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Advanced nanoscale carrier-based approaches to overcome biopharmaceutical issues associated with anticancer drug 'Etoposide'

Choudhury H, Maheshwari R, Pandey M, Tekade M, Gorain B, Tekade RK

Mater Sci Eng C Mater Biol Appl, 2020 Jan;106:110275.
PMID: 31753398 DOI: 10.1016/j.msec.2019.110275

Etoposide (ETS), topoisomerase-II inhibitor, is a first-line anticancer therapeutics used in diverse cancer types. However, the therapeutic potential of this molecule has mainly impeded due to its detrimental toxicity profile, unfavorable rejection by the cancer cells due to P-glycoprotein (P-gp) efflux activity, and rapid hepatic clearance through extensive metabolism by Cytochrome-P450. To increase the therapeutic potency without significant adverse effects, the implication of novel ETS-nanoformulation strategies have recommended mainly. Nanomedicine based nanoformulation approaches based on nanoparticles (NPs), dendrimers, carbon-nanotubes (CNTs), liposomes, polymeric micelles, emulsions, dendrimers, solid-lipid NPs, etc offers immense potential opportunities to improve the therapeutic potential of pharmaceutically problematic drugs. This review provides an up-to-date argument on the work done in the field of nanomedicine to resolve pharmacokinetic and pharmacodynamic issues associated with ETS. The review also expounds the progress in regards to the regulatory, patenting and clinical trials related to the innovative formulation aspects of ETS.

Matched MeSH terms: Solubility
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: Solubility
Could choline chloride-citric acid monohydrate molar ratio in deep eutectic solvent affect structural, functional and antioxidant properties of pectin?

Shafie MH, Gan CY

Int J Biol Macromol, 2020 Apr 15;149:835-843.
PMID: 32027904 DOI: 10.1016/j.ijbiomac.2020.02.013

The deep eutectic solvents (DESs), which were made from different molar ratios (3:1, 2:1, 1:1, 1:2, 1:3) of choline chloride and citric acid monohydrate, were used as media for the pectic polysaccharide extraction from Averrhoa bilmbi (ABP). The physico-chemical, structural, functional and antioxidant properties of ABP were subsequently determined. The ABP was found to be xylogalacturonan. Moreover, results showed that different structures (i.e. linearity of pectin and branch size) of ABP were obtained, hence, affecting the solubility and functional properties due to the surface availability and steric effect. In addition, when increasing the molar ratio of citric acid monohydrate in DES, lower pH and higher TPC values were observed. These values were correlated with antioxidant activities (i.e. free radical scavenging activity and ferric reducing antioxidant power) of ABP. In conclusion, the molar ratio of the DES components plays an important role in extracting ABP with the aforementioned properties.

Matched MeSH terms: Solubility
Fulltext Genome sequence of an uncharted halophilic bacterium Robertkochia marina with deciphering its phosphate-solubilizing ability

Lam MQ, Chen SJ, Goh KM, Abd Manan F, Yahya A, Shamsir MS, et al.

Braz J Microbiol, 2021 Mar;52(1):251-256.
PMID: 33141351 DOI: 10.1007/s42770-020-00401-2

The wide use of whole-genome sequencing approach in the modern genomic era has opened a great opportunity to reveal the prospective applications of halophilic bacteria. Robertkochia marina CC-AMO-30DT is one of the halophilic bacteria that was previously taxonomically identified without any inspection on its biotechnological potential from a genomic aspect. In this study, we present the whole-genome sequence of R. marina and demonstrated the ability of this bacterium in solubilizing phosphate by producing phosphatase. The genome of R. marina has 3.57 Mbp and contains 3107 predicted genes, from which 3044 are protein coding, 52 are non-coding RNAs, and 11 are pseudogenes. Several phosphatases such as alkaline phosphatases and pyrophosphatases were mined from the genome. Further genomic study (phylogenetics, sequence analysis, and functional mechanism) and experimental data suggested that the alkaline phosphatase produced by R. marina could potentially be utilized in promoting plant growth, particularly for plants on saline-based agricultural land.

