Romeo Martina, Mazzotta Elisabetta, Perrotta Ida Daniela, Muzzalupo Rita
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, Italy.
Centre for Microscopy and Microanalysis (CM2), Department of Biology Ecology and Earth Sciences, University of Calabria, 87036 Arcavacata di Rende, Italy.
Pharmaceutics. 2022 Oct 14;14(10):2190. doi: 10.3390/pharmaceutics14102190.
Lidocaine is a local anaesthetic drug with an amphiphilic structure able to self-associate, under certain conditions, in molecular aggregates playing the role of both carrier and drug. The aim of this study was to determine the optimal conditions for obtaining vesicular carriers, called lidosomes. The new formulations were obtained using both lidocaine and lidocaine hydrochloride and different hydration medias (distilled water, acid, and basic aqueous solution). Lidosomes formulations were characterized in terms of size, ζ-potential, drug retained, stability formulation, and ex vivo permeation profile. Moreover, lidosomes were incorporated in two different gel structures: one based on carboxymethylcellulose and one based on pluronic F-127 to achieve suitable properties for a topical application. Results obtained showed that lidocaine showed a better performance to aggregate in vesicular carriers in respect to hydrochloride form. Consequently, only formulations comprised of lidocaine were studied in terms of skin permeation performance and as carriers of another model drug, capsaicin, for a potential combined therapy. Lidocaine, when in form of vesicular aggregates, acted as percutaneous permeation enhancer showing better permeation profiles with respect to drug solutions. Moreover, lidosomes created a significant drug depot into the skin from which the drug was available for a prolonged time, a suitable feature for a successful local therapy.
利多卡因是一种具有两亲结构的局部麻醉药物，在特定条件下能够自缔合形成分子聚集体，兼具载体和药物的作用。本研究的目的是确定获得称为利多卡因脂质体的囊泡载体的最佳条件。使用利多卡因和盐酸利多卡因以及不同的水化介质（蒸馏水、酸和碱性水溶液）获得了新的制剂。对利多卡因脂质体制剂的大小、ζ电位、药物保留率、制剂稳定性和体外渗透特性进行了表征。此外，将利多卡因脂质体掺入两种不同的凝胶结构中：一种基于羧甲基纤维素，另一种基于泊洛沙姆F-127，以获得适合局部应用的特性。所得结果表明，与盐酸盐形式相比，利多卡因在囊泡载体中表现出更好的聚集性能。因此，仅对由利多卡因组成的制剂进行了皮肤渗透性能研究，并将其作为另一种模型药物辣椒素的载体用于潜在的联合治疗。当以囊泡聚集体形式存在时，利多卡因作为经皮渗透促进剂，与药物溶液相比显示出更好的渗透特性。此外，利多卡因脂质体在皮肤中形成了一个重要的药物贮库，药物可从该贮库中长时间释放，这是成功进行局部治疗的一个合适特性。
