Formulation and evaluation of an anti-epileptic drug-loaded microemulsion for nose to brain delivery

P S Kawtikwar, N P Kulkarni, S Yadav, D M Sakarkar


The aim of the present study was to formulate an anti-epileptic drug-loaded microemulsion for nose-to-brain delivery.The oil system evaluated for the preparation of a stable microemulsion was iso-propyl myristate. A non-ionic surfactant likeTween 80 was used with polyethylene glycol 400 as a co-surfactant. A pseudoternary phase diagram for various proportions of Smix:oil was constructed by the water titration method. The effect of changing concentration of alcohol as a co-surfactant  was also studied.The t-phase diagram shows that the water consumption capacity of the system was increased as the surfactant
concentration was increased. It was also found that as the concentration of the alcohol was increased, the viscosity of the microemulsion decreased. After the identification of the microemulsion region, the composition of the microemulsion was fixed at oil 9-10%, Smix 35-40% and water 45-50%.The formulated microemulsion was evaluated for various parameters like pH, conductivity, zeta potential, viscosity and in vitro drug diffusion studies. All the evaluation parameters showed satisfactory
results. Using this microemulsion, the solubility of valproic acid was increased from 1.29 to 36 mg/ml. Diffusion studies
have shown a lag period of 45 min. Thirteen percent drug diffusion was achieved in 3 h. The prepared microemulsion was
stable at 40°C and 75% relative humidity.

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Begley DJ. The blood-brain barrier: Principles for targeting peptides

and drugs to the central nervous system. J Pharm Pharmacol


Schlossauer B, Steuer H. Comparative anatomy, physiology and in vitro

models of the blood-brain and blood-retina barrier. Curr Med Chem


Crone C. The blood-brain barrier in health and disease. Ellis Harwood;

p. 17-40.

Pardridge WM. Recent advances in blood-brain barrier transport. Annu

rev pharmacol toxico 1988;28:25-39.

Illum L. Nasal drug delivery: new development strategies. Drug Discov

Today 2002;7:1184-9.

Illum L. Transport of drugs from the nasal cavity to the central nervous

system. Eur J Pharm Sci 2000;11:1-18.

Patil P. Formulation of self-emulsifying for oral drug delievery of

Simvastatin. Acta Pharma 2007;57:111-22.

Models for the Transfer of Drugs from the Nasal Cavity to the Brain.

Bjorn Jansson, Dept. of Pharmacy, Uppsala University, Sweden: 2004.

Li L, Nandi I, Kim KH. Development of an Ethyl Laurate based

microemulsion for rapid-onset intranasal delievery of Diazepam. Int J

Pharm 2002;237:77-85.

Zhang Q, Jiang X, Jiang W, Lu W, Su L, Shi Z. Preparation of Nimodipine-

loaded microemulsion for intranasal delievery and evalvation on the

targeting effiency to the brain. Int J Pharm 2004;275:85-96.

Morikawa N. Pharmacokinetic of cytosine arabinoside, methotrexate,

nimustine and valproic acid in cerebrospinal fluid during perfusion

chemotherapy. Bio and Pharma Bulletin 1985;23:784-7.



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