Preparation of Carbamazepine Chitosan Nanoparticles for Improving Nasal Absorption

Abstract

In this study the nasal administration of carbamazepine has been studied using chitosan nanopartcles. The chitosan nanoparticles were prepared by ionic gelation of chitosan (100-300mg) with Tripolyphosphate sod (100-300mg in 100ml. Nine formulations were prepared, characterized and compared in terms of morphology (Transmission electron microscopy), drug content, particle size (zetasizer) and In-vitro drug release. In-vitro drug release studies were performed in Franz diffusion cell using phosphate buffer (buffer pH 5.5) as dissolution medium. The Chitosan nanoparticles had a mean size of 124.2±05 to 580±13nm, zeta potential were found to be +21 to 26.6 mV and the entrapment efficiency were found to be 65 to 72.7%. The in-vivo study was performed on Wistar rat, nanoparticles were administered through nasal route and compared with carbamazepine given by i.v. route, the results indicate that carbamazepine loaded chitosan nanoparticles enhances the drug absorption through nose. The results showed that the carbamazepine could be directly transported into the rat brain through nose and the possible side effects could be minimized.

Preparation and Evaluation of Carbamazepine Solid Lipid Nanoparticle for Alleviating Seizure Activity in Pentylenetetrazole-Kindled Mice

“…Epilepsy is a disorder in the central nervous system (CNS) that is characterized by an increase in the number of electrical impulses that occurs in one focal locus of the brain and/or the entire brain, resulting in partial or generalized seizures [1].…”

“…Carbamazepine (CBZ) is an antiepileptic drug with a narrow therapeutic index, and it is poorly absorbed when taken by the oral route [8]. Its oral bioavailability is 75%, and its maximum achieved plasma concentration is about 4–8 h after administration [1]. Carbamazepine acts through the inactivation of sodium channels, making brain cells less excitable.…”

Polymer -Lipid Hybrid Nanoparticles for Brain Targeting Through Intranasal Delivery

“…Carbamazepine is a well-known drug for treating epileptic seizures; it is a first-line drug for the treatment of partial seizures 1,2 , with or without second generalization, and generalized tonic-clonic seizures. The t 1/2 of carbamazepine is 25-85 hr after a single dose, if dose is repeated for long time, auto-induction takes place in liver, which results in the fluctuations in the plasma conc.…”

“…The t 1/2 of carbamazepine is 25-85 hr after a single dose, if dose is repeated for long time, auto-induction takes place in liver, which results in the fluctuations in the plasma conc. this precipitates various unwanted effects like neuromuscular disorder, cardiovascular, gastrointestinal effects and some serious pathological conditions like skin allergies, dysfunction of kidney and liver 3,4 to overcome these side effects drug should be targeted directly into brain, which is a very tough job because of the anatomy and functionality of a specialized barrier, the blood brain barrier (BBB), the capillary endothelial cells which separate the blood with underlying brain cell, it does not permit the drug or other foreign material to travel into brain from systemic circulation 1,5 . The bioavailability of the particles is found to be the reason for the Nanomedicine to gain precedence.…”

“…11,12,13 These problems can be reduced by using small carriers like nanoparticles made up of mucoadhesive polymers. These nanoparticles may be used to deliver the drug directly into brain via intranasal administration, because of their nanosize and mucoadhesive characteristics 1 . The hybrid nanoparticles have the property to adhere with other substrate; it can be easily conjugated with antibody 19 .…”