Displaying publications 81 - 100 of 421 in total

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  1. Development of a novel ionic liquid-curcumin complex to enhance its solubility, stability, and activity
    Chowdhury MR, Moshikur RM, Wakabayashi R, Tahara Y, Kamiya N, Moniruzzaman M, et al.
    Chem Commun (Camb), 2019 Jun 11.
    PMID: 31184357 DOI: 10.1039/c9cc02812a
    We report a one-step emulsification and rapid freeze-drying process to develop a curcumin-ionic liquid (CCM-IL) complex that could be readily dispersed in water with a significantly enhanced solubility of ∼8 mg mL-1 and half-life (t1/2) of ∼260 min compared with free CCM (solubility ∼30 nM and t1/2 ∼ 20 min). This process using an IL consisting of a long chain carbon backbone as a surfactant, may provide an alternative way of enhancing the solubility of poorly water-soluble drugs.
    Matched MeSH terms: Solubility
  2. Absorption, distribution and elimination behaviours of cadmium treated by in vitro DIN from WLP residue using SAAM II modeling
    Yasmin Mohd Idris Perama, Nur Shahidah Abdul Rashid, Syazwani Mohd Fadzil, Khoo Kok Siong
    Sains Malaysiana, 2018;47:611-618.
    Mathematically, the human alimentary tract organs were simplified in the model structure as separate compartments with
    pathways of transfer that are kinetically homogenous and equally distributed. The development of gastro-compartment
    model follows the first order kinetics of differential equations to describe cadmium absorption, distribution and elimination
    in the human digestive system. With the aid of in vitro DIN assay, an artificial gastric and gastrointestinal fluid were
    prepared using water leach purification (WLP) residue as a sample that contained toxic metals cadmium. The Simulation,
    Analysis and Modelling II (SAAM II) V2.1 software is employed to design models easily, simulate experiments quickly and
    analyze data accurately. Based on the experimental inputs and fractional transfer rates parameter incorporated to the
    gastro-compartment model, the concentration of cadmium against time profile curves were plotted as the model output.
    The curve presented concentration of cadmium in both gastric and gastrointestinal fluid where initially absorption phase
    (first hour) occurred followed by the distribution phase (second to third hours) and elimination process (third to fifth
    hours). The concentration of cadmium obtained from the simulated model structures was in good agreement with the
    fitted model predicted measurements as statistical t-test conducted showed the values were not significantly different.
    Therefore, modeling approach with SAAM II software gave realistic and better estimation of cadmium dissolution into
    the human gastrointestinal tract.
    Matched MeSH terms: Solubility
  3. Fulltext Preparation and physicochemical characterization of fish skin gelatine hydrolysate from shortfin scad (Decapterus macrosoma)
    Rasli, H.I., Sarbon, N.M.
    International Food Research Journal, 2019;26(1):287-294.
    MyJurnal
    Enzymatic hydrolysis of proteins is an important bioprocess method to prepare bioactive peptides with many functionality and health benefits. The aims of the present work were to prepare and determine the physicochemical characteristics of gelatine hydrolysate from skin of shortfin scad (SSGH) via hydrolysis using alcalase. Analyses on chemical composition, molecular weight by SDS PAGE, protein concentration, amino acid composition, Fourier Transform Infrared Spectroscopic features, and solubility of SSGH were thus performed. The yield of SSGH obtained was 51.01% (d.b.). The chemical compositions of SSGH for moisture, protein, fat, and ash were 13.82%, 90.05%, 1.95%, and 12.48%, respectively. SSGH showed low molecular weight (
    Matched MeSH terms: Solubility
  4. Preparation, in-vitro and in-vivo characterisation of CoQ10 microparticles: electrospraying-enhanced bioavailability
    Fung WY, Liong MT, Yuen KH
    J Pharm Pharmacol, 2016 Feb;68(2):159-69.
    PMID: 26730452 DOI: 10.1111/jphp.12502
    OBJECTIVES: This study aimed to prepare Coenzyme Q10 (CoQ10) microparticles using electrospraying technology, and evaluate the in-vitro properties and in-vivo oral bioavailability.
    KEY FINDINGS: Electrospraying was successfully used to prepare CoQ10 to enhance its solubility and dissolution properties. In-vitro evaluation of the electrosprayed microparticles showed bioavailability-enhancing properties such as reduced crystallinity and particle size. The formulation was evaluated using dissolution study and in-vivo oral bioavailability using rat model. The dissolution study revealed enhanced dissolution properties of electrosprayed microparticles compared with physical mixture and raw material. The absorption profiles showed increasing mean plasma levels CoQ10 in the following order: raw material < physical mixture < electrosprayed microparticles.
    CONCLUSION: Based on the findings in this study, electrospraying is a highly prospective technology to produce functional nano- and micro-structures as delivery vehicles for drugs with poor oral bioavailability due to rate-limiting solubility.
