Gastroretentive Drug Delivery System of Propranolol HCl for the Effective treatment of Hypertension: Development, In vitro and In vivo Evaluation

This chapter investigated to develop extended-release (ER), non- effervescent floating matrix tablets of propranolol hydrochloride (PPH) to extend the gastric residence time (GRT) and prolong the drug release after oral administration. Recently, gastroretentive drug delivery systems (GRDDS) have gained wide acceptance for drugs with a narrow absorption window, decreased stability at high alkaline pH, and increased solubility at low pH. This approach develops a drug delivery system, which gets retained within gastric fluid, thereby releasing its active principles in the stomach. Different viscosity grades of hydroxypropyl methylcellulose (HPMC) polymers, such as HPMC K4M, HPMC K15M, and HPMC K100M, were used as drug-release retardants. Glyceryl behenate (Compritol 888 ATO) and glyceryl monostearate (Precirol ATO 5) were used as low-density lipids to get the desired buoyancy over a prolonged period. The most feasible approach for the drugs having an absorption window in the stomach is to achieve a prolonged and predictable drug release profile in gastrointestinal tract (GIT) by controlling the gastric residence time (GRT). Differential scanning calorimetry (DSC) was used in the pharmacological excipient compatibility investigation. Every formulation was created using the direct compression method. The produced pills' physical attributes, medication release, and buoyancy were assessed. The release and floating properties depend on the polymer type, polymer proportion, lipid type and lipid proportions. The drug release profiles of all the formulations were subjected to zero order, first order, Higuchi and Peppas kinetic models, and the optimized formulation (F7) followed the Peppas model (R2= 0.987) with non-Fickian diffusion mechanism(n>0.5). The optimized formulation was subjected to In vivo radiographic studies in healthy human volunteers (n=3). These studies revealed a mean gastric residence time of 5 hours (n=3). It is a smart idea to build a matrix-type, non-effervescent floating drug delivery system (FDDS) for propranolol HCl (PPH) in order to extend the period, the drug is released from the stomach and treat hypertension effectively.