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Published on: August 15, 2016
Development of a Hydroxypropyl-β-Cyclodextrin-Based Liquid Formulation for the Oral Administration of Propranolol in
Marzia Cirri1, Paola Mura1, Simona Benedetti2
1Department of Chemistry Ugo Schiff (DICUS), University of Florence, 50019 Sesto Fiorentino, Italy.
Insights
This study developed a stable and palatable oral propranolol (PPN) solution for children using cyclodextrin complexation. Hydroxypropyl beta-cyclodextrin (HPβCD) enhanced PPN stability against light and improved taste, addressing key formulation challenges.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Pediatric Formulations
Background:
- Propranolol (PPN) is crucial for pediatric cardiovascular conditions, but existing preparations face stability and palatability issues.
- Extemporaneous PPN preparations lack stability and quality control, necessitating improved formulations.
- Current challenges include PPN's photosensitivity, pH instability, bitter taste, and the need to avoid toxic excipients.
Purpose of the Study:
- To develop a safe, stable, and palatable oral pediatric propranolol solution.
- To utilize cyclodextrin complexation to overcome PPN formulation hurdles.
- To enhance PPN stability, taste, and overall suitability for pediatric use.
Main Methods:
- Screening of various cyclodextrins (CDs) to identify optimal complexing agents.
- Selection of hydroxypropyl beta-cyclodextrin (HPβCD) based on complexation efficiency and safety.
- Preparation of PPN-HPβCD physical mixtures and co-ground systems (1:1 or 1:2 mol:mol) for 0.2% w/v solutions.
- Evaluation of photostability, storage stability (6 months and accelerated conditions), and palatability using electronic tongue tests.
Main Results:
- HPβCD demonstrated significant photoprotective effects, reducing PPN degradation by up to 75% under UV exposure.
- PPN-HPβCD solutions maintained physical-chemical properties and drug concentration over 6 months at room temperature and under accelerated conditions (40 °C).
- Electronic tongue tests confirmed HPβCD's taste-masking capability, reducing perceived bitterness by 30%.
Conclusions:
- Cyclodextrin complexation, specifically with HPβCD, offers a viable strategy for creating stable and palatable pediatric propranolol oral solutions.
- The developed formulation addresses critical stability (light, pH) and palatability issues, potentially replacing unstable extemporaneous preparations.
- This approach enhances the safety and efficacy of propranolol administration in pediatric patients.
Abstract:
Propranolol (PPN) is widely used in children to treat various cardiovascular diseases. The availability of a suitable PPN solution should avoid recourse to extemporaneous preparations of unknown/limited stability, as commonly made in hospital pharmacies. However, the development of pediatric PPN solutions is hindered by their instability to light and stability at pH ≈ 3, bitter taste, and the need to improve palatability and avoid co-solvents, flavoring agents, or preservatives that are potentially toxic. In this study, cyclodextrin (CD) complexation has been exploited to develop a safe, stable, and palatable oral pediatric solution of PPN. An initial screening among various CDs allowed us to select HPβCD for its good complexing ability and no toxicity. Drug-HPβCD physical mixtures or co-ground systems (1:1 or 1:2 mol:mol) were used to prepare 0.2% w/v drug solutions. Photo stability studies evidenced the protective effect of HPβCD, revealing a reduction of up to 75% in the drug degradation rate after 1 h of exposure to UV radiation. Storage stability studies showed unchanged physical-chemical properties and almost constant drug concentration after 6 months and under accelerated conditions (40 °C), despite the less aggressive pH (≈5.5) of the solution. The electronic tongue test proved that the HPβCD taste-masking properties improved the formulation palatability, with a 30% reduction in drug bitterness.
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