14,999 results match your criteria solubility dissolution

Biorelevant dissolution testing and physiologically based absorption modeling to predict in vivo performance of supersaturating drug delivery systems.

Int J Pharm 2021 Jul 28:120958. Epub 2021 Jul 28.

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Mohali, Punjab, India-160062. Electronic address:

Supersaturating drug delivery systems (SDDS) enhance the oral absorption of poorly water-soluble drugs by achieving a supersaturated state in the gastrointestinal tract. The maintenance of a supersaturated state is decided by the complex interplay among inherent properties of drug, excipients and physiological conditions of gastrointestinal tract. The biopharmaceutical advantage through SDDS can be mechanistically investigated by coupling biopredictive dissolution testing with physiologically based absorption modeling (PBAM). Read More

View Article and Full-Text PDF

Coordination and Thermophysical Properties of Transition Metal Chlorocomplexes in LiCl-KCl Eutectic.

J Phys Chem B 2021 Jul 30. Epub 2021 Jul 30.

Department of Chemical and Materials Engineering, University of Nevada-Reno, Reno, Nevada 89557, United States.

Eutectic LiCl-KCl molten salt is often used in molten salt reactors as the primary coolant due to its high thermal capacity and high solubility of fission products. Thermophysical properties, such as density, heat capacity, and viscosity, are important parameters for engineering applications of molten salts but may be significantly influenced by metal solutes from corrosion of metallic structural materials. The behavior of the LiCl-KCl eutectic composition is well researched, yet the effects on these properties due to chlorocomplex formation from metals dissolved in the salt are less well known. Read More

View Article and Full-Text PDF

Colloidal and vesicular delivery system for herbal bioactive constituents.

Daru 2021 Jul 29. Epub 2021 Jul 29.

Columbia Institute of Pharmacy Raipur, Raipur, Chhattisgarh, India.

Objectives: The main objective of the present review is to explore and examine the effectiveness of currently developed novel techniques to resolve the issues which are associated with the herbal constituents/extract.

Methods: A systematic thorough search and collection of reviewed information from Science direct, PubMed and Google Scholar databases based on various sets of key phrases have been performed. All the findings from these data have been studied and briefed based on their relevant and irrelevant information. Read More

View Article and Full-Text PDF

Appraisal of Felodipine nanocrystals for solubility enhancement and pharmacodynamic parameters on cadmium chloride induced hypertension in rats.

Curr Drug Deliv 2021 Jul 28. Epub 2021 Jul 28.

Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow, U.P., India.

Background And Objective: Felodipine (FDP), an antihypertensive drug possesses low water solubility and extensive first-pass metabolism leading to poor bioavailability. This impelled us to improve its solubility, bioavailability, and pharmacodynamic properties through the nanocrystal (NC) approach.

Methods: FDP-NC were prepared with Poloxamer F125 (PXM) by the antisolvent precipitation method. Read More

View Article and Full-Text PDF

Effect Of Surfactant Chain Length On Emulsification Dynamics Of Self Emulsifying Formulation Of Poorly Soluble Drug.

Curr Drug Deliv 2021 Jul 26. Epub 2021 Jul 26.

Department of Pharmaceutical Sciences, Mohanlal Sukhadia University, Udaipur, Rajasthan, India.

Aim: In this work the aim was to study the chain length of surfactant on the self emulsifying system of a poorly soluble drug, aceclofenac. The selection of almond oil as a lipid vehicle was done on basis of solubility and compatibility of the vehicle with the drug.

Methods: The effect of varying chain length of different surfactants of Tween series namely Tween 20, Tween 40, Tween 60 and Tween 80 was evaluated on self emulsifying efficiency by constructing pseudoternary diagrams. Read More

View Article and Full-Text PDF

Systematic thermodynamic analysis of apremilast polymorphs via solubility measurement with modeling: Mechanism evaluation through molecular simulation.

Eur J Pharm Sci 2021 Jul 25;165:105958. Epub 2021 Jul 25.

State Key Laboratory of Chemical Engineering, East China University of Science and Technology, Shanghai 200237, China.

