Fabrication and Evaluation of Oral Controlled Release of Mucoadhesive Alginate Microbeads Containing Fluvastatin Sodium

Abstract

Objective: The aim of this study is to prepare oral controlled release (CR) of mucoadhesive alginate microbeads encapsulating fluvastatin by gastroretention technology.
 Methods: The mucoadhesive microbeads containing fluvastatin were produced using emulsification internal gelation technique. The effect of different variables such as sodium alginate concentration and its combination with other hydrophilic polymers, and the effect of various curing agents on particle size, entrapment efficiency, and in vitro studies were evaluated.
 Results: There was no marked change in drug entrapment efficiency, and dissolution studies occur during the stability studies of fluvastatin. The in vitro results give data that improvement in the CR of the drug from microbeads compared with marketed tablet. Hence, in this regard, to minimize the frequency of drug administration to reduce side effects. The optimum condition for the preparation of stable alginate beads and produce CR manner was occurred at a higher concentration of combined polymer mixture in equal ratios, i.e., 3% w/v. Infrared spectroscopic study (Fourier transform infrared) confirmed the no incompatibility between drug and other excipients. X-ray diffraction study and differential scanning calorimetry were provided evidence that successful entrapment of drug into the alginates microbeads and drug converted into amorphous nature. The efficiency of mucoadhesion strength of microbeads was determined by wash-off study.
 Conclusion: The kinetic modeling of the release data indicates drug release from the microbeads follow anomalous transport mechanism and super Case-II transport mechanism. Drug release is a function of pH dependent and controlled drug release depends on type and concentration of polymer blend and curing agents. The release kinetics of drug from the alginate beads followed zero order.

Development and Characterization of Gastro Retentive Mucoadhesive Microbeads Containing Simvastatin With Different Cross Linking Agents

“…The wash off was faster at simulated intestinal pH (phosphate buffer 6.8) than comparison to that at simulated gastric pH (1.2) [16]. The rapid wash-off observed intestinal pH than at gastric pH, the reason may be contributed is due to the ionization of carboxyl acid groups [17] and other functional groups present along the polymers chain at alkaline atmosphere, which increases the solubility and reduce the mucoadhesive strength.…”