Matched MeSH terms: Solubility
Effect of processing methods on xylitol-starch base co-processed adjuvant for orally disintegrating tablet application

Bin LK, Helaluddin ABM, Islam Sarker MZ, Mandal UK, Gaurav A

Pak J Pharm Sci, 2020 Mar;33(2):551-559.
PMID: 32276897

Orally disintegrating tablet (ODT) is a friendly dosage form that requires no access to water and serves as a solution to non-compliance. There are many co-processed adjuvants available in the market. However, there is no single product possesses all the ideal characteristics such as good compressibility, fast disintegration and good palatability for ODT application. The aim of this research was to produce a xylitol-starch base co-processed adjuvant which is suitable for ODT application. Two processing methods namely wet granulation and freeze drying were used to compare the characteristics of co-processed adjuvant comprising of xylitol, starch and crospovidone XL-10 mixed at various ratios. The co-processed excipients were compressed into ODT and physically characterized for powder flow, particle size, hardness, thickness, weight, friability, in-vitro disintegration time and in-situ disintegration time, lubricant sensitivity, dilution potential, Fourier transform infrared spectroscopy, scanning electronic microscopy and x-ray diffraction analysis. Formulation F6 was selected as the optimum formulation due to the fastest in-vitro (135.33±11.52 s) and in-situ disintegration time (88.67±13.56s) among all the formulations (p<0.05). Increase in starch component decreases disintegration time of ODT. The powder flow fell under the category of fair flow. Generally, it was observed that freeze drying method produced smaller particle size granules compared to wet granulation method. ODT produced from freeze drying method had shorter disintegration time compared to ODT from wet granulation batch. In conclusion, a novel co-processed excipient comprised of xylitol, starch and crospovidone XL-10, produced using freeze drying method with fast disintegration time, good compressibility and palatability was developed and characterized. The co-processed excipient is suitable for ODT application.

Matched MeSH terms: Solubility
Fulltext Pore Structure Changes Occur During CO2 Injection into Carbonate Reservoirs

Seyyedi M, Mahmud HKB, Verrall M, Giwelli A, Esteban L, Ghasemiziarani M, et al.

Sci Rep, 2020 Feb 27;10(1):3624.
PMID: 32107400 DOI: 10.1038/s41598-020-60247-4

Observations and modeling studies have shown that during CO2 injection into underground carbonate reservoirs, the dissolution of CO2 into formation water forms acidic brine, leading to fluid-rock interactions that can significantly impact the hydraulic properties of the host formation. However, the impacts of these interactions on the pore structure and macroscopic flow properties of host rock are poorly characterized both for the near-wellbore region and deeper into the reservoir. Little attention has been given to the influence of pressure drop from the near-wellbore region to reservoir body on disturbing the ionic equilibrium in the CO2-saturated brine and consequent mineral precipitation. In this paper, we present the results of a novel experimental procedure designed to address these issues in carbonate reservoirs. We injected CO2-saturated brine into a composite core made of two matching grainstone carbonate core plugs with a tight disk placed between them to create a pressure profile of around 250 psi resembling that prevailing in reservoirs during CO2 injection. We investigated the impacts of fluid-rock interactions at pore and continuum scale using medical X-ray CT, nuclear magnetic resonance, and scanning electron microscopy. We found that strong calcite dissolution occurs near to the injection point, which leads to an increase in primary intergranular porosity and permeability of the near injection region, and ultimately to wormhole formation. The strong heterogeneous dissolution of calcite grains leads to the formation of intra-granular micro-pores. At later stages of the dissolution, the internal regions of ooids become accessible to the carbonated brine, leading to the formation of moldic porosity. At distances far from the injection point, we observed minimal or no change in pore structure, pore roughness, pore populations, and rock hydraulic properties. The pressure drop of 250 psi slightly disturbed the chemical equilibrium of the system, which led to minor precipitation of sub-micron sized calcite crystals but due to the large pore throats of the rock, these deposits had no measurable impact on rock permeability. The trial illustrates that the new procedure is valuable for investigating fluid-rock interactions by reproducing the geochemical consequences of relatively steep pore pressure gradients during CO2 injection.

