Tailoring and Optimization of Nifedipine Controlled Release Organogel via Quality by Design Approach

Purpose

The primary aim of this study was to optimize, characterize, and test a controlled-release organogel of nifedipine for oral delivery. The formulation employed 12-hydroxy stearic acid as a gelator with soybean oil as a base. This research sought to investigate the potential of this organogel system to provide a controlled release alternative for nifedipine administration.

Methods

Preformulation studies and drug-excipient compatibility tests were conducted for nifedipine and the selected excipients. A controlled release organogel was created using the heating method. A quadratic model was applied to design formulations (F1-F14) with varying concentrations of 12-hydroxy stearic acid and distinct cooling rates (gradual and quick cooling) at five levels, utilizing a one-factor response surface approach. The prepared formulations were evaluated using various assessment parameters. Design Expert 7.0 was employed to statistically derive the optimized batch. Differential scanning calorimetry and Fourier-transform infrared spectroscopy were used to compare the preformulation test results between nifedipine and the excipients.

Results

The optimized controlled-release organogel exhibited a drug release profile of 86.02% at 10 h, which increased to 96.04% after 12 h. The data for the optimized formulation revealed a significant correlation between expected and actual responses, indicating the efficacy of the quadratic model and the response surface approach in predicting formulation behavior.

Conclusions

The study concluded that an organogel formulation using 12-hydroxy stearic acid as an organogelator and soybean oil as a base could be beneficial for controlled-release formulations of nifedipine. The results suggest that this organogel system is a viable alternative for the controlled release of nifedipine, offering a promising method for its oral administration.