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ChemistryOpen Dec 2021The co-crystallization approach has been used to enhance specific desirable properties of active pharmaceutical ingredients (APIs) such as solubility, dissolution rate,... (Review)
Review
The co-crystallization approach has been used to enhance specific desirable properties of active pharmaceutical ingredients (APIs) such as solubility, dissolution rate, and stability. Solubility is a fundamental property that affects the bioavailability and dosage of the API. The co-crystal approach is one of the emerging methods with the potential for improving the solubility of these drugs. This paper reviews the latest progress on improving the solubility of some antidiabetic drug molecules using the co-crystal approach.
Topics: Biological Availability; Crystallization; Hypoglycemic Agents; Solubility
PubMed: 34921592
DOI: 10.1002/open.202100246 -
International Journal of Molecular... Oct 2022Cancer has been a major health problem in the world in the past decades. It is urgent to develop new, effective and safe drugs for the treatment of cancer. There are... (Review)
Review
Cancer has been a major health problem in the world in the past decades. It is urgent to develop new, effective and safe drugs for the treatment of cancer. There are many pentacyclic triterpenoids with positive anti-tumor activity and safety in nature. Oleanolic acid (OA), as one of the pentacyclic triterpenoids, also has broad biological activities including liver protection, anti-inflammatory, hypoglycemic, antiviral and anti-tumor. Therefore, to investigate its anti-tumor activity and mechanism, many OA derivatives have been developed. Some derivatives are less toxic to normal hepatocytes, which may be due to the strong liver protection ability of OA. However, the poor water solubility of OA is one of the main reasons for the weak anti-tumor activity. It is reported that some OA derivatives could enhance solubility by chemically linking some hydrophilic groups to improve anti-tumor activity. This review not only summarizes the highly water-soluble OA derivatives that can improve anti-tumor activity reported in recent years, but also introduces their possible anti-tumor mechanisms.
Topics: Humans; Oleanolic Acid; Solubility; Triterpenes; Neoplasms; Water
PubMed: 36362079
DOI: 10.3390/ijms232113291 -
Poultry Science Jun 2022An environmentally sustainable method to extract phosphatidylcholine (PC) from chicken liver (PCCL) and its functional properties were studied. The extraction times,...
An environmentally sustainable method to extract phosphatidylcholine (PC) from chicken liver (PCCL) and its functional properties were studied. The extraction times, enzymatic hydrolysis time, the solid-liquid ratio as well as types of enzymes (protamex proteinase and neutral proteinase) were investigated. Furthermore, the content of PCCL, emulsifying properties and solubilities of PCCL were also determined. The optimum conditions of extracting PCCL were found to be: reaction time of 3.75 h, enzymatic hydrolysis time of 85.22 min, 1: 3.15 (w/v) of solid-liquid ratio, using protamex proteinase, and the yield and concentration of PCCL was 88.92% and 0.89 mg/mL, respectively. Solubility and emulsifying properties of PCCL showed that the HLB value of PCCL was 10, and in ethanol and glycerol, the solubility of PCCL was 0.5850 g/mL and 0.0965 g/mL, respectively, which was shown to have good ethanol solubility and lipophilicity. From the perspective of green production and high-value utilization of by-products, PCCL could be used as a potential new lecithin source, providing ideas for the development and application of PC of animal origin.
Topics: Animals; Chickens; Endopeptidases; Ethanol; Hydrolysis; Lecithins; Liver; Solubility
PubMed: 35512498
DOI: 10.1016/j.psj.2021.101689 -
International Journal of Pharmaceutics Jan 2018Over the last few decades, hot melt extrusion (HME) has emerged as a successful technology for a broad spectrum of applications in the pharmaceutical industry. As... (Review)
Review
Over the last few decades, hot melt extrusion (HME) has emerged as a successful technology for a broad spectrum of applications in the pharmaceutical industry. As indicated by multiple publications and patents, HME is mainly used for the enhancement of solubility and bioavailability of poorly soluble drugs. This review is focused on the recent reports on the solubility enhancement via HME and provides an update for the manufacturing/scaling up aspects of melt extrusion. In addition, drug characterization methods and dissolution studies are discussed. The application of process analytical technology (PAT) tools and use of HME as a continuous manufacturing process may shorten the drug development process; as a result, the latter is becoming the most widely utilized technique in the pharmaceutical industry. The advantages, disadvantages, and practical applications of various PAT tools such as near and mid-infrared, ultraviolet/visible, fluorescence, and Raman spectroscopies are summarized, and the characteristics of other techniques are briefly discussed. Overall, this review also provides an outline for the currently marketed products and analyzes the strengths, weaknesses, opportunities and threats of HME application in the pharmaceutical industry.
