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Formulation and optimization of orally disintegrating tablets of sumatriptan succinate

Sheshala R, Khan N, Darwis Y

Chem Pharm Bull (Tokyo), 2011;59(8):920-8.
PMID: 21804234

The aims of the present research were to mask the intensely bitter taste of sumatriptan succinate and to formulate orally disintegrating tablets (ODTs) of the taste masked drug. Taste masking was performed by coating sumatriptan succinate with Eudragit EPO using spray drying technique. The resultant microspheres were evaluated for thermal analysis, yield, particle size, entrapment efficiency and in vitro taste masking. The tablets were formulated by mixing the taste masked microspheres with different types and concentrations of superdisintegrants and compressed using direct compression method followed by sublimation technique. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. All the tablet formulations disintegrated in vitro within 37-410 s. The optimized formulation containing 5% Kollidon CL-SF released more than 90% of the drug within 15 min and the release was comparable to that of commercial product (Suminat®). In human volunteers, the optimized formulation was found to have a pleasant taste and mouth feel and disintegrated in the oral cavity within 41 s. The optimized formulation was found to be stable and bioequivalent with Suminat®.

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 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 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
Fulltext Development and Evaluation of 1'-Acetoxychavicol Acetate (ACA)-Loaded Nanostructured Lipid Carriers for Prostate Cancer Therapy

Subramaniam B, Arshad NM, Malagobadan S, Misran M, Nyamathulla S, Mun KS, et al.

Pharmaceutics, 2021 Mar 24;13(4).
PMID: 33804975 DOI: 10.3390/pharmaceutics13040439

1'-acetoxychavicol acetate (ACA) extracted from the rhizomes of Alpinia conchigera Griff (Zingiberaceae) has been shown to deregulate the NF-ĸB signaling pathway and induce apoptosis-mediated cell death in many cancer types. However, ACA is a hydrophobic ester, with poor solubility in an aqueous medium, limited bioavailability, and nonspecific targeting in vivo. To address these problems, ACA was encapsulated in a nanostructured lipid carrier (NLC) anchored with plerixafor octahydrochloride (AMD3100) to promote targeted delivery towards C-X-C chemokine receptor type 4 (CXCR4)-expressing prostate cancer cells. The NLC was prepared using the melt and high sheer homogenization method, and it exhibited ideal physico-chemical properties, successful encapsulation and modification, and sustained rate of drug release. Furthermore, it demonstrated time-based and improved cellular uptake, and improved cytotoxic and anti-metastatic properties on PC-3 cells in vitro. Additionally, the in vivo animal tumor model revealed significant anti-tumor efficacy and reduction in pro-tumorigenic markers in comparison to the placebo, without affecting the weight and physiological states of the nude mice. Overall, ACA-loaded NLC with AMD3100 surface modification was successfully prepared with evidence of substantial anti-cancer efficacy. These results suggest the potential use of AMD3100-modified NLCs as a targeting carrier for cytotoxic drugs towards CXCR4-expressing cancer cells.

Matched MeSH terms: Solubility
Fulltext PH-responsive strontium nanoparticles for targeted gene therapy against mammary carcinoma cells

Bakhtiar A, Chowdhury EH

Asian J Pharm Sci, 2021 Mar;16(2):236-252.
PMID: 33995617 DOI: 10.1016/j.ajps.2020.11.002

Genetic intervention via the delivery of functional genes such as plasmid DNA (pDNA) and short-interfering RNA (siRNA) offers a great way to treat many single or multiple genetic defects effectively, including mammary carcinoma. Delivery of naked therapeutic genes or siRNAs is, however, short-lived due to biological clearance by scavenging nucleases and circulating monocytes. Low cellular internalization of negatively-charged nucleic acids further causes low transfection or silencing activity. Development of safe and effectual gene vectors is therefore undeniably crucial to the success of nucleic acid delivery. Inorganic nanoparticles have attracted considerable attention in the recent years due to their high loading capacity and encapsulation activity. Here we introduce strontium salt-based nanoparticles, namely, strontium sulfate, strontium sulfite and strontium fluoride as new inorganic nanocarriers. Generated strontium salt particles were found to be nanosized with high affinity towards negatively-charged pDNA and siRNA. Degradation of the particles was seen with a drop in pH, suggesting their capacity to respond to pH change and undergo dissolution at endosomal pH to release the genetic materials. While the particles are relatively nontoxic towards the cells, siRNA-loaded SrF2 and SrSO3 particles exerted superior transgene expression and knockdown activity of MAPK and AKT, leading to inhibition of their phosphorylation to a distinctive extent in both MCF-7 and 4T1 cells. Strontium salt nanoparticles have thus emerged as a promising tool for applications in cancer gene therapy.

