THE USE OF NANOTECHNOLOGY FOR BRAIN TARGETING

Abstract

To achieve successful delivery to the brain, drugs should possess high lipid solubility and adequately-sufficient membrane permeability. Epilepsy is considered one of the most serious diseases worldwide that affects the brain. Zonisamide is an anti-epileptic drug (AED) that is known for its highly hydrophilic properties that hinder its passage across the blood brain barrier (BBB) efficiently. Therefore, the aim of this study is to improve the efficiency of the centrally acting Zonisamide, and the objective is to use the nanoparticles (NPs) technology for increasing the efficiency of the centrally acting Zonisamide. Nanodiamonds (NDs) carriers are known for their solubility enhancement for passing BBB. Drug loaded NDs were prepared and characterized for different in vitro aspects (particle size and zeta potential). 20 mg Zonisamide were diluted in 10 ml distilled water, NDs were added in a concentration of either 4 mg/10 ml or 6 mg/ml and sonicated in the presence of several excipients, which were added for the purpose of de-aggregation namely Albumin, Gelatin and Chitosan. Preparations were characterized for their particle size, zeta potential, in vitro drug release, as well as an in vivo biodistribution study using Tc-99 as a radio-marker. Zonisamide has been loaded on NDs successfully, the particle size of the formulation was within the nano range to be introduced through the nasal cavity, and the in vitro drug release of Zonisamide from the dialysis bag was sustained. The biodistribution study showed marked increased distribution of the formulation in the brain compared to the rest of the tissues. Thus, it can be concluded that Zonisamide loaded NDs is a successful formulation in delivery and targeting of Zonisamide to the brain.