CC BY 4.0 · Journal of Health and Allied Sciences NU 2025; 15(01): 026-031
DOI: 10.1055/s-0044-1787293
Original Article

Tolnaftate-Loaded Ethosomal Gel for Topical Delivery: Formulation and In Vitro Evaluation

1   Department of Pharmaceutics, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences (NGSMIPS), Nitte (Deemed to be university), Mangaluru, Karnataka, India
,
Preethika Shridhar
1   Department of Pharmaceutics, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences (NGSMIPS), Nitte (Deemed to be university), Mangaluru, Karnataka, India
,
Kshema Shekhara
1   Department of Pharmaceutics, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences (NGSMIPS), Nitte (Deemed to be university), Mangaluru, Karnataka, India
,
Susheela Shenthar
1   Department of Pharmaceutics, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences (NGSMIPS), Nitte (Deemed to be university), Mangaluru, Karnataka, India
,
Suraksha K. Kudva
1   Department of Pharmaceutics, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences (NGSMIPS), Nitte (Deemed to be university), Mangaluru, Karnataka, India
› Institutsangaben

Abstract

Objectives Tolnaftate (TOL) is used as a topical antifungal agent but has poor skin penetration. Therefore, the present study is designed to formulate an ethosomal gel of TOL to enhance drug penetration through the skin.

Methods Using the cold method ethosomal formulations with different concentrations of ethanol and soy phosphatidylcholine (SPC) were formulated. The formulation of ethosomes was characterized by vesicle size, polydispersity index and zeta potential, % drug entrapment efficiency (EE), and scanning electron microscopy (SEM). The optimized ethosomal formula was incorporated in a 1% Carbopol hydrogel dosage. Evaluation of in vitro penetration of prepared gel was performed on goat skin using Franz diffusion cells and compared with conventional gel.

Result The ethosomal formulation EF5 showed the highest % EE (76.82%) with a small vesicle size of 210.1 nm and was selected as the optimized formulation. The SEM result shows that the vesicles were spherical, smooth, and in the 200-nm range. In vitro, permeability study shows that steady-state flux of TOL from ethosomal and conventional gels were 6.667 and 3.685 µg/cm/h, respectively (p < 0.001). It indicated that the flux of Ethosomal hydrogel (EHG) is 2.0-fold higher than conventional hydrogel (CHG); this may be due to the flexible nature of ethosomes and ethosomal core containing ethanol, which dissolves the lipid bilayer of skin and overcomes the barrier. In vitro, an antifungal study shows that the incorporation of TOL in ethosomal hydrogel retains their activity.

Conclusion From the results, it was concluded that TOL topical ethosomal gel for antifungal activity will possibly be a good choice.



Publikationsverlauf

Artikel online veröffentlicht:
18. Juni 2024

© 2024. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting unrestricted use, distribution, and reproduction so long as the original work is properly cited. (https://creativecommons.org/licenses/by/4.0/)

Thieme Medical and Scientific Publishers Pvt. Ltd.
A-12, 2nd Floor, Sector 2, Noida-201301 UP, India

 
  • References

  • 1 Rang HP, Ritter JM, Flower RJ, Henderson G. Rang & Dale's Pharmacology. 9th ed. London, England:: Elsevier Churchill Livingstone; 2017: 678-688
  • 2 Dhurve R, Kashyap N, Mishra A, Pathak AK. A holistic review on ethosome: a promising drug delivery system for topical fungal disease. Int J Pharm Biol Arch 2014; 5 (05) 13-26
  • 3 Rakesh R, Anoop KR. Ethosomes for transdermal and topical drug delivery. Int J Pharm Pharm Sci 2012; 4 (03) 17-24
  • 4 Bhalaria MK, Naik S, Misra AN. Ethosomes: a novel delivery system for antifungal drugs in the treatment of topical fungal diseases. Indian J Exp Biol 2009; 47 (05) 368-375
  • 5 Indora N, Kaushik D. Design development and evaluation of ethosomal gel of fluconazole for topical fungal infection. Int J Engg Sci Inven Res Dev 2015; 1 (08) 280-306
  • 6 Sujitha B, Krishnamoorthy B, Muthukumaran M. Formulation and evaluation of piroxicam-loaded ethosomal gel for transdermal drug delivery. Int J Adv Pharm Gen Res. 2014; 2 (01) 34-45
  • 7 Paliwal S, Tilak A, Sharma J. et al. Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model. Lipids Health Dis 2019; 18 (01) 133
  • 8 Abousamra MM, Mohsen AM. Solid lipid nanoparticles and nanostructured lipid carriers of tolnaftate: design, optimisation and in-vitro evaluation. Int J Pharm Pharm Sci 2016; 8 (01) 380-385
  • 9 Sneh P, Jyothi D, James JP, Maxwell A. Formulation and optimisation of ethosomes loaded with ropinirole hydrochloride: application of quality by design approach. Res J Pharm Technol. 2020; 13 (09) 4339-4345
  • 10 Shukla T, Verma A, Upmanyu N, Mishra SS, Shilpi S. Development and characterisation of clopidogrel-loaded ethosomal transdermal patch for antiplatelet effect. Asian J Pharm . Suppl 2016; 10 (04) S480-S486
  • 11 Ramadon D, Anwar E, Harahap Y. In vitro penetration and bioavailability of novel transdermal quercetin-loaded ethosomal gel. Indian J Pharm Sci 2017; 79 (06) 948-956
  • 12 Kumar JR. Anticandidal activity of ethosomal gel containing miconazole nitrate in male Sprague Dawley rat. J. Pharm. Sci. & Res. 2018; 10 (12) 3400-3405
  • 13 Anju K, Priya S, Sandeep DS. et al. Formulation and optimisation of Zaltoprofen loaded ethosomal gel by using 23 full factorial designs. J Pharm Res Int 2021; 33 (24B): 30-44
  • 14 Gunda SR, Ganesh GN. Formulation and evaluation of tolnaftate-loaded topical liposomal gel for effective skin drug delivery to treat fungal diseases. J Chem Pharm Res 2014; 6 (10) 856-866
  • 15 Abdulbaqi IM, Darwis Y, Khan NA, Assi RA, Khan AA. Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials. Int J Nanomedicine 2016; 11: 2279-2304
  • 16 Peram MR, Jalalpure S, Kumbar V. et al. Factorial design based curcumin ethosomal nanocarriers for the skin cancer delivery: in vitro evaluation. J Liposome Res 2019; 29 (03) 291-311