Category: Formulation and Quality
Purpose: This study aims to maximize the antihypertensive effect of Telmisartan (TEL) by preparing optimized cubosomal vesicles to be compressed into tablets which will be evaluated in-vitro and in-vivo.
Methods: Twelve formulae were prepared according a ( 31*22) mixed factorial design to study the significance of three independent factors on the quality of the prepared formulae after using the data obtained from the individually conducted experiments to optimize the formula components and ratios. Four distinctive formulae were selected according to the results of three estimated responses. The liquid cubosomes were successfully adsorbed onto aerosil 380 to form granules. The formulae were evaluated for their flow properties. The best granules were compressed into tablets suitable for oral administration. The tablets were evaluated for its performance. The in vivo study of the best selected cubosomal tablets was checked after oral administration in the blood of albino rabbits utilizing an HPLC.
Results: Results revealed that the highest EE was shown in formulae C5 (59.68±1.3). All the prepared formulae had particle size less than 500 nm with PDI< 0.5 and the highest zeta potential results were observed in C5, C7, C9, C11 and C12 ( >30 mv). A7 and A9 prepared using aerosil 380 showed a perfect flowability. After 1 hour of dissolution testing, the commercial product showed a 66% drug release while the release of all cubosomal formulae didn`t exceed 35 % during the first hour reaching a 85% of the drug released at the end of 24 hours. A7 was selected for the In vivo study; t max of TEL absorption is increased for cubosomal formula by three folds indicating sustained release pattern. The relative bioavailability is also increased by 2.6 fold.
Conclusion: The investigation proposed the rationality of cubosome to figure an effective controlled release tablets to improve its bioavailability and expand its activity.