Displaying publications 121 - 140 of 422 in total

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  1. Rizwan M, Yahya R, Hassan A, Yar M, Abd Halim AA, Rageh Al-Maleki A, et al.
    J Mater Sci Mater Med, 2019 Jun 11;30(6):72.
    PMID: 31187295 DOI: 10.1007/s10856-019-6273-3
    The success of wound healing depends upon the proper growth of vascular system in time in the damaged tissues. Poor blood supply to wounded tissues or tissue engineered grafts leads to the failure of wound healing or rejection of grafts. In present paper, we report the synthesis of novel organosoluble and pro-angiogenic chitosan derivative (CSD) by the reaction of chitosan with 1,3-dimethylbarbituric acid and triethylorthoformate (TEOF). The synthesized material was characterized by FTIR and 13C-NMR to confirm the incorporated functional groups and new covalent connectivities. Biodegradability of the synthesized chitosan derivative was tested in the presence of lysozyme and was found to be comparable with CS. The cytotoxicity and apoptosis effect of new derivative was determined against gastric adenocarcinoma (AGS) cells and was found to be non-toxic. The CSD was found to be soluble in majority of organic solvents. It was blended with polycaprolactone (PCL) to form composite scaffolds. From an ex ovo CAM assay, it was noted that CSD stimulated the angiogenesis.
    Matched MeSH terms: Solubility
  2. Latif NHA, Rahim AA, Brosse N, Hussin MH
    Int J Biol Macromol, 2019 Jun 01;130:947-957.
    PMID: 30851323 DOI: 10.1016/j.ijbiomac.2019.03.032
    This study reports on the effects of unmodified autohydrolyzed ethanol organosolv lignin (AH EOL) and modified autohydrolyzed ethanol organosolv lignin on the structural characteristics and antioxidant properties upon incorporation of p-hydroxyacetophenone (AHP EOL). The lignin samples isolated from black liquor of oil palm fronds (OPF) were evaluated and compared using various complementary analyses; FTIR, 1H and 13C NMR spectroscopy, 2D-NMR spectroscopy (HMBC and HSQC), CHN, GPC, HPLC and thermal analyses (TGA and DSC). Chemically modified organosolv lignin (AHP EOL) provided lignin with lower molecular weight (Mw), which has smaller fragments that leads to higher solubility rate in water in comparison to unmodified organosolv lignin, AH EOL (DAHP EOL: 19.8% > DAH EOL: 14.0%). It was evident that the antioxidant properties of modified organosolv lignin has better reducing power in comparison to the unmodified organosolv lignin. Therefore, the functionalization of lignin polymers enhanced their antioxidant properties and structural features towards a various alternative approach in lignin-based applications.
    Matched MeSH terms: Solubility
  3. Maki MAA, Kumar PV, Cheah SC, Siew Wei Y, Al-Nema M, Bayazeid O, et al.
    ACS Omega, 2019 May 31;4(5):8767-8777.
    PMID: 31459966 DOI: 10.1021/acsomega.9b00109
    Several studies have shown that the mammalian target of rapamycin (mTOR) inhibitor; everolimus (EV) improves patient survival in several types of cancer. However, the meaningful efficacy of EV as a single agent for the treatment of colorectal cancer (CRC) has failed to be proven in multiple clinical trials. Combination therapy is one of the options that could increase the efficacy and decrease the toxicity of the anticancer therapy. This study revealed that the β-cyclodextrin (β-CD):FGF7 complex has the potential to improve the antiproliferative effect of EV by preventing FGF receptor activation and by enhancing EV cellular uptake and intracellular retention. Molecular docking techniques were used to investigate the possible interaction between EV, β-CD, and FGF7. Molecular docking insights revealed that β-CD and EV are capable to form a stable inclusion complex with FGF at the molecular level. The aqueous solubility of the inclusion complex was increased (3.1 ± 0.23 μM) when compared to the aqueous solubility of pure EV (1.7 ± 0.16 μM). In addition, the in vitro cytotoxic activity of a FGF7:β-CD:EV complex on Caco-2 cell line was investigated using real-time xCELLigence technology. The FGF7:β-CD:EV complex has induced apoptosis of Caco-2 cells and shown higher cytotoxic activity than the parent drug EV. With the multitargets effect of β-CD:FGF7 and EV, the antiproliferative effect of EV was remarkably improved as the IC50 value of EV was reduced from 9.65 ± 1.42 to 1.87 ± 0.33 μM when compared to FGF7:β-CD:EV complex activity. In conclusion, the findings advance the understanding of the biological combinational effects of the β-CD:FGF7 complex and EV as an effective treatment to combat CRC.
