Microemulsion-based drug delivery system for transnasal delivery of Carbamazepine: preliminary brain-targeting study.
This study reports the development and evaluation of Carbamazepine (CMP)-loaded microemulsions (CMPME) for intranasal delivery in the treatment of epilepsy. The CMPME was prepared by the spontaneous emulsification method and characterized for physicochemical parameters. All formulations were radiolabeled with (99m)Tc (technetium) and biodistribution of CMP in the brain was investigated using Swiss albino rats. Brain scintigraphy imaging in rats was also performed to determine the uptake of the CMP into the brain. CMPME were found crystal clear and stable with average globule size of 34.11 ± 1.41 nm. (99m)Tc-labeled CMP solution (CMPS)/CMPME/CMP mucoadhesive microemulsion (CMPMME) were found to be stable and suitable for in vivo studies. Brain/blood ratio at all sampling points up to 8 h following intranasal administration of CMPMME compared to intravenous CMPME was found to be 2- to 3-fold higher signifying larger extent of distribution of the CMP in brain. Drug targeting efficiency and direct drug transport were found to be highest for CMPMME post-intranasal administration compared to intravenous CMP. Rat brain scintigraphy also demonstrated higher intranasal uptake of the CMP into the brain. This investigation demonstrates a prompt and larger extent of transport of CMP into the brain through intranasal CMPMME, which may prove beneficial for treatment of epilepsy.
a A. R. College of Pharmacy & G. H. Patel Institute of Pharmacy , Vallabh Vidynagar , Gujarat , India .
Rashmin Bharatbhai
RB
Patel
b Indukaka Ipcowala College of Pharmacy , New Vallabh Vidyanagar , Gujarat , India .
Mrunali Rashmin
MR
Patel
b Indukaka Ipcowala College of Pharmacy , New Vallabh Vidyanagar , Gujarat , India .
Kashyap K
KK
Bhatt
c Department of Pharmacology & Clinical Pharmacology , Charotar University of Science and Technology , Changa , Gujarat , India , and.
Bharat G
BG
Patel
d Veterinary Nuclear Medicine Center , Bombay Veterinary College , Mumbai , India.
Rajiv V
RV
Gaikwad
D000281:Administration, Intranasal; D061605:Administration, Intravenous; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002220:Carbamazepine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004355:Drug Stability; D004655:Emulsions; D008297:Male; D010316:Particle Size; D011877:Radionuclide Imaging; D051381:Rats; D017208:Rats, Wistar; D013667:Technetium; D014014:Tissue Adhesives; D014018:Tissue Distribution
D000927:Anticonvulsants; D004655:Emulsions; D014014:Tissue Adhesives; D002220:Carbamazepine; D013667:Technetium
Brain scintigraphy; Carbamazepine; brain targeting; microemulsion; nose-to-brain delivery