Displaying publications 81 - 100 of 422 in total

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  1. Evaluation of processed green and ripe mango peel and pulp flours (Mangifera indica var. Chokanan) in terms of chemical composition, antioxidant compounds and functional properties
    Abdul Aziz NA, Wong LM, Bhat R, Cheng LH
    J Sci Food Agric, 2012 Feb;92(3):557-63.
    PMID: 25363645 DOI: 10.1002/jsfa.4606
    Mango is a highly perishable seasonal fruit and large quantities are wasted during the peak season as a result of poor postharvest handling procedures. Processing surplus mango fruits into flour to be used as a functional ingredient appears to be a good preservation method to ensure its extended consumption.
    Matched MeSH terms: Solubility
  2. Mechanical and antibacterial properties of paper coated with chitosan
    Sarani Zakaria, Chin HC, Wan Haslinda Wan Ahmad, Hatika Kaco, Soon Wei Chook, Chi HC
    Sains Malaysiana, 2015;44:905-911.
    Recent developments have found the viability of chitosan as a new alternative additive in the pulp and paper technology.
    This study was carried out to investigate the effect of chitosan as a paper coating which were prepared by dissolution in
    acetic acid solution. The mechanical properties of coated paper were improved significantly compared with non-coated
    paper. The FT-IR spectra showed peak evolution at 1558 cm-1 for coated paper due to the existence of amine group. Since
    FT-IR spectra for the coated paper was almost identical to the chitosan spectrum, it is assumed that there is an obvious
    physical interaction rather than the chemical interaction. The SEM micrographs showed that some of the chitosan has
    occupied the pores and some of them adhered only on the surface. This may be due to the chemical similarities between
    cellulose and chitosan which enhanced the strength of fiber matrixes via hydrogen bonding. The antibacterial property
    of coated paper showed that chitosan in dried form has no significant effect but effective when applied as wet solution.
    Matched MeSH terms: Solubility
  3. In-Vitro and In-Vivo Evaluation of Supersaturable Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Dutasteride
    Subramanian P, Rajnikanth PS, Kumar M, Chidambram K
    Curr Drug Deliv, 2020;17(1):74-86.
    PMID: 31721703 DOI: 10.2174/1567201816666191112111610
    OBJECTIVE: A novel, Supersaturable Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) has been prepared to improve the Dutasteride's poor aqueous solubility.

    METHODS: By adding Hydroxy Propyl Methyl Cellulose (HPMC) as a precipitation inhibitor to conventional SNEDDS, a supersaturable system was prepared. Firstly, the prepared SNEDDS played an important role in increasing the aqueous solubility and hence oral absorption due to nano-range size. Secondly, the S-SNEDDS found to be advantageous over SNEDDS for having a higher drug load and inhibition of dilution precipitation of Dutasteride. Formulated S-SNEDDS (F1-F9) ranged from 37.42 ± 1.02 to 68.92 ± 0.09 nm with PDI 0.219-0.34 and drug loading of over 95 percent.

    RESULTS: The study of in-vitro dissolution revealed higher dissolution for S-SNEDDS compared to SNEDDS and Avodart soft gelatin capsule as a commercial product. In addition, higher absorption was observed for S-SNEDDS showing approximately 1.28 and 1.27 fold AUC (0-24h) and Cmax compared to commercial products. Therefore, S-SNEDDS has proven as a novel drug delivery system with a higher drug load, higher self-emulsification efficiency, higher stability, higher dissolution and pronounced absorption.

    CONCLUSION: In conclusion, S-SNEDDS could be a newly emerging approach to enhance aqueous solubility in many folds for drugs belonging to BCS Class II and IV and thus absorption and oral bioavailability.

    Matched MeSH terms: Solubility
  4. Mechanistic insight of α-mangostin encapsulation in 2-hydroxypropyl-β-cyclodextrin for solubility enhancement
    Muchtaridi M, Triwahyuningtyas D, Muhammad Fakih T, Megantara S, Choi SB
    J Biomol Struct Dyn, 2024 Apr;42(6):3223-3232.