    Matched MeSH terms: Solubility
  4. Ang LF, Darwis Y, Koh RY, Gah Leong KV, Yew MY, Por LY, et al.
    Pharmaceutics, 2019 May 01;11(5).
    PMID: 31052413 DOI: 10.3390/pharmaceutics11050205
    Curcuminoids have been used for the management of burns and wound healing in traditional Chinese medicine practices but the wide application of curcuminoids as a healing agent for wounds has always been a known problem due to their poor solubility, bioavailability, colour staining properties, as well as due to their intense photosensitivity and the need for further formulation approaches to maximise their various properties in order for them to considerably contribute towards the wound healing process. In the present study, a complex coacervation microencapsulation was used to encapsulate curcuminoids using gelatin B and chitosan. This study also focused on studying and confirming the potential of curcuminoids in a microencapsulated form as a wound healing agent. The potential of curcuminoids for wound management was evaluated using an in vitro human keratinocyte cell (HaCaT) model and the in vivo heater-inflicted burn wound model, providing evidence that the antioxidant activities of both forms of curcuminoids, encapsulated or not, are higher than those of butylated hydroxyanisole and butylated hydroxytoluene in trolox equivalent antioxidant capacity (TEAC) and (2,2-diphenyl-1-picryl-hydrazyl-hydrate) (DPPH) studies. However, curcuminoids did not have much impact towards cell migration and proliferation in comparison with the negative control in the in vitro HaCaT study. The micoencapsulation formulation was shown to significantly influence wound healing in terms of increasing the wound contraction rate, hydroxyproline synthesis, and greater epithelialisation, which in turn provides strong justification for the incorporation of the microencapsulated formulation of curcuminoids as a topical treatment for burns and wound healing management as it has the potential to act as a crucial wound healing agent in healthcare settings.
    Matched MeSH terms: Solubility
  5. Bonthagarala B, Dasari V, Kotra V
    Ther Deliv, 2019 May 01;10(5):295-310.
    PMID: 31094300 DOI: 10.4155/tde-2019-0020
    Aim: The present study revolved around determining the effect of increase in the solubility of these drugs at the absorption site using ritonavir as a drug model. Materials & methods: Ritonavir per-oral tablets were prepared using versatile and nonionic surfactants having high solubilization rate, which were further marked with high rate of dissolution. The high rate of dissolution formula applied to the solid state characterization by means of transition electron microscopy, differential scanning calorimetry, scanning electron microscopy, X-ray diffraction and infrared spectroscopy. Results & conclusion: The drug bioavailability was seen to increase expressively by administration of liquisolid tablets as compared with conventional tablets.
    Matched MeSH terms: Solubility
  6. Philip ST, Abdulla AM, Ganapathy S, Vedam V, Rajeev V
    J Pharm Bioallied Sci, 2019 May;11(Suppl 2):S463-S467.
    PMID: 31198388 DOI: 10.4103/JPBS.JPBS_78_19
    Background: Changing lifestyle pattern and food habits has a deteriorating effect on dental tissues. Dental erosion is a pathological wear of hard tissues of teeth with increased consumption of acidic and carbonated drinks. Susceptibility to erosion in primary dentition is more compared to permanent dentition due to softer and disordered crystal structure of enamel.

    Objectives: The main aim of the study was to determine and compare the erosive potential of different fruit juices in frozen/unfrozen forms on primary teeth by studying the calcium dissolution.

    Materials and methods: pH of four different juices (pure) - apple, orange, citrus limetta (musumbi) and grapes were determined using a digital pH meter. The titratable acidity of these in frozen and unfrozen forms were determined by adding 0.2 ml of 1M NaOH to these to raise to pH=5.5(critical pH) and pH =7(neutral pH). Forty eight caries free deciduous anterior teeth specimens were prepared to study the calcium dissolution by atomic absorption spectrophotometer. The results were analysed for statistical significance using One-way Repeated Measures ANOVA and pair wise multiple comparison with Bonferroni correction.

