Department of Pharmaceutics of Drug Delivery, University of Mississippi, University, Mississippi 38677.
KLE College of Pharmacy, Bengaluru, Karnataka, India; Institute for Drug Delivery and Biomedical Research (IDBR), Pharmaceutics, Bengaluru, Karnataka, India.
J Pharm Sci. 2020 May;109(5):1747-1751. doi: 10.1016/j.xphs.2020.01.030. Epub 2020 Feb 6.
Cystic fibrosis is diagnosed in infants by estimating the levels of chloride ions present in the sweat induced by iontophoresis of pilocarpine solution. Elevated levels of chloride (≥60 mMol/L) in sweat are indicative of cystic fibrosis. However, the iontophoretic method of delivering pilocarpine is cumbersome and usually is associated with several side effects such as skin burn, skin rashes, erythema, and so forth. The objective of this study was therefore to develop a topical formulation that delivers adequate amount of pilocarpine. The drug delivery of formulation was compared with iontophoresis of aqueous solution of pilocarpine nitrate in vitro using porcine skin model. The pilocarpine levels in the skin exposed to topical pilocarpine solution under mild hyperthermia was 152.04 ± 52.23 μg/cm after 10 min of application, whereas it was 97.05 ± 27.93 μg/cm in the skin after 10 min of iontophoresis. The topical formulation was subjected to clinical evaluation to assess the efficacy of the product to induce sweat production. The average amount of the sweat secreted on application of topical formulation was found to be 77.28 ± 18.97 mg. Based on these results, it was found that the topical formulation was successful in delivering pilocarpine and to stimulate sweat secretion.
囊性纤维化是通过估计电渗析毛果芸香碱溶液引起的汗液中氯离子的水平来在婴儿中诊断的。汗液中氯离子（≥60mMol/L）升高表明存在囊性纤维化。然而，电渗析方法输送毛果芸香碱很麻烦，通常与皮肤灼伤、皮疹、红斑等副作用有关。因此，本研究的目的是开发一种可输送足够量毛果芸香碱的局部制剂。使用猪皮模型，将制剂的药物输送与硝酸毛果芸香碱水溶液的电渗析进行了体外比较。在 10 分钟的应用后，在温和的热疗下暴露于局部毛果芸香碱溶液的皮肤中毛果芸香碱的水平为 152.04±52.23μg/cm，而在电渗析 10 分钟后为 97.05±27.93μg/cm。对该局部制剂进行了临床评估，以评估产品诱导出汗的功效。发现局部制剂应用后分泌的汗液平均量为 77.28±18.97mg。基于这些结果，发现局部制剂成功地输送了毛果芸香碱并刺激了汗液分泌。
