Displaying publications 1 - 20 of 429 in total

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  1. Muchtaridi M, Triwahyuningtyas D, Muhammad Fakih T, Megantara S, Choi SB
    J Biomol Struct Dyn, 2024 Apr;42(6):3223-3232.
    PMID: 37286382 DOI: 10.1080/07391102.2023.2214237
    α-Mangostin is the most abundant compound contained in the mangostin (Garcinia mangostana L.) plant which have been developed and proven to have many promising pharmacological effects. However, the low water solubility of α-mangostin causes limitations in its development in clinical purpose. To increase the solubility of a compound, a method currently being developed is to make drug inclusion complexes using cyclodextrins. This research aimed to use in silico techniques namely molecular docking study and molecular dynamics simulation to explore the molecular mechanism and stability of the encapsulation of α-mangostin using cyclodextrins. Two types of cyclodextrins were used including β-cyclodextrin and 2-hydroxypropyl-β-cyclodextrin docked against α-mangostin. From the molecular docking results, it shows that the α-mangostin complex with 2-hydroxypropyl-β-cyclodextrin provides the lowest binding energy value of -7.99 Kcal/mol compared to β-cyclodextrin value of -6.14 Kcal/mol. The α-mangostin complex with 2-hydroxypropyl-β-cyclodextrin also showed good stability based on molecular dynamics simulation during 100 ns. From molecular motion, RDF, Rg, SASA, density, total energy analyzes, this complex shows increased solubility in water and provided good stability. This indicates that the encapsulation of α-mangostin with 2-hydroxypropyl-β-cyclodextrin can increase the solubility of the α-mangostin.Communicated by Ramaswamy H. Sarma.
    Matched MeSH terms: Solubility
  2. Loke YH, Chew YL, Janakiraman AK, Lee SK, Uddin ABMH, Goh CF, et al.
    Drug Dev Ind Pharm, 2024 Jan;50(1):36-44.
    PMID: 38149637 DOI: 10.1080/03639045.2023.2294095
    INTRODUCTION: Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited.

    OBJECTIVE: This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs.

    METHODS: A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation.

    RESULTS: The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min.

    CONCLUSION: Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.

    Matched MeSH terms: Solubility
  3. Rather SU, Sulaimon AA, Shariff AM, Qasim A, Bamufleh HS, Alhumade HA, et al.
    Chemosphere, 2023 Oct;337:139290.
    PMID: 37348612 DOI: 10.1016/j.chemosphere.2023.139290
    Carbon dioxide is a major greenhouse gas that is responsible for global warming and renders harmful effects on the atmosphere. The unconstrained release of CO2 into the atmosphere should be prevented and various techniques have been developed in this regard to capture CO2 using different solvents and other compounds. Ionic liquids are a suitable candidate to capture CO2 due to their better solubility behaviour. In this work, two ionic liquids namely tetramethylammonium bromide (TMAB) and tetraethylammonium bromide (TEAB) are employed experimentally to capture CO2 and investigate their solubility behaviour. The study is performed at the temperature values of 303 K, 313 K, and 323 K and the pressure values of 5, 10, 15, and 20 bar equivalent to 0.5, 1.0, 1.5, and 2.0 MPa respectively. The concentrations of both ionic liquid solutions are 2.5 wt%, 5.0 wt%, and 10.0 wt%. The solubility results are considered in terms of mol fraction which is the ratio of moles of CO2 captured per moles of ionic liquid. The density and viscosity values are also determined for both compounds at respective conditions. COSMO-RS is used to generate the sigma profile, sigma surface, and Henry's constant of the ions involved in the study. CO2 is found to be soluble in both ionic liquids, but TEAB showed better solubility behaviour as compared to TMAB. The solubility of CO2 is found to be increasing with the increase in pressure while it decreases with the increase in temperature.
    Matched MeSH terms: Solubility
  4. Zhou Y, Sun Y, Pan D, Xia Q, Zhou C
    J Sci Food Agric, 2023 Aug 30;103(11):5412-5421.
    PMID: 37038882 DOI: 10.1002/jsfa.12616
    BACKGROUND: Goose meat is rough and embedded with dense connective tissue, impairing protein solubility. Therefore, to improve the functional properties of goose myofibrillar protein (GMP), ultrasound was used to assist the phosphorylation of GMP.

