Formulation and development of orlistat as An antiobese agent

Abstract

newline Background: Recently, obesity is increasing at an alarming rate, which is becoming a newlinemajor public health issue with unaccountable health cost to an individual. In fact, it newlineopens the door to develop various types of the metabolic disorders such as diabetes, newlinehypertension and cardiovascular diseases, in addition to chronic diseases such as newlinestroke, osteoarthritis, sleep apnea, some cancers and inand#64258;ammatory consequences. newlineCurrently, orlistat is non-centrally acting widely used anti-obesity agent. It acts in newlinestomach and small intestine in the lumen of the gastrointestinal tract. It is obtained newlinefrom streptomyces toxytricini. It acts by inhibiting the pancreatic lipase and gastric newlinelipase. Hence, triglycerides from the diet are not hydrolyzed into absorbable free fatty newlineacids and thus excreted undigested, thereby reducing caloric intake. It plays a crucial newlinerole in digestion of long chain triglycerides. In spite of such numerous advantages, newlineOrlistat capsule which is available in market has major limitations such as newlineinsolubility, poor lipase inhibition, short half-life (lt2h) which results in multiple newlinedosing frequency (Three times in a day). In addition to this, orlistat is waxy in nature newlinehaving low melting point (44 °C) so, requires specific storage condition (2 8 °C) and newlineis poorly water soluble which limits its performance. newlineAim and Objectives: newlineThe aim of the research work was to prepare and evaluate liquisolid drug delivery newlinesystem (LSDDS) and self-emulsifying drug delivery system (SEDDS) of orlistat to newlineenhance the solubility. The objectives of the study was development and evaluation of newlineformulation like liquisolid drug delivery system (LSDDS), self-emulsifying drug newlinedelivery system (SEDDS) and In vivo pharmacodynamic study of formulations newlinefollowed by stability studies of the optimized formulations. newlineMethodology: A 3 newline2 newline full factorial design was employed to formulate and optimize the newlineLSDDS of orlistat. Two independent variables, excipients ratio and liquid load factor newlinewere determined at t