23,986 results match your criteria vitro solubility

Calcium Solubilization Ability and Anti-Inflammatory Effects of Hydrolyzed Casein.

Food Sci Anim Resour 2021 Jul 1;41(4):687-700. Epub 2021 Jul 1.

Department of Animal Resources Science, Dankook University, Cheonan 31116, Korea.

This study performed to evaluate the applicability of functional dairy food materials by comparing the calcium solubilization ability and anti-inflammatory effects of hydrolyzed casein protein. Commercial enzyme (Alcalase; Neutrase; Protamex; Flavourzyme) was added to the 10% casein solution to prepare the casein hydrolysates. Samples obtained every hour [1:200 (w/v)]. Read More

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25CN-NBOH: A selective agonist for in vitro and in vivo investigations of the serotonin 2A receptor.

ChemMedChem 2021 Jul 20. Epub 2021 Jul 20.

Kobenhavns Universitet, Department of drug design and Pharmacology, Universitetsparken 2, Danmark, 2100, Copenhagen, DENMARK.

4-(2-((2-hydroxybenzyl)amino)ethyl)-2,5-dimethoxybenzonitrile (25CN-NBOH) was first reported as a potent and selective serotonin 2A receptor (5-HT 2A R) agonist in 2014, and it has since found extensive use as a pharmacological tool in a variety of in vitro, ex vivo and in vivo studies. 25CN-NBOH is readily available from a synthetic perspective using standard chemical transformations, and displays favorable physiochemical properties in terms of stability and solubility. Due to its superior selectivity for 5-HT 2A R, 25CN-NBOH has been used to investigate the effects of selective 5-HT 2A R activation in vivo, and has thus become an important pharmacological tool for the exploration of 5-HT 2A R signaling in a range of animal models. Read More

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Preparation, Optimization and Evaluation of Chitosan-Based Avanafil Nanocomplex Utilizing Antioxidants for Enhanced Neuroprotective Effect on PC12 Cells.

Gels 2021 Jul 16;7(3). Epub 2021 Jul 16.

Department of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY 11201, USA.

(1) Introduction: in recent decades, interdisciplinary research on the utilization of natural products as "active moiety carriers" was focused on due to their superior safety profile, biodegradability, biocompatibility and the ability for sustained or controlled release activity. The nano-based neuroprotective strategy is explored as an imperative treatment for diabetic neuropathy (DN). Avanafil (AV), that selectively inhibits the degradation of cGMP-specific phosphodiesterase, thereby increasing the levels of cGMP, makes a decisive mediator for cytoprotection. Read More

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ROS-responsive biomimetic nanoparticles for potential application in targeted anti-atherosclerosis.

Regen Biomater 2021 Aug 18;8(4):rbab033. Epub 2021 Jul 18.

Key Laboratory for Biorheological Science and Technology of Ministry of Education, State and Local Joint Engineering Laboratory for Vascular Implants, Bioengineering College of Chongqing University, Chongqing 400030, China.

The development of nanomedicines provides new opportunities for the treatment of atherosclerosis (AS) due to their great advantages such as the improved drug solubility, enhanced bioavailability and reduced side effects. Despite these advantages, nanomedicines are still facing some challenges. The problems remain in the short circulation life, lack of specific targeting and poor drug release controllability. Read More

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Exosomes synergized with [email protected] enhance their immunity against hepatocellular carcinoma via promoting M1 macrophages polarization.

Int Immunopharmacol 2021 Jul 18;99:107960. Epub 2021 Jul 18.

Guilin Medical University, Guilin, Guangxi, People's Republic of China; Affiliated Hospital of Guilin Medical University, Guilin Medical University, Guilin, Guangxi, People's Republic of China. Electronic address:

Background: Hepatocellular carcinoma (HCC) is easy to relapse after resection for its lack of anti-tumor immunity due to pro-tumorigenesis by promoting M2 type macrophage polarization. Recent studies have shown that exosomes are closely related to the occurrence and development of HCC. Antigenic exosomes from HCC are able to polarize into alternatively activated macrophages M2, but do not stimulate M1 macrophages polarization. Read More

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Acid-base combination principles for preparation of anti-acne dissolving microneedles loaded with azelaic acid and matrine.

Eur J Pharm Sci 2021 Jul 17;165:105935. Epub 2021 Jul 17.

Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry of Chinese Academy of Sciences, Beijing 100190, China; University of Chinese Academy of Sciences, Beijing 100049, China; Beijing CAS Microneedle Technology Ltd, Beijing 102609, China. Electronic address:

To overcome the poor solubility, skin irritation, and low permeability of azelaic acid (AZA) existed on the marketed formulations, a co-drug principle via matrine (MAT) was adopted to prepare anti-acne dissolving microneedles (DMNs). The formula was optimized according to the solubility and antibacterial activity of novel ionic salt. The results indicated solubilization of AZA could be achieved at a molar ratio between AZA and MAT was 1:1. Read More

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Improved oral bioavailability, cellular uptake, and cytotoxic activity of zingerone via nano-micelles drug delivery system.