    Results: Total titratable acidity and calcium dissolution were found to be significantly more in the initial thawed fruit juices.

    Conclusion: Frozen fruit juices had more buffering capacity and erosive potential than unfrozen forms. The study concluded that sucking on frozen fruit juices is more damaging to teeth than unfrozen forms because more of erosion is expected to occur in a frozen state.

    Matched MeSH terms: Solubility
  7. Sheshala R, Anuar NK, Abu Samah NH, Wong TW
    AAPS PharmSciTech, 2019 Apr 15;20(5):164.
    PMID: 30993407 DOI: 10.1208/s12249-019-1362-7
    This review highlights in vitro drug dissolution/permeation methods available for topical and transdermal nanocarriers that have been designed to modulate the propensity of drug release, drug penetration into skin, and permeation into systemic circulation. Presently, a few of USFDA-approved in vitro dissolution/permeation methods are available for skin product testing with no specific application to nanocarriers. Researchers are largely utilizing the in-house dissolution/permeation testing methods of nanocarriers. These drug release and permeation methods are pending to be standardized. Their biorelevance with reference to in vivo plasma concentration-time profiles requires further exploration to enable translation of in vitro data for in vivo or clinical performance prediction.
    Matched MeSH terms: Solubility
  8. K R, G B, Banat F, Show PL, Cocoletzi HH
    Int J Biol Macromol, 2019 Apr 01;126:1234-1243.
    PMID: 30584938 DOI: 10.1016/j.ijbiomac.2018.12.196
    Health hazards associated with usage of plastic films for food preservation demands for development of active films from non-toxic and antioxidant rich bio-sources. The reported work highlights the development, characterization and application studies of chitosan films enhanced for their antioxidant activity by mango leaf extract (MLE) incorporation. Effect of MLE variation (1-5%) on the morphology, optical nature, water exposure and mechanical characteristics of the chitosan-MLE composite films was studied. Increase in the MLE concentration resulted in films with increased thickness and decreased moisture content. Contact angle, water solubility and vapor permeability analysis demonstrated the reduced hydrophilicity and water vapor penetrability of the films due to MLE inclusion. MLE films possessed better tensile strength (maximum of 23.06 ± 0.19 MPa) with reduced elongation ratio than the pure chitosan film (18.14 ± 0.72 MPa). Antioxidants assessment in terms of total phenolic content, DPPH radical scavenging, ferric reducing power and ABTS radical scavenging showed improved antioxidant activity with the incremental amounts of MLE in the chitosan films. Microscopic studies revealed the smooth, compact and dense nature of the MLE-chitosan films favouring low oxygen transport rates. Application studies to cashew nuts preservation for 28 days storage indicated 56% higher oxidation resistance for the 5% MLE film than a commercial polyamide/polyethylene film. Results highlight the potential and promising nature of MLE impregnated chitosan films as suitable alternative for active packaging films for food preservation.
    Matched MeSH terms: Solubility
  9. Chik MW, Hussain Z, Zulkefeli M, Tripathy M, Kumar S, Majeed ABA, et al.
    Drug Deliv Transl Res, 2019 04;9(2):578-594.
    PMID: 29594914 DOI: 10.1007/s13346-018-0505-9
    Carbon nanotubes (CNTs) possess outstanding properties that could be useful in several technological, drug delivery, and diagnostic applications. However, their unique physical and chemical properties are hindered due to their poor solubility. This article review's the different ways and means of solubility enhancement of single-wall carbon nanotubes (SWNTs). The advantages of SWNTs over the multi-walled carbon nanotubes (MWNTs) and the method of non-covalent modification for solubility enhancement has been the key interest in this review. The review also highlights a few examples of dispersant design. The review includes some interesting utility of SWNTs being wrapped with polymer especially in biological media that could mediate proper drug delivery to target cells. Further, the use of wrapped SWNTs with phospholipids, nucleic acid, and amphiphillic polymers as biosensors is of research interest. The review aims at summarizing the developments relating to wrapped SWNTs to generate further research prospects in healthcare.
