Displaying publications 641 - 660 of 921 in total

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  1. 2'-Aryl and 4'-arylidene substituted pyrazolones: As potential α-amylase inhibitors
    Yousuf S, Khan KM, Salar U, Chigurupati S, Muhammad MT, Wadood A, et al.
    Eur J Med Chem, 2018 Nov 05;159:47-58.
    PMID: 30268823 DOI: 10.1016/j.ejmech.2018.09.052
    Acarbose and voglibose are well-known α-amylase inhibitors used for the management of type-II diabetes mellitus. Unfortunately, these well-known and clinically used inhibitors are also associated with several adverse effects. Therefore, there is still need to develop the safer therapy. Despite of a broad spectrum of biological significances of pyrazolone, it is infrequently evaluated for α-amylase inhibition. Current study deals with the synthesis and biological screening of aryl and arylidene substituted pyrazolones 1-18 for their potential α-amylase inhibitory activity. Structures of synthetic derivatives 1-18 were identified by different spectroscopic techniques. All compounds 1-18 (IC50 = 1.61 ± 0.16 μM to 2.38 ± 0.09 μM) exhibited significant to moderate inhibitory potential when compared to standard acarbose (IC50 = 1.46 ± 0.26 μM). A number of derivatives including 8-12 (IC50 = 1.68 ± 0.1 μM to 1.97 ± 0.07 μM) and 14-16 (IC50 = 1.61 ± 0.16 μM to 1.93 ± 0.07 μM) were found to be significantly active. Limited SAR suggested that different substitutions on compounds do not have any significant effect on the inhibitory potential. Compounds were found to be mixed-type inhibitors revealed by kinetic studies. However, in silico study was identified a number of key features participating in the interaction with the binding site of α-amylase enzyme.
    Matched MeSH terms: Kinetics
  2. Nanomedicines guided nanoimaging probes and nanotherapeutics for early detection of lung cancer and abolishing pulmonary metastasis: Critical appraisal of newer developments and challenges to clinical transition
    Gao X, Guo L, Li J, Thu HE, Hussain Z
    J Control Release, 2018 12 28;292:29-57.
    PMID: 30359665 DOI: 10.1016/j.jconrel.2018.10.024
    Lung cancer (LC) is the second most prevalent type of cancer and primary cause of mortality among both men and women, worldwide. The most commonly employed diagnostic modalities for LC include chest X-ray (CXR), magnetic-resonance-imaging (MRI), computed tomography (CT-scan), and fused-positron-emitting-tomography-CT (PET-CT). Owing to several limitations associated with the use of conventional diagnostic tools such as radiation burden to the patient, misleading diagnosis ("missed lung cancer"), false staging and low sensitivity and resolution, contemporary diagnostic regimen needed to be employed for screening of LC. In recent decades, nanotechnology-guided interventions have been transpired as emerging nanoimaging probes for detection of LC at advanced stages, while producing signal amplification, better resolution for surface and deep tissue imaging, and enhanced translocation and biodistribution of imaging probes within the cancerous tissues. Besides enormous potential of nanoimaging probes, nanotechnology-based advancements have also been evidenced for superior efficacy for treatment of LC and abolishing pulmonary metastasis (PM). The success of nanotherapeutics is due to their ability to maximise translocation and biodistribution of anti-neoplastic agents into the tumor tissues, improve pharmacokinetic profiles of anti-metastatic agents, optimise target-specific drug delivery, and control release kinetics of encapsulated moieties in target tissues. This review aims to overview and critically discuss the superiority of nanoimaging probes and nanotherapeutics over conventional regimen for early detection of LC and abolishing PM. Current challenges to clinical transition of nanoimaging probes and therapeutic viability of nanotherapeutics for treatment for LC and PM have also been pondered.
    Matched MeSH terms: Kinetics
  3. Toxicity evaluation of ZnO and TiO2 nanomaterials in hydroponic red bean (Vigna angularis) plant: Physiology, biochemistry and kinetic transport
    Jahan S, Alias YB, Bakar AFBA, Yusoff IB
    J Environ Sci (China), 2018 Oct;72:140-152.
