Alaayedi Maryam H, Maraie Nidhal K
Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Iraq.
Department of Pharmaceutics, College of Pharmacy, Al-Farahidi University, Iraq.
Saudi Pharm J. 2023 Aug;31(8):101692. doi: 10.1016/j.jsps.2023.06.025. Epub 2023 Jun 28.
Nose-to-brain delivery allows the direct targeting of drug molecules bypassing the Blood Brain Barrier and systemic effect. Nanoemulsion is one of the novel strategies to deliver drug in this route due to its simplicity in manufacturing, long-term stability, and strong solubilization property for drug. The anticancer drug lomustine had poor oral bioavailability in addition to its serious side effect, therefore, developing more effective drug delivery with direct targeting towards the brain through intra-nasal administration applying nanoemulsion technology is a promising alternative. The work involved lomustine solubility screening in oils, surfactants and cosurfactants as well as emulsifier ratio (Smix) nanoemulsion area was identified using pseudo-ternary phase diagrams. Eighteen nanoemulsion formulas were produced for optimization, then characterized for droplet size, polydispersity index, zeta potential, entrapment efficiency, conductivity, transmittance, dilution, visual transparency, physical stability and in vitro release. The optimum NE formula showed droplet size, zeta potential, polydispersity index, entrapment efficiency, %transmittance, conductivity of 31.31 nm, -30.65 mV, 0.159, 98.12%, 99.08%, and 951 us/cm, respectively. The best formula released 100% lomustine within 15 min which is a promising potential drug delivery system that may deliver the drug quickly and directly to the brain as a safe and effective alternative to oral delivery.
鼻脑给药可使药物分子直接靶向，绕过血脑屏障和全身效应。纳米乳剂是通过这种途径给药的新型策略之一，因其制备简单、长期稳定性好以及对药物的强增溶性能。抗癌药物洛莫司汀除了副作用严重外，口服生物利用度也很差，因此，应用纳米乳剂技术通过鼻内给药开发更有效的直接靶向大脑的药物递送系统是一种有前途的替代方法。该工作涉及在油、表面活性剂和助表面活性剂中进行洛莫司汀的溶解度筛选，并使用伪三元相图确定乳化剂比例（Smix）纳米乳剂区域。制备了18种纳米乳剂配方用于优化，然后对其液滴大小、多分散指数、zeta电位、包封率、电导率、透光率、稀释度、视觉透明度、物理稳定性和体外释放进行表征。最佳纳米乳剂配方的液滴大小、zeta电位、多分散指数、包封率、透光率百分比、电导率分别为31.31nm、-30.65mV、0.159、98.12%、99.08%和951μs/cm。最佳配方在15分钟内释放了100%的洛莫司汀，这是一种有前途的潜在药物递送系统，可能作为口服给药的安全有效替代方法，将药物快速直接递送至大脑。