    RESULTS: The fact that GMP attached covalently with the phosphate group of sodium tripolyphosphate (GMP-STP) was disclosed directly by Fourier transform infrared spectroscopy. Furthermore, ultrasound significantly improved the hydrophobicity and solubility of GMP-STP, which could be attributed to the conversion of α-helix to β-sheet, β-turns, and random coils by sonication. The spatial stabilization of the protein phosphorylation process was boosted by ultrasound, making the droplets more dispersed, and thus an improvement in the functional properties of GMP-STP was observed. Water-holding capacity, oil-binding capacity, and emulsifying and foaming properties were best at an ultrasound power of 400 W.

    CONCLUSION: Ultrasound-assisted phosphorylation has great potential to modulate the structure-function relationship of proteins. © 2023 Society of Chemical Industry.

    Matched MeSH terms: Solubility
  5. Putra NR, Rizkiyah DN, Aziz AHA, Mamat H, Jusoh WMSW, Idham Z, et al.
    Sci Rep, 2023 Jul 05;13(1):10871.
    PMID: 37407592 DOI: 10.1038/s41598-023-32181-8
    The purpose of this work was to establish the best particle size for recovering high yields of total phenolic compounds (TPC), total anthocyanin compounds(TAC) and total flavonoid compounds (TFC) from roselle (Hibiscus sabdariffa) by applying supercritical carbon dioxide (ScCO2). The extraction rate, diffusivity and solubility of yield in ScCO2 were also studied and calculated utilizing models. Pressure (10 and 30 MPa), temperature (40 and 60 °C), and particle size (250 µm 
    Matched MeSH terms: Solubility
  6. Abd Rahim FN, Wan Ibadullah WZ, Saari N, Brishti FH, Mustapha NA, Ahmad N, et al.
    Int J Biol Macromol, 2023 Jul 01;242(Pt 3):124908.
    PMID: 37217045 DOI: 10.1016/j.ijbiomac.2023.124908
    Rice bran protein concentrates (RBPC) were extracted using mild alkaline solvents (pH: 8, 9, 10). The physicochemical, thermal, functional, and structural aspects of freeze-drying (FD) and spray-drying (SD) were compared. FD and SD of RBPC had porous and grooved surfaces, with FD having non-collapsed plates and SD being spherical. Alkaline extraction increases FD's protein concentration and browning, whereas SD inhibits browning. According to amino acid profiling, RBPC-FD9's extraction optimizes and preserves amino acids. A tremendous particle size difference was prominent in FD, thermally stable at a minimal maximum of 92 °C. Increased pH extraction gives FD greater exposal surface hydrophobicity and positively relates to denaturation enthalpy. Mild pH extraction and drying significantly impacted solubility, improved emulsion properties, and foaming properties of RBPC as observed in acidic, neutral, and alkaline environments. RBPC-FD9 and RBPC-SD10 extracts exhibit outstanding foaming and emulsion activity in all pH conditions, respectively. Appropriate drying selection, RBPC-FD or SD potentially employed as foaming/emulsifier agent or meat analog.
    Matched MeSH terms: Solubility
  7. Zhang Y, Ren H, Li B, Udin SM, Maarof H, Zhou W, et al.
    Int J Biol Macromol, 2023 Jul 01;242(Pt 2):124829.
    PMID: 37210053 DOI: 10.1016/j.ijbiomac.2023.124829
    Deep eutectic solvents (DESs) composed by amino acids (L-arginine, L-proline, L-alanine) as the hydrogen bond acceptors (HBAs) and carboxylic acids (formic acid, acetic acid, lactic acid, levulinic acid) as hydrogen bond donors (HBDs) were prepared and used for the dissolution of dealkaline lignin (DAL). The mechanism of lignin dissolution in DESs was explored at molecular level by combining the analysis of Kamlet-Taft (K-T) solvatochromic parameters, FTIR spectrum and density functional theory (DFT) calculations of DESs. Firstly, it was found that the formation of new hydrogen bonds between lignin