Displaying publications 201 - 220 of 437 in total

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  1. Mahesparan VA, Bin Abd Razak FS, Ming LC, Uddin AH, Sarker MZI, Bin LK
    Int J Pharm Compd, 2020 3 21;24(2):148-155.
    PMID: 32196477
    Orodispersible tablets disintegrate rapidly (within 3 minutes) in the oral cavity and release the medicament before swallowing. The mode of disintegrant addition might affect the properties of orodispersible tablets. The objective of this study was to formulate and evaluate orodispersible tablets by studying different modes of disintegration addition with varying concentrations of disintegrants. The wet granulation method was used to produce the orodispersible tablets. Two methods of disintegration addition were compared (i.e., intragranular, extragranular). Three disintegrants (i.e., cornstarch, sodium starch glycolate, crospovidone) were used at three levels (5%, 10%, and 15%) in the study. The formulations were tested for the powder flowability (angle of repose) and characterized physically (hardness, weight, thickness, friability, disintegration time). The mangosteen pericarp extract was used as a model active pharmaceutical ingredient to be incorporated into the optimum formulation. It was observed that the extragranular method produced granules with better flowability compared to that of the intragranular method. Crospovidone was found as the most efficient disintegrant among the three. The optimum formulation selected was one with the highest concentration of crospovidone (15%), which showed the fastest disintegration time. The mode of disintegrant addition into the orodispersible tablets formulation was found to show a marked difference in the disintegration, as well as other physical characteristics of the orodispersible tablets where the extragranular mode of addition showed better property, which caused the orodispersible tablets to disintegrate the fastest.
    Matched MeSH terms: Solubility
  2. Siti Mazlina Mustapa Kamal, Khairul Faezah Md. Yunos, Norhafizah Abdullah
    Sains Malaysiana, 2018;47:309-318.
    Tilapia is a popular freshwater fish and among the important cultured fish grown worldwide. In this study, fish protein
    hydrolysate was produced from tilapia (Oreochromis niloticus) by-product (TB) and tilapia muscle (TM) through enzymatic
    hydrolysis using alcalase. The TB and TM protein hydrolysates were evaluated for its characteristics in terms of angiotensin
    I-converting enzyme (ACE) inhibition activity, peptide size distribution, and functional properties. Hydrolysis for 1 h for
    TB and TM successfully produced low molecular weight peptides (<14.2kDa) with the highest ACE inhibitory activities.
    The findings also demonstrated that both samples have high nitrogen solubility (>80% at pH2-9) and good emulsifying,
    water and oil holding capacities. The study indicated that tilapia protein hydrolysates have the potential to be used as
    functional food products.
    Matched MeSH terms: Solubility
  3. Pui LP, Karim R, Yusof YA, Wong CW, Ghazali HM
    Acta Sci Pol Technol Aliment, 2021 4 23;20(2):135-148.
    PMID: 33884852 DOI: 10.17306/J.AFS.0801
    BACKGROUND: 'Cempedak' (Artocarpus integer) is an aromatic fruit which is similar to jackfruit. Although it is rich in vitamin A and is consumed fresh, the fruit has a short shelf life. Hence, it can be converted through a spray-drying process, to form powder, which is more stable. Powder flow properties are important when considering storage, while its reconstitution characteristics are critical for the consumer to make juice from the product.

    METHODS: The parameters of spray-dried 'cempedak' fruit powder under study include inlet air temperature (140-180°C) and maltodextrin (DE 10) concentrations (5-15% w/w). Response surface methodology involving 14 runs was used to assess the effects of inlet temperature and maltodextrin on the powder flow properties and reconstitution properties of the spray-dried 'cempedak' powder.

    RESULTS: Out of the tested responses, only bulk density, change in cake height ratio, and water solubility index had a high coefficient of determination value. Inlet air temperature was found to be the main parameter to affect the bulk density, caking and water solubility index, when compared to maltodextrin concentration. By setting minimization of caking and maximization of water solubility index as the main determinants, the optimal parameters of 160°C inlet temperature and 15% (w/w) maltodextrin DE10 were generated, with a desirability of 0.697.

    CONCLUSIONS: The powder produced under optimal conditions (160°C and 15% w/w maltodextrin) had a low bulk density (480.01 kg/m3), low caking properties (0.17 change in cake height ratio), and a high solubility index (88.69). This indicates that the powder is stable to be stored (without caking) and will have good reconstitution when added to water.

