Evaluation of in vitro mucoadhesiveness and texture profile analysis of doxycycline in situ hydrogels

Abstract

Delivery of active ingredients to the oral mucosa from topically applied formulations reduces side effects from systemic administration and enhances the treatment efficiency. The challenge however, is to maintain the formulation at the administration site due to rapid salivary flow and mechanical movements of the mouth. Therefore, addition of mucoadhesive polymers could aid in enhancing the formulation residence time by increasing the mucoadhesion capacity but this effect is negligible especially if low ratio of mucoadhesive polymers are added to the formulation. Different mucoadhesive polymers at 0.5% w/w (either single or combination of two polymers) were added to the hydrogels and tested for mucoadhesion capacity, tensile strengths, adhesiveness, cohesiveness, compressibility and hardness. 0.5% povidone showed significantly highest work of mucoadhesion, 0.5% Carbopol formulation showed least cohesiveness and 0.5% HPMC showed highest adhesiveness, but a formulation containing a combination of 0.25% HPMC and 0.25% povidone showed the ideal parameters among all the mucoadhesive polymers tested. The effect of increase in concentration of HPMC (0.5, 1, 1.5, 2%) showed linear relationship for work of mucoadhesion and tensile strengths whereas for TPA the values were non-linear. The drug release from the optimized polymer matrices was found to follow zero-order release profile and the mechanism was found to be super case-II transport relaxation release. The results of this study indicate the mucoadhesive polymers do not impact the tensile strengths (p=0.05), but the texture properties and work of mucoadhesion of the formulations can be significantly (p<0.05) altered by the choice of mucoadhesive component at 0.5%w/w, though not for all the polymers tested. The study provides scope to predict in vivo performance and helps optimize for localized delivery.