Formulation and evalution of montelukast sodium - chitosan based spray dried microspheres for pulmonary drug delivery

Abstract

The objective of present work was to prepare microspheres of montelukast sodium using a natural polymer- chitosan by spray drying method by using glutaraldehyde as a cross linking agent. The microspheres were characterized for size, shape, dissolution, swelling and mucoadhesion. It was observed that, all microspheres were spherical in shape with narrow size distribution. Microspheres had mean particle size of 7-12 μm, with % encapsulation efficiency of 78-86%. The % yield was 32-49% and drug load was 48-53%. With the increase in proportion of chitosan in formulation mucoadhesive strength was increase and also increased in particle size of microspheres. As the drug:polymer ratio increase drug loading was increase and % encapsulation efficiency was also increase.

Pulmonary drug delivery systems for tuberculosis treatment

“…Microparticles have been explored as drug delivery carriers for lung administration of drug used in pulmonary disorders like asthma, chronic obstructive pulmonary disease and infectious diseases (Panchal et al, 2012). Microencapsulation offers the advantage of protecting the drug against pulmonary metabolism, sustained and prolonged drug release.…”

Influence of potential inhalation carriers on stability of thymopentin in rat bronchoalveolar lavage fluid

“…Chitosan has been extensively employed by virtue of the adhesive properties and absorption enhancement especially for protein and peptide (Yamamoto et al, 2005). Chitosanbased carriers in micro-dimension have been prepared for pulmonary delivery (Panchal et al, 2012;Yang et al, 2012;Learoyd et al, 2008). Based on the results described, formation of complex of chitosan and TP5 reduced the enzymatic degradation rate independent of the molecule weight of chitosan.…”

Pharmacokinetic Comparison of Montelukast Sodium Formulations After a Single Oral Dose in Healthy Guinea Pigs

“…This is an acidic drug which is highly bound to plasma albumin and 64% bioavailable orally [8,9]. The main drawback of conventional montelukast formulation is that it undergoes hepatic first-pass metabolism and shows biological half-life of 2.5-5 h [10]. Chronomodulated capsules (sustained-release solid dispersion of drug enclosed in pH-sensitive film-coated hard gelatin shell) are designed to have initial 3.5-4 h release lag time with sustained release up to 10 h assuming that capsules to be consumed at bedtime.…”