Abstract
Aim
Thiocolchicoside (THC) is a drug under the category of BCS III. Due to its high molecular weight, it has poor oral bioavailability and low skin permeability. This study aims to find an alternative delivery method for THC that enhances its bioavailability through nasal application approach. In situ gels containing plain or liposomal THC with different combinations of Pluronic® F127 and PEG 400 were prepared.
Method
Liposome formulations were prepared using the thin film hydration method and tested for their characterization such as for drug content, particle size, and zeta potential. In vivo pharmacokinetic parameters of formulations such as Cmax, Tmax, and AUC were tested on the rabbit model. The formulations were also scrutinized for their cell viability properties.
Result
Formulation composition with 2% soybean phosphatidylcholine and 10 mg THC exhibited ∼94% entrapment efficiency, minimum particle size 101.32 nm, low polydispersity index 0.225 and +0.355 zeta potential. In situ liposomal dispersion containing 15% Pluronic® F127 turned into gel at nasal temperature. Cell lines were unharmed for 48 h. İn situ liposomal gels showed 1.5x higher blood concentration than the control formula.
Conclusion
In situ gels of liposomal THC formulations offer advantages over traditional nasal solutions, demonstrating comparable bioavailability to parenteral medication while also preserving the health of nasal mucosa cells.
Acknowledgements
The authors express their gratitude to The Scientific and Technological Research Council of Türkiye (TUBITAK) for the funding and to the Yeditepe University Experimental Research Center (YUDETAM).
Authors’ contributions
BU, JB, CT: methodology, validation, data curation, formal analysis. BU, JB: imaging and instrumentation; BU, JB, CT: animal study and data interpretation, BU, JB, CT: conceptualization, methodology, writing—review and editing, supervision, formal analysis.
Consent for publication
All authors agree to publish this article in Pharmaceutical Development and Technology.
Disclosure statement
The authors declare no competing interests.
Ethics statement
The study has been approved by the Yeditepe University Animal Experiments Local Ethics Committee (Approval No.2020-868)