Formulation of microencapsulated paracetamol beads in dried jelly form for paediatric

Abstract

Taste masking is required for bitter drugs to enhance patient compliance, especially among the paediatric population. Paracetamol is a drug that exhibits bitter taste because of its chemical structure. This study aims to improve the palatability of paracetamol through using microencapsulation technique to mask the bitter taste of paracetamol and jelly dosage form to make it easy for swallowing. Paracetamol was encapsulated in alginate beads using electrospray technique to create spherically shaped beads with a diameter size of less than 1.5 mm. The alginate beads were coated with 0.3% w/v low molecular weight chitosan to provide an extra barrier for taste masking properties. The optimised paracetamol beads were 1.39 ± 0.08 mm in size and spherical with an encapsulation efficiency of 99 ± 1.087%. In vitro studies show that the beads effectively masked the bitter taste of paracetamol. For the jelly dosage form, five different gelling agents including gelatin, three types of carrageenan namely kappa (κ)-, iota (ɩ)-, lambda (λ), and low acyl gellan gum were selected for the study. The jelly dosage form acts as a vehicle and eases the swallowing process. Iota-carrageenan had the best results in terms of texture, rheology and absence of syneresis. Based on this result, ɩ-carrageenan was modified to a dry form for reconstitution before use. The instant jelly form is more practical in terms of shipping, storage, stability and low amount of excipient used. The dry chitosan coated paracetamol alginate beads, and instant jelly was mixed to form a single dose (in sachet). Compatibility study was performed on the dosage form using differential scanning calorimetry (DSC) supported by attenuated total reflection-fourier transform infrared spectral studies (ATR-FTIR). The DSC and FTIR results showed compatibility between paracetamol and the instant jelly excipient. The optimised paracetamol jelly was easily reconstituted in 20 mL of water within 2 minutes. The beads were distributed in the jelly with no sedimentation. The time needed to release 80% of paracetamol ranged between 54-62 minutes, depending on the pH of the medium, and ingestion time was within 30 minutes after reconstitution to effectively mask the bitter taste. For the stability study, the dosages were packaged in semipermeable and impermeable sachets and stored both in real-time and accelerated stability chamber. The stability of paracetamol in the impermeable sachets, including appearance and drug content, met compendia specifications. Meanwhile, the semipermeable sachets stored in accelerated stability chamber underwent significant changes in formulation properties. The dry chitosan coated paracetamol alginate beads in jelly dosage had similar palatability and texture to commercial Panadol children's suspension and overcome the bitter aftertaste of paracetamol. Additionally, the jelly dosage form recorded low taste feeling score compared to commercial paracetamol suspension. In conclusion, the combined microencapsulation technique and jelly vehicle dosage form can replace the use of sweetening and flavouring agents in paracetamol dosage forms for the paediatric population and is comparable to commercial children’s paracetamol suspension.