Dalwadi Saloni, Thakkar Vaishali, Prajapati Bhupendra
Gujarat Technological University, Ahmedabad, Gujarat, 382424, India.
Department of Pharmaceutics, Anand Pharmacy College, Anand, Gujarat, 388001, India.
Pharm Nanotechnol. 2025;13(1):184-198. doi: 10.2174/0122117385294969240326052312.
Dementia associated with Alzheimer's disease (AD) is a neurological disorder. AD is a progressive neurodegenerative condition that predominantly impacts the elderly population, although it can also manifest in younger people through the impairment of cognitive functions, such as memory, cognition, and behaviour. Donepezil HCl and Memantine HCl are encapsulated in Nanostructured Lipid Carriers (NLCs) to prolong systemic circulation and minimize the systemic side effects.
This work explores the use of data mining tools to optimize the formulation of NLCs comprising of Donepezil HCl and Memantine HCl for transdermal drug delivery. Neuroprotective drugs and excipients are utilized for protecting the nervous system against damage or degeneration.
The NLCs were formulated using a high-speed homogenization technique followed by ultrasonication. NLCs were optimized using Box Behnken Design (BBD) in Design Expert Software and artificial neural network (ANN) in IBM SPSS statistics. The independent variables included the ratio of solid lipid to liquid lipid, the percentage of surfactant, and the revolutions per minute (RPM) of the high-speed homogenizer.
The NLCs that were formulated had a mean particle size ranging from 67.0±0.45 to 142.4±0.52 nm. Both drugs have a %EE range over 75%, and Zeta potential was determined to be - 26±0.36 mV. CryoSEM was used to do the structural study. The permeation study showed the prolonged release of the formulation.
The results indicate that NLCs have the potential to be a carrier for transporting medications to deeper layers of the skin and reaching systemic circulation, making them a suitable formulation for the management of Dementia. Both ANN and BBD techniques are effective tools for systematically developing and optimizing NLC formulation.
与阿尔茨海默病(AD)相关的痴呆是一种神经障碍。AD是一种进行性神经退行性疾病,主要影响老年人群,尽管它也可通过记忆、认知和行为等认知功能受损在年轻人中表现出来。盐酸多奈哌齐和美金刚被包裹在纳米结构脂质载体(NLCs)中,以延长其在体内的循环时间并将全身副作用降至最低。
本研究探索使用数据挖掘工具优化由盐酸多奈哌齐和美金刚组成的用于透皮给药的NLCs制剂。神经保护药物和辅料用于保护神经系统免受损伤或退化。
采用高速均质技术随后超声处理来制备NLCs。在Design Expert软件中使用Box Behnken设计(BBD)以及在IBM SPSS Statistics中使用人工神经网络(ANN)对NLCs进行优化。自变量包括固体脂质与液体脂质的比例、表面活性剂的百分比以及高速均质器的每分钟转数(RPM)。
所制备的NLCs的平均粒径范围为67.0±0.45至142.4±0.52 nm。两种药物的包封率(%EE)范围均超过75%,zeta电位测定为-26±(0.36 mV)。使用低温扫描电子显微镜(CryoSEM)进行结构研究。渗透研究表明该制剂具有缓释特性。
结果表明NLCs有潜力成为将药物输送到皮肤深层并进入全身循环的载体,使其成为治疗痴呆的合适制剂。ANN和BBD技术都是系统开发和优化NLC制剂的有效工具。