J Microencapsul 2021 Jul 26:1-11. Epub 2021 Jul 26.

Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, People's Republic of China.

Herein, a nano-micelle drug delivery system was developed to orally improved zingerone's bioavailability and its antitumor effect. Indeed, zingerone-loaded d-α-tocopheryl polyethylene glycol succinate micelles (ZTMs) were effectively prepared, characterised and assessed. The ZTMs had diameter, polydispersity index, and zeta potential of 50. Read More

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Exploring the potential of functional polymer-lipid hybrid nanoparticles for enhanced oral delivery of paclitaxel.

Asian J Pharm Sci 2021 May 2;16(3):387-395. Epub 2021 Mar 2.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.

Most biopharmaceutics classification system (BCS) class IV drugs, with poor solubility and inferior permeability, are also substrates of P-glycoprotein (P-gp) and cytochrome P450 (CYP450), leading to their low oral bioavailability. The objective of this study is to explore the potential of using functional polymer-lipid hybrid nanoparticles (PLHNs) to enhance the oral absorption of BCS IV drugs. In this paper, taking paclitaxel (PTX) as a drug model, PTX-loaded PLHNs were prepared by a self-assembly method. Read More

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approach in the development of inhaled drug products: Nanocrystal-based formulations with budesonide as a model drug.

Asian J Pharm Sci 2021 May 5;16(3):350-362. Epub 2021 Jan 5.

Department of Pharmaceutical Technology and Cosmetology, University of Belgrade-Faculty of Pharmacy, Vojvode Stepe 450, 11221 Belgrade, Serbia.

This study aims to understand the absorption patterns of three different kinds of inhaled formulations modeling using budesonide (BUD) as a model drug. The formulations investigated in this study are: (i) commercially available micronized BUD mixed with lactose (BUD-PT), (ii) BUD nanocrystal suspension (BUD-NC), (iii) BUD nanocrystals embedded hyaluronic acid microparticles (BUD-NEM). The deposition patterns of the three inhaled formulations in the rats' lungs were determined and predicted, which were used as inputs in GastroPlus™ software to predict drug absorption following aerosolization of the tested formulations. Read More

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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

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January 2021

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

Int J Pharm 2021 Jul 15:120893. Epub 2021 Jul 15.

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

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GSK137, a potent small molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice.

J Biol Chem 2021 Jul 15:100928. Epub 2021 Jul 15.

Leicester Cancer Research Centre and Ernest and Helen Scott Haematological Research Unit, University of Leicester, Leicester LE1 7HB, UK. Electronic address:

BCL6 is a zinc finger transcriptional repressor possessing a BTB-POZ domain, which is required for homodimerization and association with co-repressors. BCL6 has multiple roles in normal immunity, autoimmunity and some types of lymphoma. Mice bearing disrupted BCL6 loci demonstrate suppressed high affinity antibody responses to T-dependent antigens. Read More

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Ultra-long Acting Prodrug of Dolutegravir and Delivery System - Physicochemical, Pharmacokinetic and Formulation Characterizations.

Int J Pharm 2021 Jul 13:120889. Epub 2021 Jul 13.

Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, Texas A&M University, College Station, TX 77843, USA. Electronic address:

The focus of present work was to characterize ultra-long acting prodrug of dolutegravir (DTG) and develop biodegradable microparticle formulation. Palmitic acid (PA) conjugated prodrug of DTG was prepared by esterification of hydroxyl group of DTG with the carboxyl group of PA. Physicochemical properties of the prodrug was characterize by MS, NMR, FTIR, SEM, DSC, NIR-CI, pH-solubility, and solid and liquid pH-stability. Read More

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Bioavailability of iron from novel hydrogen reduced iron powders: Studies in Caco-2 cells and rat model.

J Food Sci 2021 Jul 15. Epub 2021 Jul 15.

Jamai-Osmania, ICMR-National Institute of Nutrition, Telangana, India.

The bioavailability of iron from elemental iron powders, including hydrogen reduced iron powder (HRIP), is influenced by particle size and surface area. In the present study, we investigated the solubility, bioaccessibility, and bioavailability of iron from novel HRIPs (particle size ≤25 and 38 µm generated at low [LT] and high [HT] temperature), with porous morphology and high surface area, in intestinal Caco-2 cells and in rat models. The acceptability of fortified wheat flour was tested in human volunteers. Read More

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Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.

ACS Med Chem Lett 2021 Jul 24;12(7):1077-1085. Epub 2021 Jun 24.

Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, United Kingdom.

