• MOHAMMED M. MEHANNA Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon
  • JANA K. ALWATTAR Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon


Objective: Electrohydrodynamic atomization is a technique that utilizes electrical potential differences for the fabrication of particles ranging from nano to micrometer size, where the ultra-charged droplets of drug-loaded mist deposit as nanospheres after solvent evaporation. The drug-loaded polymeric spherical nanocomposites have a small volume with large surface area, which is a beneficial characteristic for dissolution and bioavailability enhancement of class II drugs.

Methods: This facile approach is employed for the preparation of tadalafil-loaded nanosystems, a class II drug used for erectile dysfunction treatment. Tadalafil-loaded nanoparticles prepared with different polymer concentrations were evaluated through process yield, drug loading, morphology and functional performance. Further, drug solid-state and compatibility of formulation components were assessed.

Results: The results obtained pointed out that nanoparticles were of uniform spherical morphologies with a size range between 1279±141 and 374±13 nm. The system maintained a high loading efficacy of 88%, with most of the loaded drug released within 2 min during the in vitro dissolution studies. The differential scanning calorimetry, X-ray diffraction and Fourier-transform infrared spectroscopy demonstrated the presence of tadalafil in an amorphous form or as a molecular dispersion within the polymer matrix.

Conclusion: Tadalafil-loaded nanoparticles manufactured through this methodology is qualified as a strategy to ameliorate its solubility and bioavailability.

Keywords: Dissolution enhancement, Electrohydrodynamic atomization, Tadalafil, Nanoparticles, Nanosphere


