Telmisartan (TLM), a poorly water-soluble antihypertensive agent exhibits suboptimal oral bioavailability in all conventional dosage forms. The present investigation was aimed to develop an oral solid dosage form incorporating nanoparticles of TLM. TLM loaded nanosuspension was formulated by media milling technique. Preliminary trials were carried out for selecting size of milling agent, type of stabilizer, speed of stirring and time of stirring. A 32 full factorial design was implemented in order to estimatethe effect of critical factors like concentration of surfactant (X1) and amount of milling agent (X2) on two major parameters [particle size (Y1) and saturation solubility (Y2)] of drug loaded nanosuspension. The optimized batch of drug loaded nanosuspension was lucratively subjected to lyophilization using trehalose as cryoprotectant without any significant change in particle size. Saturation solubility and dissolution properties of optimized formulation were drastically improved as compared to pure drug. In-vivopharmacokinetic study also exhibited intense increase in oral bioavailability of TLM. These results propose potential use of nanosuspension to improve dissolution and oral bioavailability of poorly water-soluble drugs, like TLM.

Factorial design, lyophilization, media milling, nanosuspension, saturation solubility

Department of Pharmaceutical Sciences, SaurashtraUnirsity, Rajkot, Gujarat-360005, India