    PMID: 37286382 DOI: 10.1080/07391102.2023.2214237
    α-Mangostin is the most abundant compound contained in the mangostin (Garcinia mangostana L.) plant which have been developed and proven to have many promising pharmacological effects. However, the low water solubility of α-mangostin causes limitations in its development in clinical purpose. To increase the solubility of a compound, a method currently being developed is to make drug inclusion complexes using cyclodextrins. This research aimed to use in silico techniques namely molecular docking study and molecular dynamics simulation to explore the molecular mechanism and stability of the encapsulation of α-mangostin using cyclodextrins. Two types of cyclodextrins were used including β-cyclodextrin and 2-hydroxypropyl-β-cyclodextrin docked against α-mangostin. From the molecular docking results, it shows that the α-mangostin complex with 2-hydroxypropyl-β-cyclodextrin provides the lowest binding energy value of -7.99 Kcal/mol compared to β-cyclodextrin value of -6.14 Kcal/mol. The α-mangostin complex with 2-hydroxypropyl-β-cyclodextrin also showed good stability based on molecular dynamics simulation during 100 ns. From molecular motion, RDF, Rg, SASA, density, total energy analyzes, this complex shows increased solubility in water and provided good stability. This indicates that the encapsulation of α-mangostin with 2-hydroxypropyl-β-cyclodextrin can increase the solubility of the α-mangostin.Communicated by Ramaswamy H. Sarma.
    Matched MeSH terms: Solubility
  5. Fulltext Genome sequence of an uncharted halophilic bacterium Robertkochia marina with deciphering its phosphate-solubilizing ability
    Lam MQ, Chen SJ, Goh KM, Abd Manan F, Yahya A, Shamsir MS, et al.
    Braz J Microbiol, 2021 Mar;52(1):251-256.
    PMID: 33141351 DOI: 10.1007/s42770-020-00401-2
    The wide use of whole-genome sequencing approach in the modern genomic era has opened a great opportunity to reveal the prospective applications of halophilic bacteria. Robertkochia marina CC-AMO-30DT is one of the halophilic bacteria that was previously taxonomically identified without any inspection on its biotechnological potential from a genomic aspect. In this study, we present the whole-genome sequence of R. marina and demonstrated the ability of this bacterium in solubilizing phosphate by producing phosphatase. The genome of R. marina has 3.57 Mbp and contains 3107 predicted genes, from which 3044 are protein coding, 52 are non-coding RNAs, and 11 are pseudogenes. Several phosphatases such as alkaline phosphatases and pyrophosphatases were mined from the genome. Further genomic study (phylogenetics, sequence analysis, and functional mechanism) and experimental data suggested that the alkaline phosphatase produced by R. marina could potentially be utilized in promoting plant growth, particularly for plants on saline-based agricultural land.
    Matched MeSH terms: Solubility
  6. Fulltext PH-responsive strontium nanoparticles for targeted gene therapy against mammary carcinoma cells
    Bakhtiar A, Chowdhury EH
    Asian J Pharm Sci, 2021 Mar;16(2):236-252.
