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

Drug-Phospholipid Complex-loaded Matrix Film Formulation for the Enhanced Transdermal Delivery of Quercetin

A novel quercetin-phospholipid-complex(QPLC)-loaded matrix film for improved transdermal delivery of quercetin was developed. The QPLC formulation, prepared using a solvent-evaporation method, was optimized using a central-composite design. The optimized QPLC formulation was characterized by particle size and zeta potential analysis, thermal analysis, Fourier transform infrared spectroscopy (FTIR), and proton nuclear magnetic resonance spectroscopy (1H-NMR). QPLC formulation was functionally evaluated for solubility and in vitro dissolution of quercetin. Matrix films of pure quercetin (Q-MF)or QPLC QPLC-MF) were prepared using a solvent casting method. The prepared Q-MF and QPLC-MF were characterized for weight uniformity, folding endurance, moisture content, and moisture uptake. The films were also functionally characterized for in vitro diffusion of quercetin through a dialysis membrane and ex vivo permeability of quercetin across rat skin. Finally, the anti-inflammatory activity of the films was evaluated on carrageenan-induced paw edema in Wistar albino rats. The experimental design identified the optimal formulation and process variables for the preparation of QPLC. The validation of the obtained model using these values confirmed the suitability and robustness of the model. The physical-chemical characterization of the prepared QPLC supported the formation of a stable complex. The solubility analysis of QPLC showed a 22-fold increase in quercetin aqueous solubility, compared to pure quercetin. The dissolution results exhibited a significantly higher rate and extent of quercetin dissolution from QPLC compared to that of pure quercetin. The permeability of quercetin from Q-MF and QPLC-MF across rat skin mirrored those obtained from the dissolution studies. Topical application of QPLC-MF exhibited a significant (p\u3c0.05) inhibition of carrageenan-induced paw edema in rats compared to that of Q-MF. This study provides a promising combination approach, i.e., phospholipid-based complexation and transdermal film formulation for improved transdermal delivery of quercetin and similar pharmacologically active phytoconstituents

Effectiveness of crossword puzzle as an adjunct tool for active learning and critical thinking in Pharmacology

Background: Modern pedagogic methodologies are being introduced in Medical education and there is a growing evidence of crossword puzzle as an educational tool for active learning, problem solving and critical thinking. The aim of the study was to study the effectiveness of crossword puzzle as an adjunct to the conventional lecture for active learning and critical thinking in Pharmacology. This was a parallel group; pre and post assessment, educational intervention study conducted among second year undergraduate medical students.Methods: Second year medical students were randomly selected and assigned to two groups A (Cross word puzzle) and B (control), after an hour conventional lecture on “Drugs for Hypertension” In both the groups, pre- and post-intervention knowledge was assessed using the MCQ test. A self-designed crossword puzzle on the lecture topic was used as an intervention and students were allowed to read textbooks with a crossword puzzle in intervention group A, whereas control group B were allowed to read textbook only. After 45 minutes, the post-intervention assessment was done in both groups with the same set of MCQ and students’ feedback on crossword usefulness was obtained.Results: The average MCQ test score in Group A improved significantly from 6.65±3.4 pre-intervention to 11.26±2.5 post-intervention (p <0.05) with absolute learning gain 30.73 % and relative learning gain 69.32 %. The average test score in Group B also improved significantly from 5.7±2.9 pre-intervention to 9.59±2.5 post-intervention (p <0.05) with absolute learning gain 25.93 % and relative learning gain 68.23%. There was a significant improvement in the MCQ scores in both the groups after intervention. But the post-intervention MCQ scores in group A (crossword puzzle) was higher and statistically significant (P <0.05) in comparison to group B.Conclusions: Cross-word puzzle promotes active self-learning and develops critical thinking among medical students. It could be used as supplementary educational tool in pharmacology to enhance problem-solving skills along with the information provided through traditional teaching lectures or could be used as a micro task

Glucosamine HCl-based solid dispersions to enhance the biopharmaceutical properties of acyclovir