and DESs mainly drove the dissolution of lignin, which were accompanied by the erosion of hydrogen bond networks in both lignin and DESs. The nature of hydrogen bond network within DESs was fundamentally determined by the type and number of functional groups in both HBA and HBD, which affected its ability to form hydrogen bond with lignin. One hydroxyl group and carboxyl group in HBDs provided active protons, which facilitated proton-catalyzed cleavage of β-O-4, thus enhancing the dissolution of DESs. The superfluous functional group resulted in more extensive and stronger hydrogen bond network in the DESs, thus decreasing the lignin dissolving ability. Moreover, it was found that lignin solubility had a closed positive correlation with the subtraction value of α and β (net hydrogen donating ability) of DESs. Among all the investigated DESs, L-alanine/formic acid (1:3) with the strong hydrogen-bond donating ability (acidity), weak hydrogen-bond accepting ability (basicity) and small steric-hindrance effect showed the best lignin dissolving ability (23.99 wt%, 60 °C). On top of that, the value of α and β of L-proline/carboxylic acids DESs showed some positive correlation with the global electrostatic potential (ESP) maxima and minima of the corresponding DESs respectively, indicating the analysis of ESP quantitative distributions of DESs could be an effective tool for DESs screening and design for lignin dissolution as well as other applications.
    Matched MeSH terms: Solubility
  8. Ab'lah N, Yusuf CYL, Rojsitthisak P, Wong TW
    Int J Biol Macromol, 2023 Jun 30;241:124506.
    PMID: 37085071 DOI: 10.1016/j.ijbiomac.2023.124506
    Starch is a polysaccharide with varying amylose-to-amylopectin ratios as a function of its biological sources. It is characterized by low shear stress resistance, poor aqueous/organic solubility and gastrointestinal digestibility which limit its ease of processing and functionality display as an oral drug delivery vehicle. Modulation of starch composition through genetic engineering primarily alters amylose-to-amylopectin ratio. Greater molecular properties changes require chemical and enzymatic modifications of starch. Acetylation reduces water solubility and enzymatic digestibility of starch. Carboxymethylation turns starch acid-insoluble and aggregative at low pHs. The summative effects are sustaining drug release in the upper gut. Acid-insoluble carboxymethylated starch can be aminated to provide an ionic character essential for hydrogel formation which further reduces its drug release. Ionic starch can coacervate with oppositely charged starch, non-starch polyelectrolyte or drug into insoluble, controlled-release complexes. Enzymatically debranched and resistant starch has a small molecular size which confers chain aggregation into a helical hydrogel network that traps the drug molecules, protecting them from biodegradation. The modified starch has been used to modulate the intestinal/colon-specific or controlled systemic delivery of oral small molecule drugs and macromolecular therapeutics. This review highlights synthesis aspects of starch and starch derivatives, and their outcomes and challenges of applications in oral drug delivery.
    Matched MeSH terms: Solubility
  9. Eid EEM, Almaiman AA, Alshehade SA, Alsalemi W, Kamran S, Suliman FO, et al.
    Molecules, 2023 May 15;28(10).
    PMID: 37241838 DOI: 10.3390/molecules28104096
