Displaying publications 81 - 100 of 176 in total

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  1. Amekyeh H, Billa N, Yuen KH, Chin SL
    AAPS PharmSciTech, 2015 Aug;16(4):871-7.
    PMID: 25588365 DOI: 10.1208/s12249-014-0279-4
    The gastrointestinal (GI) transit behavior of and absorption from an amphotericin B (AmB) solid lipid nanoformulation (SLN) in rats was investigated. We aimed to estimate the gastric emptying time (GET) and cecal arrival time (CAT) of AmB SLN in rats as animal models. From these two parameters, an insight on the absorption window of AmB was ascertained. Three types of SLNs, AmB, paracetamol (PAR), and sulfasalazine (SSZ), were similarly formulated using beeswax/theobroma oil composite as the lipid matrix and characterized with regard to size, viscosity, density, migration propensity within agarose gel, in vitro drug release, morphology, gastrointestinal transit, and in vivo absorption. The GET and CAT were estimated indirectly using marker drugs: PAR and sulfapyridine (SP). All three types of SLNs exhibited identical properties with regard to z-average, viscosity, relative density, and propensity to migrate. PAR was absorbed rapidly from the small intestine following emptying of the SLNs giving the T50E (time for 50% absorption of PAR) to be 1.6 h. SP was absorbed after release and microbial degradation of SSZ from SLN in the colon with a lag time of 2 h post-administration, serving as the estimated cecal arrival time of the SLNs. AmB within SLN was favorably absorbed from the small intestine, albeit slowly.
    Matched MeSH terms: Calorimetry, Differential Scanning
  2. Tayyab S, Zaroog MS, Feroz SR, Mohamad SB, Malek SN
    Int J Pharm, 2015 Aug 1;491(1-2):352-8.
    PMID: 26142245 DOI: 10.1016/j.ijpharm.2015.06.042
    The interaction of tranilast (TRN), an antiallergic drug with the main drug transporter in human circulation, human serum albumin (HSA) was studied using isothermal titration calorimetry (ITC), fluorescence spectroscopy and in silico docking methods. ITC data revealed the binding constant and stoichiometry of binding as (3.21 ± 0.23) × 10(6)M(-1) and 0.80 ± 0.08, respectively, at 25°C. The values of the standard enthalpy change (ΔH°) and the standard entropy change (ΔS°) for the interaction were found as -25.2 ± 5.1 kJ mol(-1) and 46.9 ± 5.4 J mol(-1)K(-1), respectively. Both thermodynamic data and modeling results suggested the involvement of hydrogen bonding, hydrophobic and van der Waals forces in the complex formation. Three-dimensional fluorescence data of TRN-HSA complex demonstrated significant changes in the microenvironment around the protein fluorophores upon drug binding. Competitive drug displacement results as well as modeling data concluded the preferred binding site of TRN as Sudlow's site I on HSA.
    Matched MeSH terms: Calorimetry
  3. Liew CW, Ramesh S
    Carbohydr Polym, 2015 Jun 25;124:222-8.
    PMID: 25839815 DOI: 10.1016/j.carbpol.2015.02.024
    Biopolymer electrolytes containing corn starch, lithium hexafluorophosphate (LiPF6) and ionic liquid, 1-butyl-3-methylimidazolium hexafluorophosphate (BmImPF6) are prepared by solution casting technique. Temperature dependence-ionic conductivity studies reveal Vogel-Tamman-Fulcher (VTF) relationship which is associated with free volume theory. Ionic liquid-based biopolymer electrolytes show lower glass transition temperature (Tg) than ionic liquid-free biopolymer electrolyte. X-ray diffraction (XRD) studies demonstrate higher amorphous region of ionic liquid-added biopolymer electrolytes. In addition, the potential stability window of the biopolymer electrolyte becomes wider and stable up to 2.9V. Conclusively, the fabricated electric double layer capacitor (EDLC) shows improved electrochemical performance upon addition of ionic liquid into the biopolymer electrolyte. The specific capacitance of EDLC based on ionic liquid-added polymer electrolyte is relatively higher than that of ionic liquid-free polymer electrolyte as depicted in cyclic voltammogram.
    Matched MeSH terms: Calorimetry, Differential Scanning
  4. Feroz SR, Mohamad SB, Lee GS, Malek SN, Tayyab S
    Phytomedicine, 2015 Jun 01;22(6):621-30.