    Matched MeSH terms: Solubility
  5. Methotrexate-based ionic liquid as a potent anticancer drug for oral delivery: In vivo pharmacokinetics, biodistribution, and antitumor efficacy
    Moshikur RM, Ali MK, Wakabayashi R, Moniruzzaman M, Goto M
    Int J Pharm, 2021 Oct 25;608:121129.
    PMID: 34562557 DOI: 10.1016/j.ijpharm.2021.121129
    Oral delivery of the sparingly soluble drug methotrexate (MTX) is challenging owing to its poor bioavailability and low solubility. To address this challenge, the present study reports the conversion of MTX into a series of five ionic liquids (ILs) comprising a cationic component-i.e., cholinium (Cho), tetramethylammonium (TMA), tetrabutylphosphonium (TBP), or an amino acid ester-and an anionic component-i.e., MTX. The biocompatibility, pharmacokinetics, tissue distribution, and antitumor efficacy of each MTX-based IL were investigated to determine its usefulness as a pharmaceutical. Oral administration to mice revealed that proline ethyl ester MTX (IL[ProEt][MTX]) had 4.6-fold higher oral bioavailability than MTX sodium, followed by aspartic diethyl ester MTX, IL[TBP][MTX], IL[Cho][MTX], and IL[TMA][MTX]. The peak plasma concentration, elimination half-life, area under the plasma concentration, mean absorption time, and body clearance of IL[ProEt][MTX] were significantly (p 
    Matched MeSH terms: Solubility
  6. Fulltext Biophysical Evaluation of Water-Soluble Curcumin Encapsulated in β-Cyclodextrins on Colorectal Cancer Cells
    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
  7. Investigation of the Effects of Excipients in the Compounding of Amlodipine Besylate Orally Disintegrating Tablets
    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
  8. Fulltext Statistical Optimization for Acid Hydrolysis of Microcrystalline Cellulose and Its Physiochemical Characterization by Using Metal Ion Catalyst
    Karim MZ, Chowdhury ZZ, Hamid SBA, Ali ME
    Materials (Basel), 2014 Oct 13;7(10):6982-6999.
    PMID: 28788226 DOI: 10.3390/ma7106982
    Hydrolyzing the amorphous region while keeping the crystalline region unaltered is the key technology for producing nanocellulose. This study investigated if the dissolution properties of the amorphous region of microcrystalline cellulose can be enhanced in the presence of Fe(3+) salt in acidic medium. The process parameters, including temperature, time and the concentration of metal chloride catalyst (FeCl₃), were optimized by using the response surface methodology (RSM). The experimental observation demonstrated that temperature and time play vital roles in hydrolyzing the amorphous sections of cellulose. This would yield hydrocellulose with higher crystallinity. The factors that were varied for the production of hydrocellulose were the temperature (x₁), time (x₂) and FeCl₃ catalyst concentration (x₃). Responses were measured in terms of percentage of crystallinity (y₁) and the yield (y₂) of the prepared hydrocellulose. Relevant mathematical models were developed. Analysis of variance (ANOVA) was carried out to obtain the most significant factors influencing the responses of the percentage of crystallinity and yield. Under optimum conditions, the percentage of crystallinity and yield were 83.46% and 86.98% respectively, at 90.95 °C, 6 h, with a catalyst concentration of 1 M. The physiochemical characteristics of the prepared hydrocellulose were determined in terms of XRD, SEM, TGA and FTIR analyses. The addition of FeCl₃ salt in acid hydrolyzing medium is a novel technique for substantially increasing crystallinity with a significant morphological change.
    Matched MeSH terms: Solubility
  9. Recent Advances in Drug Delivery of Polymeric Nano-Micelles
    Aziz ZABA, Ahmad A, Mohd-Setapar SH, Hassan H, Lokhat D, Kamal MA, et al.
    Curr Drug Metab, 2017;18(1):16-29.
    PMID: 27654898 DOI: 10.2174/1389200217666160921143616
    In clinical studies, drugs with hydrophobic characteristic usually reflect low bioavailability, poor drug absorption, and inability to achieve the therapeutic concentration in blood. The production of poor solubility drugs, in abundance, by pharmaceutical industries calls for an urgent need to find the alternatives for resolving the above mentioned shortcomings. Poor water solubility drugs loaded with polymeric micelle seem to be the best alternative to enhance drugs solubility and bioavailability. Polymeric micelle, formed by self-assembled of amphiphilic block copolymers in aqueous environment, functioned as solubilizing agent for hydrophobic drug. This review discusses the fundamentals of polymeric micelle as drug carrier through representative literature, and demonstrates some applications in various clinical trials. The structure, characteristic, and formation of polymeric micelle have been discussed firstly. Next, this manuscript focuses on the potential of polymeric micelles as drug vehicle in oral, transdermal routes, and anti-cancer agent. Several results from previous studies have been reproduced in this review in order to prove the efficacy of the micelles in delivering hydrophobic drugs. Lastly, future strategies to broaden the application of polymeric micelles in pharmaceutical industries have been highlighted.
