+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine



Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine



Journal of Pharmaceutical Sciences 105(3): 1209-1220



The aim of this study was to develop and characterize an intranasal delivery system for amantadine hydrochloride (AMT). Optimal formulations consisted of a thermosensitive polymer Pluronic® 127 and either carboxymethyl cellulose or chitosan which demonstrated gel transition at nasal cavity temperatures (34 ± 1°C). Rheologically, the loss tangent (Tan δ) confirmed a 3-stage gelation phenomena at 34 ± 1°C and non-Newtonian behavior. Storage of optimized formulation carboxymethyl cellulose and optimal formulation chitosan at 4°C for 8 weeks resulted in repeatable release profiles at 34°C when sampled, with a Fickian mechanism earlier on but moving toward anomalous transport by week 8. Polymers (Pluronic® 127, carboxymethyl cellulose, and chitosan) demonstrated no significant cellular toxicity to human nasal epithelial cells up to 4 mg/mL and up to 1 mM for AMT (IC50: 4.5 ± 0.05 mM). Optimized formulation carboxymethyl cellulose and optimal formulation chitosan demonstrated slower release across an in vitro human nasal airway model (43%-44% vs 79 ± 4.58% for AMT). Using a human nasal cast model, deposition into the olfactory regions (potential nose-to-brain) was demonstrated on nozzle insertion (5 mm), whereas tilting of the head forward (15°) resulted in greater deposition in the bulk of the nasal cavity.

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 057595455

Download citation: RISBibTeXText

PMID: 26886345

DOI: 10.1016/j.xphs.2015.12.016


Related references

Preparation and evaluation of spray-dried hyaluronic acid microspheres for intranasal delivery of fexofenadine hydrochloride. European Journal of Pharmaceutical Sciences 40(1): 9, 2010

Comparison of intranasal hypertonic dead sea saline spray and intranasal aqueous triamcinolone spray in seasonal allergic rhinitis. Ear Nose and Throat Journal 84(7): 426-430, 2005

Development and evaluation of nitrendipine nanoemulsion for intranasal delivery. Journal of Biomedical Nanotechnology 5(1): 62-68, 2009

Development and evaluation of carboplatin-loaded PCL nanoparticles for intranasal delivery. Drug Delivery 23(7): 2144-2153, 2016

Intranasal drug delivery by spray and drops. Journal of Pharmacy and Pharmacology 37(5): 294-297, 1985

Acyclovir liposomes for intranasal systemic delivery: development and pharmacokinetics evaluation. Drug Delivery 15(5): 313-321, 2008

Solid lipid nanoparticles of ondansetron HCl for intranasal delivery: development, optimization and evaluation. Journal of Materials Science. Materials in Medicine 23(9): 2163-2175, 2012

Gellan gum based microparticles of metoclopromide hydrochloride for intranasal delivery: development and evaluation. Chemical and Pharmaceutical Bulletin 57(4): 388-392, 2009

Sodium alginate microspheres of metoprolol tartrate for intranasal systemic delivery: development and evaluation. Drug Delivery 10(1): 21-28, 2003

Chitosan based pentazocine microspheres for intranasal systemic delivery: development and biopharmaceutical evaluation. Die Pharmazie 56(3): 223-226, 2001

Development, Optimization, and Evaluation of Carvedilol-Loaded Solid Lipid Nanoparticles for Intranasal Drug Delivery. Aaps Pharmscitech 17(6): 1353-1365, 2016

Bioavailability of Δ⁹-tetrahydrocannabinol following intranasal administration of a mucoadhesive gel spray delivery system in conscious rabbits. Drug Development and Industrial Pharmacy 37(3): 329-334, 2011

Fentanyl pectin nasal spray: a novel intranasal delivery method for the treatment of breakthrough cancer pain. Expert Review of Clinical Pharmacology 6(1): 9, 2013

Mucosal IgA responses in healthy adult volunteers following intranasal spray delivery of a live attenuated measles vaccine. Clinical and Vaccine Immunology 18(3): 355-361, 2011

Pharmacokinetic characterization of tizanidine nasal spray, a novel intranasal delivery method for the treatment of skeletal muscle spasm. Clinical Drug Investigation 33(12): 885-891, 2013