<p>Modulation of Drug Release from Natural Polymer Matrices by Response Surface Methodology: in vitro and in vivo Evaluation</p>

Abstract

The present work aimed at challenging the efficacy of natural gums, karaya and locust bean gum, as matrix-forming polymers for the formulation of sustained-release tablets of diltiazem, a model drug. Methods: Central design composite was adopted for the formulation and optimization of tablet formulations. The two gums have been selected as independent variables. The dependent factors chosen were the amount of drug released in 1st hour (Y1), amount of drug released after 12 h (Y2), diffusion exponent (Y3), and time for half of the total drug released (T 50%) (Y4). Wet granulation approach was used for the formulation of tablets. FT-IR, DSC, in vitro dissolution, swelling-erosion investigations, SEM, and stability studies were carried out. Results and Discussion: It was evident that the release pattern from the prepared formulations was significantly influenced by the quantity of gum(s) in the tablet. FT-IR and DSC results confirm drug-polymer compatibility. Polynomial equations were used for the prediction of quantitative impact of independent factors at different levels on response variables. After ANOVA analysis, the significant factors were considered for constrained optimization to get the optimized formula. The optimized formula generated by the response surface methodology was evaluated both for in vitro and in vivo properties. The optimized formula and a sustained-release marketed product were subjected to in vivo studies in rabbits and the results of the t-test demonstrated insignificant variation in pharmacokinetic parameters among the two formulations, confirming that the prepared tablet showed sustained-release profile. Conclusion: The results indicated that karaya and locust bean gum can be effectively used to formulate sustained-release tablets.

Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

“…From the in vitro drug release data, it was clear that the drug release was decreased with an increase in polymer concentration. The drug release was found to occur through a swelling process 35 . Aceclofenac has a very short half-life (t½ 2-4 hours), so in conventional tablets, aceclofenac dosing frequency is more.…”

Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film

“…The stability evaluation of the optimized tadalafil-loaded niosomal film was assessed at two distinct storage conditions. Patches of the film were stored in aluminum packages at 25 °C with 50–60% humidity (ordinary conditions) and 40 °C with 75% humidity (accelerated conditions) for twelve weeks, then the content of tadalafil was determined, in addition to other parameters, as weight and thickness [ 44 ].…”

Plants as pharmaceutical excipients in oral sustained drug delivery systems: A review

“…delivery systems. Karaya and locust bean gums were studied for their retarding effect as sustained release matrix tablets [21]. The efficacy of drug release was evaluated at the first and twelfth hours; the diffusion exponent and the time taken to release 50 % of the active component.…”