    Matched MeSH terms: Solubility
  10. Physicochemical characterization of kappa-carrageenan (Euchema cottoni) based films incorporated with various plant oils
    R NFN, Nur Hanani ZA
    Carbohydr Polym, 2017 Feb 10;157:1479-1487.
    PMID: 27987859 DOI: 10.1016/j.carbpol.2016.11.026
    This study investigated the effects of different types of plant oil (olive oil, corn oil, soybean oil and sunflower oil) on the physical and mechanical properties of kappa-carrageenan films from Euchema cottoni species. The incorporation of plant oils increased the film thickness significantly (P<0.05). However, the moisture content, solubility and tensile strength of films decreased significantly (P<0.05) as plant oils were added. The incorporation of plant oils also contributed to a plasticizing effect, whereby the values for elongation at break increased significantly (P<0.05), from 22.3% to 108.8%. Higher oil content also led to carrageenan films with lower opacity, which contradicted with previous studies. In conclusion, the plant oils used in this research significantly improved film properties, thus demonstrating the potential of these materials to be used as food packaging films and coatings.
    Matched MeSH terms: Solubility
  11. Fulltext The effect of extrusion screw-speed on the water extractability and molecular weight distribution of arabinoxylans from defatted rice bran
    Fadel A, Plunkett A, Ashworth J, Mahmoud AM, Ranneh Y, El Mohtadi M, et al.
    J Food Sci Technol, 2018 Mar;55(3):1201-1206.
    PMID: 29487463 DOI: 10.1007/s13197-017-3010-0
    Arabinoxylans (AXs) are major dietary fibre in cereals. Recently, AXs have attracted a great deal of attention because of their biological activities. These activities have been suggested to be related to the content of low molecular weight (Mw) AXs, in particular those with Mw below 32 kDa. Rice bran is a rich source of AXs. However, water extraction of AXs is difficult and often gives low yield. Extrusion processing has been used to increase the solubility of cereal dietary fibre. The aim of this research was to study the effect of extrusion screw-speeds (80 and 160) rpm on the extraction yield and Mw of water extractable AXs from rice bran. It was found that the extraction of AXs increased significantly with an increase in screw speed and was accompanied by a significant decrease in the Mw of AXs from extruded rice bran. The percentage of very low molecular weight AXs (0.79-1.58 kDa) significantly increased with increasing screw speed.
    Matched MeSH terms: Solubility
  12. Fulltext Effects of degree of hydrolysis on physicochemical properties of cobia (Rachycentron canadum) frame hydrolysate
    Amiza, M.A., Kong, Y.L., Faazaz, A.L.
    International Food Research Journal, 2012;19(1):199-206.
    MyJurnal
    The effect of degree of hydrolysis (DH) on the physicochemical properties of cobia frame hydrolysate was determined. Three levels of degree of hydrolysis of cobia frame hydrolysate were studied, which were 53%, 71% and 96%. After enzymatic hydrolysis using Alcalase®, the samples were spray-dried. Cobia hydrolysate powder samples were analyzed for their proximate analysis and physicochemical properties. The proximate analysis showed significant differences in fat and ash content only. DH96 hydrolysate showed desirable essential amino acid profile for human requirement except for methionine and isoleucine. The study found that cobia frame hydrolysate had good colour, emulsifying capacity and excellent foaming properties. However, there were no significant differences in water-holding capacity, oil-holding capacity and peptide solubility among the hydrolysate samples. This study suggested that cobia frame hydrolysate is a potential ingredient and foaming agent for food industry.
    Matched MeSH terms: Solubility
  13. Fulltext Properties of collagen from barramundi (Lates calcarifer) skin
    Jamilah, B., Umi Hartina, M.R., Mat Hashim, D., Sazili, A.Q.
    International Food Research Journal, 2013;20(2):835-842.
    MyJurnal
    The properties of collagens from Barramundi (Lates calcarifer) skin obtained by acid solubilized (control), pepsin and papain aided extractions were investigated. The yields of collagens (dry weight basis) for acid solubilized, pepsin and papain aided extractions were 8.1, 43.6 and 44.0%, respectively. The collagens were generally colorless although collagens from the enzymes aided-extractions were slightly darker. Based on the e-nose evaluation, the collagens were considered odorless. The pH of all the collagens was in the vicinity of 3; however, those extracted with papain had significantly higher pH. The polypeptide profiles obtained in the SDS-PAGE analysis for pepsin extracted collagen were similar to those of acid solubilized collagens. Papain extracted collagen had distinctly different SDS-PAGE pattern. All the extracted collagens were of type 1 with apparent peptides molecular weight distribution of 37 to 250 kDalton. They had high solubility in pH 2 to 5 and increasing NaCl concentration up to 6%.
