Optimization of sustained-release propranolol dosage form using factorial design and response surface methodology

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Extended-release formulations aim to provide sustained drug levels, improving patient compliance and therapeutic efficacy.
• Hydroxypropylmethylcellulose (HPMC) is a widely used polymer for creating controlled-release matrices due to its gelling and swelling properties.
• Challenges in HPMC-based formulations include incomplete drug release, necessitating optimization of excipient ratios.

Purpose of the Study:

• To develop and optimize extended-release propranolol formulations using hydroxypropylmethylcellulose (HPMC).
• To investigate the impact of HPMC and avicel on propranolol release kinetics.
• To establish an optimal formulation predicting desired drug release profiles.

Main Methods:

• Formulation development utilizing hydroxypropylmethylcellulose (HPMC) and avicel.
• Application of response surface methodology (RSM) with a quadratic polynomial equation for optimization.
• Factorial design to study the effects of HPMC/drug ratio (X1) and avicel level (X2).
• Dissolution testing at various time points (1.5, 4, 8, 14, 24 hours) to assess drug release.

Main Results:

• High HPMC concentrations led to incomplete drug release.
• Avicel addition improved drug release percentages at later stages.
• Optimized formulation demonstrated a dissolution pattern matching the predicted curve.
• Drug release followed quasi-Fickian diffusion mechanism from HPMC matrices.

Conclusions:

• Response surface methodology is effective for optimizing extended-release propranolol formulations.
• The optimized formulation achieved desired drug release specifications.
• Quasi-Fickian diffusion governs drug release from these HPMC-based matrices, providing insights for future drug delivery system design.