Synthetic endoperoxide antimalarials, such as 1,2,4-trioxolanes and 1,2,4,5-tetraoxanes, are promising successors for current front-line antimalarials, semisynthetic artemisinin derivatives. However, limited solubility of second-generation analogues in biological-relevant media represents a barrier in clinical development. We present methodology for the synthesis of nonlinear analogues of second-generation tetraoxane antimalarials E209 and N205 to investigate reduced molecular symmetry on in vitro antimalarial activity and physicochemical properties. Read More

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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

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Stent conditioned media for in vitro evaluation of hydrophobic stent coatings.

Toxicol In Vitro 2021 Jul 13;76:105212. Epub 2021 Jul 13.

Department of Chemical Sciences, Bernal Institute, University of Limerick, Limerick, Ireland. Electronic address:

In vitro cell studies of hydrophobic drugs face difficulties associated with their low aqueous solubility. To study poorly soluble drugs in bio-relevant media, solubilizing agents are frequently used to make stock solutions before final reconstitution in media. This results in drug concentrations that are not representative of in vivo conditions and may pose adverse effects on cells' biological functions. Read More

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Improving the color and functional properties of seabuckthorn seed protein with phytase treatment combined with alkaline solubilization and isoelectric precipitation.

J Sci Food Agric 2021 Jul 15. Epub 2021 Jul 15.

School of Chemical Sciences, The University of Auckland, Auckland, New Zealand.

Background: Reducing anti-nutritional factors like phytates in seed protein products requires an ongoing effort. This study was the first to investigate the phytic acid content in seabuckthorn seed protein (SSP) and its reduction by an exogenous phytase during protein isolation from seabuckthorn seed meal through the common alkaline solubilization-isoelectric precipitation process.

Results: The additional phytase treatment could reduce the content of phytic acid from 22. Read More

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Docetaxel-loaded exosomes for targeting non-small cell lung cancer: preparation and evaluation and .

Drug Deliv 2021 Dec;28(1):1510-1523

School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou, China.

Non-small cell lung cancer (NSCLC) is a highly lethal disease and the majority of NSCLC patients are desperate for therapies that can effectively target their cancer and ultimately improve their overall survival. Docetaxel (DTX) represents the first-line of the antitumor agent that is used to treat NSCLC; however, it has poor solubility in water and unsatisfactory encapsulation efficiency. In our study, exosomes were isolated from A549 cancer cells by ultracentrifugation and then characterized using transmission electron microscopy (TEM), nanoparticle tracking analysis (NTA), and Western blot (WB). Read More

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December 2021

Pea protein isolate characteristics modulate functional properties of pea protein-cranberry polyphenol particles.

Food Sci Nutr 2021 Jul 24;9(7):3740-3751. Epub 2021 May 24.

Plants for Human Health Institute North Carolina State University Kannapolis NC USA.

Plant polyphenols have a natural binding affinity for proteins, and their interaction can be exploited to form diverse aggregate particles. Protein-polyphenol particles utilized as food ingredients allow consumers to incorporate more health-benefiting plant bioactives into their diets. The functional properties of the protein-polyphenol particles can be influenced by many factors, including complexation conditions and starting material properties. Read More

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Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.

J Med Chem 2021 Jul 14. Epub 2021 Jul 14.

WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, Thomas Graham Building, 259 Cathedral Street, Glasgow G1 1XL, U.K.

Herein, a series of 2,3-dihydrobenzofurans have been developed as highly potent bromo and extra-terminal domain (BET) inhibitors with 1000-fold selectivity for the second bromodomain (BD2) over the first bromodomain (BD1). Investment in the development of two orthogonal synthetic routes delivered inhibitors that were potent and selective but had raised clearance and suboptimal solubility. Insertion of a quaternary center into the 2,3-dihydrobenzofuran core blocked a key site of metabolism and improved the solubility. Read More

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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

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Development of Apigenin-Loaded Niosomes Using Ecological Probe Sonication Technique for enhanced oral delivery: Application of Box-Behnken Design.

Md Ali Mujtaba

Curr Pharm Biotechnol 2021 Jul 9. Epub 2021 Jul 9.

Department of Pharmaceutics, Faculty of Pharmacy, Northern Border University, Saudi Arabia.

Background: Apigenin (APG), a natural bioactive flavonoid, has multiple pharmacological effects. However, its poor aqueous solubility hinders its clinical benefits.

Objective And Methods: The work aimed to develop novel apigenin-loaded niosomes (APG-NIO) with ecological probe sonication techniques. Read More

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α-amyrin-loaded nanocapsules produce selective cytotoxic activity in leukemic cells.

Biomed Pharmacother 2021 Jul 8;139:111656. Epub 2021 May 8.

