Abstract
Abstract
Pediatric therapy is frequently challenged by dysphagia, bitter medication taste, and liquid dosing errors. Risperidone, an atypical antipsychotic with low solubility (BCS class II) indicated for schizophrenia, bipolar mania, and autism-associated irritability, suffers from poor pediatric compliance due to its bitter taste. To overcome medication refusal and improve pediatric adherence, more focus on advanced taste-masking strategies is needed. Preventing intraoral drug release at salivary pH 6.8 using pH-dependent Eudragit E is a promising approach to mask bitterness. Nanoparticles were prepared via nanoprecipitation/solvent-evaporation method by dropwise addition of an organic phase (2 mg risperidone and 10 mg Eudragit E dissolved in 1 mL methanol) into 10 mL of aqueous phase (0.001 M phosphate buffer, pH 7.4, containing 0.3% w/v PVA as stabilizer) under magnetic stirring at 500 rpm and 37 °C for 30 minutes. Formulation screening identified 0.3% w/v PVA with a 1:5 risperidone-to-Eudragit E ratio as the optimal formula, yielding the highest entrapment efficiency of 74.9% ± 3.3% with an average hydrodynamic diameter of 344.17 ± 22.42 nm and a narrow polydispersity index (PDI) of 0.24 ± 0.07. FESEM images confirmed discrete spherical nanoparticles with diameters between 39 nm and 52 nm. Conversion of risperidone into an amorphous state within the Eudragit E matrix was demonstrated by DSC and XRD analyses, as evidenced by the disappearance of the sharp crystalline melting peak at 172.3 °C and the loss of distinct risperidone diffraction peaks. FTIR spectra confirmed physical compatibility without unwanted chemical interactions among optimal formula components. Furthermore, in vitro dissolution in phosphate buffer pH 6.8 demonstrated a significant reduction in drug release from 24.08% ± 0.13% for unformulated risperidone to only 1.73% ± 0.15% for the optimized nanoparticles. These results confirm that the optimized risperidone-loaded Eudragit E formula reduced drug release at pH 6.8, highlighting the formula’s potential for use in the development of advanced taste-masked oral dosage forms.
| Has the manuscript been published | not published |
|---|---|
| Intend to be published in the IJPS ? | Yes |
