PLGA Nanoparticle-Embedded Oral Films for Sustained Eletriptan Delivery

Objectives

The study aimed to fabricate and characterize Oral Dispersible Film (ODF) containing PLGA polymeric nanoparticles of Eletriptan Hydrobromide (EH). The ODF system is designed to circumvent pre-systemic metabolism of drug and thereby augment the issue of low oral bioavailability of EH.

Materials and Methods

Polymeric nanoparticles were prepared by the nanoprecipitation method using PLGA (50:50) as the polymer and poloxamer 188 as the surfactant. A Box-Behnken Design was employed to achieve optimized nanoparticle size, higher drug entrapment efficiency and Polydispersity Index (PDI) of PNPs. The oral dispersible film was prepared by using the pullulan as the polymeric film former and propylene glycol as the plasticizing agent, employing the solvent casting technique. The optimized film formulation was characterized in terms of physicochemical attributes, in vitro release behaviour, pharmacokinetic performance, and histopathological safety.

Results

The optimized PNPs exhibited a mean particle size of 205±0.42, a high drug entrapment efficiency of 82±0.6%, and a narrow PDI of 0.195±0.11. The designed film formulation appeared opaque, uniform and well distributed. The in vitro data revealed that the PNPs-loaded ODF has the highest (91.14%) and extended release of drug (24 hr) occurred as compared to ODF containing free or un-encapsulated drug. Furthermore, histopathological study showed that the ODF is safe and effective formulation for transmucosal administration.

Conclusion

The PNP-based ODF disintegrated rapidly in mouth so that unabsorbed drug could results quick therapeutic action. Therefore, the incorporation of PLGA-based nanoparticles into ODF provides a promising strategy to achieve both rapid therapeutic onset and prolonged release of drug.