Solubility enhancement and study of molecular interactions of poorly soluble ibuprofen in presence of urea, a hydrotropic agent

Singh, Sulochana; Dash, Upendra Nath; Talukdar, Malabika

doi:10.1016/j.matpr.2020.01.289

Cited by 8 publications

(3 citation statements)

References 16 publications

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“…As a result, the number of water molecules tied up in the orientation zone decreased as the concentration of hydrotropic agents increased, and the solubility of rosuvastatin correspondingly increased. A similar finding was reported by Singh et al when they worked on Ibuprofen, as a poorly water-soluble drug [ 27 ].…”

Section: Resultssupporting

confidence: 87%

Solubility Enhancement of a Poorly Water-Soluble Drug Using Hydrotropy and Mixed Hydrotropy-Based Solid Dispersion Techniques

Ali

Omer

2022

Advances in Pharmacological and Pharmaceutical Sciences

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Purpose. The biopharmaceutics classification system places rosuvastatin calcium in class II has a low and fluctuating oral bioavailability. The research focus is to maximize rosuvastatin calcium solubility in water and dissolution rate by employing and combining various hydrotropic agents to make a solid dispersion using solvent evaporation techniques. Methodology. The experimental study was conducted at Duhok University, College of Pharmacy. Initially, assess rosuvastatin’s solubility in hydrotropic agents including urea, mannitol, citric acid, sodium benzoate, and sodium salicylate at concentrations of 10, 20, 30, and 40% w/v. Then, various ratios of 2 and 3 hydrotropic agents were employed to reduce the concentration of each hydrotropic agent. By using a solvent evaporation procedure, solid dispersions were made. The solid dispersion powders underwent evaluation for their percentage drug content, percentage yield, solubility, dissolution test, XRD, DSC, SEM, and FTIR. For statistical analysis, GraphPad InStat Demo software was used to conduct a two-way analysis of variance (ANOVA). Results. In comparison to the pure drug, the solubility of hydrotropic solid dispersions and physical mixtures of rosuvastatin with a combination of hydrotropic agents (sodium salicylate, sodium benzoate, and urea) in the ratio of 13.33 for each increased in all formulations significantly, and all manufactured formulations’ drug release ranged from 98.83 to 104.78%, indicating a noticeably higher dissolution rate. Conclusion. The concept of mixed hydrotropic solid dispersion was shown to be an original, risk-free, and cost-effective method for enhancing the bioavailability of drugs that have a low degree of solubility in water.

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Section: Resultssupporting

confidence: 87%

Solubility Enhancement of a Poorly Water-Soluble Drug Using Hydrotropy and Mixed Hydrotropy-Based Solid Dispersion Techniques

Ali

Omer

2022

Advances in Pharmacological and Pharmaceutical Sciences

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“…Despite the instability of this type of DES in a binary mixture with water (> 30%) ( 16 ), previous studies have shown their capacity for the solubilization of drugs ( 17 ). In these systems, urea as hydrotrope ( 18 ) and glycerol ( 19 ) as cosolvent was proposed as a common mechanism for the solubilization of drugs.…”

Section: Introductionmentioning

confidence: 99%

Solubility of Some Drugs in Aqueous Solutions of Choline Chloride-Based Deep Eutectic Solvent Systems: Experimental Data, Modeling, and the Impact of Solution pH

2023

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Background: The solubility of drugs in water and organic solvents is a crucial factor in numerous pharmaceutical processes. In recent years, a new type of solvent called deep eutectic solvents (DESs) has been developed as a useful solvent for drugs. Choline chloride-glycerol/urea (ChCl-G/U) systems are DESs recognized as a novel category of environmentally friendly solvents. One recent application of this type of DES in water is the solubilization of drugs. Objectives: This study aimed to investigate the solubility of certain drugs in ChCl-G/U. In addition, the solubilization mechanisms of the DESs studied, and quantitative structure-property relationship (QSPR) models for solubilization were proposed. Methods: The solubility of 13 drugs in an aqueous solution of the ChCl-G/U system with a 1:2 molar ratio was investigated using the shake flask method. The study was conducted at 10% and 50% mass fractions of the studied systems. Multiple linear regression models were used to develop mathematical relationships between the solubilization of the studied compounds in the presence of ChCl-G/U + water mixture using QSPR models. Results: The solubility of the compounds showed a significant increase upon adding ChCl-G/U to the aqueous solutions. Based on the data obtained, QSPR models were developed using solubilization ratio and structural descriptors. Conclusions: The experimental data demonstrates the potential of utilizing ChCl-G/U as a medium to enhance the solubility of poorly soluble drugs in water. Solubilization of solutes in ChCl-G/U + water mixtures could be correlated with the structural properties of drugs. Moreover, the final pH of the solutions in ChCl-U is a critical factor that must be considered when using this system for solubilization.

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“…Researchers are faced with a lot of challenges in their attempts to find new or to improve existing drug delivery systems to achieve safer and more efficient therapy of various diseases. This is especially significant in cancer therapy, since many anticancer drugs are poorly water soluble and have severe side effects [1]. Encapsulation and targeted delivery of these drugs can improve their bioavailability, decrease side effects and reduce the number of required therapeutic dosages.…”

Section: Introductionmentioning

confidence: 99%

Effect of Crosslinker Amount on Hybrid Hydrogels Swelling and Drug Release

Markovič¹,

Panic²,

Tadić³

et al. 2021

Book of Proceedings: 1st International Conference on Chemo and BioInformatics

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Targeted drug delivery is powerful tool which researchers use to achieve safer and more efficient therapy of many diseases, including various types of cancer. Many chemotherapeutics are poorly water- soluble, so their encapsulation and targeted delivery remain quite challenge. Hydrogels based on poly(methacrylic acid) (PMAA) are widely investigated for targeted drug delivery due to their pH sensitivity, non-toxicity and biocompatibility. Still, due to the PMAA highly hydrophilic nature, PMAA can only be used for encapsulation and targeted delivery of water-soluble drugs. Our previous research was directed towards overcoming this limitation: PMAA was modified with amphiphilic protein – casein and poorly-water soluble model drug – caffeine – was encapsulated (PMAC). Present study is focused on investigation how variation of amount of one of the most important hydrogels network parameter such as crosslinker affect PMAC swelling properties and caffeine release. The group of hybrid hydrogels – PMAC – was synthesized with various amount of crosslinker: 0.4mol%, 0.8mol%, 1.6mol% and 3.2mol% with respect to methacrylic acid. Swelling behavior of hybrid hydrogels and caffeine release was investigated in two environments which simulated human stomach and intestines. Obtained results showed that targeted delivery of poorly water-soluble model drug was achieved and that its release can be prolonged up to 24h. Also, kinetic of poorly water-soluble drug release can be easily modified only by changing crosslinker amount. PMAC hybrid hydrogels have huge potential for targeted delivery of poorly water-soluble active substances.

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Solubility enhancement and study of molecular interactions of poorly soluble ibuprofen in presence of urea, a hydrotropic agent

Cited by 8 publications

References 16 publications

Solubility Enhancement of a Poorly Water-Soluble Drug Using Hydrotropy and Mixed Hydrotropy-Based Solid Dispersion Techniques

Solubility Enhancement of a Poorly Water-Soluble Drug Using Hydrotropy and Mixed Hydrotropy-Based Solid Dispersion Techniques

Solubility of Some Drugs in Aqueous Solutions of Choline Chloride-Based Deep Eutectic Solvent Systems: Experimental Data, Modeling, and the Impact of Solution pH

Effect of Crosslinker Amount on Hybrid Hydrogels Swelling and Drug Release

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