Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKMs NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, Maharashtra 400056, India.
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKMs NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, Maharashtra 400056, India.
Int J Biol Macromol. 2020 Dec 1;164:717-725. doi: 10.1016/j.ijbiomac.2020.07.168. Epub 2020 Jul 19.
Naringenin, a bioflavonoid, is a natural alternative for atopic dermatitis that possesses anti-inflammatory, antioxidant and photo-protective action. The primary objective of this study is to prepare and evaluate naringenin-loaded microsponge gel for dermatitis. Ethyl cellulose based microsponges of naringenin were prepared by quasi-emulsion-solvent diffusion and statistically optimized by 3 factorial design. After in vitro characterization, optimized microsponge batch (Trial 3) was incorporated into Carbopol base to prepare 1% naringenin-loaded microsponge gel (NGMSG1%) which was evaluated for skin irritation, in vivo efficacy and drug deposition in DNFB-challenged albino Wistar rats in comparison to 1% plain naringenin gel (NGG1%). The average particle size and in vitro drug release of optimized microsponge formulation was observed to be 180 μm and 92.3% ± 2.37 at the end of 24 h, and entrapment was achieved till 82%. SEM study confirmed porous, spherical shaped microsponges whereas FTIR and DSC data supported the formation of microsponges. No skin irritation was observed with NGMSG and NGG in animals. NGMSG1% showed faster healing, substantial reduction in thickness of swollen earflap and WBC count than NGG1%. Similarly, NGMSG showed 3-fold greater drug deposition in skin than plain gel. Thus, naringenin loaded microsponge gel can be further explored as natural remedy for atopic dermatitis.
柚皮苷是一种生物类黄酮,是一种天然的异位性皮炎替代药物,具有抗炎、抗氧化和光保护作用。本研究的主要目的是制备和评价柚皮苷负载微海绵凝胶治疗皮炎。采用准乳液-溶剂扩散法制备柚皮苷乙基纤维素微海绵,并通过 3 因素设计进行统计学优化。体外特性评价后,将优化后的微海绵批次(试验 3)加入卡波姆基质中,制备 1%柚皮苷负载微海绵凝胶(NGMSG1%),并与 1%普通柚皮苷凝胶(NGG1%)进行比较,评估其对二硝基氟苯(DNFB)诱导的白化 Wistar 大鼠的皮肤刺激性、体内疗效和药物沉积。优化后的微海绵制剂的平均粒径和体外药物释放观察到在 24 小时结束时为 180μm 和 92.3%±2.37,包封率达到 82%。SEM 研究证实了多孔、球形微海绵,而 FTIR 和 DSC 数据支持微海绵的形成。NGMSG 和 NGG 在动物中均未引起皮肤刺激。NGMSG1%在肿胀耳瓣厚度和白细胞计数方面的愈合速度更快,显著减少,与 NGG1%相比。同样,NGMSG 在皮肤中的药物沉积量是普通凝胶的 3 倍。因此,柚皮苷负载微海绵凝胶可进一步探索作为治疗异位性皮炎的天然药物。