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. 2025 Jun 17;30(12):2629.
doi: 10.3390/molecules30122629.

Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne

Samiksha Sakarkar  1 , Swati Jagdale  1 , Shrikant Dargude  1 , Anuruddha Chabukswar  1 , Shabana Urooj  2 , Anusha Bilal  3 , Hanan Abdullah Mengash  4
Affiliations

Optimization of Anthralin Microemulgel Targeted Delivery for Psoriasis and Acne

Samiksha Sakarkar et al. Molecules. .

Abstract

Background: 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. Method: 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 Result: 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% w/v 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 P. acne 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. Conclusions: Combination therapy with Clindamycin might improve efficacy while reducing antibiotic resistance risks.

Keywords: acne; anthralin; central-composite design; microemulgel; molecular docking; psoriasis.

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Conflict of interest statement

The authors declare no conflicts of interest.

Figures

Figure 1
Figure 1
Screening of excipients.
Figure 2
Figure 2
Pseudo-ternary phase diagram.
Figure 3
Figure 3
(a1–a3) Perturbation plots and (b1–b3) actual vs. predicted plot of PS, ZP, and %T.
Figure 4
Figure 4
Three-dimensional surface plots of the PS, ZP, and %T.
Figure 5
Figure 5
Two-dimensional contour plots of the PS, ZP, and %T.
Figure 6
Figure 6
Optimized batch of ME.
Figure 7
Figure 7
Particle size and zeta potential of optimized batch of ME and microemulgel.
Figure 8
Figure 8
Evaluation of microemulgel batch.
Figure 9
Figure 9
In vitro release profiles of microemulgel batch.
Figure 10
Figure 10
MTT assay and zone of inhibition for Propionibacterium organism of microemulgel batch.
Figure 11
Figure 11
Molecular docking of psoriasis proteins with anthralin.
Figure 12
Figure 12
Molecular docking of P. acne proteins with anthralin (ANT) and Clindamycin (CLN).
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