    PMID: 30244741 DOI: 10.1016/j.jes.2017.12.022
    The toxicity and kinetic uptake potential of zinc oxide (ZnO) and titanium dioxide (TiO2) nanomaterials into the red bean (Vigna angularis) plant were investigated. The results obtained revealed that ZnO, due to its high dissolution and strong binding capacity, readily accumulated in the root tissues and significantly inhibited the physiological activity of the plant. However, TiO2 had a positive effect on plant physiology, resulting in promoted growth. The results of biochemical experiments implied that ZnO, through the generation of oxidative stress, significantly reduced the chlorophyll content, carotenoids and activity of stress-controlling enzymes. On the contrary, no negative biochemical impact was observed in plants treated with TiO2. For the kinetic uptake and transport study, we designed two exposure systems in which ZnO and TiO2 were exposed to red bean seedlings individually or in a mixture approach. The results showed that in single metal oxide treatments, the uptake and transport increased with increasing exposure period from one week to three weeks. However, in the metal oxide co-exposure treatment, due to complexation and competition among the particles, the uptake and transport were remarkably decreased. This suggested that the kinetic transport pattern of the metal oxide mixtures varied compared to those of its individual constituents.
    Matched MeSH terms: Kinetics
  4. Parametric optimization of polycaprolactone synthesis catalysed by Candida antarctica lipase B using response surface methodology
    Pakalapati H, Arumugasamy SK, Jewaratnam J, Wong YJ, Khalid M
    Biopolymers, 2018 Dec;109(12):e23240.
    PMID: 30489632 DOI: 10.1002/bip.23240
    A statistical approach with D-optimal design was used to optimize the process parameters for polycaprolactone (PCL) synthesis. The variables selected were temperature (50°C-110°C), time (1-7 h), mixing speed (50-500 rpm) and monomer/solvent ratio (1:1-1:6). Molecular weight was chosen as response and was determined using matrix-assisted laser desorption/ionization time of flight (MALDI TOF). Using the D-optimal method in design of experiments, the interactions between parameters and responses were analysed and validated. The results show a good agreement with a minimum error between the actual and predicted values.
    Matched MeSH terms: Kinetics
  5. Concerted inhibition of NADP+-specific isocitrate dehydrogenase by oxalacetate and glyoxylate. I. Oxalomalate formation and stability, and nature of the enzyme inhibition
    Johanson RA, Reeves HC
    Biochim. Biophys. Acta, 1977 Jul 08;483(1):24-34.
    PMID: 18195
    Oxalacetate and glyoxylate are each weak inhibitors of NADP+-specific isocitrate dehydrogenase (threo-DS-isocitrate:NADP+ oxidoreductase (decarboxylating), EC 1.1.1.42)9 Together, however, they act in a concerted manner and strongly inhibit the enzyme. The rates of formation and dissociation of the enzyme inhibitor complex, and the rate of formation and the stability of the aldol condensation product of oxalacetate and glyoxylate, oxalomalate, were examined. The data obtained do not support the often suggested possibility that oxalomalate, per se, formed non-enzymatically in isocitrate dehydrogenase assay mixtures containing oxalacetate and glyoxylate, is responsible for the observed inhibition of the enzyme. Rather, the data presented in this communication suggest that oxalacetate binds to the enzyme first, and that the subsequent binding of glyoxylate leads to the formation of a catalytically inactive enzyme-inhibitor complex.
    Matched MeSH terms: Kinetics
  6. Formate assay in body fluids: application in methanol poisoning
    Makar AB, McMartin KE, Palese M, Tephly TR
    Biochem Med, 1975 Jun;13(2):117-26.
    PMID: 1
    Matched MeSH terms: Kinetics
  7. A porous-cross linked enzyme aggregates of maltogenic amylase from Bacillus lehensis G1: Robust biocatalyst with improved stability and substrate diffusion
    Nawawi NN, Hashim Z, Manas NHA, Azelee NIW, Illias RM
    Int J Biol Macromol, 2020 Apr 01;148:1222-1231.