The polymorphism of apremilast has been investigated. Two polymorphs have been identified and characterized by differential scanning calorimeter, fourier transform infrared spectroscopy, and powder X-ray diffractometer. Solubilities of apremilast forms B and E in three binary solvents of methanol-water, acetonitrile-water, and acetonitrile-methanol have been measured using the static method at a temperature ranging from 288. Read More

View Article and Full-Text PDF

Rapidly dissolving microneedle patch of amphotericin B for intracorneal fungal infections.

Drug Deliv Transl Res 2021 Jul 23. Epub 2021 Jul 23.

School of Pharmacy, Medical Biology Centre, Queen's University Belfast, 97 Lisburn Road, Belfast, BT9 7BL, Northern Ireland, UK.

Chronic fungal infection of the cornea could lead to blindness if not treated properly. Topical amphotericin B (AMP-B) is considered the first treatment of choice for ocular fungal infection. However, factors related to its poor solubility and penetration through intact cornea lead to poor bioavailability. Read More

View Article and Full-Text PDF

The dissolution of fluorapatite by phosphate-solubilizing fungi: a balance between enhanced phosphorous supply and fluorine toxicity.

Environ Sci Pollut Res Int 2021 Jul 23. Epub 2021 Jul 23.

College of Resources and Environmental Sciences, Nanjing Agricultural University, Nanjing, 210095, Jiangsu, China.

Fluorapatite (FAp) is the largest phosphorous (P) reservoir on Earth. However, due to its low solubility, dissolved P is severely deficient in the pedosphere. Fungi play a significant role in P dissolution via excretion of organic acids, and in this regard, it is important to understand their impact on P cycling. Read More

View Article and Full-Text PDF

A tool for identifying green solvents for printed electronics.

Nat Commun 2021 Jul 23;12(1):4510. Epub 2021 Jul 23.

The Organic Photonics and Electronics Group, Department of Physics, Umeå University, Umeå, Sweden.

The emerging field of printed electronics uses large amounts of printing and coating solvents during fabrication, which commonly are deposited and evaporated within spaces available to workers. It is in this context unfortunate that many of the currently employed solvents are non-desirable from health, safety, or environmental perspectives. Here, we address this issue through the development of a tool for the straightforward identification of functional and "green" replacement solvents. Read More

View Article and Full-Text PDF

Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments.

Polymers (Basel) 2021 Jul 11;13(14). Epub 2021 Jul 11.

Institut des Sciences Analytiques et de Physico-Chimie pour l'Environnement et les Matériaux, University Pau & Pays Adour, 64000 Pau, France.

Olmesartan medoxomil (OLM) is one of the prominent antihypertensive drug that suffers from low aqueous solubility and dissolution rate leading to its low bioavailability. To improve the oral bioavailability of OLM, a delivery system based on ethylcellulose (EC, a biobased polymer) nanosponges (NSs) was developed and evaluated for cytotoxicity against the A549 lung cell lines and antihypertensive potential in a rat model. Four OLM-loaded NSs (ONS1-ONS4) were prepared and fully evaluated in terms of physicochemical properties. Read More

View Article and Full-Text PDF

Challenges and Progress in Nonsteroidal Anti-Inflammatory Drugs Co-Crystal Development.

Molecules 2021 Jul 9;26(14). Epub 2021 Jul 9.

Department of Pharmacochemistry, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, Indonesia.

Co-crystal innovation is an opportunity in drug development for both scientists and industry. In line with the "green pharmacy" concept for obtaining safer methods and advanced pharmaceutical products, co-crystallization is one of the most promising approaches to find novel patent drugs, including non-steroidal anti-inflammatory drugs (NSAID). This kind of multi-component system improves previously poor physicochemical and mechanical properties through non-covalent interactions. Read More

View Article and Full-Text PDF

Solvent Screening for Solubility Enhancement of Theophylline in Neat, Binary and Ternary NADES Solvents: New Measurements and Ensemble Machine Learning.

Int J Mol Sci 2021 Jul 8;22(14). Epub 2021 Jul 8.

Department of Physical Chemistry, Faculty of Pharmacy, Collegium Medicum of Bydgoszcz, Nicolaus Copernicus University in Toruń, Kurpińskiego 5, 85-950 Bydgoszcz, Poland.

