D.V. R. N. Bhikshapathi

Nimodipine, a poorly soluble drug, was considered to be fit for solid dispersions to improve its solubility and bioavailability. Our study intended to prepare Nimodipine solid dispersions by solvent evaporation method using various novel polymers. Solubility and dissolution studies indicate that Kolliwax RH 40 and SLS is the most suitable polymer. The solubility studies were corresponded with dissolution data and the formulation SD15 was found to be having highest drug release of about 98.96±5.15% in about 90 minutes. In-vitro release data from several formulations containing XRD and SEM studies indicate no crystallinity in the optimized formulation SD15. FTIR studies suggested good drug excipient compatibility between all components of prepared formulation. From in vivo bioavailability studies, Cmax of the optimized formulation SD15 was 4.34±0.08ng /ml, was significantly higher as compared to pure drug suspension, i.e., 2.78±0.35ng/ml. Tmax of optimized formulation was decreased significantly when compared with pure drug (1.00±0.05hr, 2.00±0.01hr), AUC0-? and AUC0-t for optimized solid dispersion formulation was significantly higher (p<0.05) as compared to pure drug suspension. The present study demonstrated that formulation of Nimodipine solid dispersion by solvent evaporation technique is a highly effective strategy for enhancing the bioavailability of poorly water soluble Nimodipine.

Lovastatin belongs to the class of cholesterol lowering drugs and is the first clinically used statin. It is available as conventional and extended release tablets, but its low aqueous solubility finally escorts it to low oral bioavailability (less than 5 %). Therefore, improvement in aqueous solubility of Lovastatin is the foremost aim. In the present work Self-nanoemulsifying drug delivery systems (SNEDDS) of Lovastatin is being formulated to increase the water solubility. Lovastatin SNEDDS was formulated with various oils, surfactants and co-surfactants and tested for its maximum solubility and drug release. The optimized Lovastatin SNEDDS formulation (F8) has a composition of Acrysol EL 135 as oil phase, Lauro glycol 90 and Capmul MCM as surfactant and co-surfactant respectively. Formulation F8 was found to be best formulation based on evaluation parameters. No drug precipitation or phase separation was observed in the optimized formulation. The particle size of the optimized formulation was found to be 4.9 nm & Z-Average of 71.5 nm indicating all the particles were in the nanometer range. The zeta potential of the optimized SNEDDS formulation was found to be -13.7 mV which comply with the requirement of the zeta potential for stability. The current investigation of nano emulsion may serve as a promising approach for the formulation development of poorly soluble drug Lovastatin, which has undoubtedly proved the potential effectiveness of SNEDDS for formulating Lovastatin with improved solubility and dissolution. Key words: Lovastatin, SNEDDS, Statin, Lauro Glycol 90, Solubility  

In the present investigation efforts were made to develop Misoprostal loaded microspheres to obtain a desirable drug release profile by Ionic gelation method using hydrophilic polymers and cross linking agent to decrease the gastric irritation and to enhance the drug penetration. Microspheres were prepared by using sodium alginate and calcium chloride in different ratios.  All the microspheres were evaluated for particle size, percentage yield, drug entrapment efficiency, stability studies and for in vitro release kinetics and found to be within the limits. Among all the formulations S7 was selected as optimized formulation based on the physico chemical properties and drug release studies. In vitro drug release study of formulation S7 showed 97.17% drug release up to 12h in a controlled manner, which is essential for an anti ulcer therapy. The innovator Misoprostal marketed product shows the drug release of 95.23 in 1 h. The drug release of optimized formulation S7 followed zero order release and Higuchi kinetics indicating diffusion controlled drug release. FT- IR study showed no drug excipient interaction takes place.