Shrotriya S N, Ranpise N S, Vidhate B V
Sinhgad College of Pharmacy, Vadgaon(Bk.), Pune S. No 44/1, Vadgaon (Bk), Off Sinhgad Road, Pune, MS, 411041, India.
Drug Deliv Transl Res. 2017 Feb;7(1):37-52. doi: 10.1007/s13346-016-0350-7.
Irritant contact dermatitis (ICD) is a chronic and relapsing skin disease with severe eczematous lesions. Despite its growing prevalence, therapeutic treatments remain limited. Long-term topical corticosteroid treatment can induce skin atrophy, hypopigmentation, and increase in transepidermal water loss. An innovative dermal treatment is essential to reduce the side effects of corticosteroids. Topical resveratrol (RES), although effective for ICD, is a challenging molecule due to low solubility and poor bioavailability. The objective of this work was to build RES-loaded solid lipid nanoparticles (RES-SLNs) with skin targeting. For this purpose, RES-SLNs were prepared using the probe ultrasonication method utilizing Precirol ATO 5 and Tween 20. The RES-SLNs were evaluated for particle size, entrapment efficiency (EE), and transmission electron microscopy (TEM) studies. Further, RES-SLNs were incorporated into Carbopol gel and investigated for ex vivo skin permeation, deposition study on human cadaver skin, and finally skin irritation study on New Zealand White rabbits. It was further assessed for possible beneficial effects on ICD using BALB/c mice. RES-SLN showed mean size below 100 nm and 68-89% EE. TEM studies confirmed spherical particles in the nanometer range. An ex vivo study of RES-SLN-loaded gel exhibited controlled drug release up to 24 h; similarly, in vitro drug deposition studies showed potential of skin targeting with no skin irritation. RES-SLN gel confirmed competent suppression of ear swelling and reduction in skin water content in the BALB/c mouse model of ICD when compared to marketed gel. Thus, the formulated RES-SLN gel would be a safe and effective alternative to conventional vehicles for treatment of ICD.
刺激性接触性皮炎（ICD）是一种伴有严重湿疹样病变的慢性复发性皮肤病。尽管其患病率不断上升，但治疗方法仍然有限。长期局部使用皮质类固醇治疗可导致皮肤萎缩、色素减退，并增加经表皮水分流失。一种创新的皮肤治疗方法对于减少皮质类固醇的副作用至关重要。局部使用白藜芦醇（RES）虽然对ICD有效，但由于其低溶解度和差的生物利用度，是一种具有挑战性的分子。这项工作的目的是构建具有皮肤靶向性的载RES固体脂质纳米粒（RES-SLNs）。为此，使用Precirol ATO 5和吐温20通过探头超声法制备RES-SLNs。对RES-SLNs进行了粒径、包封率（EE）和透射电子显微镜（TEM）研究。此外，将RES-SLNs掺入卡波姆凝胶中，并研究其体外皮肤渗透、在人体尸体皮肤上的沉积研究，最后在新西兰白兔上进行皮肤刺激性研究。使用BALB/c小鼠进一步评估其对ICD可能的有益作用。RES-SLN的平均粒径低于100 nm，包封率为68-
89%。TEM研究证实了纳米级的球形颗粒。对载有RES-SLN的凝胶进行的体外研究显示药物可控制释放长达24小时；同样，体外药物沉积研究表明其具有皮肤靶向潜力且无皮肤刺激性。与市售凝胶相比，RES-SLN凝胶在ICD的BALB/c小鼠模型中证实了对耳部肿胀的有效抑制和皮肤水分含量的降低。因此，所制备的RES-SLN凝胶将是治疗ICD的传统载体的一种安全有效的替代品。
