article · Pharmaceutics
Clinical applications of 6-gingerol are frequently restricted by its poor solubility and chemical stability. To address these limitations, researchers created and optimized cyclodextrin-functionalised transethoniosomes as a specialised nanocarrier delivery system. Transethoniosomes are ultra-deformable vesicles prepared with ethanol and edge activators, while cyclodextrin functionalisation improves the solubility and stability of encapsulated compounds. Formulations were prepared via the ethanol injection technique with varying components to assess their drug entrapment efficiency and drug release over 24 hours. An optimized formulation, designated as F8, emerged from the evaluation. This formulation exhibited superior entrapment efficiency, permeation, deformability, and physical stability compared to conventional niosomes and other related vesicular formulations. Furthermore, the optimised nanocarrier system demonstrated greater cytotoxic and anti-inflammatory activity than pure 6-gingerol.
Natural compounds such as 6-gingerol possess useful therapeutic properties, but their tendency to break down quickly and dissolve poorly hinders effective use. Developing specialized, highly flexible nano-sized carriers allows these compounds to remain stable, penetrate biological barriers more effectively, and exert stronger anti-inflammatory and cytotoxic effects, which helps make plant-derived bioactive molecules more viable for healthcare treatments.
This work could enable improved delivery vehicles for pharmaceutical or dermatological formulations containing poorly soluble bioactive agents like 6-gingerol. Potential users include drug developers, formulation scientists, and pharmaceutical manufacturers targeting inflammatory conditions. The technology appears to be at an applied and tested, early laboratory stage, having demonstrated in vitro characterisation, stability, and cell-based efficacy without evidence yet of clinical or in vivo testing.
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The poor solubility and stability of 6-gingerol (6-G) could hamper its clinical applications. The aim of the current study was to develop a novel ultra-deformable cyclodextrin-functionalized transethoniosomes (CD-TENs) as a promising delivery system for 6-G. Transethoniosomes (TENs) are flexible niosomes (NVs) due to their content of ethanol and edge activators (EAs). CD-functionalized nanoparticles could improve drug solubility and stability compared to the corresponding nanovesicles. 6-G-loaded ethoniosomes (ENs) were formulated by the ethanol injection technique in the presence and absence of EA and CD to explore the impact of the studied independent variables on entrapment efficiency (EE%) and % 6-G released after 24 h (Q<sub>24h</sub>). According to the desirability criteria, F8 (CD-functionalized transethoniosomal formula) was selected as the optimized formulation. F8 demonstrated higher EE%, permeation, deformability and stability than the corresponding TENs, ENs and NVs. Additionally, F8 showed higher cytotoxic and anti-inflammatory activity than pure 6-G. The synergism between complexation with CD and novel ultra-deformable nanovesicles (TENs) in the form of CD-TENs can be a promising drug delivery carrier for 6-G.
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DOI: 10.3390/pharmaceutics14061170
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