Matched MeSH terms: Solubility
Fulltext Novel Drug Delivery Systems for Loading of Natural Plant Extracts and Their Biomedical Applications

Rahman HS, Othman HH, Hammadi NI, Yeap SK, Amin KM, Abdul Samad N, et al.

Int J Nanomedicine, 2020;15:2439-2483.
PMID: 32346289 DOI: 10.2147/IJN.S227805

Many types of research have distinctly addressed the efficacy of natural plant metabolites used for human consumption both in cell culture and preclinical animal model systems. However, these in vitro and in vivo effects have not been able to be translated for clinical use because of several factors such as inefficient systemic delivery and bioavailability of promising agents that significantly contribute to this disconnection. Over the past decades, extraordinary advances have been made successfully on the development of novel drug delivery systems for encapsulation of plant active metabolites including organic, inorganic and hybrid nanoparticles. The advanced formulas are confirmed to have extraordinary benefits over conventional and previously used systems in the manner of solubility, bioavailability, toxicity, pharmacological activity, stability, distribution, sustained delivery, and both physical and chemical degradation. The current review highlights the development of novel nanocarrier for plant active compounds, their method of preparation, type of active ingredients, and their biomedical applications.

Matched MeSH terms: Solubility
Fulltext Ionic Liquid-In-Oil Microemulsions Prepared with Biocompatible Choline Carboxylic Acids for Improving the Transdermal Delivery of a Sparingly Soluble Drug

Islam MR, Chowdhury MR, Wakabayashi R, Kamiya N, Moniruzzaman M, Goto M

Pharmaceutics, 2020 Apr 24;12(4).
PMID: 32344768 DOI: 10.3390/pharmaceutics12040392

The transdermal delivery of sparingly soluble drugs is challenging due to of the need for a drug carrier. In the past few decades, ionic liquid (IL)-in-oil microemulsions (IL/O MEs) have been developed as potential carriers. By focusing on biocompatibility, we report on an IL/O ME that is designed to enhance the solubility and transdermal delivery of the sparingly soluble drug, acyclovir. The prepared MEs were composed of a hydrophilic IL (choline formate, choline lactate, or choline propionate) as the non-aqueous polar phase and a surface-active IL (choline oleate) as the surfactant in combination with sorbitan laurate in a continuous oil phase. The selected ILs were all biologically active ions. Optimized pseudo ternary phase diagrams indicated the MEs formed thermodynamically stable, spherically shaped, and nano-sized (<100 nm) droplets. An in vitro drug permeation study, using pig skin, showed the significantly enhanced permeation of acyclovir using the ME. A Fourier transform infrared spectroscopy study showed a reduction of the skin barrier function with the ME. Finally, a skin irritation study showed a high cell survival rate (>90%) with the ME compared with Dulbecco's phosphate-buffered saline, indicates the biocompatibility of the ME. Therefore, we conclude that IL/O ME may be a promising nano-carrier for the transdermal delivery of sparingly soluble drugs.

Matched MeSH terms: Solubility
Fulltext Modeling the Effect of Composition on Formation of Aerosolized Nanoemulsion System Encapsulating Docetaxel and Curcumin Using D-Optimal Mixture Experimental Design

