About Authors:
Yamini Pendyala*, Sudha Talasila, M.sulthana
Department of Pharmaceutics,
Padmavathi College of Pharmacy and Research Institute,
Periyanahalli, Tamilnadu.
*Yamini.pendyala45@gmail.com
ABSTRACT
The purpose of this research was to formulate and systemically evaluate in-vitro and in-vivo performances of mucoadhesive Ramipril microspheres for its potential use in the treatment of hypertension, myocardial infraction. Ramipril mucoadhesive microspheres, containing chitosan as mucoadhesive polymer and ethyl cellulose as carrier polymer, were prepared by an emulsion-solvent evaporation technique. Preformulation studies were carried out before formulation design. Total seven formulations were prepared.Microspheres were discrete, spherical, free-flowing and showed a good percentage of drug entrapment efficiency. An in-vitro wash off test showed that Ramipril mucoadhesive microspheres adhered more strongly to the gastric mucous layer and could be retained in the gastrointestinal tract for an extended period of time. In-vitro dissolution test was carried out by using phosphate buffer pH 6.8. All the formulations showed good dissolution profiles. Among all the formulation F5 showed good dissolution profile with 81.0% of drug release in 12 hours. In-vitro release kinetic data of Ramipril microspheres showed that the drug release mechanism was diffusion controlled as the plots of Higuichi model was linear. All formulations exhibited Non-Fickian diffusion (n value is in between 0.5 to 1) mechanism. Stability studies were done for the selected formulation indicates that there is no change in drug content of the formulation.The results showed a sustained anti-hypertensive effect over a longer period of time in case of mucoadhesive microspheres, compared to the powder. In conclusion, the prolonged gastrointestinal residence time and slow release of Ramipril resulting from the mucoadhesive microspheres, could contribute to the provision of a sustained anti-hypertensive effect.