    Thymoquinone (TQ) is a quinone derived from the black seed Nigella sativa and has been extensively studied in pharmaceutical and nutraceutical research due to its therapeutic potential and pharmacological properties. Although the chemopreventive and potential anticancer effects of TQ have been reported, its limited solubility and poor delivery remain the major limitations. In this study, we aimed to characterize the inclusion complexes of TQ with Sulfobutylether-β-cyclodextrin (SBE-β-CD) at four different temperatures (293-318 K). Additionally, we compared the antiproliferative activity of TQ alone to TQ complexed with SBE-β-CD on six different cancer cell lines, including colon, breast, and liver cancer cells (HCT-116, HT-29, MDA-MB-231, MCF-7, SK-BR-3, and HepG2), using an MTT assay. We calculated the thermodynamic parameters (ΔH, ΔS, and ΔG) using the van't Holf equation. The inclusion complexes were characterized by X-ray diffraction (XRD), Fourier transforms infrared (FT-IR), and molecular dynamics using the PM6 model. Our findings revealed that the solubility of TQ was improved by ≥60 folds, allowing TQ to penetrate completely into the cavity of SBE-β-CD. The IC50 values of TQ/SBE-β-CD ranged from 0.1 ± 0.01 µg/mL against SK-BR-3 human breast cancer cells to 1.2 ± 0.16 µg/mL against HCT-116 human colorectal cancer cells, depending on the cell line. In comparison, the IC50 values of TQ alone ranged from 0.2 ± 0.01 µg/mL to 4.7 ± 0.21 µg/mL. Overall, our results suggest that SBE-β-CD can enhance the anticancer effect of TQ by increasing its solubility and bioavailability and cellular uptake. However, further studies are necessary to fully understand the underlying mechanisms and potential side effects of using SBE-β-CD as a drug delivery system for TQ.
    Matched MeSH terms: Solubility
  10. Kannan SK, Esakkiappa S, Anthonysamy E, Sudalaimuthu S, Sulaiman Y, Khan MM, et al.
    Mikrochim Acta, 2023 Feb 10;190(3):87.
    PMID: 36759372 DOI: 10.1007/s00604-023-05664-8
    Spermine (SPM) is considered a biomarker for prostate cancer and detecting it becomes highly challenging due to its electro- and optical-inactive nature. SPM has a tendency to interact with groups such as phosphates and sulfides to form macrocyclic arrangements known as nuclear aggregates of polyamines. Using this tendency, an electrochemical sensor has been developed using a polysulfide (PS) modified Au electrode (PS@Au electrode). PS has been synthesized from elemental sulfur by hydrothermal method and characterized using UV-Vis, fluorescence, FTIR, SEM, and XPS analyses. The PS@Au electrode was employed for electrochemical sensing of SPM. In the presence of SPM, a decrease in gold oxide reduction current was noted which is proportional to the concentration of SPM. The decrease in gold oxide reduction (0.5 V) current was attributed to the complexing nature of SPM-PS at the electrode interface. The reason for the decrease in current has been substantiated using XRF, XPS, and spectroelectrochemical studies. Under the optimized conditions, the PS@Au electrode exhibited a linear range of 1.55-250 µM with LOD of 0.511 ± 0.02 µM (3σ). The electrochemical strategy for SPM sensing exhibited better selectivity even in the presence of possible interferents. The selectivity stems from the selective interaction of SPM with PS on the Au electrode surface; the tested amino acids, and other molecules do not complex with PS and hence they could not interfere. The PS@Au electrode has been subjected to the determination of SPM in artificial urine samples and exhibited outstanding performance in the synthetic sample.
    Matched MeSH terms: Solubility
  11. Bashir MA, Khan A, Shah SI, Ullah M, Khuda F, Abbas M, et al.
    Drug Des Devel Ther, 2023;17:261-272.
    PMID: 36726738 DOI: 10.2147/DDDT.S377686
    BACKGROUND: Self-emulsifying drug-delivery systems (SEDDSs) are designed to improve the oral bioavailability of poorly water-soluble drugs. This study aimed at formulating and characterization of SEDDS-based tablets for simvastatin using castor and olive oils as solvents and Tween 60 as surfactant.