Asmawi AA, Salim N, Abdulmalek E, Abdul Rahman MB

Int J Mol Sci, 2020 Jun 19;21(12).
PMID: 32575390 DOI: 10.3390/ijms21124357

The synergistic anticancer effect of docetaxel (DTX) and curcumin (CCM) has emerged as an attractive therapeutic candidate for lung cancer treatment. However, the lack of optimal bioavailability because of high toxicity, low stability, and poor solubility has limited their clinical success. Given this, an aerosolized nanoemulsion system for pulmonary delivery is recommended to mitigate these drawbacks. In this study, DTX- and CCM-loaded nanoemulsions were optimized using the D-optimal mixture experimental design (MED). The effect of nanoemulsion compositions towards two response variables, namely, particle size and aerosol size, was studied. The optimized formulations for both DTX- and CCM-loaded nanoemulsions were determined, and their physicochemical and aerodynamic properties were evaluated as well. The MED models achieved the optimum formulation for DTX- and CCM-loaded nanoemulsions containing a 6.0 wt% mixture of palm kernel oil ester (PKOE) and safflower seed oils (1:1), 2.5 wt% of lecithin, 2.0 wt% mixture of Tween 85 and Span 85 (9:1), and 2.5 wt% of glycerol in the aqueous phase. The actual values of the optimized formulations were in line with the predicted values obtained from the MED, and they exhibited desirable attributes of physicochemical and aerodynamic properties for inhalation therapy. Thus, the optimized formulations have potential use as a drug delivery system for a pulmonary application.

Matched MeSH terms: Solubility
Fulltext Gliclazide loaded PLGA-HPMC second generation nanocrystals for oral delivery: design, development and in vitro performance characterization

Krishnamoorthy R., Bibhu Prasad Panda, Shivashekaregowda N. K. H., Low B. S., Bhattamisra S. K.

Malaysian Journal of Medicine and Health Sciences, 2019;15(102):44-44.
MyJurnal

Introduction: Second generation functionalized nanocrystal is the advancement of nanocrystal technology with great potential to accommodate BCS (Biopharmaceutical Classification System) class II drugs to meet their formulation and drug delivery challenges. Gliclazide is a BCS class II drug used in the treatment of type 2 diabetes, shows poor water solubility and low rate of dissolution, leads to poor and variable oral bioavailability. The second generation poly(D,L-lactide-co-glycolide) (PLGA) Hydroxypropyl methylcellulose (HPMC) based functionalized nanocrystals of gliclazide were prepared by a combination method of emulsion diffusion-high pressure homogenization-solvent evaporation. Methods: Gliclazide second generation nanocrystals were fabricated with taguchi orthogonal experimental design in combination of step up and top down nanoformulation strategies using drug-polymer (PLGA) ratio at 1:0.5, 1:0.75, 1:1 with HPMC(0.5, 0.75, 1% w/v) as stabilizer. The formulated gliclazide PLGA-HPMC nanocrystals were investigated on particle size, polydispersity index, zeta potential, solubility study, drug entrapment efficiency, in vitro drug release, and surface morphology and compatibility studies. The gliclazide PLGA nanocrystals formulation was prepared with Drug : PLGA at 1: 1 ratio with concentrations 0.75% w/v HPMC at 5 homogenization cycles with 1000bar produce optimized gliclazide nanocrystals. Results: The optimized MSGNC8 formulation
showed particle size of 239.9 nm, entrapment efficiency 98.62%, and drug release of 43.75%, 82.12% and 98.08% at 3hrs, 24hrs, and 48hrs compared to pure gliclazide % drug release of 28.73%, 67.51% and 78.41% at 3hrs, 24hrs, 48hrs respectively. The solubility study of optimized formulation shows eight folds increased in saturation solubility compared to pure drug. Scanning electron microscopy (SEM) analysis of the gliclazide nanocrystals revealed that
gliclazide retained its crystal morphology in polymeric nanocrystals. Further, fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies on gliclazide PLGA-HPMC nanocrystals emphasize drug and excipient compatibility in development of gliclazide nanocrystals. Conclusion: The potential outcomes of research findings emphasize that the developed gliclazide second-generation nanocrystals, which resulted in increase in drug solubility and rate of dissolution with delayed modified release, can be explored in delivery of gliclazide for type 2 diabetes management.