    Matched MeSH terms: Solubility
  10. Ruslan AR, Vadivelu VM
    J Environ Sci (China), 2019 Mar;77:148-155.
    PMID: 30573078 DOI: 10.1016/j.jes.2018.06.023
    The effect of pre-treatment of dewatered sludge using different nitrite concentrations and pH for microbial fuel cell (MFC) application was investigated. The results show that the addition of nitrite was feasible to increase the solubilization rate of the sludge and may reduce mass transfer limitation at the anode. This helped the MFC to reach higher voltage and to generate more power. The higher free nitrous acid (FNA) concentration under the acidic condition helped to increase sludge solubilization. However, under an alkaline condition, during which the FNA concentration was relatively low, the solubilization of the sludge was higher. The highest voltage and power density produced was 390 mV and 153 mW/m2, respectively, with the addition of nitrite at 100 mg-N/L and pH 9. Furthermore, it was found that elevated levels of FNA could inhibit electrogenic bacteria thus reducing power generation.
    Matched MeSH terms: Solubility
  11. Karim ME, Shetty J, Islam RA, Kaiser A, Bakhtiar A, Chowdhury EH
    Pharmaceutics, 2019 Feb 20;11(2).
    PMID: 30791612 DOI: 10.3390/pharmaceutics11020089
    Inorganic nanoparticles hold great potential in the area of precision medicine, particularly for treating cancer owing to their unique physicochemical properties, biocompatibility and improved pharmacokinetics properties compared to their organic counterparts. Here we introduce strontium sulfite nanoparticles as new pH-responsive inorganic nanocarriers for efficient transport of siRNAs into breast cancer cells. We employed the simplest nanoprecipitation method to generate the strontium sulfite nanoparticles (SSNs) and demonstrated the dramatic roles of NaCl and d-glucose in particle growth stabilization in order to produce even smaller nanosize particles (Na-Glc-SSN) with high affinity towards negatively charged siRNA, enabling it to efficiently enter the cancer cells. Moreover, the nanoparticles were found to be degraded with a small drop in pH, suggesting their potential capability to undergo rapid dissolution at endosomal pH so as to release the payload. While these particles were found to be nontoxic to the cells, they showed higher potency in facilitating cancer cell death through intracellular delivery and release of oncogene-specific siRNAs targeting ros1 and egfr1 mRNA transcripts, than the strontium sulfite particles prepared in absence of NaCl and d-glucose, as confirmed by growth inhibition assay. The mouse plasma binding analysis by Q-TOF LC-MS/MS demonstrated less protein binding to smaller particles of Na-Glc-SSNs. The biodistribution studies of the particles after 4 h of treatment showed Na-Glc-SSNs had less off-target distribution than SSNs, and after 24 h, all siRNAs were cleared from all major organs except the tumors. ROS1 siRNA with its potential therapeutic role in treating 4T1-induced breast tumor was selected for subsequent in vivo tumor regression study, revealing that ROS1 siRNA-loaded SSNs exerted more significant anti-tumor effects than Na-Glc-SSNs carrying the same siRNA following intravenous administration, without any systemic toxicity. Thus, strontium sulfite emerged as a powerful siRNA delivery tool with potential applications in cancer gene therapy.
    Matched MeSH terms: Solubility
  12. Long CM, Tang K, Chokshi H, Fotaki N
    AAPS PharmSciTech, 2019 Feb 13;20(3):113.
    PMID: 30761437 DOI: 10.1208/s12249-019-1317-z
    The aim of this study is to investigate the dissolution properties of poorly soluble drugs from their pure form and their amorphous formulation under physiological relevant conditions for oral administration based on surface dissolution ultraviolet (UV) imaging. Dissolution of two poorly soluble drugs (cefuroxime axetil and itraconazole) and their amorphous formulations (Zinnat® and Sporanox®) was studied with the Sirius Surface Dissolution Imager (SDI). Media simulating the fasted state conditions (compendial and biorelevant) with sequential media/flow rate change were used. The dissolution mechanism of cefuroxime axetil in simulated gastric fluid (SGF), fasted state simulated gastric fluid (FaSSGF) and simulated intestinal fluid (SIF) is predominantly swelling as opposed to the convective flow in fasted state simulated intestinal fluid (FaSSIF-V1), attributed to the effect of mixed micelles. For the itraconazole compact in biorelevant media, a clear upward diffusion of the dissolved itraconazole into the bulk buffer solution is observed. Dissolution of itraconazole from the Sporanox® compact is affected by the polyethylene glycol (PEG) gelling layer and hydroxypropyl methylcellulose (HPMC) matrix, and a steady diffusional dissolution pattern is revealed. A visual representation and a quantitative assessment of dissolution properties of poorly soluble compounds and their amorphous formulation can be obtained with the use of surface dissolution imaging under in vivo relevant conditions.