    PMID: 31759025 DOI: 10.1016/j.ijbiomac.2019.10.101
    Enzymatic synthesis of maltooligosaccharides is hampered due to lack of stability of soluble enzyme. This limitation can be tackled by cross linked enzyme aggregates (CLEAs) immobilization approach. However, substrate diffusion is a major bottleneck in cross linking technology. Herein, CLEAs of maltogenic amylase from Bacillus lehensis G1 (Mag1) was developed with addition of porous agent (Mag1-p-CLEAs). Comparison of thermal, pH and kinetic analysis with CLEAs without porous agent (Mag1-CLEAs) and free Mag1 was performed. Mag1-p-CLEAs with porous structure prepared at 0.8% (w/v) of citrus pectin (porous agent), 0.25% (w/v) of chitosan (cross linker) and cross linked for 1.5 h yielded 91.20% activity. 80% of activity is retained after 30 min of incubation at 40 °C and showed longer half-life than free Mag1 and Mag1-CLEAs. Mag1-p-CLEAs also showed pH stability at acidic and alkaline pH. The 1.68-fold increase in Vmax value in comparison to Mag1-CLEAs showed that the presence of pores of Mag1-p-CLEAs enhanced the beta-cyclodextrin accessibility. The increase in high catalytic efficiency (Kcat/Km) value, 1.90-fold and 1.05-fold showed that it also has better catalytic efficiency than free Mag1 and Mag1-CLEAs, respectively. Mag1-p-CLEAs not only improved substrate diffusibility of CLEAs, but also leads to higher thermal and pH stability of Mag1.
    Matched MeSH terms: Kinetics
  8. Fulltext Adsorption of Rhodamine B dye from aqueous solution onto acid treated banana peel: Response surface methodology, kinetics and isotherm studies
    Oyekanmi AA, Ahmad A, Hossain K, Rafatullah M
    PLoS One, 2019;14(5):e0216878.
    PMID: 31091269 DOI: 10.1371/journal.pone.0216878
    The adsorption of rhodamine B (RhB) using acid modified banana peels has been examined. Chemical characteristics of the adsorbents were observed in order to determine active functional groups. The major functional groups on the surface were OH, C = O, C = C and C-O-C. Interactions between operational parameters were studied using the central composite design (CCD) of response surface methodology (RSM). The predictions of the model output indicated that operational factors influenced responses at a confidence level of 95% (P<0.05). The optimum conditions for adsorption were pH 2 at a 0.2 g/L dose within 60 minutes of contact time. Isotherm studies were carried out using the optimized process variables. The data revealed that RhB adsorption fitted the Langmuir isotherm equation while the reduction of COD followed the Freundlich isotherm. Kinetic experiments fitted the pseudo second order model for RhB removal and COD reduction. The adsorption mechanism was not the only rate controlling step. Diffusion through the boundary layer described the pattern of adsorption.
    Matched MeSH terms: Kinetics
  9. Comparison of the transmission potential of two genetically distinct Sindbis viruses after oral infection of Aedes aegypti (Diptera: Culicidae)
    Myles KM, Pierro DJ, Olson KE
    J Med Entomol, 2004 Jan;41(1):95-106.
    PMID: 14989352
    Within mosquitoes, arboviruses encounter barriers to infection and dissemination that are critical determinants of vector competence. The molecular mechanisms responsible for these barriers have yet to be elucidated. The prototype Sindbis (SIN) strain, AR339, and viruses derived from this strain, such as TR339 virus, have limited infection and transmission potential in the medically important arthropod vector, Aedes aegypti (L.). However, the Malaysian SIN virus strain, MRE16, disseminates in nearly 100% of Ae. aegypti 14 d after oral infection. Here, we compare the spatial and temporal infection patterns of MRE16 and TR339 viruses in Ae. aegypti. The results indicate that a midgut escape barrier is primarily responsible for the significantly lower dissemination and transmission potentials observed after oral infection with TR339 virus. MRE16 and TR339 viruses now represent a well-characterized model system for the further study of virus determinants of vector infection, particularly determinants affecting the midgut escape barrier in Ae. aegypti.
    Matched MeSH terms: Kinetics
  10. Selective adsorption and recovery of volatile fatty acids from fermented landfill leachate by activated carbon process
    Talebi A, Razali YS, Ismail N, Rafatullah M, Azan Tajarudin H
    Sci Total Environ, 2020 Mar 10;707:134533.