Matched MeSH terms: Solubility
Characterization of pH sensitive sago starch films enriched with anthocyanin-rich torch ginger extract

Xue Mei L, Mohammadi Nafchi A, Ghasemipour F, Mat Easa A, Jafarzadeh S, Al-Hassan AA

Int J Biol Macromol, 2020 Dec 01;164:4603-4612.
PMID: 32941902 DOI: 10.1016/j.ijbiomac.2020.09.082

The development of intelligent packaging based on natural and biodegradable resources is getting more attention by researchers in recent years. The aim of this study was to develop and characterize a pH-sensitive films based on sago starch and incorporated with anthocyanin from torch ginger. The pH-sensitive films were fabricated by casting method with incorporation of different torch ginger extract (TGE) concentration. The surface morphology, physicochemical, barrier, and mechanical properties as well as the pH-sensitivity of films were investigated. The film with the highest concentration of TGE showed the lowest tensile strength (4.26 N/m2), toughness (2.54 MJ/m3), Young's modulus (73.96 MPa) and water vapour permeability (2.6 × 10-4 g·m/day·kPa·m2). However, its elongation at break (85.14%), moisture content (0.27%) and water solubility (37.92%) were the highest compared to other films. pH sensitivity analysis showed that the films containing TGE extract, changes in colour by changing the pH. The colour of films changed from pink to slightly green as the pH increased from pH 4 to 9. Thus, the developed pH-sensitive film with torch ginger extract has potential as intelligent packaging for detection of food freshness or spoilage to ensure their quality and safe consumption.

Matched MeSH terms: Solubility
Fulltext Biodegradable carboxymethyl cellulose based material for sustainable packaging application

Yaradoddi JS, Banapurmath NR, Ganachari SV, Soudagar MEM, Mubarak NM, Hallad S, et al.

Sci Rep, 2020 12 15;10(1):21960.
PMID: 33319818 DOI: 10.1038/s41598-020-78912-z

The main goal of the present work was to develop a value-added product of biodegradable material for sustainable packaging. The use of agriculture waste-derived carboxymethyl cellulose (CMC) mainly is to reduce the cost involved in the development of the film, at present commercially available CMS is costly. The main focus of the research is to translate the agricultural waste-derived CMC to useful biodegradable polymer suitable for packaging material. During this process CMC was extracted from the agricultural waste mainly sugar cane bagasse and the blends were prepared using CMC (waste derived), gelatin, agar and varied concentrations of glycerol; 1.5% (sample A), 2% (sample B), and 2.5% (sample C) was added. Thus, the film derived from the sample C (gelatin + CMC + agar) with 2.0% glycerol as a plasticizer exhibited excellent properties than other samples A and B. The physiochemical properties of each developed biodegradable plastics (sample A, B, C) were characterized using Fourier Transform Infra-Red (FTIR) spectroscopy and Differential Scanning Calorimetry (DSC), Thermogravimetric analysis (TGA). The swelling test, solubility in different solvents, oil permeability coefficient, water permeability (WP), mechanical strength of the produced material was claimed to be a good material for packaging and meanwhile its biodegradability (soil burial method) indicated their environmental compatibility nature and commercial properties. The reflected work is a novel approach, and which is vital in the conversion of organic waste to value-added product development. There is also another way to utilize commercial CMC in preparation of polymeric blends for the packaging material, which can save considerable time involved in the recovery of CMC from sugarcane bagasse.

Matched MeSH terms: Solubility
Fulltext Lyophilized Amorphous Dispersion of Telmisartan in a Combined Carrier-Alkalizer System: Formulation Development and In Vivo Study

Al-Japairai KAS, Alkhalidi HM, Mahmood S, Almurisi SH, Doolaanea AA, Al-Sindi TA, et al.

ACS Omega, 2020 Dec 22;5(50):32466-32480.
PMID: 33376884 DOI: 10.1021/acsomega.0c04588

Telmisartan suffers from low oral bioavailability due to its poor water solubility. The research work presents a formulation of solid dispersed (SD) telmisartan formulation as a ternary mixture of a drug, a polymeric carrier (poly(vinylpyrrolidone) (PVP) K30), and an alkalizer (Na2CO3). The preparation method, which was lyophilization of an aqueous solution containing the ingredients, was free from any organic solvent. The developed SD formulations resulted in a significant improvement in in vitro dissolution (>90% drug dissolution in 15 min) compared to pure telmisartan. Solid-state characterization by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) studies indicated the conversion of crystalline telmisartan into an amorphous form. Fourier transform infrared (FTIR) spectroscopy revealed the drug-polymer interaction that was responsible for reducing the chances of recrystallization. A short-term stability study showed that selected SD formulations were stable in terms of in vitro dissolution and retained their amorphous structure in ambient and accelerated conditions over 2 months. Selected formulations (drug/PVP K30/Na2CO3 as 1:1:2 or 1:2:2 weight ratio) resulted in >2.48 times relative oral bioavailability compared to marketed formulations. It was considered that the incorporation of an alkalizer and a hydrophilic polymer, and amorphization of telmisartan by lyophilization, could enhance in vitro dissolution and improve oral bioavailability.