    METHODS: The liquids were adsorbed on microcrystalline cellulose, and all developed formulations were compressed using 10.5 mm shallow concave round punches.

    RESULTS: The resulting tablets were evaluated for different quality-control parameters at pre- and postcompression levels. Simvastatin showed better solubility in a mixture of oils and Tween 60 (10:1). All the developed formulations showed lower self-emulsification time (˂200 seconds) and higher cloud point (˃60°C). They were free of physical defects and had drug content within the acceptable range (98.5%-101%). The crushing strength of all formulations was in the range of 58-96 N, and the results of the friability test were within the range of USP (≤1). Disintegration time was within the official limits (NMT 15 min), and complete drug release was achieved within 30 min.

    CONCLUSION: Using commonly available excipients and machinery, SEDDS-based tablets with better dissolution profile and bioavailability can be prepared by direct compression. These S-SEDDSs could be a better alternative to conventional tablets of simvastatin.

    Matched MeSH terms: Solubility
  12. Budiman A, Rusdin A, Subra L, Aulifa DL
    Int J Nanomedicine, 2023;18:5473-5493.
    PMID: 37791322 DOI: 10.2147/IJN.S426120
    In 2020, there were 2.21 million new instances of lung cancer, making it the top cause of mortality globally, responsible for close to 10 million deaths. The physicochemical problems of chemotherapy drugs are the primary challenge that now causes a drug's low effectiveness. Solubility is a physicochemical factor that has a significant impact on a drug's biopharmaceutical properties, starting with the rate at which it dissolves and extending through how well it is absorbed and bioavailable. One of the most well-known methods for addressing a drug's solubility is mesoporous silica, which has undergone excellent development due to the conjugation of polymers and ligands that increase its effectiveness. However, there are still very few papers addressing the success of this discovery, particularly those addressing its molecular pharmaceutics and mechanism. Our study's objectives were to explore and summarize the effects of targeting mediator on drug development using mesoporous silica with and without functionalized polymer. We specifically focused on highlighting the molecular pharmaceutics and mechanism in this study's innovative findings. Journals from the Scopus, PubMed, and Google Scholar databases that were released during the last ten years were used to compile this review. According to inclusion and exclusion standards adjusted. This improved approach produced very impressive results, a very significant change in the characteristics of mesoporous silica that can affect effectiveness. Mesoporous silica approaches have the capacity to greatly enhance a drug's physicochemical issues, boost therapeutic efficacy, and acquire superb features.
    Matched MeSH terms: Solubility
  13. Kumar P, Chaudhary B, Jain V, Baboota S, Shivanandy P, Alharbi KS, et al.
    Curr Drug Deliv, 2023;20(9):1262-1274.
    PMID: 36380413 DOI: 10.2174/1567201820666221114113637
    Molecular pharmaceutics play a critical role in the drug delivery system, representing the direct interconnection of drug bioavailability with its molecular form. There is a diversity in the molecular structures by which it affects its properties, such as amorphous form, crystalline form, partialamorphous molecular dispersion, and disordered state. The active pharmaceutical ingredient (API) and the excipients utilized in the formulation process contain various divergent modes used in the formulation process. They include better formulations of any type to obtain good quality pharmaceutical products. This review reveals how the molecular states affect the API and are important in maintaining the quality of dosage forms. Furthermore, the physio-chemical properties of the components and various pharmaceutical approaches employed in the formulation of dosage forms are studied from the point of view of molecular pharmaceutics.
    Matched MeSH terms: Solubility
  14. Tsuji T, Ono T, Taguchi H, Leong KH, Hayashi Y, Kumada S, et al.
    Chem Pharm Bull (Tokyo), 2023;71(7):576-583.
    PMID: 37394606 DOI: 10.1248/cpb.c23-00214
    Time-domain NMR (TD-NMR) was used for continuous monitoring of the hydration behavior of hydrophilic matrix tablets. The model matrix tablets comprised high molecular weight polyethylene oxide (PEO), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG). The model tablets were immersed in water. Their T2 relaxation curves were acquired by TD-NMR with solid-echo sequence. A curve-fitting analysis was conducted on the acquired T2 relaxation curves to identify the NMR signals corresponding to the nongelated core remaining in the samples. The amount of nongelated core was estimated from the NMR signal intensity. The estimated values were consistent with the experiment measurement values. Next, the model tablets immersed in water were monitored continuously using TD-NMR. The difference in hydration behaviors of the HPMC and PEO matrix tablets was then characterized fully. The nongelated core of the HPMC matrix tablets disappeared more slowly than that of the PEO matrix tablets. The behavior of HPMC was significantly affected by the PEG content in the tablets. It is suggested that the TD-NMR method has potential to be utilized to evaluate the gel layer properties, upon replacement of the immersion medium: purified (nondeuterated) water is replaced with heavy (deuterated) water. Finally, drug-containing matrix tablets were tested. Diltiazem hydrochloride (a highly water-soluble drug) was employed for this experiment. Reasonable in vitro drug dissolution profiles, which were in accordance with the results from TD-NMR experiments, were observed. We concluded that TD-NMR is a powerful tool to evaluate the hydration properties of hydrophilic matrix tablets.
    Matched MeSH terms: Solubility
  15. Khan AA, Akhtar S, Yadav Y, Atiya A, Alelwani W, Bannunah AM, et al.
    Curr Drug Deliv, 2023;20(10):1474-1486.
    PMID: 35980056 DOI: 10.2174/1567201819666220817111054
    BACKGROUND: The antiretroviral protease inhibitor drug, lopinavir (LPV), is used to treat HIV-1 infection. LPV is known to have limited oral bioavailability, which may be attributed to its poor aqueous solubility, low efficacy and high first-pass metabolism. Self-nanoemulsifying drug delivery systems (SNEDDS) for LPV have been developed and optimised to counter the current issues.