    PMID: 26055127 DOI: 10.1016/j.phymed.2015.03.016
    BACKGROUND: 6-Shogaol, one of the main bioactive constituents of Zingiber officinale has been shown to possess various therapeutic properties. Interaction of a therapeutic compound with plasma proteins greatly affects its pharmacokinetic and pharmacodynamic properties.

    PURPOSE: The present investigation was undertaken to characterize the interaction between 6-shogaol and the main in vivo transporter, human serum albumin (HSA).

    METHODS: Various binding characteristics of 6-shogaol-HSA interaction were studied using fluorescence spectroscopy. Thermal stability of 6-shogaol-HSA system was determined by circular dichroism (CD) and differential scanning calorimetric (DSC) techniques. Identification of the 6-shogaol binding site on HSA was made by competitive drug displacement and molecular docking experiments.

    RESULTS: Fluorescence quench titration results revealed the association constant, Ka of 6-shogaol-HSA interaction as 6.29 ± 0.33 × 10(4) M(-1) at 25 ºC. Values of the enthalpy change (-11.76 kJ mol(-1)) and the entropy change (52.52 J mol(-1) K(-1)), obtained for the binding reaction suggested involvement of hydrophobic and van der Waals forces along with hydrogen bonds in the complex formation. Higher thermal stability of HSA was noticed in the presence of 6-shogaol, as revealed by DSC and thermal denaturation profiles. Competitive ligand displacement experiments along with molecular docking results suggested the binding preference of 6-shogaol for Sudlow's site I of HSA.

    CONCLUSION: All these results suggest that 6-shogaol binds to Sudlow's site I of HSA through moderate binding affinity and involves hydrophobic and van der Waals forces along with hydrogen bonds.

    Matched MeSH terms: Calorimetry, Differential Scanning
  5. Tan IS, Lee KT
    Bioresour Technol, 2015 May;184:386-94.
    PMID: 25465785 DOI: 10.1016/j.biortech.2014.10.146
    A novel concept for the synthesis of a stable polymer hybrid matrix bead was developed in this study. The beads were further applied for enzyme immobilization to produce stable and active biocatalysts with low enzyme leakage, and high immobilization efficiency, enzyme activity, and recyclability. The immobilization conditions, including PEI concentration, activation time and pH of the PEI solution were investigated and optimized. All formulated beads were characterized for its functionalized groups, composition, surface morphology and thermal stability. Compared with the free β-glucosidase, the immobilized β-glucosidase on the hybrid matrix bead was able to tolerate broader range of pH values and higher reaction temperature up to 60 °C. The immobilized β-glucosidase was then used to hydrolyse pretreated macroalgae cellulosic residue (MCR) for the production of reducing sugar and a hydrolysis yield of 73.4% was obtained. After repeated twelve runs, immobilized β-glucosidase retained about 75% of its initial activity.
    Matched MeSH terms: Calorimetry, Differential Scanning
  6. Fareez IM, Lim SM, Mishra RK, Ramasamy K
    Int J Biol Macromol, 2015 Jan;72:1419-28.
    PMID: 25450046 DOI: 10.1016/j.ijbiomac.2014.10.054
    The vulnerability of probiotics at low pH and high temperature has limited their optimal use as nutraceuticals. This study addressed these issues by adopting a physicochemical driven approach of incorporating Lactobacillus plantarum LAB12 into chitosan (Ch) coated alginate-xanthan gum (Alg-XG) beads. Characterisation of Alg-XG-Ch, which elicited little effect on bead size and polydispersity, demonstrated good miscibility with improved bead surface smoothness and L. plantarum LAB12 entrapment when compared to Alg, Alg-Ch and Alg-XG. Sequential incubation of Alg-XG-Ch in simulated gastric juice and intestinal fluid yielded high survival rate of L. plantarum LAB12 (95%) at pH 1.8 which in turn facilitated sufficient release of probiotics (>7 log CFU/g) at pH 6.8 in both time- and pH-dependent manner. Whilst minimising viability loss at 75 and 90 °C, Alg-XG-Ch improved storage durability of L. plantarum LAB12 at 4 °C. The present results implied the possible use of L. plantarum LAB12 incorporated in Alg-XG-Ch as new functional food ingredient with health claims.