Matched MeSH terms: Solubility
Oral Nanoemulsion of Fenofibrate: Formulation, Characterization, and In Vitro Drug Release Studies

Gulati N, Kumar Chellappan D, M Tambuwala M, A A Aljabali A, Prasher P, Kumar Singh S, et al.

Assay Drug Dev Technol, 2021 05 14;19(4):246-261.
PMID: 33989048 DOI: 10.1089/adt.2021.012

Nanoemulsions (NMs) are one of the most important colloidal dispersion systems that are primarily used to improve the solubility of poorly water soluble drugs. The main objectives of this study were, first, to prepare an NM loaded with fenofibrate using a high shear homogenization technique and, second, to study the effect of variable using a central composite design. Twenty batches of fenofibrate-loaded NM formulations were prepared. The formed NMs were subjected to droplet size analysis, zeta potential, entrapment efficiency, pH, dilution, polydispersity index, transmission electron microscopy (TEM), Fourier transform infrared spectrophotometry, differential scanning calorimetry (DSC), and in vitro drug release study. Analysis of variance was used for entrapment efficiency data to study the fitness and significance of the design. The NM-7 batch formulation demonstrated maximum entrapment efficiency (81.82%) with lowest droplet size (72.28 nm), and was thus chosen as the optimized batch. TEM analysis revealed that the NM was well dispersed with droplet sizes <100 nm. Incorporation of the drug into the NM was confirmed with DSC studies. In addition, the batch NM-7 also showed the maximum in vitro drug release (87.6%) in a 0.05 M sodium lauryl sulfate solution. The release data revealed that the NM followed first-order kinetics. The outcomes of the study revealed the development of a stable oral NM containing fenofibrate using the high shear homogenization technique. This approach may aid in further enhancing the oral bioavailability of fenofibrate, which requires further in vivo studies.

Matched MeSH terms: Solubility
Fulltext Preparation and characterization of nano liposomes of Orthosiphon stamineus ethanolic extract in soybean phospholipids

Aisha AF, Majid AM, Ismail Z

BMC Biotechnol, 2014;14:23.
PMID: 24674107 DOI: 10.1186/1472-6750-14-23

O. stamineus is a medicinal herb with remarkable pharmacological properties. However, poor solubility of the active principles limits its medicinal value. This study sought to prepare nano liposomes of OS ethanolic extract in unpurified soybean phospholipids in order to improve its solubility and permeability. OS liposomes were prepared by the conventional film method, and were characterized for solubility, entrapment efficiency, Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), particle size and zeta potential, release, absorption in everted rat intestinal sacs, and DPPH scavenging effect.

Matched MeSH terms: Solubility
Evaluation of solid-state bioconversion of domestic wastewater sludge as a promising environmental-friendly disposal technique