Theophylline, a typical representative of active pharmaceutical ingredients, was selected to study the characteristics of experimental and theoretical solubility measured at 25 °C in a broad range of solvents, including neat, binary mixtures and ternary natural deep eutectics (NADES) prepared with choline chloride, polyols and water. There was a strong synergistic effect of organic solvents mixed with water, and among the experimentally studied binary systems, the one containing DMSO with water in unimolar proportions was found to be the most effective in theophylline dissolution. Likewise, for NADES, the addition of water (0. Read More

View Article and Full-Text PDF

A Novel Integrated Workflow for Isolation Solvent Selection Using Prediction and Modeling.

Org Process Res Dev 2021 May 5;25(5):1143-1159. Epub 2021 May 5.

EPSRC Centre for Innovative Manufacturing in Continuous Manufacturing and Crystallisation, University of Strathclyde, 99 George Street, Glasgow G1 1RD, U.K.

A predictive tool was developed to aid process design and to rationally select optimal solvents for isolation of active pharmaceutical ingredients. The objective was to minimize the experimental work required to design a purification process by (i) starting from a rationally selected crystallization solvent based on maximizing yield and minimizing solvent consumption (with the constraint of maintaining a suspension density which allows crystal suspension); (ii) for the crystallization solvent identified from step 1, a list of potential isolation solvents (selected based on a series of constraints) is ranked, based on thermodynamic consideration of yield and predicted purity using a mass balance model; and (iii) the most promising of the predicted combinations is verified experimentally, and the process conditions are adjusted to maximize impurity removal and maximize yield, taking into account mass transport and kinetic considerations. Here, we present a solvent selection workflow based on logical solvent ranking supported by solubility predictions, coupled with digital tools to transfer material property information between operations to predict the optimal purification strategy. Read More

View Article and Full-Text PDF

The Effect of the Molecular Weight of Polyvinylpyrrolidone and the Model Drug on Laser-Induced In Situ Amorphization.

Molecules 2021 Jul 1;26(13). Epub 2021 Jul 1.

Department of Pharmacy, University of Copenhagen, 2100 Copenhagen, Denmark.

Laser radiation has been shown to be a promising approach for in situ amorphization, i.e., drug amorphization inside the final dosage form. Read More

View Article and Full-Text PDF

Piroxicam loaded polymer hybrid microspheres based tablets with modified release kinetics: Development, characterization and in vivo evaluation.

Pak J Pharm Sci 2021 Jan;34(1(Supplementary)):327-335

Institute of Pharmaceutical Sciences, Kings College London UK, London, UK.

Piroxicam (PC) is a non-steroidal anti-inflammatory drug characterized by poor aqueous solubility and reported to cause and impart crucial GIT irritation, bleeding, peptic and duodenal ulcer. Engineering of PC loaded microcapsules and its surface modification using different polymers has become the popular approach to address the said issues. The purpose of the study was to develop new PC loaded gastro-protective polymer hybrid microspheres (PHM) with subsequent conversion to tablet dosage form having modified dissolution rate and improved bioavailability. Read More

View Article and Full-Text PDF
January 2021

Impact of simulated lung fluid components on the solubility of inhaled drugs and predicted in vivo performance.

Int J Pharm 2021 Jul 16;606:120893. Epub 2021 Jul 16.

Research Center Pharmaceutical Engineering GmbH, Inffeldgasse 13, Graz 8010, Austria; Center for Medical Research, Medical University of Graz, Stiftingtalstraße 24, Graz 8010, Austria. Electronic address:

Orally inhaled products (OIPs) are gaining increased attention, as pulmonary delivery is a preferred route for the treatment of various diseases. Yet, the field of inhalation biopharmaceutics is still in development phase. For a successful correlation between various in vitro data obtained during formulation characterization and in vivo performance, it is necessary to understand the impact of parameters such as solubility and dissolution of drugs. Read More

View Article and Full-Text PDF

Formulation and Evaluation of Mucilage-Based Nanoparticles for Effective Delivery of Ezetimibe.

Int J Nanomedicine 2021 5;16:4579-4596. Epub 2021 Jul 5.

Nanobiotechnology Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Introduction: The aim of current study was to prepare mucilage (LUM) based nanoparticles, capable of encapsulating hydrophobic drug ezetimibe as nanocarriers.

Methods: Solvent evaporation and nanoprecipitation techniques were used to develop nanoparticles by encapsulating ezetimibe in the articulated matrix of polysaccharide fractions. Developed nanoparticles were characterized to determine the particle size, zeta potential, polydispersibility index (PDI), and entrapment efficiency (EE). Read More

View Article and Full-Text PDF

Deep carbon cycle constrained by carbonate solubility.

