Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka State, India.
School of Cancer & Pharmaceutical Sciences, Faculty of Life Sciences & Medicine, King's College London, London SE1 9NH, UK.
Nanomedicine (Lond). 2019 Apr;14(7):889-910. doi: 10.2217/nnm-2018-0289. Epub 2019 Mar 15.
To prepare nanostructured lipid carriers (NLCs) loaded with asenapine maleate (ASPM) to increase its oral bioavailability by intestinal lymphatic uptake.
MATERIALS & METHODS: ASPM-NLCs were prepared by ultrasound dispersion technique, by adopting Design of Experiment approach, and characterized.
The optimized formulation exhibited good physicochemical parameters. Differential scanning calorimetry and x-ray diffraction studies indicated the amorphized nature of ASPM in lipid matrix. In vitro drug release study indicated the sustained release of drug from NLCs. ASPM-NLCs showed greater permeability across Caco2 cells and everted rat ileum. ASPM-NLCs showed greater cellular uptake, superior preclinical oral bioavailability and higher efficacy in reducing the L-DOPA-carbidopa-induced locomotor count compared with plain drug.
ASPM-NLCs were successfully developed that showed enhanced performance both in vitro and in vivo.
制备载马来酸阿散普林（ASPM）的纳米结构脂质载体（NLC），通过肠淋巴摄取提高其口服生物利用度。
采用实验设计法，通过超声分散技术制备 ASPM-NLC，并对其进行表征。
优化的配方表现出良好的物理化学参数。差示扫描量热法和 X 射线衍射研究表明 ASPM 在脂质基质中呈无定形态。体外药物释放研究表明药物从 NLC 中持续释放。ASPM-NLC 表现出更大的跨 Caco2 细胞和翻转大鼠回肠的渗透性。ASPM-NLC 表现出更高的细胞摄取率，优于普通药物，具有更高的口服生物利用度和更高的疗效，可降低 L-多巴-卡比多巴诱导的运动计数。
成功制备了载马来酸阿散普林的纳米结构脂质载体，其在体外和体内均表现出增强的性能。
