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FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach

Candidal vulvovaginitis (CVV), is the second most leading vaginal infection (global prevalence > 75%), caused due to excessive growth of Candida spp., predominantly Candida albicans (>95% cases). The current treatment regimens for CVV are marred with the challenges of fungal resistance & i...

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Autores principales: Firdaus, Salma, Hassan, Nazia, Mirza, Mohd. Aamir, Ara, Tabasum, El-Serehy, Hamed A., Al-Misned, Fahad A., Iqbal, Zeenat
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7785458/
https://www.ncbi.nlm.nih.gov/pubmed/33424312
http://dx.doi.org/10.1016/j.sjbs.2020.10.005
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author Firdaus, Salma
Hassan, Nazia
Mirza, Mohd. Aamir
Ara, Tabasum
El-Serehy, Hamed A.
Al-Misned, Fahad A.
Iqbal, Zeenat
author_facet Firdaus, Salma
Hassan, Nazia
Mirza, Mohd. Aamir
Ara, Tabasum
El-Serehy, Hamed A.
Al-Misned, Fahad A.
Iqbal, Zeenat
author_sort Firdaus, Salma
collection PubMed
description Candidal vulvovaginitis (CVV), is the second most leading vaginal infection (global prevalence > 75%), caused due to excessive growth of Candida spp., predominantly Candida albicans (>95% cases). The current treatment regimens for CVV are marred with the challenges of fungal resistance & infection recurrence, subsequently leading to the compromised therapeutic efficacy of anti-fungal drugs, prolonged treatment and low patient compliance. The core of the present research was the fabrication & investigation of 2 T-SLN (solid lipid nanoparticles) gel carrying luliconazole for the amelioration of CVV. ‘2T’ symbolizes transvaginal & thermosensitive attributes of the present formulation. SLNs were prepared by a modified melt emulsification-ultra sonication method using a combination of solid lipids (Gelucire 50/13 & Precirol ATO 5), surfactant (Tween 80) and co-surfactant (Kolliphor). Formulation by design (FbD) approach was adopted to obtain appropriately screened and tailored SLNs. The optimized SLNs yielded a particle size, polydispersity index & entrapment efficiency of 62.18 nm, 0.263 & 81.5% respectively. To formulate the 2 T-gel, the final SLNs were loaded into Carbopol 971P-NF and Triethanolamine based gel. The 2 T-SLN gel was found to be easily spreadable and homogenous with mean extrudability (15 ± 0.4 g/cm(2)), viscosity (696.42 ± 2.34 Pa·s) and %drug content (93.24 ± 0.73%) values.. The pH of the prepared 2 T-SLN gel (4.5 ± 0.5) was in concordance with the vaginal pH (normal conditions). For in-vitro characterization of an optimized 2 T-SLN gel the release kinetics & anticandidal activity were assessed which offers a %cumulative drug release of 62 ± 0.5% in 72 h and 37.3 ± 1.5 mm zone of inhibition in 48 h. The visual appearance & dimensions were determined using fluorescent microscopy (spherical shape) & transmission electron microscopy (90–120 nm) respectively. The optimized 2 T-SLN gel showcases a skin-friendly profile with no significant signs of erythema and oedema and was found to be stable at room temperature for 2 months without any visual non-uniformity/cracking/breaking. In conclusion, the current research serves a new therapeutic perspective in assessing the activity of luliconazole for vaginal drug delivery using a 2 T-SLN gel system.
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spelling pubmed-77854582021-01-08 FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach Firdaus, Salma Hassan, Nazia Mirza, Mohd. Aamir Ara, Tabasum El-Serehy, Hamed A. Al-Misned, Fahad A. Iqbal, Zeenat Saudi J Biol Sci Original Article Candidal vulvovaginitis (CVV), is the second most leading vaginal infection (global prevalence > 75%), caused due to excessive growth of Candida spp., predominantly Candida albicans (>95% cases). The current treatment regimens for CVV are marred with the challenges of fungal resistance & infection recurrence, subsequently leading to the compromised therapeutic efficacy of anti-fungal drugs, prolonged treatment and low patient compliance. The core of the present research was the fabrication & investigation of 2 T-SLN (solid lipid nanoparticles) gel carrying luliconazole for the amelioration of CVV. ‘2T’ symbolizes transvaginal & thermosensitive attributes of the present formulation. SLNs were prepared by a modified melt emulsification-ultra sonication method using a combination of solid lipids (Gelucire 50/13 & Precirol ATO 5), surfactant (Tween 80) and co-surfactant (Kolliphor). Formulation by design (FbD) approach was adopted to obtain appropriately screened and tailored SLNs. The optimized SLNs yielded a particle size, polydispersity index & entrapment efficiency of 62.18 nm, 0.263 & 81.5% respectively. To formulate the 2 T-gel, the final SLNs were loaded into Carbopol 971P-NF and Triethanolamine based gel. The 2 T-SLN gel was found to be easily spreadable and homogenous with mean extrudability (15 ± 0.4 g/cm(2)), viscosity (696.42 ± 2.34 Pa·s) and %drug content (93.24 ± 0.73%) values.. The pH of the prepared 2 T-SLN gel (4.5 ± 0.5) was in concordance with the vaginal pH (normal conditions). For in-vitro characterization of an optimized 2 T-SLN gel the release kinetics & anticandidal activity were assessed which offers a %cumulative drug release of 62 ± 0.5% in 72 h and 37.3 ± 1.5 mm zone of inhibition in 48 h. The visual appearance & dimensions were determined using fluorescent microscopy (spherical shape) & transmission electron microscopy (90–120 nm) respectively. The optimized 2 T-SLN gel showcases a skin-friendly profile with no significant signs of erythema and oedema and was found to be stable at room temperature for 2 months without any visual non-uniformity/cracking/breaking. In conclusion, the current research serves a new therapeutic perspective in assessing the activity of luliconazole for vaginal drug delivery using a 2 T-SLN gel system. Elsevier 2021-01 2020-10-16 /pmc/articles/PMC7785458/ /pubmed/33424312 http://dx.doi.org/10.1016/j.sjbs.2020.10.005 Text en © 2020 The Authors http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Article
Firdaus, Salma
Hassan, Nazia
Mirza, Mohd. Aamir
Ara, Tabasum
El-Serehy, Hamed A.
Al-Misned, Fahad A.
Iqbal, Zeenat
FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach
title FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach
title_full FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach
title_fullStr FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach
title_full_unstemmed FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach
title_short FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach
title_sort fbd directed fabrication and investigation of luliconazole based sln gel for the amelioration of candidal vulvovaginitis: a 2 t (thermosensitive & transvaginal) approach
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7785458/
https://www.ncbi.nlm.nih.gov/pubmed/33424312
http://dx.doi.org/10.1016/j.sjbs.2020.10.005
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