The objective of the work presented here was to assess the feasibility of using glucosamine HCl as a solid-dispersion (SD) carrier to enhance the biopharmaceutical properties of a BCS class III/IV drug, acyclovir (ACV). The solid-dispersions of acyclovir and glucosamine HCl were prepared by an ethanol-based solvent evaporation method. The prepared formulations characterized by photomicroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transforms infrared spectrophotometry (FTIR), powder x-ray diffractometry (PXRD) and drug content analysis. The functional characterization of ACV-SD was performed by aqueous solubility evaluation, dissolution studies, fasted versus fed state dissolution comparison, ex vivo permeability, and stability studies. Photomicroscopy and SEM analysis showed different surface morphologies for pure ACV, glucosamine HCl and ACV-SD. The physical-chemical characterization studies supported the formation of ACV-SD. A 12-fold enhancement in the aqueous solubility of ACV was observed in the prepared solid dispersions, compared to pure ACV. Results from in vitro dissolution demonstrated a significant increase in the rate and extent of ACV dissolution from the prepared ACV-SD formulations, compared to pure ACV. The rate and extent of ACV permeability across everted rat intestinal membrane were also found to be significantly increased in the ACV-SD formulations. Under fed conditions, the rate and extent of the in vitro dissolution of ACV from the formulation was appreciably greater compared to fasted conditions. Overall, the results from the study suggest the feasibility of utilizing glucosamine HCl as a solid dispersion carrier/excipient for enhancement of biopharmaceutical properties of acyclovir, and similar drugs with low solubility/permeability characteristics

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&lt;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

Drug utilization pattern in dermatology outpatient department at a tertiary care hospital in Navi Mumbai

Background: Skin diseases are common and cause a huge disease burden globally. Different class of drugs and combinational products are available in dermatology for treatment. Periodic prescription analysis in the form of drug utilization study can improve the quality of prescription and curb the menace of irrational prescribing. Aim and objective of the study were to study the prescribing pattern and drug utilization trends in Dermatology outpatient department at a tertiary care hospital in Navi Mumbai.Methods: A cross-sectional, observational study was conducted over a period of three months in dermatology department of a tertiary care teaching hospital, Navi-Mumbai. A total of 102 adult patients visiting dermatology OPD were included and their prescriptions were analyzed with WHO prescribing indicators and additional indices.Results: Analysis showed that the average number of drugs per prescription was 3.27. Percentage of drugs prescribed by generic name was 31.1%. Percentage of drugs prescribed from National Essential drug list (NEDL) was 44.2%. The commonest prescribed drugs were antihistaminics followed by antifungals. Oral tablets were the commonest prescribed dosage form.Conclusions: Antihistaminics and antifungals dominated the prescribing pattern in this study with restraint on polypharmacy, but showed ample scope for improvement to prescribe generic and selection of essential drugs

Proposal for creating a centre for research in solar-terrestrial physics as an interdepartmental activity during IHY at Shivaji University, Kolhapur (16.40°N, 74.15°E)

This note describes teaching and R &amp; D activities presently being carried out in the solar-terrestrial Physics at the Space Science laboratory, Department of Physics, Shivaji University, Kolhapur. A variety of solar and geophysical ground based experiments are available, which can be operated on a regular basis during IHY, with financial help from the government funding agencies in India. The main purpose of this note is to briefly describe our experimental research facilities of relevance to IHY

Formulation and Characterization of the Improved Solubility, In Vivo Bioavailability and Antioxidant Activity of Apigenin-Phospholipid Complex (APLC)

In the present study a phospholipid based complex of apigenin (APLC) was prepared with a goal of improving its aqueous solubility, dissolution, in vivobioavailability, and antioxidant activity

Implementation Of Anonymous Vehicle Reporting And Communication System For Wrongly Parked Vehicle

Improper parking can cause several issues and problems, including Reduced Accessibility, Inconvenience for Other Drivers, Public Transportation Disruption, Environmental and Aesthetic Concerns, Public Perception, and Traffic Congestion. Addressing these issues typically calls for a combination of traffic management, public awareness campaigns, law enforcement, smart urban design, and community involvement to preserve the successful and safe usage of public spaces