    PMID: 33995617 DOI: 10.1016/j.ajps.2020.11.002
    Genetic intervention via the delivery of functional genes such as plasmid DNA (pDNA) and short-interfering RNA (siRNA) offers a great way to treat many single or multiple genetic defects effectively, including mammary carcinoma. Delivery of naked therapeutic genes or siRNAs is, however, short-lived due to biological clearance by scavenging nucleases and circulating monocytes. Low cellular internalization of negatively-charged nucleic acids further causes low transfection or silencing activity. Development of safe and effectual gene vectors is therefore undeniably crucial to the success of nucleic acid delivery. Inorganic nanoparticles have attracted considerable attention in the recent years due to their high loading capacity and encapsulation activity. Here we introduce strontium salt-based nanoparticles, namely, strontium sulfate, strontium sulfite and strontium fluoride as new inorganic nanocarriers. Generated strontium salt particles were found to be nanosized with high affinity towards negatively-charged pDNA and siRNA. Degradation of the particles was seen with a drop in pH, suggesting their capacity to respond to pH change and undergo dissolution at endosomal pH to release the genetic materials. While the particles are relatively nontoxic towards the cells, siRNA-loaded SrF2 and SrSO3 particles exerted superior transgene expression and knockdown activity of MAPK and AKT, leading to inhibition of their phosphorylation to a distinctive extent in both MCF-7 and 4T1 cells. Strontium salt nanoparticles have thus emerged as a promising tool for applications in cancer gene therapy.
    Matched MeSH terms: Solubility
  7. Fulltext Strontium Sulfite: A New pH-Responsive Inorganic Nanocarrier to Deliver Therapeutic siRNAs to Cancer Cells
    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
  8. Fulltext Production of Nanoemulsions from Palm-Based Tocotrienol Rich Fraction by Microfluidization
    Goh PS, Ng MH, Choo YM, Amru NB, Chuah CH
    Molecules, 2015;20(11):19936-46.
    PMID: 26556328 DOI: 10.3390/molecules201119666
    In the present study, tocotrienol rich fraction (TRF) nanoemulsions were produced as an alternative approach to improve solubility and absorption of tocotrienols. In the present study, droplet size obtained after 10 cycles of homogenization with increasing pressure was found to decrease from 120 to 65.1 nm. Nanoemulsions stabilized with Tween series alone or emulsifier blend Brij 35:Span 80 (0.6:0.4 w/w) homogenized at 25,000 psi and 10 cycles, produced droplet size less than 100 nm and a narrow size distribution with a polydispersity index (PDI) value lower than 0.2. However blend of Tween series with Span 80 produced nanoemulsions with droplet size larger than 200 nm. This work has also demonstrated the amount of tocols losses in TRF nanoemulsion stabilized Tweens alone or emulsifier blend Brij 35:Span 80 (0.6:0.4 w/w) ranged between 3%-25%. This can be attributed to the interfacial film formed surrounding the droplets exhibited different level of oxidative stability against heat and free radicals created during high pressure emulsification.
    Matched MeSH terms: Solubility
  9. Fulltext Curcumin Nanoformulations for Colorectal Cancer: A Review
    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
  10. Synthesis and formulation studies of griseofulvin analogues with improved solubility and metabolic stability
    Petersen AB, Andersen NS, Konotop G, Hanafiah NH, Raab MS, Krämer A, et al.
    Eur J Med Chem, 2017 Apr 21;130:240-247.
    PMID: 28258034 DOI: 10.1016/j.ejmech.2017.02.055
    Griseofulvin (1) is an important antifungal agent that has recently received attention due to its antiproliferative activity in mammalian cancer cells. Comprehensive SAR studies have led to the identification of 2'-benzyloxy griseofulvin 2, a more potent analogue with low micromolar anticancer potency in vitro. Analogue 2 was also shown to retard tumor growth through inhibition of centrosomal clustering in murine xenograft models of colon cancer and multiple myeloma. However, similar to griseofulvin, compound 2 exhibited poor metabolic stability and aqueous solubility. In order to improve the poor pharmacokinetic properties, 11 griseofulvin analogues were synthesized and evaluated for biological activity and physiological stabilities including SGF, plasma, and metabolic stability. Finally, the most promising compounds were investigated in respect to thermodynamic solubility and formulation studies. The 2'-benzylamine analogue 10 proved to be the most promising compound with low μM in vitro anticancer potency, a 200-fold increase in PBS solubility over compound 2, and with improved metabolic stability. Furthermore, this analogue proved compatible with formulations suitable for both oral and intravenous administration. Finally, 2'-benzylamine analogue 10 was confirmed to induce G2/M cell cycle arrest in vitro.
