Abstract
Abstract: Introduction: Flunarizine is a piperazine derivative, it is a selective T-type Ca++ channel blocker and it is successfully used for migraine prophylaxis. Its activity in migraine by reducing intracellular Ca++ overload due to brain hypoxia and thus prevents the deleterious effects of cellular calcium overload. Flunarizine has variable and low oral bioavailability ranging from 18%-27% due to hepatic first- pass metabolism and low water solubility. This study investigates the process of the formulation and in-vitro characterization of loading of flunarizine into novasome nanovesicles for transdermal drug delivery. Which may increase its permeability and bioavailability and also can prevent the varying inter-individual plasma levels of this drug.
Methods: Flunarizine loaded novasomes were formulated by using thin film hydration method. The composition of the formulation included span 60 as nonionic surfactant and stearic acid as permeation enhancer and cholesterol as stabilizer. Particle size (PS), polydispersity index (PDI), and entrapment efficiency (EE%) were all considered in the evaluation process.
Results: The choice of the optimized formula was based on many significant factors were included, ratio and type of non-ionic surfactant, ratio of cholesterol, ratio and type of fatty acid and sonication time and power. The optimized formula based on desirability particle size 194.1 nm and exhibited EE% of 83.65%, PDI of 0.2006.
Conclusion: The appropriate flunarizine transdermal delivery with sustain and constant blood levels could provide an effective systemic delivery of this drug with improved permeability and bioavailability. Administration of flunarizine as transdermal drug delivery system could be a novel alternative to oral administration. As an additional advantage, the risk of systemic side effects caused by this dug can be minimized.
| Has the manuscript been published | not published |
|---|---|
| Intend to be published in the IJPS ? | NO |
