International Journal of Pharmacy and Biological Sciences ISSN: 2321-3272 (Print), ISSN: 2230-7605 (Online) IJPBS | Volume 8 | Issue 2 | APR-JUN | 2018 | 240-252 Research Article | Pharmaceutical Sciences | Open Access | MCI Approved| |UGC Approved Journal | International Journal of Pharmacy and Biological Sciences Srividya Ramreddy & Krishnaveni Janapareddi* www.ijpbs.com or www.ijpbsonline.com 240 DEVELOPMENT OF CARBAMAZEPINE MUCOADHESIVE MICROEMULSIONS FOR BRAIN TARGETING: PHARMACODYNAMIC EVALUATION Srividya Ramreddy And Krishnaveni Janapareddi* Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana, 506009, India. *Corresponding Author Email: krishnavenij153@gmail.com ABSTRACT Objectives: Carbamazepine (CBZ), an anticonvulsant drug has low oral bioavailability and gastrointestinal side effects, in order to overcome these problems, the present study was to development and pharmacodynamic evaluations of carbamazepine mucoadhesive microemulsions (MME) for brain targeting via nasal route. Methods: Based on solubility, oleic acid, Labrasol and Transcutol P were selected as oil, surfactant and co-surfactant. Pseudo ternary phase diagrams were constructed to identify microemulsion region. A three factor three level Box Behnken design was used to optimize formulation. The micro emulsions (ME) were also evaluated for size, PDI, zeta potential, flux, pH, viscosity, content, surface morphology. Chitosan was added to the optimized ME at 0.5% concentration as permeation enhancer. Ex-vivo permeation studies were performed on excised porcine nasal mucosa using Franz diffusion cells. Histopathological changes in mucosa were studied. Pharmacodynamic activity of ME, MME, drug solution (D.S) and i.v CBZ solution were evaluated by Maximal Electroshock seizures (MES) method in male Wistar rats. Results: Optimized MME, composed of oleic acid (5%), Surfactant mixture (53.78%) water (45%) and chitosan (0.5%) showed mean globule size 97.43nm, PDI 0.213 and zeta potential +16.32. MME showed significantly (p<0.001) high flux of 651.53 μg/cm 2 /h compared to D.S (101.8 μg/cm 2 /h) and ME18 (551.23μg/cm 2 /h). The reduction seizure recovery time of MME was significantly (p<0.001) high compared to MEs and D.S by i.v route. Conclusion: The efficacy of ME and MME formulations via nasal route for brain targeting in comparison to i.v route was improved. KEY WORDS Box Behnken design, Carbamazepine, Chitosan, Epilepsy, Intranasal microemulsion, Maximal electroshock seizures. INTRODUCTION Carbamazepine (CBZ), an anticonvulsant drug is the drug of choice in the treatment of partial and secondarily generalized seizures. CBZ is also effective in trigeminal neuralgia and diabetic neuropathy [1,2]. It is a poorly water-soluble drug (0.17mg/ml) with low bio availability of less than 50%. Absorption of tablets by oral route is slow and irregular [3]. Oral administration of CBZ therapy is associated with adverse effects such as drowsiness, dizziness, headaches and migraines, motor coordination impairment, nausea, vomiting. In order to overcome gastro intestinal side effects, liver toxicity other side effects and also to increase bioavailability of carbamazepine using less dose of CBZ, present work of CBZ microemulsions for brain targeting via nasal route was taken up. Nasal route has several advantages like rapid onset of therapeutic action, lower doses, avoidance of liver and