Matched MeSH terms: Solubility
Fulltext Synthesis and Optimization of Mesoporous Silica Nanoparticles for Ruthenium Polypyridyl Drug Delivery

Harun SN, Ahmad H, Lim HN, Chia SL, Gill MR

Pharmaceutics, 2021 Jan 24;13(2).
PMID: 33498795 DOI: 10.3390/pharmaceutics13020150

The ruthenium polypyridyl complex [Ru(dppz)2PIP]2+ (dppz: dipyridophenazine, PIP: (2-(phenyl)-imidazo[4,5-f ][1,10]phenanthroline), or Ru-PIP, is a potential anticancer drug that acts by inhibiting DNA replication. Due to the poor dissolution of Ru-PIP in aqueous media, a drug delivery agent would be a useful approach to overcome its limited bioavailability. Mesoporous silica nanoparticles (MSNs) were synthesized via a co-condensation method by using a phenanthrolinium salt with a 16 carbon length chain (Phen-C16) as the template. Optimization of the synthesis conditions by Box-Behnken design (BBD) generated MSNs with high surface area response at 833.9 m2g-1. Ru-PIP was effectively entrapped in MSNs at 18.84%. Drug release profile analysis showed that Ru-PIP is gradually released, with a cumulative release percentage of approximately 50% at 72 h. The release kinetic profile implied that Ru-PIP was released from MSN by diffusion. The in vitro cytotoxicity of Ru-PIP, both free and MSN-encapsulated, was studied in Hela, A549, and T24 cancer cell lines. While treatment of Ru-PIP alone is moderately cytotoxic, encapsulated Ru-PIP exerted significant cytotoxicity upon all the cell lines, with half maximal inhibitory concentration (IC50) values determined by MTT (([3-(4,5-dimethylthiazol-2-yl)-2,5-dephenyltetrazolium bromide]) assay at 48 h exposure substantially decreasing from >30 µM to <10 µM as a result of MSN encapsulation. The mechanistic potential of cytotoxicity on cell cycle distribution showed an increase in G1/S phase populations in all three cell lines. The findings indicate that MSN is an ideal drug delivery agent, as it is able to sustainably release Ru-PIP by diffusion in a prolonged treatment period.

Matched MeSH terms: Solubility
Fulltext New protocols for the synthesis of 5-amino-7-(4-phenyl)-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylate esters using an efficient additive

Ghaffari Khaligh N, Mihankhah T, Titinchi S, Shahnavaz Z, Rafie Johan M

Turk J Chem, 2020;44(4):1100-1109.
PMID: 33488215 DOI: 10.3906/kim-2005-6

This work introduces a new additive named 4,4'-trimethylenedipiperidine for the practical and ecofriendly preparation of ethyl 5-amino-7-(4-phenyl)-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylate derivatives. This chemical is commercially available and easy to handle. It also possesses a low melting point and a broad liquid range temperature, high thermal stability, and good solubility in water. Based on green chemistry principles, the reaction was performed in a) a mixture of green solvents i.e. water and ethanol (1:1 v/v) at reflux temperature, and b) the additive was liquefied at 65 °C and the reaction was conducted in the liquid state of the additive. High yields of the desired triazolo-pyrimidines were obtained under both aforementioned conditions. Our results demonstrated that this additive, containing 2 Lewis base sites and able to act as an acceptor-donor hydrogen bonding group, is a novel and efficient alternative to piperidine, owing to its unique properties such as its reduced toxicity, nonflammable nature, nonvolatile state, broad liquid range temperature, high thermal stability, and ability to be safely handled. Furthermore, this additive could be completely recovered and exhibited high recyclability without any change in its chemical structure and no significant reduction in its activity. The current methodology has several advantages: (a) it avoids the use of hazardous materials, as well as toxic, volatile, and flammable solvents, (b) it does not entail tedious processes, harsh conditions, and the multistep preparation of catalysts, (c) it uses a metal-free and noncorrosive catalyst, and (d) reduces the generation of hazardous waste and simple work-up processes. The most important result of this study is that 4,4'-trimethylenedipiperidine can be a promising alternative for toxic, volatile, and flammable base reagents in organic synthesis owing to its unique properties.

