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. 2023 Nov 9;28(22):7508.
doi: 10.3390/molecules28227508.

Sulconazole-Loaded Solid Lipid Nanoparticles for Enhanced Antifungal Activity: In Vitro and In Vivo Approach

Ayesha Samee  1 , Faisal Usman  1 , Tanveer A Wani  2 , Mudassir Farooq  3 , Hamid Saeed Shah  4 , Ibrahim Javed  5 , Hassan Ahmad  6 , Riffat Khan  7 , Seema Zargar  8 , Safina Kausar  1
Affiliations

Sulconazole-Loaded Solid Lipid Nanoparticles for Enhanced Antifungal Activity: In Vitro and In Vivo Approach

Ayesha Samee et al. Molecules. .

Abstract

Solid lipid nanoparticles (SLNs) have the advantages of a cell-specific delivery and sustained release of hydrophobic drugs that can be exploited against infectious diseases. The topical delivery of hydrophobic drugs needs pharmaceutical strategies to enhance drug permeation, which is a challenge faced by conventional formulations containing a drug suspended in gel, creams or ointments. We report the fabrication and optimization of SLNs with sulconazole (SCZ) as a model hydrophobic drug and then a formulation of an SLN-based topical gel against fungal infections. The SLNs were optimized through excipients of glyceryl monostearate and Phospholipon® 90 H as lipids and tween 20 as a surfactant for its size, drug entrapment and sustained release and resistance against aggregation. The SCZ-SLNs were physically characterized for their particle size (89.81 ± 2.64), polydispersity index (0.311 ± 0.07), zeta potential (-26.98 ± 1.19) and encapsulation efficiency (86.52 ± 0.53). The SCZ-SLNs showed sustained release of 85.29% drug at the 12 h timepoint. The TEM results demonstrated spherical morphology, while DSC, XRD and FTIR showed the compatibility of the drug inside SLNs. SCZ-SLNs were incorporated into a gel using carbopol and were further optimized for their rheological behavior, pH, homogeneity and spreadability on the skin. The antifungal activity against Candida albicans and Trichophyton rubrum was increased in comparison to a SCZ carbopol-based gel. In vivo antifungal activity in rabbits presented faster healing of skin fungal infections. The histopathological examination of the treated skin from rabbits presented restoration of the dermal architecture. In summary, the approach of formulating SLNs into a topical gel presented an advantageous drug delivery system against mycosis.

Keywords: anti-fungal gel; histopathology; solid lipid nanoparticles; sulconazole.

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Conflict of interest statement

The authors have no conflict of interest to declare.

Figures

Figure 1
Figure 1
FTIR of Sulconazole (A), Phospholipon® 90 H (B), GMS (C) and SLN2 formulation (D).
Figure 2
Figure 2
TEM image of SLN2 at ×15 k (A) and ×20 k (B) magnifications.
Figure 3
Figure 3
DSC of Sulconazole (SCZ) (A), Phospholipon® 90 H (B), GMS (C) and SLN2 (D).
Figure 4
Figure 4
TGA of Sulconazole (A), Phospholipon® 90 H (B), GMS (C) and SLN2 (D).
Figure 5
Figure 5
SLN2 (A), GMS (B), Phospholipon® 90 H (C) and Sulconazole SCZ (D).
Figure 6
Figure 6
Rheograms of fabricated formulations (Mean ± SD, n = 3).
Figure 7
Figure 7
Percent drug release of all formulations in 12 h (Mean ± SD, n = 3).
Figure 8
Figure 8
Ex vivo skin permeation of solid lipid nanoparticle gel formulation (SLN2) and pure drug as control (Mean ± SD, n = 3).
Figure 9
Figure 9
In vivo study of blank gel (A), SLN2 gel (B) and sulconazole carbopol-based gel (C) at Day 1, Day 6 and Day 12.
Figure 10
Figure 10
Histopathology examination of negative control group (A), blank treatment skin (B) and SCZ-SLN2 gel (C) treatment skin.
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