NANOEMULSION AS A PLATFORM FOR PARENTERAL ADMINISTRATION OF CARBAMAZEPINE: IN VITRO AND IN VIVO STUDY
Sanaa A. Elgizawy*, Ebtessam A. Essa and Alaa A. Abu Elkhier
ABSTRACT
The aim of this work was to formulate carbamazepine (CBZ) nanoemulsion for parenteral administration. A 23 full factorial design was employed to study the influence of type of co-surfactant (either propylene glycol (PG) or polyethylene glycol 400 (PEG400)), type of surfactant (either Polysorbate 80 or Poloxamer 188) and surfactant/co-surfactant ratio (Smix), on the physicochemical characteristics of the prepared nanosystems. Nanoemulsions were prepared by spontaneous emulsification technique. In vitro and in vivo evaluation were investigated. Stability under different temperature (5.0 and 25°C) for 6 months was also tested. Droplet size ranged from 20.0±1 to123±4 nm. Encapsulation efficiency was up to 84%. According to the statistical analysis using polynomial equations and response optimization, the optimized formula was F6 with PEG400 as a co-surfactant, Polysorbate 80 as a surfactant and the highest Smix. In vitro release showed sustained release of CBZ over time that best fitted to Higuchi kinetic modeling. In vivo study revealed the superiority of the optimized formula (F6) over the marketed drug suspension with delaying of the onset and reduction of the frequency of clonic convulsion. Regarding stability, most of the prepared formulae showed nonsignificant change in particle size and entrapment efficiency indicating good physical stability.
Keywords: nanoemulsion, anticonvulsant, factorial design, epilepsy.
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