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Formulation and In Vitro-Ex vivo Evaluation of Cannabidiol and Cannabidiol-Valine-Hemisuccinate Loaded Lipid-Based Nanoformulations for Ocular Applications.
- Source :
-
International journal of pharmaceutics [Int J Pharm] 2024 May 25; Vol. 657, pp. 124110. Date of Electronic Publication: 2024 Apr 10. - Publication Year :
- 2024
-
Abstract
- The goal of this investigation is to develop stable ophthalmic nanoformulations containing cannabidiol (CBD) and its analog cannabidiol-valine-hemisuccinate (CBD-VHS) for improved ocular delivery. Two nanoformulations, nanoemulsion (NE) and nanomicelles (NMC), were developed and evaluated for physicochemical characteristics, drug-excipient compatibility, sterilization, thermal analysis, surface morphology, ex-vivo transcorneal permeation, corneal deposition, and stability. The saturation solubility studies revealed that among the surfactants tested, Cremophor EL had the highest solubilizing capacity for CBD (23.3 ± 0.1 mg/mL) and CBD-VHS (11.2 ± 0.2 mg/mL). The globule size for the lead CBD formulations (NE and NMC) ranged between 205 and 270 nm while CBD-VHS-NMC formulation had a particle size of about 78 nm. The sterilized formulations, except for CBD-VHS-NMC at 40 °C, were stable for three months of storage (last time point tested). Release, in terms of CBD, in the in-vitro release/diffusion studies over 18 h, were faster from the CBD-VHS nanomicelles (38 %) compared to that from the CBD nanoemulsion (16 %) and nanomicelles (33 %). Transcorneal permeation studies revealed improvement in CBD permeability and flux with both formulations; however, a greater improvement was observed with the NMC formulation compared to the NE formulation. In conclusion, the nanoformulations prepared could serve as efficient topical ocular drug delivery platforms for CBD and its analog.<br />Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2024. Published by Elsevier B.V.)
- Subjects :
- Animals
Rabbits
Micelles
Valine analogs & derivatives
Valine chemistry
Valine administration & dosage
Valine pharmacokinetics
Drug Liberation
Lipids chemistry
Excipients chemistry
Permeability
Chemistry, Pharmaceutical methods
Drug Compounding methods
Surface-Active Agents chemistry
Ophthalmic Solutions administration & dosage
Cannabidiol administration & dosage
Cannabidiol chemistry
Cannabidiol pharmacokinetics
Cornea metabolism
Cornea drug effects
Administration, Ophthalmic
Nanoparticles chemistry
Emulsions
Solubility
Drug Stability
Particle Size
Subjects
Details
- Language :
- English
- ISSN :
- 1873-3476
- Volume :
- 657
- Database :
- MEDLINE
- Journal :
- International journal of pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 38604539
- Full Text :
- https://doi.org/10.1016/j.ijpharm.2024.124110