Abstract:
Aim of the present investigation was to develop nanoparticulate solid oral dosage forms of a poorly water soluble
antihypertensive agent, telmisartan (TLM) by converting the optimized batch of drug loaded nanosuspensions
into a tablet dosage form using lyophilization technique. The TLM loaded nanosuspensions were optimized by
implementation of 32 full factorial design along with principal component analysis (PCA) with concentration
of stabilizer and amount of milling agents as factors. The optimized batch of TLM loaded nanosuspension exhibited a mean particle size of 334.67 ± 10.43 nm. The results of various instrumental techniques illustrated retention of drug crystallinity after milling and lyophilization. The results of in vitro drug release study of tablets
containing drug nanocrystals revealed remarkable improvement in the dissolution rate as compared to the
marketed tablet (Sartel® 20). The results of in vivo pharmacokinetic study on Wister rats revealed 1.5-fold
enhancement in oral bioavailability for tablets containing TLM nanocrystals against the marketed tablets. The
present study proposed nanosuspension as a suitable approach for developing nanosized solid oral dosage
forms of poorly water soluble drugs like telmisartan using design of experiment and principal component analysis as two important paradigms of quality by design technique.