    Matched MeSH terms: Calorimetry, Differential Scanning
  7. Khanmirzaei MH, Ramesh S, Ramesh K
    Sci Rep, 2015;5:18056.
    PMID: 26659087 DOI: 10.1038/srep18056
    Gel polymer electrolytes using imidazolium based ionic liquids have attracted much attention in dye-sensitized solar cell applications. Hydroxypropyl cellulose (HPC), sodium iodide (NaI), 1-methyl-3-propylimidazolium iodide (MPII) as ionic liquid (IL), ethylene carbonate (EC) and propylene carbonate (PC) are used for preparation of non-volatile gel polymer electrolyte (GPE) system (HPC:EC:PC:NaI:MPII) for dye-sensitized solar cell (DSSC) applications. The highest ionic conductivity of 7.37 × 10(-3) S cm(-1) is achieved after introducing 100% of MPII with respect to the weight of HPC. Temperature-dependent ionic conductivity of gel polymer electrolytes is studied in this work. XRD patterns of gel polymer electrolytes are studied to confirm complexation between HPC polymer, NaI and MPII. Thermal behavior of the GPEs is studied using simultaneous thermal analyzer (STA) and differential scanning calorimetry (DSC). DSSCs are fabricated using gel polymer electrolytes and J-V centeracteristics of fabricated dye sensitized solar cells were analyzed. The gel polymer electrolyte with 100 wt.% of MPII ionic liquid shows the best performance and energy conversion efficiency of 5.79%, with short-circuit current density, open-circuit voltage and fill factor of 13.73 mA cm(-2), 610 mV and 69.1%, respectively.
    Matched MeSH terms: Calorimetry, Differential Scanning
  8. Ng WK, Saiful Yazan L, Yap LH, Wan Nor Hafiza WA, How CW, Abdullah R
    Biomed Res Int, 2015;2015:263131.
    PMID: 25632388 DOI: 10.1155/2015/263131
    Thymoquinone (TQ) has been shown to exhibit antitumor properties. Thymoquinone-loaded nanostructured lipid carrier (TQ-NLC) was developed to improve the bioavailability and cytotoxicity of TQ. This study was conducted to determine the cytotoxic effects of TQ-NLC on breast cancer (MDA-MB-231 and MCF-7) and cervical cancer cell lines (HeLa and SiHa). TQ-NLC was prepared by applying the hot high pressure homogenization technique. The mean particle size of TQ-NLC was 35.66 ± 0.1235 nm with a narrow polydispersity index (PDI) lower than 0.25. The zeta potential of TQ-NLC was greater than -30 mV. Polysorbate 80 helps to increase the stability of TQ-NLC. Differential scanning calorimetry showed that TQ-NLC has a melting point of 56.73°C, which is lower than that of the bulk material. The encapsulation efficiency of TQ in TQ-NLC was 97.63 ± 0.1798% as determined by HPLC analysis. TQ-NLC exhibited antiproliferative activity towards all the cell lines in a dose-dependent manner which was most cytotoxic towards MDA-MB-231 cells. Cell shrinkage was noted following treatment of MDA-MB-231 cells with TQ-NLC with an increase of apoptotic cell population (P < 0.05). TQ-NLC also induced cell cycle arrest. TQ-NLC was most cytotoxic towards MDA-MB-231 cells. It induced apoptosis and cell cycle arrest in the cells.
    Matched MeSH terms: Calorimetry, Differential Scanning
  9. Madan JR, Pawar KT, Dua K
    Int J Pharm Investig, 2015 Apr-Jun;5(2):114-20.