Matched MeSH terms: Solubility
Fulltext Investigation of struvite crystals formed in palm oil mill effluent anaerobic digester

Ngatiman M, Jami MS, Abu Bakar MR, Subramaniam V, Loh SK

Heliyon, 2021 Jan;7(1):e05931.
PMID: 33490684 DOI: 10.1016/j.heliyon.2021.e05931

The formation of struvite crystals or magnesium ammonium phosphate (MgNH4PO4) in palm oil mill effluent (POME) occurs as early as in the secondary stage of POME treatment system. Its growth continues in the subsequent tertiary treatment which reduces piping diameter, thus affecting POME treatment efficiency. Hypothesis. The beneficial use of the crystal is the motivation. This occurrence is rarely reported in scientific articles despite being a common problem faced by palm oil millers. The aim of this study is to characterize struvite crystals found in an anaerobic digester of a POME treatment facility in terms of their physical and chemical aspects. The compositions, morphology and properties of these crystals were determined via energy dispersive spectroscopy (EDS), elemental analysis, scanning electron microscopy (SEM) and x-ray diffraction (XRD). Solubility tests were carried out to establish solubility curve for struvite from POME. Finally, crystal growth experiment was done applying reaction crystallization method to demonstrate struvite precipitation from POME. Results showed that high phosphorous (P) (24.85 wt%) and magnesium (Mg) (21.33 wt%) content was found in the struvite sample. Elemental analysis detected carbon (C), hydrogen (H), nitrogen (N) and sulfur (S) below 4 wt%. The crystals analysed by XRD in this study were confirmed as struvite with 94.8% struvite mineral detected from its total volume. Having an orthorhombic crystal system, struvite crystals from POME recorded an average density of 1.701 g cm-3. Solubility curve of struvite from POME was established with maximum solubility of 275.6 mg L-1 at pH 3 and temperature 40 °C. Minimum solubility of 123.6 mg L-1 was recorded at pH 7 and temperature 25 °C. Crystal growth experiment utilizing POME as the source medium managed to achieve 67% reduction in phosphorous content. This study concluded that there is a potential of harnessing valuable nutrients from POME in the form of struvite. Struvite precipitation technology can be adapted in the management of POME in order to achieve maximum utilization of the nutrients that are still abundant in POME. At the same time maximization of nutrient extractions from POME will also reduce pollutants loading in the final discharge.

Matched MeSH terms: Solubility
Fulltext Optimisation of the production of fish gelatine nanoparticles as a carrier for sunflower-derived biopeptide

Akbar, I., Jaswir, I., Jamal, P.

