Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol

The current work describes the formulation and evaluation of a phospholipid complex of kaempferol toenhance the latter’s aqueous solubility, in vitro dissolution rate, in vivo antioxidant and hepatoprotectiveactivities, and oral bioavailability. The kaempferol-phospholipid complex was synthesized using a freeze-drying method with the formulation being optimized using a full factorial design (32) approach. The resultsinclude the validation of the mathematical model in order to ascertain the role of specific formulation andprocess variables that contribute favorably to the formulation’s development. The final product wascharacterized and confirmed by Differential Scanning Calorimetry (DSC), Fourier Transform InfraredSpectroscopy (FTIR), Proton Nuclear Magnetic Resonance Spectroscopy (1H-NMR), and Powder X-rayDiffraction (PXRD) analysis. The aqueous solubility and the in vitro dissolution rate were enhanced comparedto that of pure kaempferol. The in vivo antioxidant properties of the kaempferol-phospholipid complex wereevaluated by measuring its impact on carbon tetrachloride (CCl4)-intoxicated rats. The optimizedphospholipid complex improved the liver function test parameters to a significant level by restoration of allelevated liver marker enzymes in CCl4-intoxicated rats. The complex also enhanced the in vivo antioxidantpotential by increasing levels of GSH (reduced glutathione), SOD (superoxide dismutase), catalase anddecreasing lipid peroxidation, compared to that of pure kaempferol. The final optimized phospholipidcomplex also demonstrated a significant improvement in oral bioavailability demonstrated by improvementsto key pharmacokinetic parameters, compared to that of pure kaempferol

INVESTIGATION OF EFFECT OF PHOSPHOLIPIDS ON PHYSICAL AND FUNCTIONAL CHARACTERIZATION OF PACLITAXEL LIPOSOMES

Objective: Aim of the present investigation was to determine the effect of various synthetic grades of phospholipids on paclitaxel liposomes (PTL).Methods: The PTL formulations using various grades of phospholipids were prepared by film hydration method. The prepared PTL formulations were physicochemically characterized by entrapment efficiency (EE, %w/w), vesicular size and particle size distribution. These formulations were also characterized for function parameters such as in vitro release and hemolytic toxicity assay.Results: The synthetic grades of phospholipids significantly influenced PTL formulations. The stoichiometric ratio (1:1) between CH and various synthetic phospholipids was found to be optimized one, from rest of the ratios. The characterization confirmed the formation of PTL. The EE was observed to be high (86.67%) as increasing the ratios between CH and phospholipids but then declined suddenly as further increasing the ratio. The best liposomal formulations showed that the spherical shape was found to be within size ranging from<10 µm, with a higher rate and extent of the release, ~86.22% of paclitaxel from PTL formulation. The results of the hemolytic toxicity study demonstrated that PTL formulations with a ratio (1:1) exhibited a significantly lower hemolytic toxicity (2.70%), compared to all formulations.Conclusion: The result revealed the excellent effect of phospholipids on paclitaxel liposomes. The paclitaxel liposomes prepared with CH: PL90G ratio (1:1) was found to be optimized one. The entrapment efficiency, particle size distribution, in vitro release and hemolytic activity with this ratio shown to be excellent as compared to other ratios

Polymeric micelle as a nanocarrier for delivery of therapeutic agents: A comprehensive review

For selective and effective drug delivery of therapeutic agent nanocarriers are the most effective agents. Micelles are an aggregate of surfactant molecules that dispersed in a liquid colloid. Micelles have a variety of shapes such as spheres, rods, vesicles, tubules, and lamellae. The shape and size of a micelle are a function of the molecular geometry of its surfactant molecules and solution conditions such as surfactant concentration, temperature, pH, and ionic strength. Poly Ethylene Glycol (PEG) is the most commonly used hydrophilic segment of micelles for drug delivery. Besides PEG, other polymers including poly (N-vinyl pyrrolidone) (PVP) and poly (N-isopropyl acrylamide) (pNIPAM) have also been used as hydrophilic portion of micelles. In this review we all discus about the polymeric micelles (PMs) as a nanocarriers for delivery of therapeutic agents. Keywords: Polymeric Micelles, Colloids, Nanocarriers, Drug Delivery, Poly Ethylene Glycol(PEG

Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol

The current work describes the formulation and evaluation of a phospholipid complex of kaempferol to enhance the latter’s aqueous solubility, in vitro dissolution rate, in vivo antioxidant and hepatoprotective activities, and oral bioavailability. The kaempferol-phospholipid complex was synthesized using a freeze-drying method with the formulation being optimized using a full factorial design (32) approach. Our results include the validation of the mathematical model in order to ascertain the role of specific formulation and process variables that contribute favorably to the formulation’s development. The final product was characterized and confirmed by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), Proton Nuclear Magnetic Resonance Spectroscopy (1H-NMR), and Powder X-ray Diffraction (PXRD) analysis. The aqueous solubility and the in vitro dissolution rate were enhanced compared to that of pure kaempferol. The in vivo antioxidant properties of the kaempferol-phospholipid complex were evaluated by measuring its impact on carbon tetrachloride (CCl4)-intoxicated rats. The optimized phospholipid complex improved the liver function test parameters to a significant level by restoration of all elevated liver marker enzymes in CCl4-intoxicated rats. The complex also enhanced the in vivo antioxidant potential by increasing levels of GSH (reduced glutathione), SOD (superoxide dismutase), catalase and decreasing lipid peroxidation, compared to that of pure kaempferol. The final optimized phospholipid complex also demonstrated a significant improvement in oral bioavailability demonstrated by improvements to key pharmacokinetic parameters, compared to that of pure kaempferol

APPLICATION OF RESPONSE SURFACE METHODOLOGY IN OPTIMIZATION OF PACLITAXEL LIPOSOMES PREPARED BY THIN FILM HYDRATION TECHNIQUE

Objective: The present investigation was aimed to optimize the formula of paclitaxel-loaded liposomes (PTL) by using the application of response surface methodology (RSM).Methods: Paclitaxel-loaded liposome (PTL) was optimized by response surface methodology based on two parameters, namely, percent entrapment efficiency (% EE) and percent in vitro drug release at 12 h (% DR). The liposome formula was prepared using 32 factorial design, and the selected independent variables were, phospholipid (phospholipon 90G) and cholesterol (CH) concentrations. Nine formulas of paclitaxel-loaded liposome were prepared by thin film hydration technique (THF). The entrapment efficiency, in vitro release studies and drug content, were evaluated using on UV-visible spectrophotometer at λmax-230 nm. The developed PTL formulation vesicle morphology, particle size, polydispersity index (PDI) and zeta potential (ζ) were evaluated by Motic digital microscope and Malvern zetasizer respectively.Results: Using response surface methodology the estimated coefficient values obtained for independent variables in the regression equations, exhibited that the phospholipid (PL90G) and cholesterol (CH) molar concentration was observed to be highly influencing variables in optimizing % EE (86.67±0.67) and % DR (63.49±1.21). In the prediction of % EE and % DR values, the percent relative errors (PRE) was found to be low (–0.290%) and (0.058%) respectively. This suggests that design-developed model was found to be suitable for PTL formulations and thus, validate the model.Conclusion: Experimental results show that the observed responses were in close agreement with the predicted values and this demonstrates the reliability of the RSM in an optimization of % EE and % DR in paclitaxel liposomal (PTL) formulations

Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol

The current work describes the formulation and evaluation of a phospholipid complex of kaempferol toenhance the latter’s aqueous solubility, in vitro dissolution rate, in vivo antioxidant and hepatoprotectiveactivities, and oral bioavailability. The kaempferol-phospholipid complex was synthesized using a freeze-drying method with the formulation being optimized using a full factorial design (32) approach. The resultsinclude the validation of the mathematical model in order to ascertain the role of specific formulation andprocess variables that contribute favorably to the formulation’s development. The final product wascharacterized and confirmed by Differential Scanning Calorimetry (DSC), Fourier Transform InfraredSpectroscopy (FTIR), Proton Nuclear Magnetic Resonance Spectroscopy (1H-NMR), and Powder X-rayDiffraction (PXRD) analysis. The aqueous solubility and the in vitro dissolution rate were enhanced comparedto that of pure kaempferol. The in vivo antioxidant properties of the kaempferol-phospholipid complex wereevaluated by measuring its impact on carbon tetrachloride (CCl4)-intoxicated rats. The optimizedphospholipid complex improved the liver function test parameters to a significant level by restoration of allelevated liver marker enzymes in CCl4-intoxicated rats. The complex also enhanced the in vivo antioxidantpotential by increasing levels of GSH (reduced glutathione), SOD (superoxide dismutase), catalase anddecreasing lipid peroxidation, compared to that of pure kaempferol. The final optimized phospholipidcomplex also demonstrated a significant improvement in oral bioavailability demonstrated by improvementsto key pharmacokinetic parameters, compared to that of pure kaempferol