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Nanoemulgel for Improved Topical Delivery of Desonide: Formulation Design and Characterization

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Abstract

This research aimed to develop a novel drug delivery system to improve treatment of skin disorders. The system is comprised of a Carbopol 980-based nanoemulgel (NE-gel) containing a desonide (DES; 0.05%, w/w) nanoemulsion (NE), which has a small particle size, high encapsulation efficiency, good thermodynamic stability, good permeation ability, and high skin retention. DES-loaded NE (DES-NE) was prepared by high-pressure homogenization. The developed formulation was characterized by differential scanning calorimetry (DSC), X-ray diffraction, drug release, skin permeation, and drug retention. DES in vitro release and skin permeation studies with different formulations of artificial membrane and rat abdominal skin were performed with the Franz diffusion cell system. Confocal laser scanning microscopy (CLSM) was used to detect the localization and permeation pathways of drugs in the skin. Compared with commercially available gel (CA-gel) and NE, the NE-gel release process conformed to the Higuchi release model (R2 = 0.9813). NE-gel prolonged the drug release time and allowed for reduced administration dose and frequency. The unit cumulative permeation of NE and NE-gel through the skin for 12 h was 63.13 ± 2.78 and 42.53 ± 2.06 μg/cm2, respectively, values significantly higher (p < 0.01) than that of the CA-gel (30.65 ± 1.25 μg/cm2) and CA-cream (15.21 ± 0.97 μg/cm2). The DES-NE and DES NE-gel skin drug retention was significantly higher than commercially available formulations (p < 0.01). Hence, the prepared NE-gel is a potential vehicle for improved topical DES delivery for better treatment of skin disorders.

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Funding

This work was supported by the Science and Technology Project of Guangdong Province (grant numbers 201802010047); Innovation and Entrepreneurship Team special Fund project of Guangdong Province (grant numbers 2014ZT05Y018), and Biomedical Innovation Institution of Hong Kong & Guangdong Pharmaceutical University.

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Authors and Affiliations

  1. Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, 510006, China

    Qiuyan Ma, Jing Zhang, Bohong Lu, Huaqing Lin & Xuee Li

  2. Bright Future Pharmaceutical Lab. Ltd, Hong Kong, 999077, China

    Rajib Sarkar & Tao Wu

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  1. Qiuyan Ma
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  2. Jing Zhang
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Correspondence to Huaqing Lin.

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Animal experiments were performed according to internationally accepted ethical guidelines for the care of laboratory animals, and were approved by the Institutional Animal Care and Use Committee of Guangdong Pharmaceutical University.

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We report a nanoemulgel system with good penetrating ability and a sustained release effect that can reduces adverse reactions and side effects caused by clinical medication overdose. Here, we examine the preparation, characterization, permeability, release kinetics, rheology, and topical mechanism of a nanoemulgel.

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Ma, Q., Zhang, J., Lu, B. et al. Nanoemulgel for Improved Topical Delivery of Desonide: Formulation Design and Characterization. AAPS PharmSciTech 22, 163 (2021). https://doi.org/10.1208/s12249-021-02035-5

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