    Matched MeSH terms: Solubility
  13. Ismail I, Hwang YH, Bakhsh A, Joo ST
    Asian-Australas J Anim Sci, 2019 Feb;32(2):282-289.
    PMID: 30208691 DOI: 10.5713/ajas.18.0347
    OBJECTIVE: This study aimed to elucidate whether innovative sous vide treatment has a significant influence on the beef semitendinosus muscle as compared to common sous vide treatment and traditional cooking.

    METHODS: The innovative sous vide treatments were cooked at 45°C and 65°C for 6 h (SV45-65), common sous vide treatment at 45°C and 65°C for 3 h (SV45 and SV65) and traditional cooking at 75°C for 30 min (CON75). Water loss and cooking loss, as well as the physical properties (color and shear force) and chemical properties (protein and collagen solubility) of the treated meat, were investigated.

    RESULTS: The results obtained indicated that the innovative sous vide with double thermal treatment (SV45-65) and cooked with air presence (CON75) resulted to lower a* and higher b* values, respectively. The water loss and cooking loss increased when temperature increased from 45°C to 65°C, and lower water loss was recorded in SV45 and CON75. These samples presented higher water content and revealed strong correlation to protein solubility. Warner-Bratzler shear force (SF) analysis showed the marked interaction between cooking temperature and time. Sample cooked at a high temperature (CON75) and a long period (SV45-65) showed a significantly lower value of SF than sample SV65 (p<0.05). Interestingly, there was no difference in SF values between SV45-65 and CON75.

    CONCLUSION: The innovative sous vide treatment with double thermal effect appears an attractive cooking method as compared to common sous vide and traditional cooking method, as it has a potential for improving tenderness values of cooked beef semitendinosus muscle.

    Matched MeSH terms: Solubility
  14. Siram K, Divakar S, Raghavan CV, Marslin G, Rahman H, Franklin G
    Colloids Surf B Biointerfaces, 2019 Feb 01;174:443-450.
    PMID: 30497005 DOI: 10.1016/j.colsurfb.2018.11.033
    The physico-chemical properties of lipids influencing the solubilisation of imatinib mesylate (IM) in lipid matrix were evaluated and a statistical model to predict the same has been derived in the present study. After experimental quantification of IM solubility in various lipids, Hansen Hildebrand's total solubility parameters were calculated in order to study the role of various forces connected to lipid-drug interaction. To develop a relationship between the various descriptors of the lipids and experimental solubility of IM in lipids (% w/w), quantitative structure-solubility relationship (QSSR) was used. To generate equations that can predict the solubility of IM in lipids (%w/w), multiple linear regression was used. Amongst the various lipids tested, glyceryl monostearate and behenic acid solubilised the highest (6.19 ± 0.22%) and lowest (0.01 ± 0.01%) amounts of IM respectively. Our results suggested that alkyl chain length, polarity of the lipids, index of cohesive interaction in solids, estimated number of hydrogen bonds that would be accepted by the solute from water molecules in an aqueous solution, estimated number of hydrogen bonds that would be donated by the solute to water molecules in an aqueous solution and solvent accessible surface area collectively play a significant role in solubilising IM in the lipids. The equation developed could predict the solubility of IM in lipids with good accuracy (R2pred = 0.912).
    Matched MeSH terms: Solubility
  15. Ndlovu ST, Ullah N, Khan S, Ramharack P, Soliman M, de Matas M, et al.
    Drug Deliv Transl Res, 2019 Feb;9(1):284-297.
