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Updated: Mar 5, 2026
Formulation and Characterization of Bioactive Agent Containing Nanodisks
Published on: March 17, 2023
PDE5 Inhibitors-Loaded Nanovesicles: Physico-Chemical Properties and In Vitro Antiproliferative Activity
Roberta F De Rose1, Maria Chiara Cristiano2, Marilena Celano3
1Department of Health Sciences, University "Magna Græcia" of Catanzaro, Campus Universitario "S. Venuta", Viale S. Venuta, Germaneto, Catanzaro I-88100, Italy. robertafra87@gmail.com.
Abstract:
Novel therapeutic approaches are required for the less differentiated thyroid cancers which are non-responsive to the current treatment. In this study we tested an innovative formulation of nanoliposomes containing sildenafil citrate or tadalafil, phosphodiesterase-5 inhibitors, on two human thyroid cancer cell lines (TPC-1 and BCPAP). Nanoliposomes were prepared by the thin layer evaporation and extrusion methods, solubilizing the hydrophilic compound sildenafil citrate in the aqueous phase during the hydration step and dissolving the lipophilic tadalafil in the organic phase. Nanoliposomes, made up of 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine monohydrate (DPPC), cholesterol, and N-(carbonyl-methoxypolyethylene glycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE-mPEG2000) (6:3:1 molar ratio), were characterized by a mean diameter of ~100 nm, a very low polydispersity index (~0.1) and a negative surface charge. The drugs did not influence the physico-chemical properties of the systems and were efficiently retained in the colloidal structure. By using cell count and MTT assay, we found a significant reduction of the viability in both cell lines following 24 h treatment with both nanoliposomal-encapsulated drugs, notably greater than the effect of the free drugs. Our findings demonstrate that nanoliposomes increase the antiproliferative activity of phosphodiesterase-5 inhibitors, providing a useful novel formulation for the treatment of thyroid carcinoma.
Insights
Novel nanoliposome formulations of phosphodiesterase-5 inhibitors, sildenafil citrate and tadalafil, significantly enhanced anti-cancer activity against thyroid cancer cell lines. This innovative drug delivery system shows promise for treating unresponsive thyroid carcinomas.
Area of Science:
- Oncology
- Nanotechnology
- Pharmacology
Background:
- Less differentiated thyroid cancers often resist conventional therapies, necessitating novel treatment strategies.
- Phosphodiesterase-5 inhibitors (PDE5i) like sildenafil citrate and tadalafil are being explored for anti-cancer effects.
- Drug delivery systems are crucial for improving the efficacy of anti-cancer agents.
Purpose of the Study:
- To develop and evaluate nanoliposome formulations of sildenafil citrate and tadalafil for thyroid cancer treatment.
- To assess the antiproliferative effects of these nanoliposomal PDE5i on human thyroid cancer cell lines.
- To compare the efficacy of encapsulated PDE5i with their free drug counterparts.
Main Methods:
- Nanoliposomes were prepared using thin-film evaporation and extrusion, encapsulating sildenafil citrate and tadalafil.
- Nanoliposome characteristics (size, polydispersity, surface charge) were determined.
- Thyroid cancer cell lines (TPC-1, BCPAP) were treated with nanoliposomal PDE5i and free drugs.
- Cell viability was assessed using cell count and MTT assays.
Main Results:
- Nanoliposomes exhibited a mean diameter of ~100 nm, low polydispersity, and negative surface charge.
- Encapsulated sildenafil citrate and tadalafil were efficiently retained within the nanoliposomes.
- Both nanoliposomal PDE5i significantly reduced thyroid cancer cell viability compared to free drugs.
- The antiproliferative effect was observed in both TPC-1 and BCPAP cell lines after 24 hours.
Conclusions:
- Nanoliposome encapsulation enhances the antiproliferative activity of sildenafil citrate and tadalafil against thyroid cancer cells.
- This novel nanoliposomal formulation offers a promising therapeutic approach for thyroid carcinoma, particularly for treatment-resistant types.
- Further research into nanoliposomal PDE5i could lead to improved thyroid cancer therapies.
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