Hossain Molla A, Fakhru'l-Razi A, Zahangir Alam M

Water Res, 2004 Nov;38(19):4143-52.
PMID: 15491662

Natural and environmental-friendly disposal of wastewater sludge is a great concern. Recently, biological treatment has played prominent roles in bioremediation of complex hydrocarbon- rich contaminants. Composting is quite an old biological-based process that is being practiced but it could not create a great impact in the minds of concerned researchers. The present study was conducted to evaluate the feasibility of the solid-state bioconversion (SSB) processes in the biodegradation of wastewater sludge by exploiting this promising technique to rejuvenate the conventional process. The Indah Water Konsortium (IWK) domestic wastewater treatment plant (DWTP) sludge was considered for evaluation of SSB by monitoring the microbial growth and its subsequent roles in biodegradation under two conditions: (i) flask (F) and (ii) composting bin (CB) cultures. Sterile and semi-sterile environments were allowed in the F and the CB, respectively, using two mixed fungal cultures, Trichoderma harzianum with Phanerochaete chrysosporium 2094 (T/P) and T. harzianum with Mucor hiemalis (T/M) and two bulking materials, sawdust (SD) and rice straw (RS). The significant growth and multiplication of both the mixed fungal cultures were reflected in soluble protein, glucosamine and color intensity measurement of the water extract. The color intensity and pH of the water extract significantly increased and supported the higher growth of microbes and bioconversion. The most encouraging results of microbial growth and subsequent bioconversion were exhibited in the RS than the SD. A comparatively higher decrease of organic matter (OM) % and C/N ratio were attained in the CB than the F, which implied a higher bioconversion. But the measurement of soluble protein, glucosamine and color intensity exhibited higher values in the F than the CB. The final pH drop was higher in the CB than the F, which implied that a higher nitrification occurred in the CB associated with a higher release of H+ ions. Both the mixed cultures performed almost equal roles in all cases except the changes in moisture content.

Matched MeSH terms: Solubility
Fulltext The differential expression of aqueous soluble proteins in breast normal and cancerous tissues in relation to ethnicity of the patients; Chinese, Malay and Indian

Liang S, Singh M, Gam LH

Dis Markers, 2010;28(3):149-65.
PMID: 20534901 DOI: 10.3233/DMA-2010-0694

Female breast cancer is one of the leading causes of female mortality worldwide. In Malaysia, breast cancer is the most commonly diagnosed cancer in women. Of the women in Malaysia, the Chinese have the highest number of breast cancer cases, followed by the Indian and the Malay. The most common type of breast cancer is infiltrating ductal carcinoma (IDC). A proteomic approach was applied in this study to identify changes in the protein profile of cancerous tissues compared with normal tissues from 18 patients; 8 Chinese, 6 Malay and 4 Indian were analysed. Twenty-four differentially expressed hydrophilic proteins were identified. We evaluated the potential of these proteins as biomarkers for infiltrating ductal carcinoma based on their ethnic-specific expressions. Three of the upregulated proteins, calreticulin, 14-3-3 protein zeta and 14-3-3 protein eta, were found to be expressed at a significantly higher level in the cancerous breast tissues when compared with the normal tissues in cases of infiltrating ductal carcinoma. The upregulation in expression was particularly dominant in the Malay cohort.

Matched MeSH terms: Solubility
Centrifugal air-assisted melt agglomeration for fast-release "granulet" design

Wong TW, Musa N

Int J Pharm, 2012 Jul 1;430(1-2):184-96.
PMID: 22531845 DOI: 10.1016/j.ijpharm.2012.04.026

Conventional melt pelletization and granulation processes produce round and dense, and irregularly shaped but porous agglomerates respectively. This study aimed to design centrifugal air-assisted melt agglomeration technology for manufacture of spherical and yet porous "granulets" for ease of downstream manufacturing and enhancing drug release. A bladeless agglomerator, which utilized shear-free air stream to mass the powder mixture of lactose filler, polyethylene glycol binder and poorly water-soluble tolbutamide drug into "granulets", was developed. The inclination angle and number of vane, air-impermeable surface area of air guide, processing temperature, binder content and molecular weight were investigated with reference to "granulet" size, shape, texture and drug release properties. Unlike fluid-bed melt agglomeration with vertical processing air flow, the air stream in the present technology moved centrifugally to roll the processing mass into spherical but porous "granulets" with a drug release propensity higher than physical powder mixture, unprocessed drug and dense pellets prepared using high shear mixer. The fast-release attribute of "granulets" was ascribed to porous matrix formed with a high level of polyethylene glycol as solubilizer. The agglomeration and drug release outcomes of centrifugal air-assisted technology are unmet by the existing high shear and fluid-bed melt agglomeration techniques.

