Design and Invitro Evaluation of Mucoadhesive Microspheres containing Amodel Antibacterial agent for Periodontitis

Abstract

In the present work, mucoadhesive microspheres of Chitosan, Hydroxypropyl Guar and Sodium alginate were formulated to deliver Doxycycline monohydrate to oral cavity infections(periodontitis).The present investigation involves formulation and evaluation of mucoadhesive microspheres with doxycycline monohydrate as model drug for prolongation of drug release time. The microsphere formulations were prepared by using three different polymers (Chitosan, Hydroxypropyl Guar and sodium alginate), DOSS and Span 80 were used as emulsifiers; Calcium chloride as a cross linking agent.The ratio of Polymer to drug for each polymer were varied in the microsphere preparation and then they were evaluated for % yield, % drug entrapment efficiency,particle size analysis, in vitro mucoadhesion tests, degree of swelling, morphological study by SEM and In – vitro drug diffusion profile.Further the analysis of release mechanism was carried out by fitting the drug diffusion data to various kinetic equations like, Zero order, First order Korsmeyer- Peppas, Higuchi (matrix) and Hixson Crowell equations and from the values so obtained, the best fit model were arrived at The results obtained have been discussed in the chapter 6. Results of FT-IR revealed that there was no chemical interaction between the drug and the polymer used. The obtained microspheres were spherical, free flowing and had a particle size ideal for oral cavity delivery. The prepared microspheres had good mucoadhesiveness and revealed good degree of swelling. The release pattern of the formulations was observed to be biphasic characterized by initial burst effect followed by a slow release. The kinetic model fitting data shows that the release of drug from the microspheres follow Higuchi (matrix) model. From the above the results CDX3, HDX2 and SDX2 were found to be best formulations for the oral delivery of doxycycline monohydrate that complied with all the parameters. However, in – vivo experiments need to be carried out to know the absorption pattern and bioavailability of drug from the microspheres and thus enabling us to establish in vitro – in vivocorrelation.