title: Surface engineered nanostructured lipid carriers for efficient nose to brain delivery of ondansetron HCl using Delonix regia gum as a natural mucoadhesive polymer.
abstract: 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.
authors.affiliation: Department of Pharmaceutics, Rajarshi Shahu College of Pharmacy and Research, Tathawade, Pune 411033, India.
authors.forename: Tejas B
authors.initials: TB
authors.lastname: Devkar
authors.affiliation: Department of Pharmaceutics, Rajarshi Shahu College of Pharmacy and Research, Tathawade, Pune 411033, India. Electronic address: avitekade@gmail.com.
authors.forename: Avinash R
authors.initials: AR
authors.lastname: Tekade
authors.affiliation: Department of Pharmaceutics, Rajarshi Shahu College of Pharmacy and Research, Tathawade, Pune 411033, India.
authors.forename: Kishanchandra R
authors.initials: KR
authors.lastname: Khandelwal
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D001812:Blood-Brain Barrier; D001921:Brain / Q000378:metabolism*; D002152:Calorimetry, Differential Scanning; D007887:Fabaceae / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D049329:Nanostructures; D017294:Ondansetron / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010316:Particle Size; D011108:Polymers / Q000737:chemistry*; D012756:Sheep; D013499:Surface Properties; D014018:Tissue Distribution; D014961:X-Ray Diffraction
chemical_list: D008055:Lipids; D011108:Polymers; D017294:Ondansetron
keywords: Delonix regia gum; Mucoadhesion; Nanostructured lipid carrier; Nose to brain delivery; Ondansetron HCl; Surface modification