Nat Commun 2021 Jul 14;12(1):4311. Epub 2021 Jul 14.

Asian School of the Environment, Nanyang Technological University, 50 Nanyang Avenue, Singapore, 639798, Singapore.

Earth's deep carbon cycle affects atmospheric CO, climate, and habitability. Owing to the extreme solubility of CaCO, aqueous fluids released from the subducting slab could extract all carbon from the slab. However, recycling efficiency is estimated at only around 40%. Read More

View Article and Full-Text PDF

Emergent Fluorous Molecules and Their Uses in Molecular Imaging.

Acc Chem Res 2021 Jul 14. Epub 2021 Jul 14.

ConspectusThis Account summarizes recent advances in the chemistry of fluorocarbon nanoemulsion (FC NE) functionalization. We describe new families of fluorous molecules, such as chelators, fluorophores, and peptides, that are soluble in FC oils. These materials have helped transform the field of molecular imaging by enabling sensitive and cell-specific imaging using magnetic resonance imaging (MRI), positron emission tomography (PET), and fluorescence detection. Read More

View Article and Full-Text PDF

Novel amorphous solid dispersion based on natural deep eutectic solvent for enhancing delivery of anti-tumor RA-XII by oral administration in rats.

Eur J Pharm Sci 2021 Jul 10:105931. Epub 2021 Jul 10.

Department of TCMs Pharmaceuticals, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198, People's Republic of China. Electronic address:

At present, oral chemotherapy showing the advantages of non-invasiveness, convenience, and high patient compliance, is gradually replacing traditional intravenous chemotherapy to treat patients with cancer. RA-XII, a unique natural cyclopeptide, exhibits various biological activities, such as anti-tumor, anti-angiogenic, and anti-metastatic activities. Designing an orally available formulation of RA-XII is of great importance in the development of clinically useful anticancer agents. Read More

View Article and Full-Text PDF

Impact of altered hydrophobicity and reduced agglomeration on dissolution of micronized poorly water-soluble drug powders after dry coating.

Int J Pharm 2021 Jul 10;606:120853. Epub 2021 Jul 10.

New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, NJ 07102, USA. Electronic address:

The impact of dry coating with hydrophobic or hydrophilic nano-silica at 25-100% surface area coverage on dissolution of micronized poorly water-soluble drugs was investigated by examining their agglomeration and surface hydrophobicity. Ibuprofen (20 µm and 10 µm) and griseofulvin (10 µm) were selected having differing solubility, hydrophobicity, and surface morphology. Characterization involved particle agglomeration via two dry dispersion methods, drug dissolution using the USP IV method, cohesion reduction through shear testing, and powder wettability via the modified Washburn method. Read More

View Article and Full-Text PDF

Potential and Comparative Tablet Disintegrant Properties of Pectin Obtained from Five Okra Genotypes in Ghana.

Scientifica (Cairo) 2021 19;2021:2902335. Epub 2021 Jun 19.

Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.

Okra pectin has been studied as a potential excipient in tablet formulations for pharmaceutical industries. Okra is widely grown and available in Ghana and other parts of the world. The prospective use of pectin from okra genotypes grown in Ghana as tablet disintegrants has not been reported. Read More

View Article and Full-Text PDF

Development of a Spontaneous Emulsifying Technique Using Porous Microparticles withWater-soluble Polymers.

J Oleo Sci 2021 Jul 9. Epub 2021 Jul 9.

Graduate School of Science & Technology for Innovation, Yamaguchi University.

A novel spontaneous emulsification method using porous polymer particles was investigated for the facile preparation of emulsions without mechanical manipulation. Porous water-soluble polymer particles prepared by spray freeze-drying could absorb soybean oil via capillary action. When the particles were added to water, emulsification proceeded rapidly with the dissolution of the polymer. Read More

View Article and Full-Text PDF

A hydrothermal apparatus for x-ray absorption spectroscopy of hydrothermal fluids at DESY.

Rev Sci Instrum 2021 Jun;92(6):063903

Université Grenoble Alpes, CNRS, Grenoble INP, Institut Néel, 38000 Grenoble, France.

