paliperidone-loaded mucoadhesive microemulsion in treatment of schizophrenia: formulation consideration

this paper describes formulation considerations and in vitro evaluation of a microemulsion drug delivery system designed for intranasal administration of paliperidone.

methods

drug-loaded microemulsions were successfully prepared by a water titration. prepared formulations were subjected to physicochemical characterization, and evaluated for in vitro diffusion, nasal cilio toxicity, and in vitro mucoadhesion.

results

the microemulsion, containing 4 % oleic acid, 30 % surfactant mixture of [labrasol/cremophor rh 40 (1:1)]/[transcutol p] (3:1) and 66 % (wt/wt) aqueous phase, that displayed a 99.93 % optical transparency, globule sizes of 20.01 ± 1.28 nm, and a polydispersity index of 0.117 ± 0.034 was selected for the incorporation of polyelectrolytic polymer (polycarbophil) as the mucoadhesive component. the mucoadhesive microemulsion formulation of paliperidone that contains 0.5 % by weight of polycarbophil displayed higher in vitro mucoadhesive potential (18.0 ± 2.5 min) and diffusion coefficient (3.83 × 10−6 ± 0.019 × 10−6) than microemulsion. also, they were found to be free from nasal ciliotoxicity and had stability for 6 months.

conclusion

the in vitro studies demonstrated the potential of developing mucoadhesive microemulsion formulation for intranasal delivery of paliperidone.