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Dapsone-Loaded Mixed Micellar Gel for Treatment OF Acne Vulgaris

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Abstract

Mixed polymeric micelles are potential nanocarriers for topical drug delivery. Dapsone (DAP) is an antibacterial used as anti-acne agent, but challenged by low water solubility and poor skin permeability. In the present study, DAP-loaded mixed micellar gel was developed comprising Pluronics F-68 and F-127. Micelles were prepared by solvent evaporation method and particle size, ex vivo permeation, drug loading, and entrapment efficiency were determined. Central Composite Design was used to optimize formulation. Independent variables were concentration of Pluronics at three levels while micelle size and drug loading capacities were dependent variables. Droplet size ranged from 400 to 500 nm. Transmission electron microscopy revealed spherical morphology of micelles. Optimized micelles were incorporated into gel base using HPMC K100M, Sodium CMC, and Carbopol 980 as gelling agents. Gels were evaluated for pH, drug content, spreadability, rheology, syneresis, ex vivo permeation, and subacute dermal toxicity. Compared with solubility of free DAP (0.24+0.056 µg/ml), solubility in mixed micelles was 18.42±3.4 µg/ml in water at room temperature. Order of spreadability of gels was Na CMC < HPMC < Carbopol 980. Carbopol gels displayed thixotropy with index of 3.17. Syneresis for all gels from day 0 to day 30 was found to be in range of 4.2 to 15.6% w/w. Subacute dermal toxicity studies showed no signs of erythema and edema on rat skin until 21 days. These results suggest that mixed micelles can significantly increase solubility and permeability and sustain release of DAP and are suitable carriers for topical DAP delivery in anti-acne therapies.

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Acknowledgements

We thank the Department of Science and Technology (DST), Ministry of Science and Technology, Government of India, for their support for TEM analysis of sample. The authors would also like to thank Dr. Makarand Kulkarni, Scientific Expert, Instrumentation Center, Punyashlok Ahilyadevi Holkar Solapur University, Solapur, for the residual solvent analysis by GC-MS.

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This work is self-funded and it has not received funding from any government or nongovernment sources.

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Authors and Affiliations

  1. Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Near R.T.O., Maharashtra, 411001, Pune, India

    Monica RP Rao

  2. Department of Pharmaceutical Quality Assurance, AISSMS College of Pharmacy, Kennedy Road, Near R.T.O., Pune, 411001, India

    Sushant Deshpande & Padmanabh Deshpande

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  1. Monica RP Rao
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Dr. Monica RP Rao: conceptualization; data curation, writing—review and editing.

Mr. Sushant Deshpande: formal analysis, investigation; methodology; resources; software

Dr. Padmanabh Deshpande: supervision; validation; visualization

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Correspondence to Monica RP Rao.

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Rao, M.R., Deshpande, S. & Deshpande, P. Dapsone-Loaded Mixed Micellar Gel for Treatment OF Acne Vulgaris. AAPS PharmSciTech 24, 109 (2023). https://doi.org/10.1208/s12249-023-02564-1

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