Gobbato Cíntia, Gobbato André, Magalhães Tainah B, Mendes Gustavo D, Ilha Jaime O, Moreno Ronilson A, Antunes Natalícia J, De Nucci Gilberto
Department of Pharmacology, Faculty of Medical Sciences, State University of Campinas (UNICAMP), Campinas, Brazil.
Galeno Research Unit, Campinas, Brazil.
Lasers Surg Med. 2019 Sep;51(7):609-615. doi: 10.1002/lsm.23071. Epub 2019 Feb 27.
Nanotechnology may increase the speed of penetration into the skin. This study evaluated the efficacy, safety, and pharmacokinetics of a novel topical anesthetic nanocapsule formulation (2 g) containing 2.5% lidocaine and 2.5% prilocaine (nanorap-test formulation) compared to placebo (control formulation) in skin types I-III patients of both sexes submitted to the ablative fractional CO laser treatment.
The patients (n = 120) included in this double-blind, single-center, randomized trial, received topical application of 2 g of the test formulation (50 mg lidocaine + 50 mg prilocaine) and placebo on the forehead region. Efficacy was assessed as pain sensation in four quadrants of each side of the forehead using a visual analogue scale immediately (0 min) and at 30, 60, and 90 minutes after laser application compared to placebo. The safety and tolerability of the test product were evaluated based on the occurrence of systemic adverse events as well as the occurrence of immediate and late skin reactions. Pharmacokinetic evaluation was performed in plasma of eight patients using a validated LC-MS/MS method for drugs quantification.
Nanorap induced a clinically significant reduction in the pain assessment at all evaluated times (57.2%, 41.6%, 38.6%, and 37.3% at 0, 30, 60, and 90 minutes after drug application, respectively. Mean values of C were 14.20 and 5.36 ng/ml and t were 3.5 and 1.8 hour for lidocaine and prilocaine, respectively. No systemic adverse events were observed.
The nanorap formulation demonstrated a clinically and statistically significant efficacy providing analgesia after the ablative fractional CO laser therapy in the investigated patients, when compared to placebo. The product also presented good safety and tolerability. Lasers Surg. Med. © 2019 Wiley Periodicals, Inc.
纳米技术可能会提高药物渗透皮肤的速度。本研究评估了一种新型局部麻醉纳米胶囊制剂（2g）的疗效、安全性和药代动力学，该制剂含有2.5%利多卡因和2.5%丙胺卡因（纳米rap - 测试制剂），并将其与安慰剂（对照制剂）进行比较，研究对象为接受剥脱性分数CO₂激光治疗的I - III型皮肤的男女患者。
纳入本双盲、单中心、随机试验的患者（n = 120），在前额区域局部应用2g测试制剂（50mg利多卡因 + 50mg丙胺卡因）和安慰剂。与安慰剂相比，在激光治疗后立即（0分钟）以及30、60和90分钟时，使用视觉模拟量表评估前额两侧四个象限的疼痛感觉来评价疗效。基于全身不良事件的发生情况以及即时和迟发性皮肤反应的发生情况来评估测试产品的安全性和耐受性。使用经过验证的LC - MS/MS方法对八名患者的血浆进行药物定量，以进行药代动力学评估。
纳米rap在所有评估时间均使疼痛评估有临床显著降低（用药后0、30、60和90分钟时分别降低57.2%、41.6%、38.6%和37.3%）。利多卡因和丙胺卡因的Cmax均值分别为14.20和5.36ng/ml，tmax分别为3.5和1.8小时。未观察到全身不良事件。
与安慰剂相比，纳米rap制剂在接受调查的患者中，在剥脱性分数CO₂激光治疗后显示出临床和统计学上显著的镇痛疗效。该产品还具有良好的安全性和耐受性。激光外科与医学。©2019威利期刊公司。
