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In Situ Gelling Hydroxypropyl Cellulose Formulation Comprising Cannabidiol-Loaded Block Copolymer Micelles for
Katya Kamenova1, Denitsa Momekova2, Georgy Grancharov1
1Institute of Polymers, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.
International Journal of Molecular Sciences
|November 25, 2023
Summary
This study developed a novel hydroxypropyl cellulose-based in situ gelling formulation to improve cannabidiol (CBD) solubility and delivery. The injectable nanocomposite hydrogels offer prolonged drug release and maintained cytotoxicity for enhanced therapeutic applications.
Area of Science:
- Drug Delivery and Pharmaceutical Technology
- Polymer Science and Engineering
- Nanotechnology
Background:
- Cannabidiol (CBD) is a pharmacologically active compound with limited medical use due to poor water solubility.
- Polymeric nanocarriers show promise for improving the solubility and efficacy of lipophilic drugs like CBD.
- Developing advanced drug delivery systems is crucial for unlocking CBD's therapeutic potential.
Purpose of the Study:
- To create a novel hydroxypropyl cellulose (HPC)-based in situ gelling formulation for controlled cannabidiol (CBD) delivery.
- To enhance CBD solubility and therapeutic activity using polymeric nanocarriers and nanocomposite hydrogels.
- To evaluate the drug release profile and cytotoxicity of the developed CBD-loaded in situ gels.
Main Methods:
- Fabrication of nanosized polymeric micelles using PEO-b-P(CyCL-co-CL) diblock copolymers for CBD encapsulation.
- Optimization of hydroxypropyl cellulose (HPC) sol-to-gel transition using K2SO4 for in situ gel formation under physiological conditions.
- Characterization of injectable nanocomposite hydrogels, including drug release studies and in vitro cytotoxicity assays against human tumor cell lines.
Main Results:
- Selected PEO-b-P(CyCL-co-CL) copolymers effectively increased CBD solubility with high encapsulation efficiency and drug loading capacity.
- Optimal HPC-based formulations formed physical gels under physiological conditions, confirmed by microcalorimetry and rheology.
- The developed injectable in situ gels demonstrated prolonged CBD release over 12 hours, primarily controlled by gel erosion.
- Formulated CBD exhibited comparable cytotoxicity to free CBD against tested human tumor cell lines.
Conclusions:
- Novel HPC-based in situ gelling systems effectively encapsulate CBD within polymeric micelles, significantly enhancing its solubility.
- The developed injectable nanocomposite hydrogels provide a promising platform for controlled and sustained delivery of cannabidiol.
- The formulation maintains the therapeutic efficacy of CBD, as evidenced by its comparable cytotoxicity to the free drug, paving the way for improved pharmaceutical applications.
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