International Food Research Journal, 2020;27(1):171-181.
MyJurnal

Gelatine obtained from fish skin has become a potential source of preparing nanoparticles and
encapsulation of bioactive compounds. Within these fish skin, gelatine nanoparticles show
potent benefits for application in pharmaceutical and cosmetic industry. The encapsulated
bioactive ingredients within nanoparticles have improved bioavailability, delivery properties,
and solubility of the nutraceuticals within the human body and blood stream. Many of such
bioactive peptides (biopeptides) are potent antioxidants; and as oxidative stress is the main
cause of the onset of various chronic diseases, encapsulation of antioxidant biopeptides within
fish gelatine nanoparticles could be a potential remedy to prevent or delay the onset of such
diseases and for better health prospects. The purpose of the present work was to prepare a
simple, safe, and reproducible novel food delivery nanoparticle system encapsulating a desirable antioxidant biopeptide. An optimisation study was conducted to produce a desirable size
of gelatine nanoparticles which showed a higher encapsulation efficiency of an antioxidant
biopeptide. Sunflower biopeptide was chosen as the antioxidant biopeptide, as the activity of
this protein hydrolysate is quite high at DPPH of 89% and FRAP assay of 968 µm/L. Tilapia
fish was used as gelatine source at an average yield of the process at 10% wt/wt. Effects of
parameters such as pH, biopeptide concentration, and cross-linking agent ‘glutaraldehyde’ on
the size, stability, and encapsulation efficiency on the nanoparticles were studied. The average
diameter of the biopeptide loaded gelatine nanoparticle was between 228.3 and 1,305 nm.
Encapsulation efficiency was 76% at an optimal pH of 2, glutaraldehyde concentration of 2
mL, and biopeptide concentration of 0.1 mg/mL exhibited DPPH at 92% and FRAP assay of
978 µm/L. To understand the absorption of sunflower biopeptide in stomach, blood stream,
and biopeptide release of the gelatine nanoparticles, biopeptide loaded gelatine nanoparticles
were subjected to simulated gastrointestinal conditions mimicking human stomach and
intestine; and showed peptide release of 0.1464 and 0.277 mg/mL upon pepsin and pancreatin
digestion, respectively.

Matched MeSH terms: Solubility
Acid-activated spent bleaching earth as a sorbent for chromium (VI) in aqueous solution

Low KS, Lee CK, Lee TS

Environ Technol, 2003 Feb;24(2):197-204.
PMID: 12675017

Spent bleaching earth, an industrial waste produced after the bleaching of crude palm oil, was investigated for its potential in removing Cr(VI) from aqueous solution. The earth was treated with different amounts of sulfuric acid and under different activation temperatures. Results show that the optimum treatment process involved 10% sulfuric acid at 350 degrees C. The effects of contact time, pH, initial concentration, sorbent dosage, temperature, sorption isotherms and the presence of other anions on its sorption capacity were studied. Isotherm data could be fitted into a modified Langmuir isotherm model implying monolayer coverage of Cr(VI) on acid activated spent bleaching earth. The maximum sorption capacity derived from the Langmuir isotherm was 21.2 mg g(-1). This value was compared with those of some other low cost sorbents. Studies of anion effect on the uptake of Cr(VI) on acid activated spent bleaching earth provided the following order of suppression: EDTA >PO4(3-)>SO4(2-)>NO3(-)>Cl(-).

Matched MeSH terms: Solubility
Precipitation of Hevea brasiliensis latex proteins with trichloroacetic acid and phosphotungstic acid in preparation for the Lowry protein assay

Yeang HY, Yusof F, Abdullah L

Anal Biochem, 1995 Mar 20;226(1):35-43.
PMID: 7785777

Many proteins derived from the latex of Hevea brasiliensis that remain soluble in trichloroacetic acid (TCA) can be precipitated by phosphotungstic acid (PTA). A combination of 5% TCA and 0.2% PTA precipitates a wide range of proteins effectively even when they are present in low concentrations (below 1 microgram ml-1). In addition to its protein purification function, acid precipitation also increases the sensitivity of the subsequent protein assay by allowing the test sample to be concentrated. Another advantage of protein precipitation by TCA and PTA is that very small amounts of protein (of the order of 10 micrograms) can be repeatably recovered without the use of precipitate-bulking agents such as sodium deoxycholate. This general procedure of protein purification and concentration is simple and rapid, but the use of PTA may not be fully compatible with the Bradford protein assay. A modified Lowry microassay is described which enables about 3 micrograms ml-1 to be quantitated at the photometric absorbance of 0.05. When used in conjunction with protein concentration by precipitating with TCA/PTA, approximately 0.4 microgram ml-1 protein present in 6 ml of solution can be assayed.

Matched MeSH terms: Solubility
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: Solubility

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