    PMID: 30387048 DOI: 10.1007/s13346-018-00596-w
    The aim of this study was to employ experimental and molecular modelling approaches to use molecular level interactions to rationalise the selection of suitable polymers for use in the production of stable domperidone (DOMP) nanocrystals with enhanced bioavailability. A low-energy antisolvent precipitation method was used for the preparation and screening of polymers for stable nanocrystals of DOMP. Ethyl cellulose was found to be very efficient in producing stable DOMP nanocrystals with particle size of 130 ± 3 nm. Moreover, the combination of hydroxypropyl methylcellulose and polyvinyl alcohol was also shown to be better in producing DOMP nanocrystals with smaller particle size (200 ± 3.5 nm). DOMP nanosuspension stored at 2-8 °C and at room temperature (25 °C) exhibited better stability compared to the samples stored at 40 °C. Crystallinity of the unprocessed and processed DOMP was monitored by differential scanning calorimetry and powder X-ray diffraction. DOMP nanocrystals gave enhanced dissolution rate compared to the unprocessed drug substance. DOMP nanocrystals at a dose of 10 mg/kg in rats showed enhanced bioavailability compared to the raw drug substance and marketed formulation. A significant increase in plasma concentration of 2.6 μg/mL with a significant decrease in time (1 h) to reach maximum plasma concentration was observed for DOMP nanocrystals compared to the raw DOMP. Molecular modelling studies provided underpinning knowledge at the molecular level of the DOMP-polymer nanocrystal interactions and substantiated the experimental studies. This included an understanding of the impact of polymers on the size of nanocrystals and their associated stability characteristics.
    Matched MeSH terms: Solubility
  16. Izadiyan Z, Basri M, Fard Masoumi HR, Abedi Karjiban R, Salim N, Kalantari K
    Mater Sci Eng C Mater Biol Appl, 2019 Jan 01;94:841-849.
    PMID: 30423770 DOI: 10.1016/j.msec.2018.10.015
    Nanoemulsions have been used as a drug carrier system, particularly for poorly water-soluble drugs. Sorafenib is a poorly soluble drug and also there is no parenteral treatment. The aim of this study is the development of nanoemulsions for intravenous administration of Sorafenib. The formulations were prepared by high energy emulsification method and optimized by using Response Surface Methodology (RSM). Here, the effect of independent composition variables of lecithin (1.16-2.84%, w/w), Medium-Chain Triglycerides (2.32-5.68%, w/w) and polysorbate 80 (0.58-1.42%, w/w) amounts on the properties of Sorafenib-loaded nanoemulsion was investigated. The three responses variables were particle size, zeta potential, and polydispersity index. Optimization of the conditions according to the three dependent variables was performed for the preparation of the Sorafenib-loaded nanoemulsions with the minimum value of particle size, suitable rage of zeta potential, and polydispersity index. A formulation containing 0.05% of Sorafenib kept its properties in a satisfactory range over the evaluated period. The composition with 3% Medium-Chain Triglycerides, 2.5% lecithin and 1.22% polysorbate 80 exhibited the smallest particle size and polydispersity index (43.17 nm and 0.22, respectively) with the zeta potential of -38.8 mV was the optimized composition. The fabricated nanoemulsion was characterized by the transmission electron microscope (TEM), viscosity, and stability assessment study. Also, the cytotoxicity result showed that the optimum formulations had no significant effect on a normal cell in a low concentration of the drug but could eliminate the cancer cells. The dose-dependent toxicity made it a suitable candidate for parenteral applications in the treatment of breast cancer. Furthermore, the optimized formulation indicated good storage stability for 3 months at different temperatures (4 ± 2 °C, 25 ± 2 °C and 45 ± 2 °C).
    Matched MeSH terms: Solubility
  17. Izadi E, Afshan G, Patel RP, Rao VM, Liew KB, Meor Mohd Affandi MMR, et al.
    Front Pharmacol, 2019;10:881.