    PMID: 31865088 DOI: 10.1016/j.scitotenv.2019.134533
    An adsorption-desorption process was applied on fermented landfill leachate to adsorb and recover acetic and butyric acid, using activated carbon. In this study, the first, volatile fatty acids adsorption process from fermented leachate was optimized, by investigating various affecting factors such as pH, time, agitation speed, activated carbon dosage, and temperature. The optimum condition for maximum adsorption of 88.94% acetic acid and 98.53% butyric acid, was 19.79 %wt activated carbon dosage, 40.00 rpm of agitation speed, in 9.45 °C and contact time of 179.89 h, while the pH of the substrate was kept fixed at pH:3.0. Results of X-ray fluorescence (XRF) spectrometry, X-ray diffraction (XRD), Fourier transform infrared (FT-IR) and zeta potential revealed that carbon is the dominant component in the adsorbent with a significant effect to remove organic impurities, and it was observed that the activated carbon after the adsorption process showed an amorphous structure peak with a large internal surface area and pore volume. The results exposed that the adsorption on the surface of activated carbon was due to the chemisorption, and the chemisorption mechanism was supported by covalent bonding. The kinetic study displayed excellent fit to Pseudo-second order kinetics model. The second phase of this study was to recover the adsorbed VFAs using multistage desorption unit, in which application of deionized water and ethanol (as desorption agents) resulted in 89.1% of acetic acid and 67.8% of the butyric acid recovery.
    Matched MeSH terms: Kinetics
  11. Fulltext Dechlorination of polychlorobiphenyl degradation metabolites by a recombinant glutathione S-transferase from Acidovorax sp. KKS102
    Shehu D, Alias Z
    FEBS Open Bio, 2019 03;9(3):408-419.
    PMID: 30868049 DOI: 10.1002/2211-5463.12405
    A glutathione S-transferase (GST) with a potential dehalogenation function against various organochlorine substrates was identified from a polychlorobiphenyl (PCB)-degrading organism, Acidovorax sp. KKS102. A homolog of the gene BphK (biphenyl upper pathway K), named BphK-KKS, was cloned, purified and biochemically characterized. Bioinformatic analysis indicated several conserved amino acids that participated in the catalytic activity of the enzyme, and site-directed mutagenesis of these conserved amino acids revealed their importance in the enzyme's catalytic activity. The wild-type and mutant (C10F, K107T and A180P) recombinant proteins displayed wider substrate specificity. The wild-type recombinant GST reacted towards 1-chloro-2,4-dinitrobenzene (CDNB), ethacrynic acid, hydrogen peroxide and cumene hydroperoxide. The mutated recombinant proteins, however, showed significant variation in specific activities towards the substrates. A combination of a molecular docking study and a chloride ion detection assay showed potential interaction with and a dechlorination function against 2-, 3- and 4-chlorobenzoates (metabolites generated during PCB biodegradation) in addition to some organochlorine pesticides (dichlorodiphenyltrichloroethane, endosulfan and permethrin). It was demonstrated that the behavior of the dechlorinating activities varied among the wild-type and mutant recombinant proteins. Kinetic studies (using CDNB and glutathione) showed that the kinetic parameters Km, Vmax, Kcat and Km/Kcat were all affected by the mutations. While C10F and A180P mutants displayed an increase in GST activity and the dechlorination function of the enzyme, the K107T mutant displayed variable results, suggesting a functional role of Lys107 in determining substrate specificity of the enzyme. These results demonstrated that the enzyme should be valuable in the bioremediation of metabolites generated during PCB biodegradation.
    Matched MeSH terms: Kinetics
  12. Nutritional optimization of Arthrospira platensis for starch and Total carbohydrates production
    Lai YH, Puspanadan S, Lee CK
    Biotechnol Prog, 2019 05;35(3):e2798.
