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American Journal of Drug Discovery and Development

Year: 2011 | Volume: 1 | Issue: 3 | Page No.: 174-187
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Authors

Manju Rawat Singh

Deependra Singh

Swarnlata Saraf

Keywords

Research Article

Formulation Optimization of Controlled Delivery System for Antihypertensive Peptide using Response Surface Methodology

Manju Rawat Singh, Deependra Singh and Swarnlata Saraf
The aim of present study was to apply experimental design methodology in the development and optimization of carrier system for highly water-soluble polypeptide in salt form. Enalapril Maleate (EM), developed for hypertension and congestive heart failure, was used as a model peptide. A three-level three-factorial Box-Behnken experimental design was used to characterize and optimize three physicochemical parameters, i.e., drug concentration (10, 20 and 30 mg), External Aqueous Phase volume (EAP) (50, 100 and 150 mL) and stabilizer (Tween 80) concentration (0.1, 0.15 and 0.2% v/v) on the entrapment and size of Eudragit S100 microspheres prepared by modified double emulsion solvent evaporation technique. The Response Surface Methodology (RSM) and multiple response optimization utilizing the polynomial equation were used to select optimal formulation with maximum entrapment and particle size in range. The maximum entrapment (80.62±1.56%) was achieved with 10 mg drug, 50 mL EAP and 0.15% v/v Tween 80 and the observed responses coincided well with the predicted values from the RSM optimization technique. The drug release from formulations showed a controlled-release pattern following Higuchi Kinetics. HPLC chromatograms of drug released from microspheres showed the intact nature of peptide. In conclusion, a novel, oral controlled-release delivery system for highly water soluble peptide was successfully developed by experimental design methodology. It is an economical way of obtaining the maximum amount of information in a short period of time and with the fewest number of experiments.
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