Microsponges are highly cross linked, patented, porous polymeric microparticles and each particle consists of a myriad of interconnected voids within a non-collapsible structure. Moreover, they may enhance stability, reduce side effects and modify drug release favourably. They are designed to deliver a pharmaceutical active ingredient efficiently at the minimum dose and also to enhance stability reduce side effects and modify drug release. The rationale behind present work was to formulate valsartan entrapped micro porous micro particles (microsponges) to control the release of the drug. Valsartan microsponges was prepared using quasi emulsion solvent diffusion method. In order to optimize the micro sponge formulation, factors affecting the physical properties of micro sponges were determined. Compatibility of the drug with excipients was studied by FT-IR, Production yield, loading efficiency and surface morphology of microsponges were performed. It was shown that the drug: polymer ratio and stirring rate influenced the particle size and drug release behaviour of micro sponges. The results showed that, generally an increase in the ratio of the drug: polymer and stirring rate resulted the cumulative percentage drug release up to 8 hrs for M7, M8, M9 were 72%, 89% and 94% respectively and entrapment efficiency values of 33.8 -84.5 respectively.

Objective: The project was aimed to fabricate and evaluate a pulsatile capsule to program the release of dual antihypertensive drugs to mimic the circadian pattern of Blood Pressure. The formulation was optimized to repeatedly release the drug in pulses during the vulnerable period of 4 a.m. to noon upon administration during bed time. Methods: Formulation was prepared by means of Pulsincap technology. It consisted of an insoluble capsule body housing a layer of swellable polymer, a Losartan tablet sealed by an erodible polymer tablet. The system was capsulated in non-biodegradable body capped with water soluble cap containing fast releasing Amlodipine-sorbitol granules. The developed formulation was studied for physical characteristics, lag time determination, in vitro and ex vivo release. Results: The capsule cap dissolved in acidic pH released 99.29% of the amlodipine within 3h. The swellable polymer layer at the base of capsule pushed the plug along with losartan tablet out after a lag time of 6-7 h with 85.93% drug being released at the end of 12 h providing a time controlled need based release. Pulsincap formulated with Amlodipine-Sorbitol granules of G3 formulation, Losartan core tablet of C4 formulation and Erodible tablet of Guar gum with E4 formulation showed highest drug release over the period of 12 h and release was found to be followed Higuchi model kinetics. The present research study results have confirmed that the modified pulsincap of dual drugs is a suitable device for the time dependent and site specific delivery. Conclusion: This approach can be useful for the timed release of a combination antihypertensive medication and may provide effective 24 h control of Blood Pressure in hypertensive patients. The formulation was successfully designed to achieve enhanced bioavailability and dual pulsatile release. Bedtime dosing will more efficiently control the circadian spikes of hypertension in the morning.

Aim: The objective of this study was to develop a novel self-nanoemulsifying drug delivery system which produced very small and uniform emulsion droplets, resulting in enhanced solubility, dissolution, and oral bioavailability of poorly water-soluble rosuvastatin calcium. Material and Methods: The effects of oil, surfactant, and cosurfactant on the drug solubility were assessed, and pseudoternary phase diagrams were plotted. Among the liquid SNEDDS formulations tested, the liquid SNEDDS composed of cinnamon oil (oil), Cremophor RH 40 (surfactant), and Transcutol P (cosurfactant) at a ratio of 1:5 (o/S mix), produced the smallest emulsion droplet size. The rosuvastatinloaded liquid SNEDDS formulation was assessed for the emulsion droplet size, solubility, and dissolution of the emulsified SNEDDS and compared to the pure drug. Different SNEDDS formulations of rosuvastatin calcium were prepared by aqueous phase titration method. Prepared SNEDDS was filled in capsule shells as drugs with high solubility or low dose can be filled in capsule shell. Prepared SNEDDS was subjected to different thermodynamic stability tests. Thermodynamically stable SNEDDS was selected for self-nanoemulsification efficiency test. Selected formulations were characterized in terms of droplet size distribution, viscosity. Finally, selected SNEDDS (F1-F8) was subjected to in vitro dissolution/drug release studies. Results and Discussion: Droplet size and viscosity of formulation F6 were found to be lowest as compared to other formulations. The results of zeta potential indicated the formation of stable SNEDDS. In vitro drug release studies showed 97.7% release of drug from optimized formulation F6, where initial drug release profile of rosuvastatin calcium from optimized formulation F6 was found to be much faster than marketed rosuvastatin calcium capsule. Conclusion: Thus, this novel SNEDDS developed represents a potentially powerful oral delivery system for rosuvastatin calcium to enhance solubility and thereby bioavailability.

Aim:The objective of this study was to develop a novel self-nanoemulsifying drug delivery system (SNEDDS) which produced very small and uniform emulsion droplets, resulting in enhanced solubility, dissolution, and oral bioavailability of poorly water-soluble rosuvastatin (RST) calcium. Materials and Methods: The effects of oil, surfactant, and cosurfactant on the drug solubility were assessed, and pseudoternary phase diagrams were plotted. Among the liquid SNEDDS formulations tested, the liquid SNEDDS composed of cinnamon oil (oil), Cremophor EL (surfactant), and transcutol P (cosurfactant) at a ratio of 2:1 (S mix ) and 1:5 (oil:Smix) ratio, produced the smallest emulsion droplet size. The RST-loaded liquid SNEDDS formulation was assessed for the emulsion droplet size, solubility, and dissolution of the emulsified SNEDDS and compared to the pure drug. Different SNEDDS formulations of RST calcium were prepared by aqueous phase titration method. Selected formulations were characterized in terms of self-emulsification time, cloud point temperature, drug content, and particle size. Finally, selected SNEDDS (F1-F8) was subjected to in vitro dissolution/drug release studies. Results and Discussion: Droplet size of formulation F5 was found to be lowest as compared to other formulations. In vitro drug release studies showed 98.3% release of drug from optimized formulation, which was found to be much faster than marketed RST calcium. Conclusion: Thus, this novel SNEDDS developed represents a potentially powerful oral delivery system for RST calcium to enhance solubility and thereby bioavailability.