharm
January 2025
Institut Galien Paris-Saclay, CNRS UMR8612, 17 avenue des Sciences, 91400 Orsay, France. Electronic address:
Multiparticulate drug delivery systems offer advantages in controlled release, dose flexibility, and personalized medicine. Fusion prilling, a process that produces spherical lipid-based microparticles through vibrating nozzles, is gaining interest in the field. This study aims to explore the use of fusion prilling to encapsulate crystallizable water-in-oil emulsions, enabling the incorporation of hydrophilic active pharmaceutical ingredients (APIs) within lipid matrices.
View Article and Find Full Text PDFTurk J Pharm Sci
January 2025
Gazi University Faculty of Pharmacy, Department of Pharmaceutical Technology, Ankara, Türkiye.
Objectives: Variations in the types and quantities of excipients used to prepare liposomes can affect the physicochemical properties of liposome formulations. This study aimed to provide information about the design and fabrication of 5-fluorouracil (5-FU)-loaded liposome formulations using different lipid and cholesterol (CHOL) derivatives.
Materials And Methods: Passive loading via a small-volume incubation method was used to prepare liposomes.
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