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 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.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10728849 | PMC |
http://dx.doi.org/10.5812/ijpr-137011 | DOI Listing |
AAPS PharmSciTech
January 2025
Laboratory of Advanced Theranostic Materials and Technology, Ningbo Institute of Materials Technology and Engineering, Chinese Academy of Sciences, Ningbo, 315201, China.
Amorphous solid dispersion (ASD) is one of the most studied strategies for improving the dissolution performance of poorly water-soluble drugs, but ASDs often have low drug loadings, thereby necessitating larger dosage sizes. This study intended to create Soluplus® (SOL)-based microparticle ASDs with high drug loading (up to 60 w/w%) and long-term stability (at least 16 months) using electrospraying to enhance the dissolution of poorly water-soluble celecoxib (CEL). X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analyses showed that the electrosprayed SOL-CEL microparticles were amorphous, and Fourier transform infrared spectroscopy (FTIR) data indicated the presence of hydrogen bonding between SOL and CEL in the microparticles, which helped stabilize the ASDs.
View Article and Find Full Text PDFAm J Chin Med
January 2025
Henan Key Laboratory of Digestive Organ Transplantation, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, P. R. China.
has been widely used in traditional Chinese medicine for several thousands of years. This plant is known for tonifying kidney Yang, strengthening muscles and bones, and dispelling wind and dampness. It is worth noting that icaritin, a prenylated flavonoid isolated from , has received increasing attention in recent years due to its wide range of pharmacological activities.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Arbuzov Str. 8, Kazan, Russia.
The aim of the present study was to obtain new metal complexes of citrus pectin with cobalt ions based on potassium polygalacturonate and to prepare a new pharmacological composition (PC) PGKCo: PGNaCo (1:1) with antitumor activity based on potassium cobalt polygalacturonate (PGKCo) and sodium cobalt polygalacturonate (PGNaCo). The study of the effect of PGKCo, PGNaCo and PC on the cell viability of tumor cell lines of different genesis in vitro showed that the obtained compounds are soluble in water and exhibit selective cytotoxic activity against the tumor cell lines of human lung carcinoma A549, breast adenocarcinoma MCF-7 and cervical carcinoma M-HeLa, with no significant toxic effect on normal human cells. The possible mechanism of action of the investigated PC on M-HeLa cancer cells was investigated.
View Article and Find Full Text PDFJ Pharm Sci
January 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, POBOX-2457, Riyadh 11451, Kingdom of Saudi Arabia; Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Kingdom of Saudi Arabia. Electronic address:
Background And Purpose: Liquid self-nanoemulsifying drug delivery systems (SNEDDS) face challenges related to stability, handling, and storage. In particular, lipophilic and unstable drugs, such as ramipril (RMP) and thymoquinone (THQ), face challenges in oral administration due to poor aqueous solubility and chemical instability. This study aimed to develop and optimize multi-layer self-nanoemulsifying pellets (ML-SNEP) to enhance the stability and dissolution of ramipril (RMP) and thymoquinone (THQ).
View Article and Find Full Text PDFInt J Pharm
January 2025
EPSRC CMAC Future Manufacturing Research Hub, Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 99 George Street, Glasgow G1 1RD UK; The Cancer Research UK Formulation Unit, Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral St, Glasgow G4 0RE UK.
Oral drug delivery remains the preferred method of drug administration but due to poor solubility many active pharmaceutical ingredients (APIs) are ill suited to this. A number of methods to improve solubility of poorly soluble Biopharmaceutical Classification System (BCS) Class II drugs already exist but there is a lack of scalable, flexible methods. As such the current study applies the innovative technique of aerosol jet printing to increase the dissolution capabilities of a Class II drug in a manner which permits flexibility to allow dosage form tailoring.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!