Intranasal administration of carbamazepine-loaded carboxymethyl chitosan nanoparticles for drug delivery to the brain

• Main Authors: Shanshan Liu (Author), Shili Yang (Author), Paul C. Ho (Author)
• Format: Book
• Published: Elsevier, 2018-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 1818-0876; 10.1016/j.ajps.2017.09.001
• Keywords: Carbamazepine; Blood-brain barrier; Nanoparticles; Nasal drug delivery; Pharmacokinetics; Chitosan; Therapeutics. Pharmacology; RM1-950
• Source: Asian Journal of Pharmaceutical Sciences, Vol 13, Iss 1, Pp 72-81 (2018)

Epilepsy is considered as a common and diverse set of chronic neurological disorders and its symptoms can be controlled by antiepileptic drugs (AEDs). The presence of p-glycoprotein and multi-drug resistance transporters in the blood-brain barrier could prevent the entry of AEDs into the brain, causing drug resistant epilepsy. To overcome this problem, we propose using carboxymethyl chitosan nanoparticles as a carrier to deliver carbamazepine (CBZ) intra-nasally with the purpose to bypass the blood-brain barrier thus to enhance the brain drug concentration and the treatment efficacy. Results so far indicate that the developed CBZ-NPs have small particle size (218.76 ± 2.41 nm) with high drug loading (around 35%) and high entrapment efficiency (around 80%). The in vitro release profiles of CBZ from the NPs are in accordance with the Korsmeyer-peppas model. The in vivo results show that both encapsulation of CBZ in nanoparticles and the nasal route determined the enhancement of the drug bioavailability and brain targeting characteristics.