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Taste masking of propranolol hydrochloride by microbeads of EUDRAGIT® E PO obtained with prilling technique for
Antonio Lopalco1, Nunzio Denora1, Valentino Laquintana1
1Department of Pharmacy-Pharmaceutical Sciences, University of Bari "Aldo Moro", Bari, Italy.
Insights
This study developed new solid propranolol hydrochloride (PR) microbeads for children, overcoming taste and dosage issues. The novel formulations effectively mask bitterness and offer stable, swallowable options for pediatric use.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Pediatric Formulations
Background:
- Propranolol hydrochloride (PR) is crucial for pediatric diseases, including infantile hemangioma.
- Existing liquid PR formulations suffer from poor palatability (bitter, salty taste), impacting pediatric compliance.
- Adult-centric solid PR formulations lack pediatric-specific flexible dosing based on weight.
Purpose of the Study:
- To develop a novel solid pediatric formulation for propranolol hydrochloride (PR).
- To address challenges of taste masking and appropriate pediatric dosing.
- To create matrix microbeads using EUDRAGIT® E PO for improved palatability and flexible administration.
Main Methods:
- Manufacture of matrix microbeads containing PR using the prilling-congealing technique.
- Utilized two nozzle sizes (300 and 450 μm) to achieve homogenous microbead diameters (333-699 μm).
- Investigated drug:matrix ratios (1:25, 1:15, 1:10) in aqueous and tert-butyl alcohol/aqueous media.
- Characterization included encapsulation efficiency, drug loading, SEM analysis, dissolution studies, and electronic tongue measurements.
Main Results:
- Microbeads exhibited high encapsulation efficiency (22-100%) and drug loading (22-77 mg/g), suitable for variable pediatric doses.
- SEM revealed porous, spongy matrix structures, resulting in soft floating microbeads.
- Formulations demonstrated low drug release in artificial saliva and prompt dissolution in simulated gastric media.
- Electronic tongue confirmed significant taste masking of PR, particularly for the 1:25 drug:matrix ratio (F1n and F1).
Conclusions:
- The developed EUDRAGIT® E PO matrix microbeads (F1 and F1n) successfully addressed palatability and dosing challenges for pediatric propranolol hydrochloride.
- These stable, swallowable microbeads offer a promising new solid oral formulation for children.
- The findings support the potential for improved therapeutic compliance in pediatric patients.
Abstract:
The purpose of this study was to develop a new solid paediatric formulation for propranolol hydrochloride (PR). This drug is used to treat various paediatric diseases, and recently received clearance to treat haemangioma. However, PR has a bitter salty taste that does not facilitate high rates of compliance among children, especially in liquid formulations. In addition, the solid formulations are designed for adults and often their dosage is not suitable for children that require a flexible dose based on their weight. Therefore, matrix microbeads of EUDRAGIT® E PO containing PR were manufactured to overcome these limitations. Nine different samples were prepared using the prilling-congealing technique with high yield. Using 2 nozzles, 300 and 450 μm (code n), the diameters obtained of microbeads (from 333 to 699 μm) were homogenous and appropriate to be swallowed by children. In this study, the ratio drug:matrix for the microbeads was also examined in detail: 1:25 (F1), 1:15 (F2) and 1:10 (F3) in aqueous and tert-butyl alcohol/aqueous (code t) media. Most of the examined microbeads were characterized by high percentage of encapsulation efficiency (22-100%) and drug loading (22-77 mg of drug per g of matrix) effective for the administration of low and high doses of PR. SEM analysis revealed a matrix with a radial or a spongy structure, with numerous pores that generated soft floating microbeads in aqueous solution. Release studies confirmed a low release and dissolution of the drug in artificial saliva, mainly F1n > F1 > F2nt, and a prompt dissolution in simulated gastric media. Finally, electronic tongue measurements revealed the ability of these formulations to mask the bitter drug taste, especially for the sample with a ratio 1:25 (F1n and F1). These samples were chemically and physically stable for six months. In conclusion, the projected microbeads F1, and F1n reached the goal of the study, and could be proposed as new solid oral formulations dedicated to use by children.
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