Laboratory of Pharmaceutical Technology (LTF), Faculty of Pharmacy, Food and Nutrition, Universidade Federal do Mato Grosso do Sul, Av. Costa e Silva, Pioneiros, Campo Grande, MS CEP 79070-900, Brazil. Electronic address:

Introduction: Amyrins are triterpenes that have attractive pharmacological potential; however, their low water solubility and erratic stomach absorption hinders their use as a drug. The aim of this paper was to develop a novel α-amyrin-loaded nanocapsule for intestinal delivery and evaluate, preliminarily, its cytotoxic ability against leukemic cells.

Material And Methods: Five nanocapsule formulations were designed by the solvent displacement-evaporation method. Read More

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Biodegradable polymers-based nanoparticles to enhance the antifungal efficacy of fluconazole against Candida albicans.

Curr Pharm Biotechnol 2021 Jul 7. Epub 2021 Jul 7.

Pharmaceutics Department, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.

Background: Fluconazole (FLZ), a potent antifungal medication, is characterized by poor water solubility that reduced its antifungal efficacy.

Objective: This study aimed to prepare FLZ-loaded polymeric nanoparticles (NPs) by using different polymers and techniques as a mean of enhancing the antifungal activity of FLZ.

Methods: NP, NP, and NP were prepared by the double emulsion/solvent evaporation method using PLGA, PCL, and PLA, respectively. Read More

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Formulation development of anti-stress compressed lozenges using a fractional factorial Latin cube design and ANOVA approach.

Ceska Slov Farm 2021 ;70(2):66-78

The aim of this work was to develop anti-stress compressed lozenges containing 100 mg of glycine and 250 mg of magnesium citrate obtained by the direct compression method. To choose optimal excipient composition providing the sufficient pharmaco-technical properties of the tablet blend, mechanical strength of tablets and non-disintegrating, slow-dissolving behavior of compressed lozenges during sucking, 27 experimental formulations according to fractional factorial Latin cube design were prepared and tested. The excipients used in the study were: Mannogem® EZ, Cellactose® 80 and GalenIQ 721 (fillers); Plasdone S-630, Kollidon® 90 F and Avicel® PH-101 (dry binders); Metolose® 90SH-4000SR and guar gum (gel-forming binders); PRUV®, Neusilin® US2, and Compritol® 888 CG ATO (antifriction excipients). Read More

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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

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Overcoming Tumor Hypoxia through Multiple Pathways Using an All-in-One Polymeric Therapeutic Agent to Enhance Synergistic Cancer Photo/Chemotherapy Effects.

Bioconjug Chem 2021 Jul 8. Epub 2021 Jul 8.

State Key Laboratory of Organic Electronics and Information Displays & Jiangsu Key Laboratory for Biosensors, Institute of Advanced Materials & Institute of Flexible Electronics (Future Technology), Nanjing University of Posts and Telecommunications, 9 Wenyuan Road, Nanjing, 210023, China.

Hypoxia is a significant characteristic of tumors, which causes aggressive tumor growth and strong therapy resistance. Inspired by the improved therapeutic efficacy of synergistic treatment, herein, an all-in-one polymeric therapeutic agent was developed, which could overcome tumor hypoxia through multiple pathways. Multiple therapeutic agents were incorporated into the polymer, including the singlet oxygen (O) carrier unit to store cytotoxic reactive oxygen species, the photosensitized and photothermal unit to trigger the capture and release of O, and the hypoxia-responsive prodrug unit to maintain a long-term tumor inhibition. Read More

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One-Pot Microwave-Assisted Synthesis of Carbon Dots and and Antimicrobial Photodynamic Applications.

Front Microbiol 2021 21;12:662149. Epub 2021 Jun 21.

São Carlos Institute of Physics, University of São Paulo, São Carlos, Brazil.

Carbon-based photosensitizers are more attractive than the other ones based on their low cost, high stability, broadband of light absorption, tunable emission spectra, high quantum yield, water solubility, high resistance to metabolic degradation, and selective delivery. These properties allow multiple applications in the field of biology and medicine. The present study evaluated and the antimicrobial photodynamic effect of a one-pot microwave produced C-DOTS based on citric acid. Read More

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Redox responsive 7-ethyl-10-hydroxycamptothecin (SN38) lysophospholipid conjugate: synthesis, assembly and anticancer evaluation.

Int J Pharm 2021 Jul 3;606:120856. Epub 2021 Jul 3.

School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, PR China. Electronic address:

7-Ethyl-10-hydroxycamptothecin (SN38), a potent camptothecin derivative specifically targeting DNA topoisomerase I cleavage complexes, has shown great potential in the treatment of solid tumors. Because of its poor solubility and chemical and metabolic stability, the clinical application of SN38 is highly limited. To address these problems, a novel redox-responsive SN38 conjugate based liposomal formulation is developed in this report. Read More

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