Fabrication of electrospun nanofibres of BCS II drug for enhanced dissolution and permeation across skin.

The present work reports preparation of irbesartan (IBS) loaded nanofibre mats using electrospinning technique. The prepared nanofibres were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction analysis, in vitro diffusion and ex vivo skin permeation studies. FTIR studies revealed chemical compatibility of IBS and polyvinyl pyrrolidine (PVP K-30). SEM images confirmed formation of nanofibres wherein IBS existed in amorphous form as revealed by DSC and XRD analyses. The prepared nanofibre mats of IBS were found to be superior to IBS loaded as cast films when analysed for in vitro IBS release and ex vivo skin permeation studies since the flux of IBS loaded nanofibres was 17 times greater than as cast film. The improvement in drug delivery kinetics of IBS loaded nanofibres could be attributed to amorphization with reduction in particle size of IBS, dispersion of IBS at molecular level in PVP matrix and enormous increase in the surface area for IBS release due to nanonization. Thus transdermal patch of IBS loaded nanofibres can be considered as an alternative dosage form in order to improve its biopharmaceutical properties and enhance therapeutic efficacy in hypertension.

Efavirenz Self-Nano-Emulsifying Drug Delivery System: In Vitro and In Vivo Evaluation.

Self-emulsifying drug delivery system (SEDDS) is the isotropic and thermodynamically stable mixture of oil, surfactant, co-solvent/surfactant, and drug. It emulsifies spontaneously when introduced into an aqueous phase under a mild agitation. The current study was aimed to prepare SNEDDS to augment solubility, release rate, and oral bioavailability of BCS class II drug, efavirenz (EFV). A series of oil, surfactant, and co-surfactant was screened out by a ternary phase diagram to locate a better homogenous mixture. The prepared SNEDDS was evaluated regarding its appearance, mean droplet size, phase separation, in vitro drug release, and oral bioavailability. Among the screened oil, surfactant, and co-surfactant, Labrafil M 2125 CS, Tween 80, and Transcutol®P mixture exhibited superior solubilizing capacity, respectively. Optimized SNEDDS exhibits 98.39% drug release. SNEDDS dissolution behavior was attributed to oil/surfactant ratios and properties of the surfactant phase. It also demonstrates threefold increments in the area under curve (AUC) in comparison to neat EFV. Furthermore, the optimized SNEDDS does not show any vitrification during its 3-month storage. In the present study, better performance of SNEDDS is explained by various factors like (i) improved surface area of droplets, (ii) superior solubilization potential for hydrophobic drugs due to Labrafil M 2125 CS, and (iii) result of surfactant on mucosal permeability. This study demonstrated that SNEDDS may be an alternative approach for the poorly soluble drugs to improve their solubility and oral bioavailability.

Development of photostable gastro retentive formulation for nifedipine using low-density polypropylene microporous particles.

The aim of this study was to develop photostable gastro retentive formulation for nifedipine loading into low-density polypropylene microporous particles (Accurel MP 1000®) by a solvent evaporation technique using the 3² factorial design. Yield, drug loading, surface topography, thermal properties, crystal characteristics, photostability and in vitro drug release were studied. Optimized microparticles formulated into a capsule were evaluated for the dissolution study and compared with marketed formulation. Higher values of T(50%), time required for 50% degradation of drug with threefold and 1.5-fold decrease in degradation rate constant (K) under UV and fluorescent lamp were observed for the microparticles, respectively, as compared to pure nifedipine indicated remarkable improved photostability. Microparticles showed good floating ability in 0.1N HCl with initial burst release (16-29%) followed by the zero-order drug release up to 8 h. The capsule formulation followed the ideal modified release pattern.