1. Gomez Estaca J, Balaguer MP, Gavara R, Hernandez Munoz P. Formation of zein nanoparticles by electrohydrodynamic atomization: effect of the main processing variables and suitability for encapsulating the food coloring and active ingredient curcumin. Food Hydrocoll 2012;28:82–91.
2. Bohr A, Kristensen J, Dyas M, Edirisinghe M, Stride E. Release profile and characteristics of electrosprayed particles for oral delivery of a practically insoluble drug. J R Soc Interface 2012;9:2437–49.
3. Xie J, Marijnissen JCM, Wang CH. Microparticles developed by electrohydrodynamic atomization for the local delivery of an anticancer drug to treat C6 glioma in vitro. Biomaterials 2006;27:3321–32.
4. Zolkepali NK, Abu bakar NF, Naim MN, Anuar N, Kamalul Aripin NF, Abu Bakar MR, et al. Formation of fine and encapsulated mefenamic acid form I particles for dissolution improvement via electrospray method. Part Sci Technol 2018;36:298–307.
5. Vemula VR, Lagishetty V, Lingala S. Solubility enhancement techniques. Int J Pharm Sci Rev Res 2010;5:41–51.
6. Yu H, Teo J, Chew JW, Hadinoto K. Dry powder inhaler formulation of high-payload antibiotic nanoparticle complex intended for bronchiectasis therapy: spray drying versus spray freeze drying preparation. Int J Pharm 2016;499:38–46.
7. Das S, Banerjee R, Bellare J. Aspirin loaded albumin nanoparticles by coacervation: implications in drug delivery. Trends Biomater Artif Organs 2005;18:203–12.
8. Kwon HY, Lee JY, Choi SW, Jang Y, Kim JH. Preparation of PLGA nanoparticles containing estrogen by an emulsification-diffusion method. Colloids Surf A 2001;182:123–30.
9. Desgouilles S, Vauthier C, Bazile D, Vacus J, Grossiord JL, Veillard M, et al. The design of nanoparticles obtained by solvent evaporation: a comprehensive study. Langmuir 2003;19:9504–10.
10. Zamani M, Prabhakaran MP, Ramakrishna S. Advances in drug delivery via electrospun and electrosprayed nanomaterials. Int J Nanomed 2013;8:2997–3017.
11. Abdel-Aziz A-AH, Asiri YA, El-Azab A, Al-Omar MA, Kunieda T. Tadalafil. Profiles Drug Subst Excipients Relat Methodol 2011;36:287–329.
12. Doggrell SA. Comparison of clinical trials with sildenafil, vardenafil and tadalafil in erectile dysfunction. Expert Opin Pharmacother 2005;6:75–84.
13. Lu M, Xing H, Yang T, Yu J, Yang Z, Sun Y, et al. Dissolution enhancement of tadalafil by liquisolid technique. Pharm Dev Technol 2017;22:77–89.
14. Refaat A, Sokar M, Ismail F, Boraei N. Tadalafil oral disintegrating tablets: an approach to enhance tadalafil dissolution. J Pharm Investig 2015;45:481–91.
15. Badr-Eldin SM, Elkheshen SA, Ghorab MM. Inclusion complexes of tadalafil with natural and chemically modified???-cyclodextrins. I: preparation and in vitro evaluation. Eur J Pharm Biopharm 2008;70:819–27.
16. Obeidat WM, Sallam ASA. Evaluation of tadalafil nanosuspensions and their PEG solid dispersion matrices for enhancing its dissolution properties. AAPS PharmSciTech 2014;15:364–74.
17. Vinesha V, Sevukarajan M, Rajalakshmi R, Chowdary GT, Haritha K. Enhancement of solubility of tadalafil by cocrystal approach. Int Res J Pharm 2016;4:218–23.
18. Mehanna MM, Motawaa AM, Samaha MW. Tadalafil inclusion in microporous silica as an effective dissolution enhancer: optimization of loading procedure and molecular state characterization. J Pharm Sci 2011;100:1805–18.
19. Shen X, Yu D, Zhu L, Branford White C, White K, Chatterton NP. Electrospun diclofenac sodium loaded Eudragit?? L 100-55 nanofibers for colon-targeted drug delivery. Int J Pharm 2011;408:200–7.
20. Mehanna MM, Alwattar JK, Elmaradny HA. Optimization, physicochemical characterization and in vivo assessment of spray-dried emulsion: a step toward bioavailability augmentation and gastric toxicity minimization. Int J Pharm 2015;496:766–79.
21. Mehanna MM, Motawaa AM, Samaha MW. Insight into tadalafil-block copolymer binary solid dispersion: mechanistic investigation of dissolution enhancement. Int J Pharm 2010;402:78–88.
22. Sakuma S, Matsumoto S, Ishizuka N, Mohri K, Fukushima M, Ohba C, et al. Enhanced boosting of oral absorption of lopinavir through electrospray coencapsulation with ritonavir. J Pharm Sci 2015;104:2977–85.
23. Li C, Yu DG, Williams GR, Wang ZH. Fast-dissolving core-shell composite microparticles of quercetin fabricated using a coaxial electrospray process. PLoS One 2014;9:1–9.
24. Yousaf AM, Mustapha O, Kim DW, Kim DS, Kim KS, Jin SG, et al. Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate. Int J Nanomed 2016;11:213–21.
25. Zhou Y, Qi P, Zhao Z, Liu Q, Li Z. Fabrication and characterization of fibrous HAP/PVP/PEO composites prepared by sol-electrospinning. RSC Adv 2014;4:16731.
26. Bhattarai N, Edmondson D, Veiseh O, Matsen FA, Zhang M. Electrospun chitosan-based nanofibers and their cellular compatibility. Biomaterials 2005;26:6176–84.
27. Hong SI, Oh SY. Dissolution kinetics and physical characterization of the three-layered tablet with poly(ethylene oxide) core matrix capped by carbopol. Int J Pharm 2008;356:121–9.
28. Nasir M, Matsumoto H, Danno T, Minagawa M, Irisawa T, Shioya M, et al. Control of diameter, morphology, and structure of PVDF nanofiber fabricated by electrospray deposition. J Polymer Sci Part B: Polymer Physics 2006;44:779–86.
29. Huang L, Nagapudi K, Apkarian RP, Chaikof EL. Engineered collagen–PEO nano bers and fabrics. J Biomater Sci Polym Edn 2001;12:979–93.
30. Ajao JA, Abiona AA, Chigome S, Fasasi AY, Osinkolu GA, Maaza M. Electric-magnetic field-induced aligned electrospun poly (ethylene oxide) (PEO) nanofibers. J Mater Sci 2010;45:2324–9.
31. Yu DG, Branford White C, Shen XX, Zhang XF, Zhu LM. Solid dispersions of ketoprofen in drug-loaded electrospun nanofibers. J Dispers Sci Technol 2010;31:902–8.
32. Noor SAM, Ahmad A, Talib IA, Rahman MYA. Morphology, chemical interaction, and conductivity of a PEO-ENR50 based on solid polymer electrolyte. Ionics (Kiel) 2010;16:161–70.
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How to Cite
MEHANNA, M. M., and J. K. ALWATTAR. “NANOSPHERE-LOADED TADALAFIL WITH ENHANCED ORAL BIOAVAILABILITY: INNOVATIVE APPLICATION OF ELECTROHYDRODYNAMIC TECHNIQUE”. International Journal of Current Pharmaceutical Research, Vol. 12, no. 1, Jan. 2020, pp. 28-34, doi:10.22159/ijcpr.2020v12i1.36828.
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