    Matched MeSH terms: Solubility
  4. Khanuja HK, Awasthi R, Mehta M, Satija S, Aljabali AAA, Tambuwala MM, et al.
    Recent Pat Nanotechnol, 2021;15(4):351-366.
    PMID: 33357187 DOI: 10.2174/1872210514666201224103010
    BACKGROUND: Nanosuspensions are colloidal systems consisting of pure drug and stabilizers, without matrix or lyophilized into a solid matrix. Nanosuspensions improve the solubility of the drug both in the aqueous and organic phases. Nanosuspensions are also known as brick dust molecules, as they increase the dissolution of a system and improve absorption.

    METHODS: Extensive information related to nanosuspensions and its associated patents were collected using Pub Med and Google Scholar.

    RESULTS: Over the last decade nanosuspensions have attracted tremendous interest in pharmaceutical research. It provides unique features including, improved solubility, high drug loading capacity, and passive targeting. These particles are cost-effective, simple, and have lesser side effects with minimal dose requirements. However, the stability of nanosuspensions still warrants attention.

    CONCLUSION: Nanosuspensions play a vital role in handling the numerous drug entities with difficult physico-chemical characteristics such as solubility and can further aid with a range of routes that include nasal, transdermal, ocular, parenteral, pulmonary etc. This review highlights the relevance of nanosuspensions in achieving safe, effective and targeted drug delivery.

