Abstract. The objective of this study was to investigate the pH-dependent solubility and dissolution of weakly basic Biopharmaceutical Classification Systems (BCS) class II drugs, characterized by low solubility and high permeability, using carvedilol, a weak base with a pK a value of 7.8, as a model drug. A series of solubility and in vitro dissolution studies was carried out using media that simulate the gastric and intestinal fluids and cover the physiological pH range of the GI from 1.2 to 7.8. The effect of ionic strength, buffer capacity, and buffer species of the dissolution media on the solubility and dissolution behavior of carvedilol was also investigated. The study revealed that carvedilol exhibited a typical weak base pH-dependent solubility profile with a high solubility at low pH (545.1-2591.4 μg/mL within the pH range 1.2-5.0) and low solubility at high pH (5.8-51.9 μg/mL within the pH range 6.5-7.8). The dissolution behavior of carvedilol was consistent with the solubility results, where carvedilol release was complete (95.8-98.2% released within 60 min) in media simulating the gastric fluid (pH 1.2-5.0) and relatively low (15.9-86.2% released within 240 min) in media simulating the intestinal fluid (pH 6.5-7.8). It was found that the buffer species of the dissolution media may influence the solubility and consequently the percentage of carvedilol released by forming carvedilol salts of varying solubilities. Carvedilol solubility and dissolution decreased with increasing ionic strength, while lowering the buffer capacity resulted in a decrease in carvedilol solubility and dissolution rate.
Background: Conventional medication; traditional or folk medicine as well as herbal medicines; have been widely used since ancient times. In Jordan traditional medicines are freely available and self-prescribed as well. No previous study has investigated believes and knowledge with regards to herb-drug interaction in Mutah geographical in Jordan.
Objectives: This study aims to investigate and evaluate knowledge and attitude about self-medication using herbal medicine and its drug interaction among the public in Mutah.
Materials and methods: A questionnaire-based survey conducted. Survey took place in different locations in the Mutah region in Al-Karak city from Jordan, during December 2017 and January 2018. Data analyzed by SPSS.
Results: The majority of responders (82%) use self-prepared herbal preparation. While (56%) go for self-medication rather than visiting a physician. About (63%) participants responded that physicians didn’t ask them about if they use any herbal medication and about (50%) not willing to tell their physician about their self-medication. Knowledge about herbs gained from the family in the first place (38%); TV (21%) and friends (15%). Almost (79%) responders agree that herbs are safer and easier to be used compared to physician-prescribed medicine.
Conclusion: A high belief in herbal therapy use. Responders gain their knowledge primarily from their families which they obtain their knowledge primarily from their tradition. They are not aware of their interaction with other therapies. Care-givers in this region should be aware of the high percentage of herbal medicine use and are encouraged to discuss potential use with their patients to avoid future complications.
The aim of the current work was to elucidate whether the encapsulation of curcumin in nanoparticles (of microemulsion type) would allow its exertion of anticancer activity on several cancer cell lines or not. Curcumin microemulsion was prepared using the water dilution method, in which oleic acid constituted the oily phase, and tween 20, ethanol constituted the surfactant and cosurfactant respectively. The microemulsion was tested for its particle size, charge, morphology using transmission electron microscopy, in vitro curcumin release, stability and anticancer activity on HCT-116 colon cancer line, A549 lung cancer cell line, and PC3 prostate cancer cell line. The safety of the formulation was tested on fibroblasts cell line. Results revealed that curcumin microemulsion was successfully prepared with a particle size of 11.45±0.21 nm, and a negative charge of -9.07 mV, and it was able to sustain the release of drug for 24 hours with a cumulative percent released of 66.72%. Its spherical morphology was confirmed using transmission electron microscopy. No significant changes in particle size or charge were observed upon storage, suggesting the physical stability of the microemulsion. Curcumin microemulsion was proven safe on the normal fibroblasts cell line, and it preserved the anticancer activity of curcumin against A549, HCT116, and PC3 cell lines. Results of this study delineate that microemulsion is a suitable nanodelivery system for curcumin, which needs to be tested on animal tumor models for verification of the anticancer properties in vivo.
The aim of the current work was to elucidate whether the nanoencapsulation of meloxicam would allow its exertion of anticancer activity on colon cancer cells despite lacking COX-2 expression.
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