Cross linked alginate beads of montelukast sodium coated with eudragit for chronotherapy: statistical optimization, in vitro and in vivo evaluation

The objective of the current investigation is to prepare delayed-release beads (DRBs) containing montelukast sodium (MKS) for chronotherapy of asthma.METHODS: Delayed-release beads of alginate were prepared using a simple method, i.e., ionotropic gelation. The effect of cross-linking agents (zinc or calcium ions) and the concentration of chitosan on the properties of the beads were investigated. The prepared beads were coated by a polymer having pH-independent solubility, i.e., Eudragit RSPO and Eudragit RLPO in different ratios to achieve the desired lag time of 4-5 h. Beads were evaluated for surface morphology, practical yield, encapsulation efficiency, XRD, and in vitro release study. The pharmacokinetic study was carried out in New Zealand white male rabbits.RESULTS: There are no major differences in the drug release profile observed between Ca++ & Zn++ cross-linked beads. Although, a slight slow release was seen in the case of chitosan reinforced beads. MKS releases from cross-linked alginate beads were slightly altered with sodium alginate concentration, cross-linking time, and talc. At a higher concentration of alginate, slow drug release was observed whereas the addition of talc to alginate increased the release rate. The in vitro release study shows that the optimal formulation of DRBs has a lag time (4.5 h) and the release at 6 h is 74.9%. In vivo pharmacokinetic study of the beads has shown Tmax at 7 h with an initial lag time of 4 h. Concluion: The prepared c...
Source: Current Drug Delivery - Category: Drugs & Pharmacology Authors: Source Type: research