    Matched MeSH terms: Solubility
  5. Aziz HA, Peh KK, Tan YT
    Drug Dev Ind Pharm, 2007 Nov;33(11):1263-72.
    PMID: 18058323
    Curcumin, the main active constituent of turmeric herb (Curcuma longa L.) have been reported to possess many medicinal values. The application of curcumin in dermatological preparations is limited by their intense yellow color property, which stains the fabric and skin. The objectives of this study were to reduce the color staining effect and enhance the stability of curcumin via microencapsulation using gelatin simple coacervation method. As for curcumin, ethanol and acetone were used as coacervating solvents. Curcumin was dispersed in ethanol while dissolved in acetone. Irrespective of the types of coacervating solvents used, microencapsulation resolved the color-staining problem and enhanced the flow properties and photo-stability of curcumin. Nevertheless, it was found that more spherical curcumin microcapsules with higher yield, higher curcumin loading, and higher entrapment efficiency were obtained with acetone than ethanol. The in vitro release of curcumin after microencapsulation was slightly prolonged. Further evaluation of the effects of solubility of core materials in coacervating solvent or polymeric aqueous solution using six different drug compounds, namely, ketoconazole, ketoprofen, magnesium stearate, pseudoephedrine HCl, diclofenac sodium, and paracetamol, suggested that the solubility of core materials in aqueous polymeric solution determined the successful formation of microcapsules. Microcapsules could only be formed if the core materials were not dissolved in the aqueous polymeric solution while the core materials could either be dissolved or dispersed in the coacervating solvent. In summary, microencapsulation not only circumvents the color-staining problem but also improved the stability and flowability of curcumin. The solubility of core material in aqueous polymeric solution plays a pivotal role in determining the successful formation of microcapsules.
    Matched MeSH terms: Solubility
  6. Rodriguez O, Stone W, Schemitsch EH, Zalzal P, Waldman S, Papini M, et al.
    Heliyon, 2017 Oct;3(10):e00420.
    PMID: 29034340 DOI: 10.1016/j.heliyon.2017.e00420
    In an attempt to combat the possibility of bacterial infection and insufficient bone growth around metallic, surgical implants, bioactive glasses may be employed as coatings. In this work, silica-based and borate-based glass series were synthesized for this purpose and subsequently characterized in terms of antibacterial behavior, solubility and cytotoxicity. Borate-based glasses were found to exhibit significantly superior antibacterial properties and increased solubility compared to their silica-based counterparts, with BRT0 and BRT3 (borate-based glasses with 0 and 15 mol% of titanium dioxide incorporated, respectively) outperforming the remainder of the glasses, both borate and silicate based, in these respects. Atomic Absorption Spectroscopy confirmed the release of zinc ions (Zn(2+)), which has been linked to the antibacterial abilities of glasses SRT0, BRT0 and BRT3, with inhibition effectively achieved at concentrations lower than 0.7 ppm. In vitro cytotoxicity studies using MC3T3-E1 osteoblasts confirmed that cell proliferation was affected by all glasses in this study, with decreased proliferation attributed to a faster release of sodium ions over calcium ions in both glass series, factor known to slow cell proliferation in vitro.
    Matched MeSH terms: Solubility
  7. Khalil I, Julkapli NM, Yehye WA, Basirun WJ, Bhargava SK
    Materials (Basel), 2016 May 24;9(6).
    PMID: 28773528 DOI: 10.3390/ma9060406
    Graphene is a single-atom-thick two-dimensional carbon nanosheet with outstanding chemical, electrical, material, optical, and physical properties due to its large surface area, high electron mobility, thermal conductivity, and stability. These extraordinary features of graphene make it a key component for different applications in the biosensing and imaging arena. However, the use of graphene alone is correlated with certain limitations, such as irreversible self-agglomerations, less colloidal stability, poor reliability/repeatability, and non-specificity. The addition of gold nanostructures (AuNS) with graphene produces the graphene-AuNS hybrid nanocomposite which minimizes the limitations as well as providing additional synergistic properties, that is, higher effective surface area, catalytic activity, electrical conductivity, water solubility, and biocompatibility. This review focuses on the fundamental features of graphene, the multidimensional synthesis, and multipurpose applications of graphene-Au nanocomposites. The paper highlights the graphene-gold nanoparticle (AuNP) as the platform substrate for the fabrication of electrochemical and surface-enhanced Raman scattering (SERS)-based biosensors in diverse applications as well as SERS-directed bio-imaging, which is considered as an emerging sector for monitoring stem cell differentiation, and detection and treatment of cancer.
    Matched MeSH terms: Solubility
  8. Lee WH, Lai CW, Hamid SBA
    Materials (Basel), 2015 Aug 28;8(9):5702-5714.
    PMID: 28793530 DOI: 10.3390/ma8095270