    PMID: 25838997 DOI: 10.4103/2230-973X.153390
    Low aqueous solubility is a major problem faced during formulation development of new drug molecules. Lurasidone HCl (LRD) is an antipsychotic agent specially used in the treatments of schizophrenia and is a good example of the problems associated with low aqueous solubility. Lurasidone is practically insoluble in water, has poor bioavailability and slow onset of action and therefore cannot be given in emergency clinical situations like schizophrenia. Hence, purpose of this research was to provide a fast dissolving oral dosage form of Lurasidone. This dosage form can provide quick onset of action by using the concept of mixed hydrotropy. Initially, solubility of LRD was determined individually in nicotinamide, sodium citrate, urea and sodium benzoate at concentration of 10, 20, 30 and 40% w/v solutions using purified water as a solvent. Highest solubility was obtained in 40% sodium benzoate solution. In order to decrease the individual hydrotrope concentration mixed hydrotropic agents were used. Highest solubility was obtained in 15:20:5 ratio of Nicotinamide + sodium benzoate + sodium citrate. This optimized combination was utilized in the preparation of solid dispersions by using distilled water as a solvent. Solid dispersions were evaluated for X-ray diffraction, differential scanning calorimetry and Fourier-transform infrared to show no drug-hydrotropes interaction has occurred. This solid dispersion was compressed to form fast dissolving tablets. Dissolution studies of prepared tablets were done using USP Type II apparatus. The batch L3 tablets show 88% cumulative drug release within 14 min and in vitro dispersion time was 32 min. It was concluded that the concept of mixed hydrotropic solid dispersion is novel, safe and cost-effective technique for enhancing the bioavailability of poorly water-soluble drugs. The miraculous enhancement in solubility and bioavailability of Lurasidone is clear indication of the potential of mixed hydrotropy to be used in future for other poorly water-soluble drugs in which low bioavailability is a major concern.
    Matched MeSH terms: Calorimetry, Differential Scanning
  10. Nurrulhidayah, A.F., Arieff, S.R., Rohman, A., Amin, I., Shuhaimi, M., Khatib, A.
    MyJurnal
    Differential scanning calorimetry (DSC) is developed and used for detection of butter adulteration with lard. Butter has the similar characteristics to lard makes lard a desirable adulterant in butter. DSC provides unique thermal profiling for lard and butter. In the heating thermogram of the mixture, there was one major endothermic peak (peak A) with a smaller shoulder peak embedded in the major peak that gradually smoothed out to the major peak as the lard percent increased. In the cooling thermogram, there were one minor peak (peak B) and two major exothermic peaks, peak C which increased as lard percent increased and peak D which decreased in size as the lard percent increased. From Stepwise Multiple Linear Regression (SMLR) analysis, two independent variables were found to be able to predict lard percent adulteration in butter with R2 (adjusted) of 95.82. The SMLR equation of lard percent adulteration in butter is 293.1 - 11.36 (Te A) - 2.17 (Tr D); where Te A is the endset of peak A and Tr D is the range of thermal transition for peak D. These parameters can serve as a good measurement parameter in detecting lard adulteration in butter. DSC is a very useful means for halal screening technique to enhance the authenticity of Halal process.
    Matched MeSH terms: Calorimetry, Differential Scanning
  11. Mat Uzir Wahi, Azman Hassan, Akos Noel Ibrahim, Nurhayati Ahmad Zawawi, Kunasegeran K
    Sains Malaysiana, 2015;44:1615-1623.
    Polylactic acid (PLA)/Epoxidized natural rubber (ENR-50) blends were prepared by melt extrusion followed by injection
    molding to fabricate the test samples. The effect of ENR-50 loadings on the morphological, mechanical, chemical
    resistance and water absorption properties of the blends were studied using standard methods. The toughness of the
    blend improved with ENR loading up to 20 wt. % but flexural and tensile strength decreased. The balanced mechanical
    properties were obtained at 20 wt. % ENR-50 loading. SEM showed good distribution and increased ENR particle size
    as ENR content increased from 10 to 30 wt. %. The differential scanning calorimeter (DSC) showed a steady drop in
    crystallization temperature (Tc
    ) as ENR content increases while the glass transition temperature (Tg
    ) remained unchanged.
    Water absorption was observed to increase with ENR loadings. Increase in ENR content was also observed to reduce the
    chemical resistance of the blends.
    Matched MeSH terms: Calorimetry, Differential Scanning
  12. Zulkifli FH, Hussain FSJ, Rasad MSBA, Mohd Yusoff M
    Carbohydr Polym, 2014 Dec 19;114:238-245.
