Fabrication and characterization of nanostructured lipid carrier system for effective delivery of poorly water-soluble drug quetiapine fumarate

The aim of present study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of quetiapine fumarate, a second-generation antipsychotic drug. Quetiapine Fumarate (QF) loaded NLC were prepared by hot homogenization followed by an ultrasonication method. Response surface methodology - central composite design (CCD) was used to systemically examine the influence of concentration of capmul MCM EP, concentration of poloxamer 188 and concentration of egg lecithin on particle size (PS) and % entrapment efficiency (% EE) and to optimize the NLC formulation. The CCD consists of three factored design with five levels, plus and minus alpha (axial points), plus and minus 1 (factorial points) and the centre point. A mathematical relationship between variables was created by using Design Expert software Version 12. The statistical evaluations revealed that three independent variables were the important factors that affected the PS and % EE of QF loaded NLC. The best fitted mathematical model was linear and quadratic for PS and % EE respectively. The optimized formulations found with 218.1±0.14nm of PS and 93±0.16% of % EE. Results illustrated the superiority of developed QF loaded NLC formulation as a stable drug delivery system, providing better bioavailability with the possibility of better treatment for psychological disorders.

Review on Polymer Based Nanoparticles for Increase the Bioavalibilty of Poorly Water Soluble Drug

In this review study about the polymeric nanoparticles and how polymer based nanoparticles increase bioavailability of less water soluble drugs. Polymeric nanoparticles have a matrix of biodegradable and biocompatible polymers of synthetic and natural origin. Polymer based nanoparticles are very useful for increase the solubility of the poor water-soluble drugs by decrease the particles size. Polymeric nanoparticles are very useful for targeting the drug to the specific site. Polymeric nanoparticles are also used to maintain and control the release of the drug. In present review study on the type of polymer used for the preparation of the polymer based nanoparticles. The choice of method depends on a number of factors, such as, particles size, area of application and characterization of polymeric nanoparticles.

Improved Bioavailability of Poorly Water-Soluble Drug by Targeting Increased Absorption through Solubility Enhancement and Precipitation Inhibition

Itraconazole (ITZ) is a class II drug according to the biopharmaceutical classification system. Its solubility is pH 3-dependent, and it is poorly water-soluble. Its pKa is 3.7, which makes it a weak base drug. The aim of this study was to prepare solid dispersion (SD) pellets to enhance the release of ITZ into the gastrointestinal environment using hot-melt extrusion (HME) technology and a pelletizer. The pellets were then filled into capsules and evaluated in vitro and in vivo. The ITZ changed from a crystalline state to an amorphous state during the HME process, as determined using DSC and PXRD. In addition, its release into the gastrointestinal tract was enhanced, as was the level of ITZ recrystallization, which was lower than the marketed drug (Sporanox®), as assessed using an in vitro method. In the in vivo study that was carried out in rats, the AUC0–48h of the commercial formulation, Sporanox®, was 1073.9 ± 314.7 ng·h·mL−1, and the bioavailability of the SD pellet (2969.7 ± 720.6 ng·h·mL−1) was three-fold higher than that of Sporanox® (*** p < 0.001). The results of the in vivo test in beagle dogs revealed that the AUC0–24h of the SD-1 pellet (which was designed to enhance drug release into gastric fluids) was 3.37 ± 3.28 μg·h·mL−1 and that of the SD-2 pellet (which was designed to enhance drug release in intestinal fluids) was 7.50 ± 4.50 μg·h·mL−1. The AUC of the SD-2 pellet was 2.2 times higher than that of the SD-1 pellet. Based on pharmacokinetic data, ITZ would exist in a supersaturated state in the area of drug absorption. These results indicated that the absorption area is critical for improving the bioavailability of ITZ. Consequently, the bioavailability of ITZ could be improved by inhibiting precipitation in the absorption area.

Eco-friendly and Economical Spectrophotometric Estimation of the Low Water-Soluble Drug (Norfloxacin) Applying the Concept of Mixed Hydrotropy

Objectives The main aim of the research was to analyze an economical and eco-friendly approach to improve the solubility of norfloxacin. The current analysis was to utilize the hydrotropic solutions to extract the drugs from their dosage forms, avoiding the use of costlier and harmful organic solvents. Materials and Methods In this study, an ultraviolet–visible spectrophotometer (model 1800, Shimadzu Corporation) was used to analyze the norfloxacin drug. The mixed hydrotropy approach was used to determine the solubility of norfloxacin. In this work, a blend solution (20% of urea + 20% of sodium benzoate) was used as a hydrotropic solubilizing agent. Results The solubility of norfloxacin drug in water was very low at ∼0.88 mg/mL and the solubility of norfloxacin drug in the blend solution was 11 mg/mL. From 98.96 (tablet II) to 99.35 (tablet I), the percent estimation value was achieved. This value was nearly 100, so the proposed method was correct. Standard deviation (0.2540–0.4156), percentage coefficient of variation (0.2566–0.4183), and the value of standard error (0.1481–0.2415) are also very low; hence, we can say that the proposed method is accurate. Conclusion To avoid the use of organic solvents, the mixed hydrotropy concept can be used for spectrophotometric estimation of low water-soluble drugs from bulk drug samples. It provides an economical and environmentally friendly mechanism.

Formulation and Evaluation of Solid Self-Nanoemulsifying Drug Delivery System for Enhancing the Solubility and Dissolution Rate of Budesonide

Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.

Formulation and Evaluation of Orodispersible Tablet of poorly water Soluble Drug ‘Fenofibrate’ by Using Solubility Enhancement Technique

In the recent years scientific and technological advancements have been made in the research and development of oral drug delivery systems. The aim of this study was to formulate and evaluate of orodispersible tablets by direct compression for fenofibrate by using super fast disintegrating agents like croscarmellose sodium. The use of super disintegrant and excipient for preparation of fast disintegrating is highly effective and commercially feasible. In the present investigation poorly water soluble drug is one of the most important parameters of oral formulations sucessfully developed fenofibrate was using solvent evaporation method drug: PEG 6000 in (1:5 w/w). The formulation F7 was the optimized formula that showed satisfactory results with various physicochemical evaluation parameters like thickness, hardness, weight variation, friability, drug content, % drug release almost 79.98% within 15 min. and it was follow the maximum higuchi release kinetics that regression coefficient values ‘r2’= 0.995.