Topics: Drug Delivery Systems; Equipment Design; Pharmaceutical Preparations; Solubility; Technology, Pharmaceutical
PubMed: 29102700
DOI: 10.1016/j.ijpharm.2017.10.056 -
Indian Journal of Dental Research :... 2020Calcium hydroxide [Ca(OH)] is a material used during pulp capping treatment, despite being readily soluble in both water and acid. In contrast, propolis constitutes a...
BACKGROUND
Calcium hydroxide [Ca(OH)] is a material used during pulp capping treatment, despite being readily soluble in both water and acid. In contrast, propolis constitutes a nontoxic resin which is not easily dissolved in water. Therefore, a combination of Ca(OH)and propolis is assumed to be capable of increasing the mechanical properties of Ca(OH)and to diffuse into the dentinal tubules.
OBJECTIVE
This research aimed to reveal the solubility and water sorption ability of a combination of Ca(OH)and propolis as pulp capping material.
MATERIALS AND METHOD
The samples comprised 18 Ca(OH)and Ca(OH)-propolis chips, 15 mm × 1 mm in dimension, all of which were stored in an incubator for 24 h at 37°C. Each sample was then divided into two groups: one dissolved in 50 mL of artificial saliva for 24 h at 37°C and another for 7 days before being weighed, dried, incubated, and weighed for a second time. The result of the reduction in mass divided by the volume of the samples was considered to constitute the level of solubility and water sorption. The difference between the solubility and water sorption ability was analyzed using an independent t-test with significant difference <0.05.
RESULTS
The solubility of Ca(OH)-propolis is lower than that of Ca(OH) after immersion for 1 day (P = 0.001) and 7 days (P = 0.000). The water sorption ability of Ca(OH)-propolis is no different than that of Ca(OH)after immersion for 1 day (P = 0.088) and 7 days (P = 0.635). However, the water sorption ability of Ca(OH)-propolis after 1-day immersion is higher than immersion for 7 days (P = 0.012).
CONCLUSION
The solubility Ca(OH)-propolis is lower than that of Ca(OH), but its water sorption is higher than that of Ca(OH)
Topics: Dental Pulp Capping; Materials Testing; Propolis; Solubility; Water
PubMed: 33107456
DOI: 10.4103/ijdr.IJDR_422_19 -
Drug Delivery Dec 2022Self-emulsifying drug delivery systems (SEDDS) are a proven method for poorly soluble substances works by increasing the solubility and bioavailability. SEDDS and... (Review)
Review
Self-emulsifying drug delivery systems (SEDDS) are a proven method for poorly soluble substances works by increasing the solubility and bioavailability. SEDDS and isotropic mixtures, are composed of oils, surfactants, and occasionally cosolvents. The ability of these formulations and methods to produce microemulsions or fine oil-in-water (o/w) emulsions after moderate stirring and dilution by water phase along the GI tract might be a promising technique for lipophilic agents with dissolution rate-limited absorption. This review provides an outline of SEDDS's numerous advances and biopharmaceutical elements, types, manufacturing, characterization, limitations, and future prospects. The evaluation of SEDDS and its applications are also discussed, focusing on the advances of SEDDS's solid self-emulsifying delivery mechanism and dosage form. By integrating suitable polymer into the formulation, SEDDS may be studied for the creation of a formulation with sustained drug release. This technology's improvement might lead to a new application in the field of medicine delivery. SEDDS has been demonstrated to be quite efficient in increasing oral bioavailability of lipophilic products. SEDDS is one of the promising methods for controlling the characteristics of medications that are not great choices for oral delivery. It is also worth mentioning that SEDDS may be made in variety of solid dosage forms that are acceptable for both oral and parenteral administration.
Topics: Administration, Oral; Biological Availability; Drug Delivery Systems; Emulsions; Solubility; Water
PubMed: 35666090
DOI: 10.1080/10717544.2022.2083724 -
Scientific Reports Oct 2022Measurement of saturation solubility of drugs in a supercritical fluid is an important parameter for the implementation of supercritical technology in pharmaceutical...
Measurement of saturation solubility of drugs in a supercritical fluid is an important parameter for the implementation of supercritical technology in pharmaceutical industry. CO is the most sorted substance as a supercritical fluid since it has attractive properties like easily achievable critical temperature, moderate pressure. Cancer is increasingly affecting the mankind, a proper dosage while treating would help in minimizing the drug usage. The bioavailability of the drug is mainly influenced by the drug particle size. An appropriate technology is always useful in making suitable drug particles; thus, supercritical fluid technology (SFT) is considered as promising technique for the production of micro and nanoparticles. Since, particle production process through SFT needs solubility information, appropriate solubility information is necessary. In the present work, Crizotinib (anti-cancer drug) solubility in supercritical carbon dioxide (scCO) is measured and reported, for the first time. The obtained solubilities are at temperatures 308, 318, 328,338 K and pressures 12, 15, 18, 21, 24 to 27 MPa. The measured solubilities are ranged in terms of mole fraction from (0.483 × 10 to 0.791 × 10) at 308 K, (0.315 × 10 to 0.958 × 10) at 318 K, (0.26 × 10 to 1.057 × 10) at 328 K, (0.156 × 10 to 1.219 × 10) at 338 K. The cross over region is observed at 14.5 MPa. To expand the application of the solubility data, few important solubility models and three cubic equations of sate (cubic EoS) models along with Kwak and Mansoori mixing rules are investigated. Sublimation and salvation enthalpies of Crizotinib dissolution in scCO are calculated.