Matched MeSH terms: Solubility
Polysaccharide-anchored fatty acid liposome

Tan HW, Misran M

Int J Pharm, 2013 Jan 30;441(1-2):414-23.
PMID: 23174410 DOI: 10.1016/j.ijpharm.2012.11.013

In this study, the preparation of N-pamitoyl chitosan (ChP) anchored oleic acid (OA) liposome was demonstrated. Two different types of water-soluble ChPs with different degrees of acylation (DA) were selected for this study. The presence of ChPs on the surface of OA liposome was confirmed with their micrographs and physicochemical properties. The "peeling off" effect on the surface of the ChP-anchored OA (OAChP) liposomes was observed on the atomic force microscope micrographs and confirmed the presence of the ChPs layer on the liposome surface. The surface tension of the OAChPs liposome solution was found to be higher than that of the OA liposome solution. This result indicated the removal of OA monomer by ChPs from the air-water interface. The increase in the minimum area per headgroup (A(min)) of the OA with the presence of ChPs has further proved the interaction between OA monomer and the hydrophobic moieties of the ChPs. The ChPs anchored onto the OA monolayer increased the curvature of the OAChP liposomes monolayer and reduced the liposome size. The size of the OAChP liposomes was reduced by 30 nm as compared with the unmodified OA liposome. Results revealed that the anchored ChPs can improve the integrity and rigidity of the OA liposome.

Matched MeSH terms: Solubility
Designing cellulose hydrogels from non-woody biomass

Wong LC, Leh CP, Goh CF

Carbohydr Polym, 2021 Jul 15;264:118036.
PMID: 33910744 DOI: 10.1016/j.carbpol.2021.118036

Hydrogels are an attractive system for a myriad of applications. While most hydrogels are usually formed from synthetic materials, lignocellulosic biomass appears as a sustainable alternative for hydrogel development. The valorization of biomass, especially the non-woody biomass to meet the growing demand of the substitution of synthetics and to leverage its benefits for cellulose hydrogel fabrication is attractive. This review aims to present an overview of advances in hydrogel development from non-woody biomass, especially using native cellulose. The review will cover the overall process from cellulose depolymerization, dissolution to crosslinking reaction and the related mechanisms where known. Hydrogel design is heavily affected by the cellulose solubility, crosslinking method and the related processing conditions apart from biomass type and cellulose purity. Hence, the important parameters for rational designs of hydrogels with desired properties, particularly porosity, transparency and swelling characteristics will be discussed. Current challenges and future perspectives will also be highlighted.

Matched MeSH terms: Solubility
Improving oral bioavailability of medicinal herbal compounds through lipid-based formulations - A Scoping Review

Tan OJ, Loo HL, Thiagarajah G, Palanisamy UD, Sundralingam U

Phytomedicine, 2021 Sep;90:153651.
PMID: 34340903 DOI: 10.1016/j.phymed.2021.153651

BACKGROUND: Although numerous medicinal herbal compounds demonstrate promising therapeutic potential, their clinical application is often limited by their poor oral bioavailability. To circumvent this barrier, various lipid-based herbal formulations have been developed and trialled with promising experimental results.
PURPOSE: This scoping review aims to describe the effect of lipid-based formulations on the oral bioavailability of herbal compounds.
METHODS: A systematic search was conducted across three electronic databases (Medline, Embase and Cochrane Library) between January 2010 and January 2021 to identify relevant studies. The articles were rigorously screened for eligibility. Data from eligible studies were then extracted and collated for synthesis and descriptive analysis using Covidence.
RESULTS: A total of 109 studies were included in the present review: 105 animal studies and four clinical trials. Among the formulations investigated, 50% were emulsions, 34% lipid particulate systems, 12% vesicular systems, and 4% were other types of lipid-based formulations. Within the emulsion system classification, self-emulsifying drug delivery systems were observed to produce the best improvements in oral bioavailability, followed by mixed micellar formulations. The introduction of composite lipid-based formulations and the use of uncommon surfactants such as sodium oleate in emulsion preparation was shown to consistently enhance the bioavailability of herbal compounds with poor oral absorption. Interestingly, the lipid-based formulations of magnesium lithospermate B and Pulsatilla chinensis produced an absolute bioavailability greater than 100% indicating the possibility of prolonged systemic circulation. With respect to chemical conjugation, D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) was the most frequently used and significantly improved the bioavailability of its phytoconstituents.
CONCLUSION: Our findings suggest that there is no distinct lipid-based formulation superior to the other. Bioavailability improvements were largely dependent on the nature of the phytoconstituents. This scoping review, however, provided a detailed summary of the most up-to-date evidence on phytoconstituents formulated into lipid preparations and their oral bioavailability. We conclude that a systematic review and meta-analysis between bioavailability improvements of individual phytoconstituents (such as kaempferol, morin and myricetin) in various lipid-based formulations will provide a more detailed association. Such a review will be highly beneficial for both researchers and herbal manufacturers.

