Devkar Tejas B, Tekade Avinash R, Khandelwal Kishanchandra R
Department of Pharmaceutics, Rajarshi Shahu College of Pharmacy and Research, Tathawade, Pune 411033, India.
Department of Pharmaceutics, Rajarshi Shahu College of Pharmacy and Research, Tathawade, Pune 411033, India.
Colloids Surf B Biointerfaces. 2014 Oct 1;122:143-150. doi: 10.1016/j.colsurfb.2014.06.037. Epub 2014 Jul 2.
The objective of this investigation was to fabricate ondansetron hydrochloride [OND] loaded mucoadhesive nanostructured lipid carriers [NLCs] for efficient delivery to brain through nasal route. Mucoadhesive NLCs thereby sustaining drug release for longer time in nasal cavity. NLCs were prepared by high pressure homogenization [HPH] technique using glycerol monostearate [GMS]; as solid lipid, Capryol 90; as liquid lipid, soya lecithin; as surfactant and poloxamer 188; as cosurfactant. In the fabrication of NLCs, Delonix regia gum [DRG], isolated from seeds of D. regia belonging to family fabiaceae was used as a mucoadhesive polymer. The NLCs were evaluated for particle size, morphology, drug-entrapment efficiency [%EE], mucoadhesive strength, in vitro drug release, histological examination, ex vivo permeation study, in vivo biodistribution and pharmacokinetic studies in the brain/blood following intravenous [i.v.] and intranasal [i.n.] administration. Particle size, PDI, Zeta potential was observed in the range of 92.28-135nm, 0.32-0.46, and -11.5 to -36.2 respectively. Prepared NLCs achieved thermodynamic stability, control release pattern with minor histopathological changes in sheep nasal mucosa. The significantly [P<0.05] higher values for selected batch was observed, when administered by i.n. route showed higher drug targeting efficiency [506%] and direct transport percentage [97.14%] which confirms the development of promising OND-loaded NLC for efficient nose-to-brain delivery.
本研究的目的是制备载有盐酸昂丹司琼[OND]的黏膜黏附性纳米结构脂质载体[NLCs],以通过鼻腔途径有效地将药物输送到脑部。黏膜黏附性NLCs可在鼻腔中长时间维持药物释放。使用单硬脂酸甘油酯[GMS]作为固体脂质、辛酸癸酸甘油三酯90[Capryol 90]作为液体脂质、大豆卵磷脂作为表面活性剂以及泊洛沙姆188作为助表面活性剂,通过高压均质[HPH]技术制备NLCs。在制备NLCs时,使用从豆科植物凤凰木种子中分离出的凤凰木胶[DRG]作为黏膜黏附性聚合物。对NLCs进行了粒径、形态、药物包封率[%EE]、黏膜黏附强度、体外药物释放、组织学检查、离体渗透研究、静脉内[i.v.]和鼻内[i.n.]给药后在脑部/血液中的体内生物分布和药代动力学研究。观察到粒径、多分散指数[PDI]、zeta电位分别在92.28 - 135nm、0.32 - 0.46和 - 11.5至 - 36.2的范围内。制备的NLCs实现了热力学稳定性、控释模式,且对绵羊鼻黏膜的组织病理学变化较小。当通过鼻内途径给药时,所选批次的数值显著[P<0.05]更高,显示出更高的药物靶向效率[506%]和直接转运百分比[