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

• Published in: Colloids and surfaces, B, Biointerfaces Vol. 122; pp. 143 - 150
• Main Authors: Devkar, Tejas B., Tekade, Avinash R., Khandelwal, Kishanchandra R.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.10.2014
• Subjects: Administration, Intranasal; Animals; Blood-Brain Barrier; Brain; Brain - metabolism; Calorimetry, Differential Scanning; Carriers; Delonix regia; Delonix regia gum; Drug delivery systems; Fabaceae - chemistry; Homogenizing; Lipids; Lipids - chemistry; Microscopy, Electron, Scanning; Mucoadhesion; Nanostructure; Nanostructured lipid carrier; Nanostructures; Nose to brain delivery; Ondansetron - administration & dosage; Ondansetron - pharmacokinetics; Ondansetron HCl; Particle Size; Polymers - chemistry; Sheep; Surface modification; Surface Properties; Sustaining; Tissue Distribution; X-Ray Diffraction; Surface modification; Nanostructured lipid carrier; Ondansetron HCl; Nose to brain delivery; Delonix regia gum; Mucoadhesion
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2014.06.037

•Exploring application of natural Delonix regia gum as a mucoadhesive polymer.•Nose to brain delivery of ondansetron HCl through nanostructured lipid carriers.•Particle size was observed in the narrow range of 92.28–135nm.•Significantly higher DTE [506%] and DTP [97.14%] values for selected batch (F11). 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.