    WO₃-decorated TiO₂ nanotube arrays were successfully synthesized using an in situ anodization method in ethylene glycol electrolyte with dissolved H₂O₂ and ammonium fluoride in amounts ranging from 0 to 0.5 wt %. Anodization was carried out at a voltage of 40 V for a duration of 60 min. By using the less stable tungsten as the cathode material instead of the conventionally used platinum electrode, tungsten will form dissolved ions (W(6+)) in the electrolyte which will then move toward the titanium foil and form a coherent deposit on the titanium foil. The fluoride ion content was controlled to determine the optimum chemical dissolution rate of TiO₂ during anodization to produce a uniform nanotubular structure of TiO₂ film. Nanotube arrays were then characterized using FESEM, EDAX, XRD, as well as Raman spectroscopy. Based on the FESEM images obtained, nanotube arrays with an average pore diameter of up to 65 nm and a length of 1.8 µm were produced. The tungsten element in the samples was confirmed by EDAX results which showed varying tungsten content from 0.22 to 2.30 at%. XRD and Raman results showed the anatase phase of TiO₂ after calcination at 400 °C for 4 h in air atmosphere. The mercury removal efficiency of the nanotube arrays was investigated by photoirradiating samples dipped in mercury chloride solution with TUV (Tube ultraviolet) 96W UV-B Germicidal light. The nanotubes with the highest aspect ratio (15.9) and geometric surface area factor (92.0) exhibited the best mercury removal performance due to a larger active surface area, which enables more Hg(2+) to adsorb onto the catalyst surface to undergo reduction to Hg⁰. The incorporation of WO₃ species onto TiO₂ nanotubes also improved the mercury removal performance due to improved charge separation and decreased charge carrier recombination because of the charge transfer from the conduction band of TiO₂ to the conduction band of WO₃.
    Matched MeSH terms: Solubility
  9. Sadri R, Hosseini M, Kazi SN, Bagheri S, Abdelrazek AH, Ahmadi G, et al.
    J Colloid Interface Sci, 2018 Jan 01;509:140-152.
    PMID: 28898734 DOI: 10.1016/j.jcis.2017.07.052
    In this study, we synthesized covalently functionalized graphene nanoplatelet (GNP) aqueous suspensions that are highly stable and environmentally friendly for use as coolants in heat transfer systems. We evaluated the heat transfer and hydrodynamic properties of these nano-coolants flowing through a horizontal stainless steel tube subjected to a uniform heat flux at its outer surface. The GNPs functionalized with clove buds using the one-pot technique. We characterized the clove-treated GNPs (CGNPs) using X-ray photoelectron spectroscopy (XPS) and transmission electron microscopy (TEM). We then dispersed the CGNPs in distilled water at three particle concentrations (0.025, 0.075 and 0.1wt%) in order to prepare the CGNP-water nanofluids (nano-coolants). We used ultraviolet-visible (UV-vis) spectroscopy to examine the stability and solubility of the CGNPs in the distilled water. There is significant enhancement in thermo-physical properties of CGNPs nanofluids relative those for distilled water. We validated our experimental set-up by comparing the friction factor and Nusselt number for distilled water obtained from experiments with those determined from empirical correlations, indeed, our experimental set-up is reliable and produces results with reasonable accuracy. We conducted heat transfer experiments for the CGNP-water nano-coolants flowing through the horizontal heated tube in fully developed turbulent condition. Our results are indeed promising since there is a significant enhancement in the Nusselt number and convective heat transfer coefficient for the CGNP-water nanofluids, with only a negligible increase in the friction factor and pumping power. More importantly, we found that there is a significant increase in the performance index, which is a positive indicator that our nanofluids have potential to substitute conventional coolants in heat transfer systems because of their overall thermal performance and energy savings benefits.
    Matched MeSH terms: Solubility
  10. Brishti, F.H., Zarei, M., Muhammad, S.K.S., Ismail-Fitry, M.R., Shukri, R., Saari, N.
    MyJurnal
    Mung bean is considered a ‘green pearl’ for its relatively high protein content; however, it has limited application as a raw material for industrial food products. As the potential use of mung beans relies on its protein behavior, this study characterized the functional properties of mung bean protein isolates and the results were compared with soy protein isolates. The protein isolates were prepared from mung bean and soy bean flours via extraction with 1 N NaOH, precipitated at pH 4, and subsequently freeze-dried. The amino acid profile as well as the hydrophilic and hydrophobic ratio of mung bean protein isolate, had been comparable with soy protein isolate. The water and oil absorption capacities as well as the denaturation temperature of mung bean protein isolate, were found to be similar with those of soy bean protein isolate. However, foaming capacity (89.66%) of mung bean protein isolate was higher than that of soy protein isolate (68.66%). Besides, least gelation concentration (LGC) of mung bean protein isolate (12%) was also close to LGC of soy protein isolate (14%), while the protein solubility was comparable between both the isolated proteins. The physical features of the textured mung bean were close to the commercial textured soy protein, which showed a heterogeneous and porous network like matrix when the mung bean flour was extruded to measure its potentiality to produce textured vegetable protein.all seaweed extracts. Results showed that extraction parameters had significant effect (p < 0.05) on the antioxidant compounds and antioxidant capacities of seaweed. Sargassum polycystum portrayed the most antioxidant compounds (37.41 ± 0.01 mg GAE/g DW and 4.54 ± 0.02 mg CE/g DW) and capacities (2.00 ± 0.01 μmol TEAC/g DW and 0.84 ± 0.01 μmol TEAC/g DW) amongst four species of seaweed.
