Surface engineered nanostructured lipid carriers for efficient nose to brain delivery of ondansetron HCl using Delonix regia gum as a natural mucoadhesive polymer

被引:87
作者
Devkar, Tejas B. [1 ]
Tekade, Avinash R. [1 ]
Khandelwal, Kishanchandra R. [1 ]
机构
[1] Rajarshi Shahu Coll Pharm & Res, Dept Pharmaceut, Pune 411033, Maharashtra, India
关键词
Nanostructured lipid carrier; Ondansetron HCl; Nose to brain delivery; Delonix regia gum; Surface modification; Mucoadhesion; DRUG-DELIVERY; INTRANASAL DELIVERY; NANOPARTICLES; BARRIER; FORMULATION; TRANSPORT;
D O I
10.1016/j.colsurfb.2014.06.037
中图分类号
Q6 [生物物理学];
学科分类号
071011 ;
摘要
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 92.28-135 nm, 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 197.14%] which confirms the development of promising OND-loaded NLC for efficient nose-to-brain delivery. (C) 2014 Elsevier B.V. All rights reserved.
引用
收藏
页码:143 / 150
页数:8
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