    Matched MeSH terms: Solubility
  14. Fulltext Effect of extrusion barrel temperatures on residence time and physical properties of various flour extrudates
    Sue Shan, L., Sulaiman, R., Sanny, M., Nur Hanani, Z.A.
    International Food Research Journal, 2015;22(3):965-972.
    MyJurnal
    The aim of this study was to evaluate the effect of barrel temperature and flour types on the residence time and physical properties of various flour extrudates. Corn flour, rice flour, corn flour with potato starch (30% w/w, d.b), and rice flour with potato starch (30%w/w, d.b) were extruded at screw speed of 75rpm, feed moisture at 25% (w/w, w.b.), barrel temperature ranging from 80°C to 140°C and die size of 1.88mm. The extrudates were dried at 50°C overnight and further analysed. Results showed that an increase in extruder barrel temperature decreased the residence time of the flours in the extruder (from 4.11-11.32min to 2.24-6.76min), but increased the expansion ratio, rehydration ratio, water absorption index, water solubility index and b value of the extrudate (p≤0.05). The extrudates had the mean residence time and physical properties of rice flour
    Matched MeSH terms: Solubility
  15. Cassava/sugar palm fiber reinforced cassava starch hybrid composites: Physical, thermal and structural properties
    Edhirej A, Sapuan SM, Jawaid M, Zahari NI
    Int J Biol Macromol, 2017 Aug;101:75-83.
    PMID: 28288881 DOI: 10.1016/j.ijbiomac.2017.03.045
    A hybrid composite was prepared from cassava bagasse (CB) and sugar palm fiber (SPF) using casting technique with cassava starch (CS) as matrix and fructose as a plasticizer. Different loadings of SPF (2, 4, 6 and 8% w/w of dry starch) were added to the CS/CB composite film containing 6% CB. The addition of SPF significantly influenced the physical properties. It increased the thickness while decreasing the density, water content, water solubility and water absorption. However, no significant effect was noticed on the thermal properties of the hybrid composite film. The incorporation of SPF increased the relative crystallinity up to 47%, compared to 32% of the CS film. SEM micrographs indicated that the filler was incorporated in the matrix. The film with a higher concentration of SPF (CS-CB/SPF8) showed a more heterogeneous surface. It could be concluded that the incorporation of SPF led to changes in cassava starch film properties, potentially affecting the film performances.
    Matched MeSH terms: Solubility
  16. Fulltext Gliclazide in Binary and Ternary Systems Improves Physicochemical Properties, Bioactivity, and Antioxidant Activity
    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
  17. Fulltext Development and Evaluation of Self-Emulsifying Drug-Delivery System-Based Tablets for Simvastatin, a BCS Class II Drug
    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
  18. Chemical speciation and bioavailability of rare earth elements (REEs) in the ecosystem: a review
    Khan AM, Bakar NKA, Bakar AFA, Ashraf MA
    Environ Sci Pollut Res Int, 2017 Oct;24(29):22764-22789.
    PMID: 27722986 DOI: 10.1007/s11356-016-7427-1
    Rare earths (RE), chemically uniform group of elements due to similar physicochemical behavior, are termed as lanthanides. Natural occurrence depends on the geological circumstances and has been of long interest for geologist as tools for further scientific research into the region of ores, rocks, and oceanic water. The review paper mainly focuses to provide scientific literature about rare earth elements (REEs) with potential environmental and health effects in understanding the research. This is the initial review of RE speciation and bioavailability with current initiative toward development needs and research perceptive. In this paper, we have also discussed mineralogy, extraction, geochemistry, analytical methods of rare earth elements. In this study, REEs with their transformation and vertical distribution in different environments such as fresh and seawater, sediments, soil, weathering, transport, and solubility have been reported with most recent literature along key methods of findings. Speciation and bioavailability have been discussed in detail with special emphasis on soil, plant, and aquatic ecosystems and their impacts on the environment. This review shows that REE gained more importance in last few years due to their detrimental effects on living organisms, so their speciation, bioavailability, and composition are much more important to evaluate their health risks and are discussed thoroughly as well.
    Matched MeSH terms: Solubility
  19. Fulltext How Key Alterations of Mesoporous Silica Nanoparticles Affect Anti-Lung Cancer Therapy? A Comprehensive Review of the Literature
    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
  20. Fulltext Characterization of Thymoquinone-Sulfobutylether-β-Cyclodextrin Inclusion Complex for Anticancer Applications
    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
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