    Matched MeSH terms: Solubility
  11. Shariffa, Y.N., Uthumporn, U., Karim, A.A., Zaibunnisa, A.H
    MyJurnal
    This study investigated the effect of annealing treatment (at 50°C for 72 h) on hydrolysis of tapioca and sweet potato starches using a raw starch hydrolyzing enzyme namely STARGEN 001 (a blend from fungal α-amylase and glucoamylase) at sub-gelatinization temperature (35°C) for 24 h. The degree of hydrolysis of the starches was evaluated based on the dextrose equivalent (DE) value. The hydrolyzed starches were then characterized in terms of its morphology, swelling power and solubility, gelatinization and pasting properties, amylose content and x-ray diffraction pattern. After 24 h of hydrolysis, annealed starches were hydrolyzed to a greater degree with higher DE value compared to native starches (40% vs 33% for tapioca; and 29% vs 24% for sweet potato starch). Scanning electron microscopy (SEM) micrographs revealed a more porous granules and rougher surface in annealed starches than their native counterparts. The swelling power and solubility of annealed starches decreased significantly. Annealing was found to affect the pasting properties of the starches appreciably and increase the starch gelatinization temperature. The amylose content in hydrolyzed annealed tapioca and sweet potato starches increased while no significant changes observed in the X-ray diffraction of those starches. This study shows that the annealing treatment can be used as a way to increase the degree of hydrolysis of tapioca and sweet potato starches at sub-gelatinization temperature using a raw starch hydrolyzing enzyme.
    Matched MeSH terms: Solubility
  12. Karim FT, Ghafoor K, Ferdosh S, Al-Juhaimi F, Ali E, Yunus KB, et al.
    J Food Drug Anal, 2017 Jul;25(3):654-666.
    PMID: 28911651 DOI: 10.1016/j.jfda.2016.11.017
    In order to improve the encapsulation process, a newly supercritical antisolvent process was developed to encapsulate fish oil using hydroxypropyl methyl cellulose as a polymer. Three factors, namely, temperature, pressure, and feed emulsion rate were optimized using response surface methodology. The suitability of the model for predicting the optimum response value was evaluated at the conditions of temperature at 60°C, pressure at 150 bar, and feed rate at 1.36 mL/min. At the optimum conditions, particle size of 58.35 μm was obtained. The surface morphology of the micronized fish oil was also evaluated using field emission scanning electron microscopy where it showed that particles formed spherical structures with no internal voids. Moreover, in vitro release of oil showed that there are significant differences of release percentage of oil between the formulations and the results proved that there was a significant decrease in the in vitro release of oil from the powder when the polymer concentration was high.
    Matched MeSH terms: Solubility
  13. Koh PT, Chuah JN, Talekar M, Gorajana A, Garg S
    Indian J Pharm Sci, 2013 May;75(3):291-301.
    PMID: 24082345 DOI: 10.4103/0250-474X.117434
    The aim of this study was to enhance the dissolution rate of efavirenz using solid dispersion systems (binary and ternary). A comparison between solvent and fusion method was also investigated. Solid dispersions of efavirenz were prepared using polyethylene glycol 8000, polyvinylpyrrolidone K30 alone and combination of both. Tween 80 was incorporated to obtain a ternary solid dispersion system. Dissolution tests were conducted and evaluated on the basis of cumulative percentage drug release and dissolution efficiency. Physicochemical characterizations of the solid dispersions were carried out using differential scanning calorimetric, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. Dissolution was remarkably improved in both systems compared to pure efavirenz (P<0.05). An optimum ratio was identified at a drug:polymer of 1:10. Incorporation of Tween 80 to 1:10 formulations formed using solvent method showed further improvement in the dissolution rate. Physicochemical characterization results suggested that efavirenz existed in the amorphous form in all the solid dispersion systems providing evidence of improvement in dissolution. No statistically significant difference (P>0.05) in dissolution was observed between the two methods. Binary and ternary solid dispersion systems both have showed a significant improvement in the dissolution rate of efavirenz. Formulations with only polyvinylpyrrolidone K30 showed best dissolution profile and 1:10 was identified as an optimum drug-polymer weight ratio.
    Matched MeSH terms: Solubility
  14. Ng WK, Lim TS, Lai NS
