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

渗透 差示扫描量热法 色谱法 凝胶渗透色谱法 化学 粒径 聚合物 有机化学 热力学 生物化学 物理 物理化学
作者
Qiuyan Ma,Jing Zhang,Bohong Lu,Huaqing Lin,Rajib Sarkar,Tao Wu,Xuee Li
出处
期刊:Aaps Pharmscitech [Springer Science+Business Media]
卷期号:22 (5) 被引量:18
标识
DOI:10.1208/s12249-021-02035-5
摘要

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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