title: Development, characterization and nasal delivery of rosmarinic acid-loaded solid lipid nanoparticles for the effective management of Huntington's disease.
abstract: OBJECTIVE
  The objective of the present study was to investigate the potential use of solid lipid nanoparticles (SLNs) as a drug delivery system to enhance the brain-targeting efficiency of rosmarinic acid (RA) following intranasal (i.n.) administration.
  
  
  METHODS
  The RA-loaded SLNs was prepared by the hot homogenization technique, in which glycerol monostearate (GMS) as lipid, tween 80 and soya lecithin were used as surfactant along with hydrogenated soya phosphatidyl choline (HSPC) as a stabilizer, and were characterized for particle size, zeta potential (ZP), in vitro study. Nasal delivery of the developed formulation followed by the study of behavioral (locomotor, narrow beam, body weight) and biochemical parameters (glutathione, lipid peroxidation, catalase and nitrite) in wistar rat was carried out.
  
  
  RESULTS
  Optimized RA-loaded SLNs using tween 80 (SLNPRT) have the mean size of (149.2 ± 3.2 nm), ZP (-38.27 mV) entrapment efficiency (61.9 ± 2.2%). 3-NP-treated rat significantly increased behavioral alterations, oxidative damage as compared with the control group. SLNPRT treatment significantly improved behavioral abnormalities and attenuated the oxidative stress in 3NP-treated rats. However, the nasal delivery of SLNPRT produced significant therapeutic action as compared to intravenous application. In the organ distribution study, brain drug concentration was found to be 5.69 µg, in pharmacokinetic study Cmax, tmax, t1/2, AUC values were found to be 0.284 µg/ml, 1.5 h, 3.17 h, and 1.505 µg/ml/h, respectively.
  
  
  CONCLUSIONS
  The encouraging results confirmed the developed optimized RA-loaded SLNs formulation following the non-invasive nose-to-brain drug delivery that is a promising therapeutic approach for the effective management in Huntington disease.
authors: a Department of Pharmaceutics and.
authors: Rahul
authors: R
authors: Bhatt
authors: a Department of Pharmaceutics and.
authors: Devendra
authors: D
authors: Singh
authors: b Department of Pharmacology , I.S.F. College of Pharmacy , Moga , Punjab , India.
authors: Atish
authors: A
authors: Prakash
authors: a Department of Pharmaceutics and.
authors: Neeraj
authors: N
authors: Mishra
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D019540:Area Under Curve; D001522:Behavior, Animal / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002934:Cinnamates / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D053630:Depsides / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D006207:Half-Life; D006816:Huntington Disease / Q000188:drug therapy; D008055:Lipids / Q000737:chemistry; D008297:Male; D053758:Nanoparticles; D018384:Oxidative Stress / Q000187:drug effects; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D013501:Surface-Active Agents / Q000737:chemistry; D014018:Tissue Distribution; D000097123:Rosmarinic Acid
chemical_list: D000975:Antioxidants; D002934:Cinnamates; D053630:Depsides; D005079:Excipients; D008055:Lipids; D013501:Surface-Active Agents; D000097123:Rosmarinic Acid
keywords: 3-NP; HSPC; RA; SLNs; huntington; intra nasal