    PMID: 30828976 DOI: 10.1002/btpr.2798
    Present study aims to optimize the production of starch and total carbohydrates from Arthrospira platensis. Growing concerns toward unprecedented environmental issues associated with plastic pollution has created a tremendous impetus to develop new biomaterials for the production of bioplastic. Starch-based biopolymers from algae serve as sustainable feedstock for thermoplastic starch production due to their abundant availability and low cost. A. platensis was cultivated in Zarrouk's medium at 32 ± 1°C and exposed to red light with a photoperiod of 12:12 hr light/dark. Growth kinetics studies showed that the maximum specific growth rate (μmax ) obtained was 0.059 day-1 with the doubling time (td ) of 11.748 days. Subsequently, Zarrouk's medium with different concentrations of sulfur, phosphorus and nitrogen was prepared to establish the nutrient-limiting conditions to enhance the accumulation of starch and total carbohydrates. In this study, the highest starch accumulated was 6.406 ± 0.622 mg L-1 under optimized phosphorus limitation (0.025 g L-1 ) conditions. Nitrogen limitation (0.250 g L-1 ) results demonstrated significant influenced (p 
    Matched MeSH terms: Kinetics
  13. Synthesis of γ-N-modified 8-oxo-2'-deoxyguanosine triphosphate and its characterization
    Thavoncharoensub N, Maruyama K, Heh CH, Hoong Leong K, Shi H, Shigematsu Y, et al.
    Nucleosides Nucleotides Nucleic Acids, 2019;38(8):578-589.
    PMID: 30929604 DOI: 10.1080/15257770.2019.1586919
    8-OxodGTP is generated by the reaction between dGTP and reactive oxygen species and a considered mutagenic nucleotide. It can be incorporated into the duplex DNA during replication processes by the DNA polymerase, and thus the repair enzyme removes oxodGTP from the nucleotide pools in living cells. On the other hand, the γ-modified triphosphates show interesting properties for use as biological tools. Therefore, the γ-N-pyrenylalkyl-oxodGTP derivatives were synthesized and their effect on the enzymatic reactions were evaluated. The γ-N-pyrenylmethyl-oxodGTP was found to be accepted by the DNA polymerase just like oxodGTP, but showed a competitive inhibition property for the human oxodGTPase.
    Matched MeSH terms: Kinetics
  14. Effect of temperature, oxygen and light on the degradation of β-carotene, lutein and α-tocopherol in spray-dried spinach juice powder during storage
    Syamila M, Gedi MA, Briars R, Ayed C, Gray DA
    Food Chem, 2019 Jun 30;284:188-197.
    PMID: 30744845 DOI: 10.1016/j.foodchem.2019.01.055
    The aim of this study was to evaluate the interaction between packaging parameters (transmission of light and oxygen) and storage temperatures (4, 20, 40 °C) on nutrient retention of Spinach (Spinacia oleracea) juice, spray-dried in the absence of an added encapsulant. β-Carotene was more susceptible to degradation compared with lutein and α-tocopherol. Under our experimental conditions, it was observed that excluding low fluorescent light intensity and air by vacuum packaging at 20 °C did not seem to improve nutrient retention loss over time (p > 0.05). The rate of β-carotene, lutein and α-tocopherol loss displayed first order reaction kinetic with low activation energy of 0.665, 2.650 and 13.893 kJ/mol for vacuum, and 1.089, 4.923 and 14.142 kJ/mol for non-vacuum, respectively. The reaction kinetics and half-life for β-carotene, lutein and α-tocopherol at 4 °C and non-vacuumed were 2.2 × 10-2, 1.2 × 10-2, and 0.8 × 10-2 day-1, and 32.08, 58.25 and 85.37 day, respectively.
    Matched MeSH terms: Kinetics
  15. Fulltext Feedforward Artificial Neural Network-Based Model for Predicting the Removal of Phenolic Compounds from Water by Using Deep Eutectic Solvent-Functionalized CNTs
    Ibrahim RK, Fiyadh SS, AlSaadi MA, Hin LS, Mohd NS, Ibrahim S, et al.
    Molecules, 2020 Mar 26;25(7).
    PMID: 32225061 DOI: 10.3390/molecules25071511
    In the recent decade, deep eutectic solvents (DESs) have occupied a strategic place in green chemistry research. This paper discusses the application of DESs as functionalization agents for multi-walled carbon nanotubes (CNTs) to produce novel adsorbents for the removal of 2,4-dichlorophenol (2,4-DCP) from aqueous solution. Also, it focuses on the application of the feedforward backpropagation neural network (FBPNN) technique to predict the adsorption capacity of DES-functionalized CNTs. The optimum adsorption conditions that are required for the maximum removal of 2,4-DCP were determined by studying the impact of the operational parameters (i.e., the solution pH, adsorbent dosage, and contact time) on the adsorption capacity of the produced adsorbents. Two kinetic models were applied to describe the adsorption rate and mechanism. Based on the correlation coefficient (R2) value, the adsorption kinetic data were well defined by the pseudo second-order model. The precision and efficiency of the FBPNN model was approved by calculating four statistical indicators, with the smallest value of the mean square error being 5.01 × 10-5. Moreover, further accuracy checking was implemented through the sensitivity study of the experimental parameters. The competence of the model for prediction of 2,4-DCP removal was confirmed with an R2 of 0.99.
