Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne

<b>Background:</b> Anthralin is known for its efficacy in treating psoriasis and acne, possessing poor solubility. Addressing these limitations, the present study endeavors to develop a microemulgel formulation of anthralin aimed at enhancing solubility. <b>Method:</b> The so...

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Main Authors: Samiksha Sakarkar, Swati Jagdale, Shrikant Dargude, Anuruddha Chabukswar, Shabana Urooj, Anusha Bilal, Hanan Abdullah Mengash
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/12/2629
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author Samiksha Sakarkar
Swati Jagdale
Shrikant Dargude
Anuruddha Chabukswar
Shabana Urooj
Anusha Bilal
Hanan Abdullah Mengash
author_facet Samiksha Sakarkar
Swati Jagdale
Shrikant Dargude
Anuruddha Chabukswar
Shabana Urooj
Anusha Bilal
Hanan Abdullah Mengash
author_sort Samiksha Sakarkar
collection DOAJ
description <b>Background:</b> Anthralin is known for its efficacy in treating psoriasis and acne, possessing poor solubility. Addressing these limitations, the present study endeavors to develop a microemulgel formulation of anthralin aimed at enhancing solubility. <b>Method:</b> The solubility study was performed in various solvents. An o/w (oil-in-water) emulsion was formed using the water titration method, which was optimized by statistical experimental design half-run CCD. The final optimized batch was evaluated for physicochemical and in vitro properties <b>Result:</b> The final optimized batch showed a particle size (PS) of 417 nm, −25.2 mV zeta potential (ZP) and pH 5.8, which remained stable upon centrifugation, heating–cooling and freeze–thawing cycle. Furthermore, microemulsion with Carbopol 943 5% <i>w</i>/<i>v</i> was selected as the gel base for the formation of microemulgel characterized by PS, ZP, pH, and viscosity of 230 nm, −50.6 mV, 6.9 and 14,200 cps, respectively, that ensured it a high enough stability. In silico molecular docking between ligand and protein provides the binding energies validating the interaction. Hence, the in silico study was performed for psoriasis and <i>P. acne</i> proteins. An in vitro antibacterial activity study on Propionibacterium revealed a significant efficiency of the formulation and MTT assay using L929 cell line in the presence of the drug-loaded microemulgel indicated an inhibition of growth proving that formulation has anti-psoriatic activity. <b>Conclusions:</b> Combination therapy with Clindamycin might improve efficacy while reducing antibiotic resistance risks.
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spelling doaj-art-42ece3102cf64f2eb89e78bda61344892025-08-20T03:27:38ZengMDPI AGMolecules1420-30492025-06-013012262910.3390/molecules30122629Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and AcneSamiksha Sakarkar0Swati Jagdale1Shrikant Dargude2Anuruddha Chabukswar3Shabana Urooj4Anusha Bilal5Hanan Abdullah Mengash6Department of Pharmaceutical Sciences, School of Health Sciences and Technology, Dr. Vishwanath Karad MIT World Peace University, Kothrud, Pune 411038, IndiaDepartment of Pharmaceutical Sciences, School of Health Sciences and Technology, Dr. Vishwanath Karad MIT World Peace University, Kothrud, Pune 411038, IndiaDepartment of Pharmaceutical Sciences, School of Health Sciences and Technology, Dr. Vishwanath Karad MIT World Peace University, Kothrud, Pune 411038, IndiaDepartment of Pharmaceutical Sciences, School of Health Sciences and Technology, Dr. Vishwanath Karad MIT World Peace University, Kothrud, Pune 411038, IndiaDepartment of Electrical Engineering, College of Engineering, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi ArabiaDepartment of Food Science and Nutrition, University of Leeds, Leeds LS2 9JT, UKDepartment of Information Systems, College of Computer and Information Sciences, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia<b>Background:</b> Anthralin is known for its efficacy in treating psoriasis and acne, possessing poor solubility. Addressing these limitations, the present study endeavors to develop a microemulgel formulation of anthralin aimed at enhancing solubility. <b>Method:</b> The solubility study was performed in various solvents. An o/w (oil-in-water) emulsion was formed using the water titration method, which was optimized by statistical experimental design half-run CCD. The final optimized batch was evaluated for physicochemical and in vitro properties <b>Result:</b> The final optimized batch showed a particle size (PS) of 417 nm, −25.2 mV zeta potential (ZP) and pH 5.8, which remained stable upon centrifugation, heating–cooling and freeze–thawing cycle. Furthermore, microemulsion with Carbopol 943 5% <i>w</i>/<i>v</i> was selected as the gel base for the formation of microemulgel characterized by PS, ZP, pH, and viscosity of 230 nm, −50.6 mV, 6.9 and 14,200 cps, respectively, that ensured it a high enough stability. In silico molecular docking between ligand and protein provides the binding energies validating the interaction. Hence, the in silico study was performed for psoriasis and <i>P. acne</i> proteins. An in vitro antibacterial activity study on Propionibacterium revealed a significant efficiency of the formulation and MTT assay using L929 cell line in the presence of the drug-loaded microemulgel indicated an inhibition of growth proving that formulation has anti-psoriatic activity. <b>Conclusions:</b> Combination therapy with Clindamycin might improve efficacy while reducing antibiotic resistance risks.https://www.mdpi.com/1420-3049/30/12/2629anthralinpsoriasisacnemicroemulgelcentral-composite designmolecular docking
spellingShingle Samiksha Sakarkar
Swati Jagdale
Shrikant Dargude
Anuruddha Chabukswar
Shabana Urooj
Anusha Bilal
Hanan Abdullah Mengash
Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne
Molecules
anthralin
psoriasis
acne
microemulgel
central-composite design
molecular docking
title Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne
title_full Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne
title_fullStr Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne
title_full_unstemmed Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne
title_short Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne
title_sort optimization of anthralin microemulgel targeted delivery for psoriasis and acne
topic anthralin
psoriasis
acne
microemulgel
central-composite design
molecular docking
url https://www.mdpi.com/1420-3049/30/12/2629
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AT swatijagdale optimizationofanthralinmicroemulgeltargeteddeliveryforpsoriasisandacne
AT shrikantdargude optimizationofanthralinmicroemulgeltargeteddeliveryforpsoriasisandacne
AT anuruddhachabukswar optimizationofanthralinmicroemulgeltargeteddeliveryforpsoriasisandacne
AT shabanaurooj optimizationofanthralinmicroemulgeltargeteddeliveryforpsoriasisandacne
AT anushabilal optimizationofanthralinmicroemulgeltargeteddeliveryforpsoriasisandacne
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