Topics: Solubility; Carbon Dioxide; Crizotinib; Nanoparticles; Particle Size
PubMed: 36261497
DOI: 10.1038/s41598-022-22366-y -
Biological Chemistry Sep 2023ATP is an important small molecule that appears at outstandingly high concentration within the cellular medium. Apart from its use as a source of energy and a... (Review)
Review
ATP is an important small molecule that appears at outstandingly high concentration within the cellular medium. Apart from its use as a source of energy and a metabolite, there is increasing evidence for important functions as a cosolute for biomolecular processes. Owned to its solubilizing kosmotropic triphosphate and hydrophobic adenine moieties, ATP is a versatile cosolute that can interact with biomolecules in various ways. We here use three models to categorize these interactions and apply them to review recent studies. We focus on the impact of ATP on biomolecular solubility, folding stability and phase transitions. This leads us to possible implications and therapeutic interventions in neurodegenerative diseases.
Topics: Solubility; Adenosine Triphosphate
PubMed: 37656203
DOI: 10.1515/hsz-2023-0202 -
Scientific Reports Sep 2022Knowledge of the solubilities of hydrocarbon components of natural gas in pure water and aqueous electrolyte solutions is important in terms of engineering designs and...
Knowledge of the solubilities of hydrocarbon components of natural gas in pure water and aqueous electrolyte solutions is important in terms of engineering designs and environmental aspects. In the current work, six machine-learning algorithms, namely Random Forest, Extra Tree, adaptive boosting support vector regression (AdaBoost-SVR), Decision Tree, group method of data handling (GMDH), and genetic programming (GP) were proposed for estimating the solubility of pure and mixture of methane, ethane, propane, and n-butane gases in pure water and aqueous electrolyte systems. To this end, a huge database of hydrocarbon gases solubility (1836 experimental data points) was prepared over extensive ranges of operating temperature (273-637 K) and pressure (0.051-113.27 MPa). Two different approaches including eight and five inputs were adopted for modeling. Moreover, three famous equations of state (EOSs), namely Peng-Robinson (PR), Valderrama modification of the Patel-Teja (VPT), and Soave-Redlich-Kwong (SRK) were used in comparison with machine-learning models. The AdaBoost-SVR models developed with eight and five inputs outperform the other models proposed in this study, EOSs, and available intelligence models in predicting the solubility of mixtures or/and pure hydrocarbon gases in pure water and aqueous electrolyte systems up to high-pressure and high-temperature conditions having average absolute relative error values of 10.65% and 12.02%, respectively, along with determination coefficient of 0.9999. Among the EOSs, VPT, SRK, and PR were ranked in terms of good predictions, respectively. Also, the two mathematical correlations developed with GP and GMDH had satisfactory results and can provide accurate and quick estimates. According to sensitivity analysis, the temperature and pressure had the greatest effect on hydrocarbon gases' solubility. Additionally, increasing the ionic strength of the solution and the pseudo-critical temperature of the gas mixture decreases the solubilities of hydrocarbon gases in aqueous electrolyte systems. Eventually, the Leverage approach has revealed the validity of the hydrocarbon solubility databank and the high credit of the AdaBoost-SVR models in estimating the solubilities of hydrocarbon gases in aqueous solutions.
Topics: Electrolytes; Gases; Hydrocarbons; Machine Learning; Salts; Solubility; Water
PubMed: 36056055
DOI: 10.1038/s41598-022-18983-2 -
Cold Spring Harbor Perspectives in... Dec 2011According to the "generic view" of protein aggregation, the ability to self-assemble into stable and highly organized structures such as amyloid fibrils is not an... (Review)
Review
According to the "generic view" of protein aggregation, the ability to self-assemble into stable and highly organized structures such as amyloid fibrils is not an unusual feature exhibited by a small group of peptides and proteins with special sequence or structural properties, but rather a property shared by most proteins. At the same time, through a wide variety of techniques, many of which were originally devised for applications in other disciplines, it has also been established that the maintenance of proteins in a soluble state is a fundamental aspect of protein homeostasis. Taken together, these advances offer a unified framework for understanding the molecular basis of protein aggregation and for the rational development of therapeutic strategies based on the biological and chemical regulation of protein solubility.
Topics: Homeostasis; Humans; Kinetics; Protein Folding; Proteostasis Deficiencies; Solubility; Thermodynamics
PubMed: 21825020
DOI: 10.1101/cshperspect.a010454