    METHODS: The titration method was used to prepare LPV-loaded SNEDDS (LPV-SNEDDS). Six different pseudo-ternary phase diagrams were constructed to identify the nanoemulsifying region. The developed formulations were chosen in terms of globule size < 100 nm, dispersity ≤ 0.5, dispersibility (Grade A) and% transmittance > 85. Heating-cooling cycle, freeze-thaw cycle, and centrifugation studies were performed to confirm the stability of the developed SNEDDS.

    RESULTS: The final LPV-SNEDDS (L-14) droplet size was 58.18 ± 0.62 nm, with polydispersity index, zeta potential, and entrapment efficiency (EE%) values of 0.326 ± 0.005, -22.08 ± 1.2 mV, and 98.93 ± 1.18%, respectively. According to high-resolution transmission electron microscopy (HRTEM) analysis, the droplets in the optimised formulation were < 60 nm in size. The selected SNEDDS released nearly 99% of the LPV within 30 min, which was significantly (p < 0.05) higher than the LPV-suspension in methylcellulose (0.5% w/v). It indicates the potential use of SNEDDS to enhance the solubility of LPV, which eventually could help improve the oral bioavailability of LPV. The Caco-2 cellular uptake study showed a significantly (p < 0.05) higher LPV uptake from the SNEEDS (LPV-SNEDDS-L-14) than the free LPV (LPV-suspension).

    CONCLUSION: The LPV-SNEDDS could be a potential carrier for LPV oral delivery.

