Salatin Sara, Barar Jaleh, Barzegar-Jalali Mohammad, Adibkia Khosro, Kiafar Farhad, Jelvehgari Mitra
Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Science, Tabriz, I.R. Iran; Student Research Committee, Tabriz University of Medical Science, Tabriz, I.R. Iran.
Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Science, Tabriz, I.R. Iran; Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, I.R. Iran.
Res Pharm Sci. 2017 Feb;12(1):1-14. doi: 10.4103/1735-5362.199041.
Rivastigmine hydrogen tartrate (RHT), one of the potential cholinesterase inhibitors, has received great attention as a new drug candidate for the treatment of Alzheimer's disease. However, the bioavailability of RHT from the conventional pharmaceutical forms is low because of the presence of the blood brain barrier. The main aim of the present study was to prepare positively charged Eudragit RL 100 nanoparticles as a model scaffold for providing a sustained release profile for RHT. The formulations were evaluated in terms of particle size, zeta potential, surface morphology, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). Drug entrapment efficiency and release properties of lyophilized nanoparticles were also examined. The resulting formulations were found to be in the size range of 118 nm to 154 nm and zeta potential was positive (+22.5 to 30 mV). Nanoparticles showed the entrapment efficiency from 38.40 ± 8.94 to 62.00 ± 2.78%. An increase in the mean particle size and the entrapment efficiency was observed with an increase in the amount of polymer. The FTIR, XRD, and DSC results ruled out any chemical interaction between the drug and Eudragit RL100 polymer. RHT nanoparticles containing low ratio of polymer to drug (4:1) presented a faster drug release and on the contrary, nanoparticles containing high ratio of polymer to drug (10:1) were able to give a more sustained release of the drug. The study revealed that RHT nanoparticles were capable of releasing the drug in a prolonged period of time and increasing the drug bioavailability.
酒石酸氢卡巴拉汀（RHT）是一种潜在的胆碱酯酶抑制剂，作为治疗阿尔茨海默病的新药候选物受到了广泛关注。然而，由于血脑屏障的存在，传统剂型的RHT生物利用度较低。本研究的主要目的是制备带正电荷的Eudragit RL 100纳米颗粒，作为为RHT提供缓释特性的模型支架。对制剂进行了粒径、zeta电位、表面形态、X射线衍射（XRD）、傅里叶变换红外光谱（FTIR）和差示扫描量热法（DSC）等方面的评估。还研究了冻干纳米颗粒的药物包封率和释放特性。所得制剂的粒径范围为118 nm至154 nm，zeta电位为正（+22.5至30 mV）。纳米颗粒的包封率为38.40±8.94%至62.00±2.78%。随着聚合物用量的增加，平均粒径和包封率均有所增加。FTIR、XRD和DSC结果排除了药物与Eudragit RL100聚合物之间的任何化学相互作用。聚合物与药物比例低（4:1）的RHT纳米颗粒药物释放较快，相反，聚合物与药物比例高（10:1）的纳米颗粒能够使药物更持续地释放。该研究表明，RHT纳米颗粒能够长时间释放药物并提高药物生物利用度。
