Appraisal of Felodipine Nanocrystals for Solubility Enhancement and Pharmacodynamic Parameters on Cadmium Chloride Induced Hypertension in Rats.

AIM: Felodipine (FDP), an antihypertensive drug possesses low water solubility and extensive first-pass metabolism leading to poor bioavailability. This impelled us to improve its solubility, bioavailability, and pharmacodynamic properties through the Nanocrystal (NC) approach. METHODS: FDP-NC were prepared with Poloxamer F125 (PXM) by the antisolvent precipitation method. The experimental setup aimed at fine-tuning polymer concentration, the proportion of antisolvent to solvent, and the duration of ultrasonication for NC formulation. RESULTS: Optimized formulation was characterized for particle size, solubility, and PDI. Particle reduction of 74.96 times was achieved with a 9X solubility enhancement as equated to pure FDP. The morphology of NC was found to be crystalline through scanning electron microscopy observation. The formation of the crystal lattice in FDP-NC was further substantiated by the XRD and DSC results. Lowering of the heat of fusion of FDP-NC is a clear indication of size reduction. The stability studies showed no substantial change in physical parameters of the FDP-NC as assessed by particle size, zeta potential, and drug content. CONCLUSION: The crystalline nature and improved solubility of FDP-NC improve the dissolution profile and pharmacodynamic data. The stability study data ensure that FDP-NC can be safely stored at 25°C. It is revealed that FDP-NC had a better release profile and improved pharmacodynamic effects as evident from better control over heart rate than FDP.

Cellulose Acetate 398-10 Asymmetric Membrane Capsules for Osmotically Regulated Delivery of Acyclovir.

The study was aimed at developing cellulose acetate asymmetric membrane capsules (AMCs) of acyclovir for its controlled delivery at the absorption site. The AMCs were prepared by phase inversion technique using wet process. A 2(3) full factorial design assessed the effect of independent variables (level(s) of polymer, pore former, and osmogen) on the cumulative drug release from AMCs. The buoyant optimized formulation F7 (low level of cellulose acetate; high levels of both glycerol and sodium lauryl sulphate) displayed maximum drug release of 97.88 ± 0.77% in 8 h that was independent of variation in agitational intensity and intentional defect on the cellulose acetate AMC. The in vitro data best fitted zero-order kinetics (r (2) = 0.9898). SEM micrograph of the transverse section confirmed the asymmetric nature of the cellulose acetate capsular membrane. Statistical analysis by Design Expert software indicated no interaction between the independent variables confirming the efficiency of the design in estimating the effects of variables on drug release. The optimized formulation F7 (desirability = 0.871) displayed sustenance of drug release over the drug packed in AMC in pure state proving the superiority of osmotically active formulation. Conclusively the AMCs have potential for controlled release of acyclovir at its absorption site.