    Matched MeSH terms: Solubility
  16. Alshati F, Alahmed TAA, Sami F, Ali MS, Majeed S, Murtuja S, et al.
    Curr Pharm Des, 2023;29(36):2853-2866.
    PMID: 37946351 DOI: 10.2174/0113816128266398231027100119
    Many methods, including solid dispersion, micellization, and inclusion complexes, have been employed to increase the solubility of potent drugs. Beta-cyclodextrin (βCD) is a cyclic oligosaccharide consisting of seven glucopyranoside molecules, and is a widely used polymer for formulating soluble inclusion complexes of hydrophobic drugs. The enzymatic activity of Glycosyltransferase or α-amylase converts starch or its derivatives into a mixture of cyclodextrins. The βCD units are characterized by α -(1-4) glucopyranose bonds. Cyclodextrins possess certain properties that make them very distinctive because of their toroidal or truncated cage-like supramolecular configurations with multiple hydroxyl groups at each end. This allowed them to encapsulate hydrophobic compounds by forming inclusion complexes without losing their solubility in water. Chemical modifications and newer derivatives, such as methylated βCD, more soluble hydroxyl propyl methyl βCD, and sodium salts of sulfobutylether-βCD, known as dexolve® or captisol®, have envisaged the use of CDs in various pharmaceutical, medical, and cosmetic industries. The successful inclusion of drug complexes has demonstrated improved solubility, bioavailability, drug resistance reduction, targeting, and penetration across skin and brain tissues. This review encompasses the current applications of β-CDs in improving the disease outcomes of antimicrobials and antifungals as well as anticancer and anti-tubercular drugs.
    Matched MeSH terms: Solubility
  17. Low ZX, Teo MYM, Nordin FJ, Dewi FRP, Palanirajan VK, In LLA
    Int J Mol Sci, 2022 Oct 25;23(21).
    PMID: 36361655 DOI: 10.3390/ijms232112866
    Curcumin (CUR), a curcuminoid originating from turmeric root, possesses diverse pharmacological applications, including potent anticancer properties. However, the use of this efficacious agent in cancer therapy has been limited due to low water solubility and poor bioavailability. To overcome these problems, a drug delivery system was established as an excipient allowing improved dispersion in aqueous media coupled with enhanced in vitro anticancer effects. Different analyses such as UV-vis spectroscopy, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), solubility and dissolution assays were determined to monitor the successful encapsulation of CUR within the inner cavity of a β-cyclodextrin (β-CD) complex. The results indicated that water solubility was improved by 205.75-fold compared to pure CUR. Based on cytotoxicity data obtained from MTT assays, the inclusion complex exhibited a greater decrease in cancer cell viability compared to pure CUR. Moreover, cancer cell migration rates were decreased by 75.5% and 38.92%, invasion rates were decreased by 37.7% and 35.7%, while apoptosis rates were increased by 26.3% and 14.2%, and both caused caspase 3 activation toward colorectal cancer cells (SW480 and HCT116 cells). This efficacious formulation that enables improved aqueous dispersion is potentially useful and can be extended for various chemotherapeutic applications. Preliminary toxicity evaluation also indicated that its composition can be safely used in humans for cancer therapy.
    Matched MeSH terms: Solubility
  18. Azmi NHS, Ming LC, Uddin ABMH, Sarker ZI, Bin LK
    Int J Pharm Compd, 2022 1 27;26(1):80-87.
    PMID: 35081048
    Oral drug delivery has been recognized as the most desirable drug administration method among other drug delivery routes due to its ease of administration, long shelf life, and low cost. Orally disintegrating tablets disintegrate within seconds in the mouth without the need of water for swallowing. This unique feature of orally disintegrating tablets is favorable to special populations such as geriatric and pediatric patients. Formulation optimization is significant to obtain the optimal combination of tablet constituents, as the tablet composition is influential on dosage-form characteristics. The objective of this study was to investigate the effect of different types of fillers and percentage on the physical properties of orally disintegrating tablets by using amlodipine as the model drug. Blank orally disintegrating tablets containing different fillers, namely, Sorbolac 400, Granulac 200, and CombiLac with different percentages, were prepared using the wet granulation method and were evaluated based on weight variation, hardness, thickness, friability, and disintegration time. Formulation 5 that consists of 25% Granulac 200 showed the optimal result among all formulations with the fastest disintegration time (96.17 s Å} 18.40) and sufficient tablet hardness (4.59 kg Å} 0.70). Hence, formulation 5 was selected as the optimal formulation and incorporated with amlodipine. From this study, it can be concluded that excipients have an essential role in determining the physical properties of orally disintegrating tablets.
    Matched MeSH terms: Solubility
  19. Hau EH, Teh SS, Yeo SK, Mah SH
    J Sci Food Agric, 2022 Jan 15;102(1):233-240.
    PMID: 34081335 DOI: 10.1002/jsfa.11350
    BACKGROUND: The oil palm tree produces 90% of wastes and the limited usage of these wastes causes a major disposal problem in the mills. Nevertheless, these by-products have a large amount of nutritional components. Thus, the present study aimed to determine the physicochemical and functional properties of protein hydrolysates (PH) from oil palm leaves (OPL) extracted using different concentrations of Alcalase (0-10%) at 2 h of hydrolysis time.

