In the present study, we have tried to establish the correlation between changes in Zeta potential with that of cell surface permeability using bacteria (Escherichia coli and Staphylococcus aureus). An effort has been made to establish Zeta potential as a possible marker for the assessment of membrane damage, with a scope for predicting alteration of cell viability. Cationic agents like, cetyl trimethyl ammonium bromide and polymyxin B were used for inducing alteration of Zeta potential, and the changes occurring in the membrane permeability were studied. In addition, assessment of poly-dispersity index (PDI), cell viability along with confocal microscopic analysis were performed. Based on our results, it can be suggested that alteration of Zeta potential may be correlated to the enhancement of membrane permeability and PDI, and it was observed that beyond a critical point, it leads to cell death (both Gram-positive and Gram-negative bacteria). The present findings can not only be used for studying membrane active molecules but also for understanding the surface potential versus permeability relationship.
Context: Andrographis paniculata (Burm.f.) Nees (Acanthaceae) is widely used in tribal medicine in India and some other countries for multiple clinical applications. It contains andrographolide (AG) (diterpenoid lactone), a major phytomarker which probably accounts for its medicinal properties. Objective: This study investigates the site-specific distribution of AG in different tissues of rats and its pharmacokinetic parameter evaluation by using a validated liquid chromatography tandem mass spectrometry (LC-MS/MS) method. Materials and methods: A simple and sensitive LC-MS/MS method has been developed and validated to quantify the presence of AG in plasma and various tissues of rat following oral administration of A. paniculata extract and AG in a dose of 133.33 and 100 mg/kg/day, respectively, for four weeks. Results: The present study showed that the highest concentration of AG was in kidney (156.12 ng/g) followed by liver, spleen and brain while almost same concentration was found in heart and lung. The apparent Cmax, Tmax, elimination half-life and total exposure (AUC0–α) were 115.81 ng/ml, 0.75, 2.45 and 278.44 ngh/ml, respectively. Conclusion: This was an attempt to determine the presence of AG (a known biomarker) in tissues such as kidney, heart, lungs, brain and plasma of rats using a validated LC-MS/MS method. Furthermore, the observed reduced concentration in plasma and various tissues from 1 to 8 h might be attributed to relatively rapid elimination or distribution of AG from the central compartment.
21 October 2019 in Recent Patents on Anti-Infective Drug Discovery
Background: In recent decades, enormous efforts for different drug discovery processes have led to a number of drug molecules available today to overcome different challenges of the health care system. Unfortunately, more than half of these drugs are listed in either BCS (biopharmaceutical classification system) class II/ IV or both are eliminated from the development pipeline due to their limited clinical use. A nanotechnological approach bears much hope and lipoidal fabrication is found to be suitable for the delivery of such drugs. Nanoemulsion based gel i.e. nanoemulgel out of different nanolipoidal formulations has been found to be a suitable approach to successful drug delivery through topical routes. In past few years many herbal and synthetic active pharmaceutical ingredients (APIs) has been patented as nano sized emulsified gel for various therapeutic activities. Methods: Nanoemulgel is basically an emulsion-based topical gel formulation, where nanosized emulsion globules can be prepared with the help of high energy or low energy methods and further converted into nanoemulgel by adding a suitable gelling agent. Nanoemulgel fabrication enlists various kinds of polymeric materials, surfactants and fatty substances of natural, synthetic and semi-synthetic nature with a globule size range from 5 to 500 nm. Results: Nanoemulgel can be applicable to various acute and chronic diseases through topical routes. Conclusion: Nanoemulgel preparations of many recently approved drugs are being used successfully in different areas of health care and have re-defined the significance of topical route of delivery as compared to other routes. However, along with various improvements in the current state of the delivery system, the safety factor needs to be taken into account by toxicological studies of the materials used in such formulations.
Clerodendrum glandulosum extract reduced silver nanoparticles were prepared by in situ technique within chitosan-PEG hydrogel matrix and characterized for its in vitro and in vivo diabetic wound healing activities.
The present study was undertaken to investigate the food-drug interaction of carbamazepine (CBZ). Common fruit juices [grapefruit juice (GFJ), lime juice (LJ)], known to inhibit the enzyme cytochrome P450 3A4 (CYP3A4), and some widely consumed beverages [milk (M), black tea (BT)] were involved in this study in the presence of CBZ, as might happen during clinical therapy. The effects of the beverages on the pharmacokinetics and drug-induced toxicity of CBZ was observed after concomitant administration for a period of 28 days. Accordingly, the influence of altered bioavailability of CBZ on its antiepileptic activity was investigated. A significant shift in the Cmax as well as Tmax of CBZ was observed in the presence of LJ and GFJ. This increase in bioavailability significantly enhanced hepatotoxicity and delayed the onset of tremor and piloerection against pentylene tetrazole (PTZ)-induced seizure in experimental animals. However, increased toxicity of CBZ was found to be absent with BT. Thus, from our observation, LJ or GFJ in the presence of CBZ significantly increased the bioavailability of CBZ, which might lead to increased toxicity and antiepileptic activity of the drug.