    PMID: 25263887 DOI: 10.1016/j.carbpol.2014.08.019
    In this study, a novel fibrous membrane of hydroxyethyl cellulose (HEC)/poly(vinyl alcohol) blend was successfully fabricated by electrospinning technique and characterized. The concentration of HEC (5%) with PVA (15%) was optimized, blended in different ratios (30-50%) and electrospun to get smooth nanofibers. Nanofibrous membranes were made water insoluble by chemically cross-linking by glutaraldehyde and used as scaffolds for the skin tissue engineering. The microstructure, morphology, mechanical and thermal properties of the blended HEC/PVA nanofibrous scaffolds were characterized by scanning electron microscope, Fourier transform infrared spectroscopy, differential scanning colorimetry, universal testing machine and thermogravimetric analysis. Cytotoxicity studies on these nanofibrous scaffolds were carried out using human melanoma cells by the MTT assays. The cells were able to attach and spread in the nanofibrous scaffolds as shown by the SEM images. These preliminary results show that these nanofibrous scaffolds that supports cell adhesion and proliferation is promising for skin tissue engineering.
    Matched MeSH terms: Calorimetry, Differential Scanning
  13. Dahimi O, Rahim AA, Abdulkarim SM, Hassan MS, Hashari SB, Mashitoh AS, et al.
    Food Chem, 2014 Sep 1;158:132-8.
    PMID: 24731324 DOI: 10.1016/j.foodchem.2014.02.087
    The adulteration of edible fats is a kind of fraud that impairs the physical and chemical features of the original lipid materials. It has been detected in various food, pharmaceutical and cosmeceutical products. Differential scanning calorimetry (DSC) is the robust thermo-analytical machine that permits to fingerprint the primary crystallisation of triacylglycerols (TAGs) molecules and their transition behaviours. The aims of this study was to assess the cross-contamination caused by lard concentration of 0.5-5% in the mixture systems containing beef tallow (BT) and chicken fat (CF) separately. TAGs species of pure and adulterated lipids in relation to their crystallisation and melting parameters were studied using principal components analysis (PCA). The results showed that by using the heating profiles the discrimination of LD from BT and CF was very clear even at low dose of less than 1%. Same observation was depicted from the crystallisation profiles of BT adulterated by LD doses ranging from 0.1% to 1% and from 2% to 5%, respectively. Furthermore, CF adulterated with LD did not exhibit clear changes on its crystallisation profiles. Consequently, DSC coupled with PCA is one of the techniques that might use to monitor and differentiate the minimum adulteration levels caused by LD in different animal fats.
    Matched MeSH terms: Calorimetry, Differential Scanning/methods*
  14. Jamil SNAM, Daik R, Ahmad I
    Materials (Basel), 2014 Sep 01;7(9):6207-6223.
    PMID: 28788187 DOI: 10.3390/ma7096207
    A synthesis of acrylonitrile (AN)/butyl acrylate (BA)/fumaronitrile (FN) and AN/EHA (ethyl hexyl acrylate)/FN terpolymers was carried out by redox polymerization using sodium bisulfite (SBS) and potassium persulphate (KPS) as initiator at 40 °C. The effect of comonomers, BA and EHA and termonomer, FN on the glass transition temperature (Tg) and stabilization temperature was studied using Differential Scanning Calorimetry (DSC). The degradation behavior and char yield were obtained by Thermogravimetric Analysis. The conversions of AN, comonomers (BA and EHA) and FN were 55%-71%, 85%-91% and 76%-79%, respectively. It was found that with the same comonomer feed (10%), the Tg of AN/EHA copolymer was lower at 63 °C compared to AN/BA copolymer (70 °C). AN/EHA/FN terpolymer also exhibited a lower Tg at 63 °C when compared to that of the AN/BA/FN terpolymer (67 °C). By incorporating BA and EHA into a PAN system, the char yield was reduced to ~38.0% compared to that of AN (~47.7%). It was found that FN reduced the initial cyclization temperature of AN/BA/FN and AN/EHA/FN terpolymers to 228 and 221 °C, respectively, in comparison to that of AN/BA and AN/EHA copolymers (~260 °C). In addition, FN reduced the heat liberation per unit time during the stabilization process that consequently reduced the emission of volatile group during this process. As a result, the char yields of AN/BA/FN and AN/EHA/FN terpolymers are higher at ~45.1% and ~43.9%, respectively, as compared to those of AN/BA copolymer (37.1%) and AN/EHA copolymer (38.0%).
    Matched MeSH terms: Calorimetry, Differential Scanning
  15. Kumar GP, Phani AR, Prasad RG, Sanganal JS, Manali N, Gupta R, et al.
    Int J Pharm, 2014 Aug 25;471(1-2):146-52.