    RESULTS: Fourier transform infrared spectral analyses showed that the enzymatic hydrolysis altered functional groups of OPL where a secondary amine was present in the PH. Changes were also observed in the thermal stability where the enthalpy heat obtained for PH (933.93-1142.57 J g-1 ) was much lower than OPL (7854.11 J g-1 ). The results showed that the PH extracted by 8% Alcalase exhibited absolute zeta potential, as well as a high emulsifying activity index (70.64 m2  g-1 of protein) and emulsion stability index (60.58 min). Furthermore, this PH showed higher solubility (96.32%) and emulsifying properties compared to other PHs. It is also comparable with commercial plant proteins, indicating that 8% Alcalase is an optimum concentration for hydrolysis.

    CONCLUSION: In summary, the physicochemical and functional properties of PH extracted from OPL showed good functional properties, suggesting that it can be used as an alternative plant protein in food industries. © 2021 Society of Chemical Industry.

    Matched MeSH terms: Solubility
  20. Ibrahim M, Munir S, Ahmed S, Chughtai AH, Ahmad W, Khan J, et al.
    Oxid Med Cell Longev, 2022;2022:2100092.
    PMID: 36466089 DOI: 10.1155/2022/2100092
    The poor solubility of the antidiabetic drug gliclazide (Glc) is due to its hydrophobic nature. This research is aimed at improving Glc's solubility and drug release profile, as well as at investigating additional benefits such as bioactivity and antioxidant activity, by forming binary complexes with HPβCD at different w/w ratios (1 : 1, 1 : 2.5, 1 : 4, and 1 : 9) and ternary complexes with HPβCD and Tryp at 1 : 1 : 1, 1 : 1 : 0.27, 1 : 2.5 : 0.27, 1 : 3.6 : 3.6, 1 : 4 : 1, and 1 : 9 : 1, respectively. Complexes were prepared by the physical mixing (PM) and solvent evaporation (SE) methods. The prepared inclusion complexes were meticulously characterized by X-ray diffractometry (XRD), scanning electron microscopy (SEM), and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectra. To verify our findings, the inclusion complexes were evaluated by equilibrium solubility, in vitro drug release profile, kinetic models, and antidiabetic and antioxidant activities in animal models. Our results demonstrated that the solubility and drug release profile were found to be enhanced through binary as well as ternary complexes. Notably, ternary complexes with a ratio of 1 : 9 : 1 showed the highest solubility and drug release profile compared to all other preparations. Data on antioxidant activity indicated that the ternary complex had the higher total antioxidant status (TAS), superoxide dismutase (SOD), and catalase (CAT) activity than the binary complex and Glc alone, in contrast to the diabetic group. In vivo antidiabetic activity data revealed a high percentage reduction in the blood glucose level by ternary complexes (49-52%) compared to the binary complexes (45-46%; p ≤ 0.05). HPβCD and Tryp provide a new platform for overcoming the challenges associated with poorly soluble Glc by providing greater complexing and solubilizing capabilities and imparting ancillary benefits to improve the drug's antidiabetic and antioxidant activities.
    Matched MeSH terms: Solubility
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