    PMID: 31474853 DOI: 10.3389/fphar.2019.00881
    Counterfeit and substandard medicines are recognized as one of serious threats to public health. The product quality of antibacterial medicine will compromise patients' recovery and increase the chance of antibacterial resistance. The review aims to provide a summary of low quality levofloxacin issues and the risk factors as well as suggesting the aspects of product quality that need to be regulated strictly. Quality of the active ingredient, levofloxacin, has an important role to contribute to successful therapy. The poor quality of raw material, directly and indirectly, causes treatment failure as the presence of insufficient dose, mislabeled content, and poor dissolution characteristics can lead to lower bioavailability. Identifying and reporting these factors can potentially help in improving the quality of drug marketed in various developing countries and may also reduce the incidences of treatment failure. Dissolution test is used for testing the dissolution profiles and the rate of drug release from solid formulation such as oral formulations, thus providing information regarding the in vivo performance of a formulation and its bioequivalence. On the other hand, quality-testing procedures are used for comparing the quality of products.
    Matched MeSH terms: Solubility
  18. Krishnamoorthy R., Bibhu Prasad Panda, Shivashekaregowda N. K. H., Low B. S., Bhattamisra S. K.
    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
  19. GUI CHAN LEE, NORIZAH MHD. SARBON
    MyJurnal
    Plastics packaging is non-biodegradable and risks to human health and environmental pollution. In contrast, gelatin-based film lack of desired mechanical, thermal and water vapour barrier properties. Thus, this study aimed to investigate the mechanical and physical properties of bio-nanocomposite films based on chicken skin gelatin with different concentration of chitosan nanoparticles (CSNPs). Gelatin/CSNPs film solutions with different CSNPs concentration (0-8%, w/w) were stirred at 45oC for 30 min and oven-dried at 45oC. Film characterization determination includes tensile strength (TS), elongation at break (EAB), Young’s modulus (YM), water solubility, water vapour permeability (WVP), film morphology and melting temperature (Tm). Results of the study indicated that incorporation of CSNPs significantly influenced film properties. The addition of CSNPs increased the TS and YM value, which lead to stronger films than the pure chicken skin gelatin films. However the addition of CSNPs decreased the EAB value. Furthermore, WVP and water solubility significantly decreased (p < 0.05) by the addition of 6% CSNPs. Morphology images showed that increased CSNPs reduced the film’s amorphous character, especially in high level, in which higher CSNPs (8%) resulted in the aggregation of particles in the composites. The nano-reinforcement films showed higher thermal stability as compared to pure chicken skin gelatin films. In conclusion, the film with 6% CSNPs showed the best formulation, as it demonstrated high in TS, YM and Tm value, while low in EAB, water solubility and WVP value compared to other films. The results presented in this study showed the feasibility of using bio-nanocomposite technology to improve the properties of biopolymer films based on chicken skin gelatin.
    Matched MeSH terms: Solubility
  20. Wong KE, Ngai SC, Chan KG, Lee LH, Goh BH, Chuah LH
    Front Pharmacol, 2019;10:152.
    PMID: 30890933 DOI: 10.3389/fphar.2019.00152
    Colorectal cancer (CRC) is the third most prevalent form of cancer, after lung cancer and breast cancer, with the second highest death incidence. Over the years, natural compounds have been explored as an alternative to conventional cancer therapies such as surgery, radiotherapy, and chemotherapy. Curcumin, an active constituent of turmeric has been associated with various health benefits. It has gained much attention as an anticancer agent due to its ability to regulate multiple cell signaling pathways, including NF-κB, STAT3, activated protein-1 (AP-1), epidermal growth response-1 (Egr-1), and p53, which are crucial in cancer development and progression. Nevertheless, the clinical application of curcumin is greatly restricted because of its low water solubility, poor oral absorption, and rapid metabolism. These issues have led to the development of curcumin nanoformulations to overcome the limitations of the compound. Nanotechnology-based delivery systems have been widely used in improving the delivery of poorly-water soluble drugs. Besides, these systems also come with the added benefits of possible cellular targeting and improvement in cellular uptake. An ideal improved formulation should display a greater anticancer activity compared to free curcumin, and at the same time be non-toxic to the normal cells. In this review, we focus on the design and development of various nanoformulations to deliver curcumin for use in CRC such as liposomes, micelles, polymer nanoparticles, nanogels, cyclodextrin complexes, solid lipid nanoparticles (SLN), phytosomes, and gold nanoparticles. We also discuss the current pre-clinical and clinical evidences of curcumin nanoformulations in CRC therapy, analyse the research gap, and address the future direction of this research area.
    Matched MeSH terms: Solubility
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