Design and Formulation of Cyclodextrin based Nano-sponges Loaded Topical Hydrogel with Enhanced Skin Permeation and Effectiveness of Luliconazole
DOI:
https://doi.org/10.37285/ijpsn.2024.17.6.4Abstract
Objective The purpose of this work was to develop an effective luliconazole topical formulation. Cyclodextrin-based nanosponges loaded hydrogel of Carbopol 934 was formulated and characterized for its in-vitro and ex-vivo permeation study.
Methods Cyclodextrin-based nanosponges were prepared in a 1:3 ratio using the dispersion-sonication method. The effectivity of topical formulation is based on its spreadability and diffusion flux. 33 Factorial design was utilized for the optimization of the hydrogel formulation using spreadability and diffusion flux as dependent variables. Optimization was done by response surface methodology by keeping the constraint constant. The optimized batch was evaluated for ex vivo skin permeation and in vitro antifungal assay in comparison to marketed and plain drug-loaded hydrogel.
Result The prepared nanosponges were of nano size and had more than 80% drug content. Powder characterization confirms the compatibility between drug and excipients and the formation of inclusion complex with cyclodextrin. Based on desirability, optimized hydrogel follows the Higuchi kinetic model of drug release with better ex vivo diffusion compared to the marketed formulation. In vitro, antifungal assay showed better effectivity of hydrogel against Candida albicans. The topography of the gel showed an irregular spherical shape. Accelerated stability studies also confirmed the stabilization of the complex in the hydrogel.
Conclusion The prepared formulation shows better effectivity and penetrability due to spherical shape and presence of penetration enhancer and can improve patient compliance.
Downloads
Keywords:
cyclodextrin, nanosponges, luliconazole, hydrogel, diffusion flux, topical formulationPublished
How to Cite
Issue
Section
References
Williams AC, Barry BW. Penetration enhancers. Advanced drug delivery reviews. 2012 Dec 1;64:128-37.
Asfaram A, Ghaedi M, Dashtian K. Ultrasound assisted combined molecularly imprinted polymer for selective extraction of nicotinamide in human urine and milk samples: spectrophotometric determination and optimization study. Ultrasonics Sonochemistry. 2017 Jan 1;34:640-50.
Abbas N, Irfan M, Hussain A, Arshad MS, Hussain SZ, Latif S, Bukhari NI. Development and evaluation of scaffold-based nanosponge formulation for controlled drug delivery of naproxen and ibuprofen. Tropical Journal of Pharmaceutical Research. 2018 Oct 5;17(8):1465-74.
Srinivas P, Sreeja K. Formulation and evaluation of voriconazole loaded nanosponges for oral and topical delivery. Int J Drug Dev Res. 2013 Jan;5(1):55-69.
Ige PP, Baria RK, Gattani SG. Fabrication of fenofibrate nanocrystals by probe sonication method for enhancement of dissolution rate and oral bioavailability. Colloids and Surfaces B: Biointerfaces. 2013 Aug 1;108:366-73.
Sundararajan M, Thomas PA, Venkadeswaran K, Jeganathan K, Geraldine P. Synthesis and characterization of chrysin-loaded β-cyclodextrin-based nanosponges to enhance in-vitro solubility, photostability, drug release, antioxidant effects and
antitumorous efficacy. Journal of Nanoscience and Nanotechnology. 2017 Dec 1;17(12):8742-51.
Kumar PS, Hematheerthani N, Ratna JV, Saikishore V. Design and characterization of miconazole nitrate loaded nanosponges containing vaginal gels. Int J Pharm Ana Res. 2016;5(3):410-7.
Bachhav YG, Patravale VB. Microemulsion based vaginal gel of fluconazole: formulation, in vitro and in vivo evaluation. International Journal of Pharmaceutics. 2009 Jan 5;365(1-2):175-9.
Iriventi P, Gupta NV, Osmani RA, Balamuralidhara V. Design & development of nanosponge loaded topical gel of curcumin and caffeine mixture for augmented treatment of psoriasis. DARU Journal of Pharmaceutical Sciences. 2020 Dec;28:489-506.
Srinivas P, Jahnavi Reddy A. Formulation and evaluation of isoniazid loaded nanosponges for topical delivery. Pharmaceutical Nanotechnology. 2015 Mar 1;3(1):68-76.
Koga H, Tsuji Y, Inoue K, Kanai K, Majima T, Kasai T, Uchida K, Yamaguchi H. In vitro antifungal activity of luliconazole against clinical isolates from patients with dermatomycoses. Journal of infection and chemotherapy. 2006 Jan 1;12(3):163-5.
Bachir YN, Medjkane M, Benaoudj F, Sahraoui N, Hadj Ziane A. Formulation of β-cyclodextrin nanosponges by polycondensation method: application for natural drugs delivery and preservation. J Mater Process Environ. 2017;5:80-5.
Sabzi NE, Kiasat AR. β-Cyclodextrin based nanosponge as a biodegradable porous three-dimensional nanocatalyst in