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Enhancing efficacy and safety of azelaic acid via encapsulation in cyclodextrin nanosponges: development, characterization and evaluation

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Abstract

Azelaic acid (AA), a promising agent for acne and hyperpigmentation disorders, is associated with side effects viz. rashes, skin irritation, dryness, burning and stinging. Its poor solubility also pose challenge in the development of suitable formulation. Therefore, this research was aimed to design cyclodextrin nanosponges (CDNS) of AA to address above-mentioned challenges. Herein, the fabrication of CDNS by melt method was demonstrated employing β-cyclodextrin (β-CD) as polymer and diphenyl carbonate (DPC) as a cross-linker. AA was loaded in CDNS via lyophilization and appropriately characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, X-ray powder diffraction and nuclear magnetic resonance. For morphological evaluation, field emission scanning electron and transmission electron microscopy were also performed. The particle size of AANS was in nanorange, with acceptable zeta potential, low polydispersity index and delayed release. The safety of the nanoformulation was assessed using Human Epidermal Keratinocyte cell lines. Further, molecular docking studies for AA was carried out. In vitro antibacterial, antioxidant and antityrosinase assay were also conducted for prepared nanoformulation. The results of all the studies performed revealed that encapsulation of AA in nanosponges led to improvement in efficacy of drug in terms of solubility, release and safety, with adequate antimicrobial, antioxidant and antityrosinase activity.

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Acknowledgements

The researchers would like to acknowledge Dr. APJ Abdul Kalam central instrument laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar for providing necessary facilities for present investigation. Jay Chem Marketing, Mumbai is also acknowledged for providing a gift sample of β-cyclodextrin. The authors also wish to thank Dr. Ajmer Singh, Department of pharmaceutical sciences, Chitkara university, Rajpura (India) for molecular docking studies.

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  1. Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, 125001, India

    Anil Kumar & Rekha Rao

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Kumar, A., Rao, R. Enhancing efficacy and safety of azelaic acid via encapsulation in cyclodextrin nanosponges: development, characterization and evaluation. Polym. Bull. 78, 5275–5302 (2021). https://doi.org/10.1007/s00289-020-03366-2

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