    Protein Expr Purif, 2016 11;127:73-80.
    PMID: 27412717 DOI: 10.1016/j.pep.2016.07.004
    Neonatal Fc-receptor (FcRn) with its affinity to immunoglobulin G (IgG) has been the subject of many pharmacokinetic studies in the past century. This protein is well known for its unique feature in maintaining the circulating IgG from degradation in blood plasma. FcRn is formed by non-covalent association between the α-chain with the β-2-microglobulin (β2m). Many studies have been conducted to produce FcRn in the laboratory, mainly using mammalian tissue culture as host for recombinant protein expression. In this study, we demonstrate a novel strategy to express the α-chain of FcRn using Escherichia coli as the expression host. The expression vector that carries the cDNA of the α-chain was transformed into expression host, Rosetta-gami 2 strain for inducible expression. The bacterial culture was grown in a modified growth medium which constitutes of terrific broth, sodium chloride (NaCl), glucose and betaine. A brief heat shock at 45 °C was carried out after induction, before the temperature for expression was reduced to 22 °C and grown for 16 h. The soluble form of the α-chain of FcRn expressed was tested in the ELISA and dot blot immunoassay to confirm its native functionality. The results implied that the α-chain of FcRn expressed using this method is functional and retains its pH-dependent affinity to IgG. Our study significantly suggests that the activity of human FcRn remain active and functional in the absence of β2m.
    Matched MeSH terms: Solubility
  15. Edueng K, Mahlin D, Gråsjö J, Nylander O, Thakrani M, Bergström CAS
    Molecules, 2019 Jul 27;24(15).
    PMID: 31357587 DOI: 10.3390/molecules24152731
    This study explores the effect of physical aging and/or crystallization on the supersaturation potential and crystallization kinetics of amorphous active pharmaceutical ingredients (APIs). Spray-dried, fully amorphous indapamide, metolazone, glibenclamide, hydrocortisone, hydrochlorothiazide, ketoconazole, and sulfathiazole were used as model APIs. The parameters used to assess the supersaturation potential and crystallization kinetics were the maximum supersaturation concentration (Cmax,app), the area under the curve (AUC), and the crystallization rate constant (k). These were compared for freshly spray-dried and aged/crystallized samples. Aged samples were stored at 75% relative humidity for 168 days (6 months) or until they were completely crystallized, whichever came first. The solid-state changes were monitored with differential scanning calorimetry, Raman spectroscopy, and powder X-ray diffraction. Supersaturation potential and crystallization kinetics were investigated using a tenfold supersaturation ratio compared to the thermodynamic solubility using the µDISS Profiler. The physically aged indapamide and metolazone and the minimally crystallized glibenclamide and hydrocortisone did not show significant differences in their Cmax,app and AUC when compared to the freshly spray-dried samples. Ketoconazole, with a crystalline content of 23%, reduced its Cmax,app and AUC by 50%, with Cmax,app being the same as the crystalline solubility. The AUC of aged metolazone, one of the two compounds that remained completely amorphous after storage, significantly improved as the crystallization kinetics significantly decreased. Glibenclamide improved the most in its supersaturation potential from amorphization. The study also revealed that, besides solid-state crystallization during storage, crystallization during dissolution and its corresponding pathway may significantly compromise the supersaturation potential of fully amorphous APIs.
    Matched MeSH terms: Solubility
  16. Huei Lim W, Jean Tan Y, Sin Lee C, Meng Er H, Fung Wong S
    Iran J Pharm Res, 2017;16(2):451-461.
    PMID: 28979300
    Palm-based lipid nanoparticle formulation loaded with griseofulvin was prepared by solvent-free hot homogenization method. The griseofulvin loaded lipid nanoparticles were prepared via stages of optimisation, by altering the high pressure homogenisation (HPH) parameters, screening on palm-based lipids and Tween series surfactants and selection of lipid to surfactant ratios. A HPLC method has been validated for the drug loading capacity study. The optimum HPH parameter was determined to be 1500 bar with 5 cycles and among the palm-based lipid materials; Lipid C (triglycerides) was selected for the preparation of lipid nanoparticles. Tween 80 was chosen from the Tween series surfactants for its highest saturated solubility of griseofulvin at 53.1 ± 2.16 µg/mL. The optimum formulation of the griseofulvin loaded lipid nanoparticles demonstrated nano-range of particle size (179.8 nm) with intermediate distribution index (PDI) of 0.306, zeta potential of -27.9 mV and drug loading of 0.77%. The formulation was stable upon storage for 1 month at room temperature (25 (°)C) and 45 (°)C with consistent drug loading capacity.
    Matched MeSH terms: Solubility
  17. Samiun WS, Ashari SE, Salim N, Ahmad S
    Int J Nanomedicine, 2020;15:1585-1594.
    PMID: 32210553 DOI: 10.2147/IJN.S198914
    BACKGROUND: Aripiprazole, which is a quinolinone derivative, has been widely used to treat schizophrenia, major depressive disorder, and bipolar disorder.