    Matched MeSH terms: Kinetics
  16. Adsorptive nanocomposite membranes for heavy metal remediation: Recent progresses and challenges
    Nasir AM, Goh PS, Abdullah MS, Ng BC, Ismail AF
    Chemosphere, 2019 Oct;232:96-112.
    PMID: 31152909 DOI: 10.1016/j.chemosphere.2019.05.174
    Heavy metal contamination in aqueous system has attracted global attention due to the toxicity and carcinogenicity effects towards living bodies. Among available removal techniques, adsorptive removal by nanosized materials such as metal oxide, metal organic frameworks, zeolite and carbon-based materials has attracted much attention due to the large active surface area, large number of functional groups, high chemical and thermal stability which led to outstanding adsorption performance. However, the usage of nanosized materials is restricted by the difficulty in separating the spent adsorbent from aqueous solution. The shift towards the use of adsorptive composite membrane for heavy metal ions removal has attracted much attention due to the synergistic properties of adsorption and filtration approaches in a same chamber. Thus, this review critically discusses the development of nanoadsorbents and adsorptive nanocomposite membranes for heavy metal removal over the last decade. The adsorption mechanism of heavy metal ions by the advanced nanoadsorbents is also discussed using kinetic and isotherm models. The challenges and future prospect of adsorptive membrane technology for heavy metal removal is presented at the end of this review.
    Matched MeSH terms: Kinetics
  17. Chitosan-glyoxal film as a superior adsorbent for two structurally different reactive and acid dyes: Adsorption and mechanism study
    Jawad AH, Norrahma SSA, Hameed BH, Ismail K
    Int J Biol Macromol, 2019 Aug 15;135:569-581.
    PMID: 31150675 DOI: 10.1016/j.ijbiomac.2019.05.127
    In this work, chitosan (Chi) was cross-linked with glyoxal (Gly) and deposited onto glass plate to be a superior adsorbent film for two structurally different reactive orange 16 (RO-16) and methyl orange (MO) dyes by using non-conventional adsorption system without filtration process. The characterizations indicate that the cross-linked chitosan-glyoxal (Chi-Gly) film has a low swelling index, high adherence strength on glass plate, amine group (NH2) content was 32.52%, and pHpzc of ∼6.0 indicating a negative surface charge occurs above pHpzc. The adsorption isotherm data of RO-16 and MO by Chi-Gly film were in agreement with Langmuir isotherm, with maximum adsorption capacities of 1554.3 mg/g and 1451.9 mg/g, respectively. The pseudo-first-order kinetic model best described the kinetic data. The adsorption process was spontaneous and exothermic in nature at Chi-Gly film thickness of 8.55 μm, and pH ~3. The mechanism of adsorption included mainly electrostatic attractions, dipole-dipole hydrogen bonding interactions, n-π stacking attractions, and Yoshida H-bonding. This study reveals that immobilized Chi-Gly film as a good candidate for adsorption of reactive and acid dyes as it does not require any filtration process and adsorbent recovery during and post-adsorption process.
    Matched MeSH terms: Kinetics
  18. Entrapment of porous cross-linked enzyme aggregates of maltogenic amylase from Bacillus lehensis G1 into calcium alginate for maltooligosaccharides synthesis
    Nawawi NN, Hashim Z, Rahman RA, Murad AMA, Bakar FDA, Illias RM
    Int J Biol Macromol, 2020 May 01;150:80-89.