    PMID: 24858388 DOI: 10.1016/j.ijpharm.2014.05.033
    Enrofloxacin is a fluoroquinolone derivative used for treating urinary tract, respiratory and skin infections in animals. However, low solubility and low bioavailability prevented it from using on humans. Polyvinylpyrrolidone (PVP) is an inert, non toxic polymer with excellent hydrophilic properties, besides it can enhance bioavailability by forming drug polymer conjugates. With the aim of increasing solubility and bioavailability, enrofloxacin thin films were prepared using PVP as a polymer matrix. The obtained oral thin films exhibited excellent uniformity and mechanical properties. Swelling properties of the oral thin films revealed that the water uptake was enhanced by 21%. The surface pH has been found to be 6.8±0.1 indicating that these films will not cause any irritation to oral mucosa. FTIR data of the oral thin films indicated physical interaction between drug and polymer. SEM analysis revealed uniform distribution of drug in polymer matrix. In vitro drug release profiles showed enhanced release profiles (which are also pH dependant) for thin films compared to pure drug. Antibacterial activity was found to be dose dependent and maximum susceptibility was found on Klebsiella pneumonia making this preparation more suitable for respiratory infections.
    Matched MeSH terms: Calorimetry, Differential Scanning
  16. Mishra RK, Ramasamy K, Lim SM, Ismail MF, Majeed AB
    J Mater Sci Mater Med, 2014 Aug;25(8):1925-39.
    PMID: 24831081 DOI: 10.1007/s10856-014-5228-y
    The present study investigates the development of methyl cellulose (MC)-sodium alginate (SA)-montmorillonite (MMT) clay based bionanocomposite films with interesting wound healing properties. The differential scanning calorimetry analysis of the composite films revealed presence of single glass transition temperature (Tg) confirming the miscible nature of the ternary blended films. The increase in MMT ratio in the composite films reduced the mobility of biopolymer chains (MC/SA) which increased the Tg of the film. Thermogravimetric analysis showed that dispersion of clay (MMT) at nano level significantly delayed the weight loss that correlated with higher thermal stability of the composite films. It was observed that the developed films were able to exhibit antimicrobial activity against four typical pathogenic bacteria found in the presence of wound. The developed films were able to significantly inhibit (10 mg/ml) the growth of Enterococcus faecium and Pseudomonas aeruginosa. In vitro scratch assay indicated potential wound closure activities of MC-2-4 bionanocomposite films at their respective highest subtoxic doses. In conclusion, these ternary bionanocomposite films were found to be promising systems for wound healing applications.
    Matched MeSH terms: Calorimetry, Differential Scanning
  17. Salehabadi A, Bakar MA, Bakar NHHA
    Materials (Basel), 2014 Jun 13;7(6):4508-4523.
    PMID: 28788689 DOI: 10.3390/ma7064508
    Multi-component nanohybrids comprising of organo-modified montmorillonite (MMT) and immiscible biopolymer blends of poly(3-hydroxybutyrate) (PHB) and epoxidized natural rubber (ENR-50) were prepared by solvent casting technique. The one and three dimensional morphology of PHB/ENR-50/MMT systems were studied using Polarizing Optical Microscopy (POM) and Scanning Electron Microscopy (SEM). Differential scanning calorimetry (DSC) technique was used to evaluate the thermal properties of the nanohybrids. The melting temperature (Tm) and enthalpy of melting (ΔHm) of PHB decrease with respect to the increase in ENR-50 as well as MMT content. The non-isothermal decomposition of the nanohybrids was studied using thermogravimetric (TG-DTG) analysis. FTIR-ATR spectra supported ring opening of the epoxide group via reaction with carboxyl group of PHB and amines of organic modifier. The reaction mechanism towards the formation of the nanohybrids is proposed.
    Matched MeSH terms: Calorimetry, Differential Scanning
  18. Kumar BS, Saraswathi R, Kumar KV, Jha SK, Venkates DP, Dhanaraj SA
    Drug Deliv, 2014 May;21(3):173-84.
