Enhancing efficacy and safety of azelaic acid via encapsulation in cyclodextrin nanosponges: development, characterizati
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Enhancing efficacy and safety of azelaic acid via encapsulation in cyclodextrin nanosponges: development, characterization and evaluation Anil Kumar1 · Rekha Rao1 Received: 16 March 2020 / Revised: 2 August 2020 / Accepted: 18 September 2020 © Springer-Verlag GmbH Germany, part of Springer Nature 2020
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. Keywords Antimicrobial · Antityrosinase · Antioxidant · Molecular docking · Solubility
* Rekha Rao [email protected] 1
Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar 125001, India
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Polymer Bulletin
Introduction Nowadays, the consumption of skin whitening agents or depigmenting agents and skin care cosmetic products comprises market share of billions of dollars and there is a great demand for such products all over the world [1]. Besides prevention of ageing and promotion of hair growth, depigmentation of skin and acne are the key cosmetic issues under current investigation. Particularly, East Asian women desire a lighter skin colour and hence, select products to reduce pigmentation [2]. To fulfil these demands, active moieties of natural origin were explored for decades by scientific community. Howbeit, from the available natural moieties, hunt for effective depigmenting agent is a challenging task before research scientists [3]. Hyperpigmentation is manifested as dark colour patches on the face or other body areas (nose, forehead, chin, upper lip and cheeks). This disorder causes mental stress to the patients, resulting in poor quality of life [4]. Excess producti
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