School of Pharmacy, Sharda University, Greater Noida, Uttar Pradesh, 201306, India.
Nanoformulation Laboratory, Department of Pharmaceutics, School of Pharmaceutical Education and Research (erstwhile Faculty of Pharmacy), Jamia Hamdard, New Delhi, 110062, India.
AAPS PharmSciTech. 2018 Feb;19(2):573-589. doi: 10.1208/s12249-017-0868-0. Epub 2017 Sep 5.
In the present study, the potential of transdermal nanoemulsion gel of selegiline hydrochloride for the treatment of Parkinson's disease was investigated. Water-in-oil nanoemulsions were developed by comparing low- and high-energy methods and were subjected to thermodynamic stability tests, in vitro permeation, and characterization studies. In vitro studies indicated that components of nanoemulsion acted as permeation enhancers with highest flux of 3.531 ± 1.94 μg/cm/h from nanoemulsion SB6 containing 0.5 mg selegiline hydrochloride, 3% distilled water, 21% S (Span 85, Tween 80, PEG 400), and 76% isopropyl myristate by weight. SB6 with the least droplet size of 183.4 ± 0.35 nm, polydispersity index of 0.42 ± 0.06 with pH of 5.9 ± 0.32 and viscosity of 22.42 ± 0.14 cps was converted to nanoemulsion gel NEGS4 (viscosity = 22,200 ± 400 cps) by addition of Viscup160® for ease of application and evaluated for permeation, safety, and pharmacokinetic profile in Wistar rats. It provided enhancement ratio 3.69 times greater than conventional gel. NEGS4 showed 6.56 and 5.53 times increase in bioavailability in comparison to tablet and conventional gel, respectively, along with sustained effect. Therefore, the developed water-in-oil nanoemulsion gel promises to be an effective vehicle for transdermal delivery of selegiline hydrochloride.
在本研究中,考察了盐酸司来吉兰经皮纳米乳凝胶治疗帕金森病的潜力。通过比较低能和高能方法开发了油包水型纳米乳,并进行了热力学稳定性试验、体外渗透和特性研究。体外研究表明,纳米乳的成分具有较高的渗透增强作用,其中包含 0.5mg 盐酸司来吉兰、3%蒸馏水、21% S(Span 85、Tween 80、PEG 400)和 76%异丙基肉豆蔻酸的纳米乳 SB6 的通量最高,为 3.531±1.94μg/cm/h。SB6 的粒径最小,为 183.4±0.35nm,多分散指数为 0.42±0.06,pH 值为 5.9±0.32,粘度为 22.42±0.14cps,通过加入 Viscup160®(粘度=22200±400cps)转化为纳米乳凝胶 NEGS4,便于应用,并在 Wistar 大鼠中评价了其渗透、安全性和药代动力学特征。与常规凝胶相比,其提供了 3.69 倍的增强比。与片剂和常规凝胶相比,NEGS4 的生物利用度分别提高了 6.56 倍和 5.53 倍,且具有持续作用。因此,所开发的水包油型纳米乳凝胶有望成为盐酸司来吉兰经皮传递的有效载体。