    PURPOSE: A Central Composite Rotatable Design (CCRD) of Response Surface Methodology (RSM) was used purposely to optimize process parameters conditions for formulating nanoemulsion containing aripiprazole using high emulsification methods.

    METHODS: This design is used to investigate the influences of four independent variables (overhead stirring time (A), shear rate (B), shear time (C), and the cycle of high-pressure homogenizer (D)) on the response variable namely, a droplet size (Y) of nanoemulsion containing aripiprazole.

    RESULTS: The optimum conditions suggested by the predicted model were: 120 min of overhead stirring time, 15 min of high shear homogenizer time, 4400 rpm of high shear homogenizer rate and 11 cycles of high-pressure homogenizer, giving a desirable droplet size of nanoemulsion containing aripiprazole of 64.52 nm for experimental value and 62.59 nm for predicted value. The analysis of variance (ANOVA) showed the quadratic polynomial fitted the experimental values with F-value (9.53), a low p-value (0.0003) and a non-significant lack of-fit. It proved that the models were adequate to predict the relevance response. The optimized formulation with a viscosity value of 3.72 mPa.s and pH value of 7.4 showed good osmolality value (297 mOsm/kg) and remained stable for three months in three different temperatures (4°C, 25°C, and 45°C).

    CONCLUSION: This proven that response surface methodology is an efficient tool to produce desirable droplet size of nanoemulsion containing aripiprazole for parenteral delivery application.

    Matched MeSH terms: Solubility
  18. Muhammad Nadzri N, Abdul AB, Sukari MA, Abdelwahab SI, Eid EE, Mohan S, et al.
    PMID: 23737847 DOI: 10.1155/2013/810632
    Zerumbone (ZER) isolated from Zingiber zerumbet was previously encapsulated with hydroxypropyl- β -cyclodextrin (HP β CD) to enhance ZER's solubility in water, thus making it highly tolerable in the human body. The anticancer effects of this new ZER-HP β CD inclusion complex via apoptosis cell death were assessed in this study for the first time in liver hepatocellular cells, HepG2. Apoptosis was ascertained by morphological study, nuclear stain, and sub-G1 cell population accumulation with G2/M arrest. Further investigations showed the release of cytochrome c and loss of mitochondrial membrane potential, proving mitochondrial dysfunction upon the ZER-HP β CD treatment as well as modulating proapoptotic and anti-apototic Bcl-2 family members. A significant increase in caspase 3/7, caspase 9, and caspase 8 was detected with the depletion of BID cleaved by caspase 8. Collectively, these results prove that a highly soluble inclusion complex of ZER-HP β CD could be a promising anticancer agent for the treatment of hepatocellular carcinoma in humans.
    Matched MeSH terms: Solubility
  19. Patil J, Pawde DM, Bhattacharya S, Srivastava S
    AAPS PharmSciTech, 2024 Apr 25;25(5):91.
    PMID: 38664316 DOI: 10.1208/s12249-024-02813-x
    Addressing poor solubility and permeability issues associated with synthetic drugs and naturally occurring active compounds is crucial for improving bioavailability. This review explores the potential of phospholipid complex formulation technology to overcome these challenges. Phospholipids, as endogenous molecules, offer a viable solution, with drugs complexed with phospholipids demonstrating a similar absorption mechanism. The non-toxic and biodegradable nature of the phospholipid complex positions it as an ideal candidate for drug delivery. This article provides a comprehensive exploration of the mechanisms underlying phospholipid complexes. Special emphasis is placed on the solvent evaporation method, with meticulous scrutiny of formulation aspects such as the phospholipid ratio to the drug and solvent. Characterization techniques are employed to understand structural and functional attributes. Highlighting the adaptability of the phospholipid complex, the review discusses the loading of various nanoformulations and emulsion systems. These strategies aim to enhance drug delivery and efficacy in various malignancies, including breast, liver, lung, cervical, and pancreatic cancers. The broader application of the drug phospholipid complex is showcased, emphasizing its adaptability in diverse oncological settings. The review not only explores the mechanisms and formulation aspects of phospholipid complexes but also provides an overview of key clinical studies and patents. These insights contribute to the intellectual and translational advancements in drug phospholipid complexes.
    Matched MeSH terms: Solubility
  20. Zhang Z, Miao W, Ji H, Lin Q, Li X, Sang S, et al.
    Food Chem, 2024 Dec 01;460(Pt 3):140792.
    PMID: 39126939 DOI: 10.1016/j.foodchem.2024.140792
    The low bioavailability of polyphenolic compounds due to poor solubility and stability is a major challenge. Encapsulation of polyphenols in zein-based composite nanoparticles can improve the water dispersion, stability, targeted delivery, and controlled release of polyphenols in the gastrointestinal tract. In this study, we investigated the fluorescence properties, bioactivity, and microstructural characteristics of polyphenols during digestion, revealing that zein nanoparticles protect polyphenols from gastric degradation and promote their sustained release in the small intestine. The effects of different ionic species and salt ion concentrations on the digestive properties of polyphenol complex delivery systems have also been explored. In addition, the formation of "protein corona" structures during digestion may affect bioavailability. These findings highlight the potential of nanoparticle formulations to improve polyphenol stability and absorption. The results of this study may provide new insights and references for the study of polyphenol bioavailability enhancement.
    Matched MeSH terms: Solubility
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