    PMID: 32035147 DOI: 10.1016/j.ijbiomac.2020.02.032
    Maltooligosaccharides (MOSs) are emerging oligosaccharides in food-based applications and can be synthesized through the enzymatic synthesis of maltogenic amylase from Bacillus lehensis G1 (Mag1). However, the lack of enzyme stability makes this approach unrealistic for industrial applications. The formation of cross-linked enzyme aggregates (CLEAs) is a promising tool for improving enzyme stability, and the substrate accessibility problem of CLEA formation was overcome by the addition of porous agents to generate porous CLEAs (p-CLEAs). However, p-CLEAs exhibited high enzyme leaching and low solvent tolerance. To address these problems, p-CLEAs of Mag1 (Mag1-p-CLEAs) were entrapped in calcium alginate beads (CA). Mag1-p-CLEAs-CA prepared with 2.5% (w/v) sodium alginate and 0.6% (w/v) calcium chloride yielded 53.16% (17.0 U/mg) activity and showed a lower deactivation rate and longer half-life than those of entrapped free Mag1 (Mag1-CA) and entrapped non-porous Mag1-CLEAs (Mag1-CLEAs-CA). Moreover, Mag1-p-CLEAs-CA exhibited low enzyme leaching and high tolerance in various solvents compared to Mag1-p-CLEAs. A kinetic study revealed that Mag1-p-CLEAs-CA exhibited relatively high affinity towards beta-cyclodextrin (β-CD) (Km = 0.62 mM). MOSs (300 mg/g) were synthesized by Mag1-p-CLEAs-CA at 50 °C. Finally, the reusability of Mag1-p-CLEAs-CA makes them as a potential biocatalyst for the continuous synthesis of MOSs.
    Matched MeSH terms: Kinetics
  19. Use of artificial neural networks to predict drug dissolution profiles and evaluation of network performance using similarity factor
    Peh KK, Lim CP, Quek SS, Khoh KH
    Pharm Res, 2000 Nov;17(11):1384-8.
    PMID: 11205731
    PURPOSE: To use artificial neural networks for predicting dissolution profiles of matrix-controlled release theophylline pellet preparation, and to evaluate the network performance by comparing the predicted dissolution profiles with those obtained from physical experiments using similarity factor.

    METHODS: The Multi-Layered Perceptron (MLP) neural network was used to predict the dissolution profiles of theophylline pellets containing different ratios of microcrystalline cellulose (MCC) and glyceryl monostearate (GMS). The concepts of leave-one-out as well as a time-point by time-point estimation basis were used to predict the rate of drug release for each matrix ratio. All the data were used for training, except for one set which was selected to compare with the predicted output. The closeness between the predicted and the reference dissolution profiles was investigated using similarity factor (f2).

    RESULTS: The f2 values were all above 60, indicating that the predicted dissolution profiles were closely similar to the dissolution profiles obtained from physical experiments.

    CONCLUSION: The MLP network could be used as a model for predicting the dissolution profiles of matrix-controlled release theophylline pellet preparation in product development.

    Matched MeSH terms: Kinetics
  20. Sustainable Dissolution Performance of a Carrier Tailored Electrospun
    Teoh XY, Yeoh Y, Yoong LK, Chan SY
    Pharm Res, 2020 Jan 07;37(2):28.
    PMID: 31912250 DOI: 10.1007/s11095-019-2734-0
    PURPOSE: This study aims to conduct an impact investigation in the hydrophobic-hydrophilic balance as an important factor for dissolution improvement of a hydrophilic carrier-based solid dispersion system.

    METHODS: Polymeric carriers with different hydrophobic to hydrophilic ratios were used to prepare several electrospun solid dispersion formulations. Physicochemical properties and surface morphology of the samples were assessed using Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR), polarized light microscopy, Differential Scanning Calorimetry (DSC), X-ray Powder Diffraction (XRPD) and Scanning Electron Microscopy (SEM). Dissolution study was conducted in a non-sink condition to assess the drug release.

    RESULTS: Incorporation of a higher amount of hydrophilic component showed an improvement in formulating a fully amorphous system based on XRPD, yet the dissolution rate increment showed no significant difference from the lower. Hence, the degree of crystallinity is proven not to be the crucial factor contributing to dissolution rate improvement. The presence of a concomitant hydrophobic component, however, showed ability in resisting precipitation and sustaining supersaturation.

    CONCLUSION: Hydrophobicity in a binary carrier system plays an important role in achieving and maintaining the supersaturated state particularly for an amorphous solid dispersion. Graphical Abstract.

    Matched MeSH terms: Kinetics
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