    PMID: 24102185 DOI: 10.3109/10717544.2013.840690
    Novel LNCs (lipid nanocrystals) were developed with an aim to improve the solubility, stability and targeting efficiency of the model drug glibenclamide (GLB). PEG 20000, Tween 80 and soybean lecithin were used as polymer, surfactant and complexing agent, respectively. GLB nanocrystals (NCs) were prepared by precipitation process and complexed using hot and cold melt technique. The LNCs were evaluated by drug loading, saturation solubility (SL), optical clarity, in vitro dissolution, solid state characterization, in vivo and stability analysis. LNCs exhibited a threefold increase in SL and a higher dissolution rate than GLB. The percentage dissolution efficiency was found to decrease with increase in PEG 20000. The average particle size was in the range of 155-842 nm and zeta potential values tend to increase after complexation. X-ray powder diffractometry and differential scanning calorimetry results proved the crystallinity prevailed in the samples. Spherical shaped particles (<1000 nm) with a lipid coat on the surface were observed in scanning electron microscopy analysis. Fourier transform infrared results proved the absence of interaction between drug and polymer and stability study findings proved that LNCs were stable. In vivo study findings showed a decrease in drug concentration to pancreas in male Wistar rats. It can be concluded that LNCs are could offer enhanced solubility, dissolution rate and stability for poorly water soluble drugs. The targeting efficiency of LNCs was decreased and further membrane permeability studies ought to be carried out.
    Matched MeSH terms: Calorimetry, Differential Scanning
  19. Tan SW, Billa N
    AAPS PharmSciTech, 2014 Apr;15(2):287-95.
    PMID: 24318197 DOI: 10.1208/s12249-013-0056-9
    We aimed to investigate the effects that natural lipids, theobroma oil (TO) and beeswax (BW), might have on the physical properties of formulated nanoparticles and also the degree of expulsion of encapsulated amphotericin B (AmB) from the nanoparticles during storage. Lecithin and sodium cholate were used as emulsifiers whilst oleic acid (OA) was used to study the influence of the state of orderliness/disorderliness within the matrices of the nanoparticles on the degree of AmB expulsion during storage. BW was found to effect larger z-average diameter compared with TO. Lecithin was found to augment the stability of the nanoparticles imparted by BW and TO during storage. An encapsulation efficiency (%EE) of 59% was recorded when TO was the sole lipid as against 42% from BW. In combination however, the %EE dropped to 39%. When used as sole lipid, TO or BW formed nanoparticles with comparatively higher enthalpies, 21.1 and 23.3 J/g respectively, which subsequently caused significantly higher degree of AmB expulsion, 81 and 83% respectively, whilst only 11.8% was expelled from a binary TO/BW mixture. A tertiary TO/BW/OA mixture registered the lowest enthalpy at 8.07 J/g and expelled 12.6% of AmB but encapsulated only 22% of AmB. In conclusion, nanoparticles made from equal concentrations of TO and BW produced the most desirable properties and worthy of further investigations.
    Matched MeSH terms: Calorimetry, Differential Scanning
  20. Venkata Srikanth M, Songa AS, Nali SR, Battu JR, Kolapalli VR
    Drug Dev Ind Pharm, 2014 Jan;40(1):33-45.
    PMID: 23317339 DOI: 10.3109/03639045.2012.744416
    The objective of the present investigation was to study the applicability of thermal sintering technique for the development of gastric floating tablets of propranolol HCl. Formulations were prepared using four independent variables, namely (i) polymer quantity, (ii) sodium bicarbonate concentration, (iii) sintering temperature and (iv) sintering time. Floating lag time and t95 were taken as dependent variables. Tablets were prepared by the direct compression method and were evaluated for physicochemical properties, in vitro buoyancy and dissolution studies. From the drug release studies, it was observed that drug retarding property mainly depends upon the sintering temperature and time of exposure. The statistically optimized formulation (PTSso) was characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry studies, and no significant chemical interaction between drug and polymer was observed. Optimized formulation was stable at accelerated conditions for a period of six months. PTSso was evaluated for in vivo buoyancy studies in humans for both fed and fasted states and found that gastric residence time of the floating tablets were enhanced by fed stage but not in fasted state. Optimized formulation PTSso and commercial formulation Ciplar LA 80 were subjected to bioavailability studies in healthy human volunteers by estimating pharmacokinetic parameters such as Cmax, Tmax, area under curve (AUC), elimination rate constant (Kel), biological half-life (t1/2) and mean residence time (MRT). There was a significant increase in the bioavailability of the propranolol HCl from PTSso formulation, which was evident from increased AUC levels and larger MRT values than Ciplar LA 80.
    Matched MeSH terms: Calorimetry, Differential Scanning
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