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Aerosolizable Lipid-Nanovesicles Encapsulating Voriconazole Effectively Permeate Pulmonary Barriers and Target Lung
Ranjot Kaur1,2, Sarah R Dennison2, Shivaprakash M Rudramurthy3
1University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh, India.
Abstract:
The entire world has recently been witnessing an unprecedented upsurge in microbial lung infections. The major challenge encountered in treating the same is to ensure the optimum drug availability at the infected site. Aerosolization of antimicrobials, in this regard, has shown immense potential owing to their localized and targeted effect. Efforts, therefore, have been undertaken to systematically develop lung-phosphatidylcholine-based lipid nanovesicles of voriconazole for potential management of the superinfections like aspergillosis. LNVs, prepared by thin-film hydration method, exhibited a globule size of 145.4 ± 19.5 nm, polydispersity index of 0.154 ± 0.104 and entrapment efficiency of 71.4 ± 2.2% with improved in vitro antifungal activity. Aerodynamic studies revealed a microdroplet size of ≤5 μm, thereby unraveling its promise to target the physical barrier of lungs effectively. The surface-active potential of LNVs, demonstrated through Langmuir-Blodgett troughs, indicated their ability to overcome the biochemical pulmonary surfactant monolayer barrier, while the safety and uptake studies on airway-epithelial cells signified their immense potential to permeate the cellular barrier of lungs. The pharmacokinetic studies showed marked improvement in the retention profile of voriconazole in lungs following LNVs nebulization compared to pristine voriconazole. Overall, LNVs proved to be safe and effective delivery systems, delineating their distinct potential to efficiently target the respiratory fungal infections.
Insights
Lung lipid nanovesicles (LNVs) loaded with voriconazole show promise for treating fungal lung infections like aspergillosis. These LNVs improve drug delivery and retention in the lungs, offering a safe and effective treatment option.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Pulmonary Medicine
Background:
- Rising incidence of microbial lung infections necessitates improved therapeutic strategies.
- Achieving optimal drug concentration at the infection site remains a significant clinical challenge.
- Antimicrobial aerosolization offers localized and targeted drug delivery for lung infections.
Purpose of the Study:
- To develop and characterize lung-phosphatidylcholine-based lipid nanovesicles (LNVs) encapsulating voriconazole.
- To evaluate the potential of these LNVs for managing fungal superinfections, such as aspergillosis.
- To assess the efficacy and safety of LNVs as a targeted drug delivery system for the lungs.
Main Methods:
- Lipid nanovesicles (LNVs) were prepared using the thin-film hydration method.
- Characterization included globule size, polydispersity index, and entrapment efficiency.
- In vitro antifungal activity, aerodynamic properties, surface activity, cell uptake, and pharmacokinetic studies were performed.
Main Results:
- LNVs demonstrated a globule size of 145.4 ± 19.5 nm and an entrapment efficiency of 71.4 ± 2.2%.
- Aerodynamic studies showed a microdroplet size ≤5 μm, suitable for lung targeting.
- Improved in vitro antifungal activity, enhanced lung retention, and good safety profiles were observed.
Conclusions:
- Lung-phosphatidylcholine-based lipid nanovesicles (LNVs) are effective for targeted delivery of voriconazole to the lungs.
- LNVs demonstrate potential to overcome physical and biochemical barriers within the lungs.
- These LNVs represent a promising and safe delivery system for treating respiratory fungal infections.
