Formulation and Characterization of Fast-Dissolving Sublingual Film of Iloperidone Using Box–Behnken Design for Enhancement of Oral Bioavailability

Abstract

Iloperidone is a second-generation antipsychotic drug which is used for the treatment of schizophrenia and has very low aqueous solubility and bioavailability. This drug also undergoes first-pass metabolism. The aim of this work is to formulate fast-dissolving sublingual films of iloperidone to improve its bioavailability. Sublingual films were prepared by solvent casting method. Hydroxypropyl methyl cellulose E5, propylene glycol 400, and transcutol HP were optimized using Box-Behnken three-level statistical design on the basis of disintegration time and folding endurance of films. Iloperidone:hydroxypropyl-β-cyclodextrin kneaded complex was used in films instead of plain drug due to its low solubility. Optimized film was further evaluated for drug content, pH, dissolution studies, ex vivo permeation studies, and pharmacokinetic studies in rats. The optimized film disintegrated within 30 s. The in vitro dissolution of the film showed 80.3 ± 3.4% drug dissolved within first 5 min. In ex vivo permeation studies using sublingual tissue, flux achieved within first 15 min by film was around 117.1 ± 0.35 (mcg/cm/h) which was ten times more than that of plain drug. This formulation showed excellent uniformity. AUC and C of film were significantly higher (p < 0.001) as compared to plain drug and relative bioavailability of the films was 148% when compared to the plain drug. Thus, this study showed optimized fast-dissolving sublingual film to improve permeation and bioavailability of iloperidone. Fast-dissolving films will be customer-friendly approach for geadiatric schizophrenic patients.

Technological evolution of cyclodextrins in the pharmaceutical field

“…Compelling research shows the promising potential of CDs for developing sublingual dosage forms [ [77] , [78] , [79] ]. Therefore, an important role of innovations in this matter is expected.…”

Process optimization of Syringa oblata Lindl. by response surface methodology and its effect on Staphylococcus xylosus biofilm

“…16 Currently, response surface methodology (RSM) is one of the most conventional and potent approaches to multivariate optimization analytical methodologies. 17,18 This statistical tool tests the applicability and reliability of optimization to improve the process, 19,20 reduce the number of experiments required to result in a less laborious task, 21 and it indicates the possible inuences of some variables on others. 18 RSM is faster and more informative than the classical one-variable-at-a-time approach or the use of full factorial designs.…”

Intervene effect on Streptococcus suis biofilm formation of emodin extracted from Rheum officinale Baill

“…Besides, the ultrasonic power was kept at 500 W in all experiments. The result from Fig [45,46]. The matrix designed by BBD and corresponding results of RSM experiments were given in Table 2.…”