Matched MeSH terms: Solubility
Fulltext Synthesis of silica fine particle by the addition of a non-ionic surfactant

Mohd Nazri Idris, Hazizan Md. Akil, Zainal Arifin Ahmad

Journal of Nuclear and Related Technologies, 2007;2005(1):29-33.
MyJurnal

Sodium silicate was used to synthesize silica fine particles at room temperature using non-ionic surfactant of triethanolamine (TEA), dissolution salt and precipitating agent. The experiments were conducted by different composition of precursor material, nonionic surfactant and dissolution salt concentrations through the sol-gel process. Various particle sizes in the range 100-300nm were synthesized. The particle size of silica powders were analyzed via Field Emission Scanning Electron Microscope (FESEM), Energy Dispersive X-ray Analysis (EDAX), X-Ray Fluorescence (XRF), and Fourier Transformation Infrared (FTIR). The result has demonstrated that the particle size can be controlled by changing the ratio of non-ionic surfactant and dissolution salt or the sodium silicate concentration.

Matched MeSH terms: Solubility
Fulltext Effect of orange sweet potato (Ipomoea batatas) flour on the physical properties of fried extruded fish crackers

Cheow, C.S., Noorakmar, A.W., Norizzah, A.R., Mohd Zahid, A., Ruzaina, I.

International Food Research Journal, 2012;19(2):657-664.
MyJurnal

The effects of orange sweet potato flour addition to tapioca starch on the expansion, oil absorption,
bulk density, water absorption index (WAI), water solubility index (WSI), hardness and colour of fried extruded fish crackers were investigated. The microstructure properties were assessed by Field Emission Scanning Electron Microscope (FESEM) and the sensory properties of fried extruded fish crackers were determined by quantitative descriptive analysis method. The shape and texture of the product were similar to that of normal breakfast cereal. Light brownish and slightly harder texture was obtained with addition of orange sweet potato flour to tapioca starch in the fried extruded fish crackers. The bulk density and water solubility index (WSI) increased with the increase in orange sweet potato flour addition. However, water absorption index (WAI), linear expansion, expansion ratio, volume expansion and oil absorption decreased as the amount of orange sweet potato increased. The microstructure studies revealed that fried extruded fish crackers with high percentage of orange sweet potato flour had small air cells and thick cell wall. The fried extruded fish crackers with 30% fish, 14% orange sweet potato flour and 56% tapioca starch had high crispiness score and accepted by the trained panellists.

Matched MeSH terms: Solubility
Fulltext Edible films from seaweed (kappaphycus alvarezii)

Siah, W.M., Aminah, A., Ishak, A.

International Food Research Journal, 2015;22(6):2230-2236.
MyJurnal

A new patent pending process is proposed in this study to produce edible film directly from seaweed (Kappaphycus alvarezii). Seaweed together with other ingredients has been used to produce the film through casting technique. Physical and mechanical tests were performed on the edible films to examine the thickness, colour, transparency, solubility, tensile strength,
elongation at break, water permeability rate, oxygen permeability rate and surface morphology. Produced film was transparent, stretchable, sealable and have basic properties as a film for food packaging. This study suggests that the edible film could be used as novel materials in food industry as sachet/pouch/bag for instant coffee, breakfast cereals drinks, seasoning powder,
candies etc; as wrapper for seasoning cube and chocolate; as interleaf for frozen foods such as burger patties to avoid the patties from sticking together; and also as material for edible logo in bakeries products. Other than that, the edible film also could be used in pharmaceutical industry as functional strips such as oral freshener strips and drug strips. In cosmetic and toiletries industries, the edible film could be used to produce facial mask and bag for pre-portioned detergent. Compared with edible film developed earlier using alginate and carrageenan, film developed in this research used seaweed directly. The developed film reduced the need to extract the alginate and carrageenan, making material preparation easier and cheaper.

Matched MeSH terms: Solubility
Synthesis and formulation studies of griseofulvin analogues with improved solubility and metabolic stability

Petersen AB, Andersen NS, Konotop G, Hanafiah NH, Raab MS, Krämer A, et al.