We present a new autoclave that enables in situ characterization of hydrothermal fluids at high pressures and high temperatures at synchrotron x-ray radiation sources. The autoclave has been specifically designed to enable x-ray absorption spectroscopy in fluids with applications to mineral solubility and element speciation analysis in hydrothermal fluids in complex compositions. However, other applications, such as Raman spectroscopy, in high-pressure fluids are also possible with the autoclave. Read More

View Article and Full-Text PDF

Computational Approach for Rapidly Predicting Temperature-Dependent Polymer Solubilities Using Molecular-Scale Models.

ChemSusChem 2021 Jul 8. Epub 2021 Jul 8.

Department of Chemical and Biological Engineering, University of Wisconsin-Madison, Madison, WI, 53706, USA.

One promising approach to recycle multicomponent plastic waste (e. g., multilayer plastic films) is selective dissolution. Read More

View Article and Full-Text PDF

Self-assembled micelles enhance the oral delivery of curcumin for the management of alcohol-induced tissue injury.

Pharm Dev Technol 2021 Jul 13:1-10. Epub 2021 Jul 13.

School of Pharmacy, Institute of Materia Medica, Chengdu Medical College, Chengdu, China.

Curcumin (CUR) shows great potential in the management of alcohol-use disorders. However, the hydrophobicity and poor oral bioavailability result in the limited therapeutic efficacy of CUR against alcohol-induced tissue injury. Here, self-assembled Soluplus® micelles (Ms) were developed for the enhanced oral delivery of CUR. Read More

View Article and Full-Text PDF

A mechanistic study of drug mass transport from supersaturated solutions across PAMPA membranes.

J Pharm Sci 2021 Jul 5. Epub 2021 Jul 5.

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, West Lafayette, Indiana, USA. Electronic address:

There is an increasing shift from dissolution testing to dissolution-permeation testing of formulations during formulation development and this has led to rise in the application of permeability measurements using parallel artificial membrane permeability assay (PAMPA) membranes. However, there is a lack of thorough analysis of the impact of variabilities in the PAMPA setup on the mass flow rate outcomes, particularly for complex solubility-enabling formulations. In this study, we investigated the impact of amorphous drug-rich nanodroplets, formed in supersaturated solutions by liquid-liquid phase separation, on membrane transport by measuring mass flow rate across PAMPA membranes. Read More

View Article and Full-Text PDF

A new gaseous cavitation model in a tilting-pad journal bearing.

Sci Prog 2021 Jul-Sep;104(3):368504211029431

Department of Energy and Power Engineering, Tsinghua University, Beijing, P.R. China.

With the higher rotational speeds and loads in bearings, the gaseous cavitation becomes more and cannot be ignorable in the bearing designs. However, there is no enough research in non-equilibrium gaseous cavitation model. This paper builds a new gaseous cavitation model based on the Bunsen solubility and bubble dynamics. Read More

View Article and Full-Text PDF

Does Anzer Propolis Have a Protective Effect on Rabbit Spinal Cord Ischemia/Reperfusion Injury?

Braz J Cardiovasc Surg 2021 Jul 7. Epub 2021 Jul 7.

Department of Cardiovascular Surgery, Afyonkarahisar Health Sciences University, Faculty of Medicine, Afyonkarahisar, Turkey.

Introduction: In this study, Anzer propolis, which can only be obtained from the Eastern Black Sea region in Turkey, is studied for its effect on spinal cord ischemia/reperfusion injury.

Methods: A total of 12 healthy male New Zealand White rabbits with an average weight of 3.0 to 3. Read More

View Article and Full-Text PDF

Classes of organic pigments meet tentative PSLT criteria and lack toxicity in short-term inhalation studies.

Regul Toxicol Pharmacol 2021 Aug 2;124:104988. Epub 2021 Jul 2.

BASF SE, Dept. Experimental Toxicology and Ecology, Dept. Material Physics, 67056, Ludwigshafen, Germany. Electronic address:

Here, we present a non-animal testing battery to identify PSLT (poorly soluble, low toxicity) substances based on their solubility in phagolysosomal lung fluid simulant, surface reactivity and effects on alveolar macrophages in vitro. This is exemplified by eleven organic pigments belonging to five chemical classes that cover a significant share of the European market. Three of the pigments were tested as both, nanoform and non-nanoform. Read More

View Article and Full-Text PDF