Eur J Med Chem, 2017 Apr 21;130:240-247.
PMID: 28258034 DOI: 10.1016/j.ejmech.2017.02.055

Griseofulvin (1) is an important antifungal agent that has recently received attention due to its antiproliferative activity in mammalian cancer cells. Comprehensive SAR studies have led to the identification of 2'-benzyloxy griseofulvin 2, a more potent analogue with low micromolar anticancer potency in vitro. Analogue 2 was also shown to retard tumor growth through inhibition of centrosomal clustering in murine xenograft models of colon cancer and multiple myeloma. However, similar to griseofulvin, compound 2 exhibited poor metabolic stability and aqueous solubility. In order to improve the poor pharmacokinetic properties, 11 griseofulvin analogues were synthesized and evaluated for biological activity and physiological stabilities including SGF, plasma, and metabolic stability. Finally, the most promising compounds were investigated in respect to thermodynamic solubility and formulation studies. The 2'-benzylamine analogue 10 proved to be the most promising compound with low μM in vitro anticancer potency, a 200-fold increase in PBS solubility over compound 2, and with improved metabolic stability. Furthermore, this analogue proved compatible with formulations suitable for both oral and intravenous administration. Finally, 2'-benzylamine analogue 10 was confirmed to induce G2/M cell cycle arrest in vitro.

Matched MeSH terms: Solubility
Fulltext Removal of dissolved organic carbon from peat swamp runoff using assorted tropical agriculture biomass

Sim, F.S., Mohd Irwan Lu, N.A.L., Lee, Z.E.T., Mohamed, M.

Pertanika Journal of Science & Technology, 2015;23(1):51-59.
MyJurnal

In this study, agriculture biomass was used to remove dissolved organic matter from peat swamp runoff. The functional groups and morphological properties of 6 tropical agriculture biomasses (coconut husk, rice husk, empty fruit bunch, sago hampas, saw dust and banana trunk) in their raw and citric acid–treated states were examined. The Fourier transform infrared (FTIR) spectra showed that various biomasses were typically characterised with lignocellulosic compounds. The spectra analysis further demonstrated that citric acid treatment resulted in the dissolution of lignin and hemicelluloses to various extents where carboxyl groups were also introduced. These changes hypothetically suggest improved adsorption ability. Treatment of peat swamp runoff with various untreated biomasses showed no adsorption. With the modified biomass, adsorption was evidenced, with rice husk illustrating the highest removal efficiency of 60% to 65%.The biosorbent can be used in the water treatment process especially for treating water with a high dissolved organic matter content. The spent sorbent can be subsequently applied as a soil conditioner as the dissolved organic fraction, commonly known as humic matter, possesses important agricultural value.

Matched MeSH terms: Solubility
New Insight in Improving Therapeutic Efficacy of Antipsychotic Agents: An Overview of Improved In Vitro and In Vivo Performance, Efficacy Upgradation and Future Prospects

Ei Thu H, Hussain Z, Shuid AN

Curr Drug Targets, 2018;19(8):865-876.
PMID: 27894237 DOI: 10.2174/1389450117666161125174625

Psychotic disorders are recognized as severe mental disorders that rigorously affect patient's personality, critical thinking, and perceptional ability. High prevalence, global dissemination and limitations of conventional pharmacological approaches compel a significant burden to the patient, medical professionals and the healthcare system. To date, numerous orally administered therapies are available for the management of depressive disorders, schizophrenia, anxiety, bipolar disorders and autism spectrum problems. However, poor water solubility, erratic oral absorption, extensive first-pass metabolism, low oral bioavailability and short half-lives are the major factors which limit the pharmaceutical significance and therapeutic feasibility of these agents. In recent decades, nanotechnology-based delivery systems have gained remarkable attention of the researchers to mitigate the pharmaceutical issues related to the antipsychotic therapies and to optimize their oral drug delivery, therapeutic outcomes, and patient compliance. Therefore, the present review was aimed to summarize the available in vitro and in vivo evidences signifying the pharmaceutical importance of the advanced delivery systems in improving the aqueous solubility, transmembrane permeability, oral bioavailability and therapeutic outcome of the antipsychotic agents.

Matched MeSH terms: Solubility

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