    Matched MeSH terms: Solubility
  11. Fulltext Pore Structure Changes Occur During CO2 Injection into Carbonate Reservoirs
    Seyyedi M, Mahmud HKB, Verrall M, Giwelli A, Esteban L, Ghasemiziarani M, et al.
    Sci Rep, 2020 Feb 27;10(1):3624.
    PMID: 32107400 DOI: 10.1038/s41598-020-60247-4
    Observations and modeling studies have shown that during CO2 injection into underground carbonate reservoirs, the dissolution of CO2 into formation water forms acidic brine, leading to fluid-rock interactions that can significantly impact the hydraulic properties of the host formation. However, the impacts of these interactions on the pore structure and macroscopic flow properties of host rock are poorly characterized both for the near-wellbore region and deeper into the reservoir. Little attention has been given to the influence of pressure drop from the near-wellbore region to reservoir body on disturbing the ionic equilibrium in the CO2-saturated brine and consequent mineral precipitation. In this paper, we present the results of a novel experimental procedure designed to address these issues in carbonate reservoirs. We injected CO2-saturated brine into a composite core made of two matching grainstone carbonate core plugs with a tight disk placed between them to create a pressure profile of around 250 psi resembling that prevailing in reservoirs during CO2 injection. We investigated the impacts of fluid-rock interactions at pore and continuum scale using medical X-ray CT, nuclear magnetic resonance, and scanning electron microscopy. We found that strong calcite dissolution occurs near to the injection point, which leads to an increase in primary intergranular porosity and permeability of the near injection region, and ultimately to wormhole  formation. The strong heterogeneous dissolution of calcite grains leads to the formation of intra-granular micro-pores. At later stages of the dissolution, the internal regions of ooids become accessible to the carbonated brine, leading to the formation of moldic porosity. At distances far from the injection point, we observed minimal or no change in pore structure, pore roughness, pore populations, and rock hydraulic properties. The pressure drop of 250 psi slightly disturbed the chemical equilibrium of the system, which led to minor precipitation of sub-micron sized calcite crystals but due to the large pore throats of the rock, these deposits had no measurable impact on rock permeability. The trial illustrates that the new procedure is valuable for investigating fluid-rock interactions by reproducing the geochemical consequences of relatively steep pore pressure gradients during CO2 injection.
    Matched MeSH terms: Solubility
  12. Mango leaf extract incorporated chitosan antioxidant film for active food packaging
    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
  13. Role of blooming in determining the storage stability of lipid-based dosage forms
    Khan N, Craig DQ
    J Pharm Sci, 2004 Dec;93(12):2962-71.
    PMID: 15459945
    Gelucire 50/13 alone and solid dispersions in this material containing two model drugs (10% w/w caffeine and paracetamol) have been studied with a view to establishing the mechanism underpinning changes in drug-release characteristics as a function of storage time and temperature. The lipid systems were fabricated into tablets and stored for up to 180 days at temperatures of 20 and 37 degrees C. The dispersions were studied using differential scanning calorimetry (DSC), scanning electron microscopy, and dissolution testing. DSC studies indicated that the Gelucire 50/13 exists in two principal melting forms (melting points 38 and 43 degrees C) that undergo transformation to the higher melting form on storage at 37 degrees C. Scanning electron microscopy studies indicated that the systems exhibit "blooming," with crystal formation on the surface being apparent on storage at both temperatures. The dissolution rate increased on storage, with the effect being particularly marked at higher storage temperatures and for the paracetamol systems. However, whereas these changes corresponded well to those seen for the morphology, the correlation between the changes in dissolution and those of the DSC profiles was poor. The study has suggested a novel explanation for the storage instability of Gelucire 50/13 whereby the change in dissolution is associated not with molecular rearrangement as such but with the gross distribution of the constituent components, this in turn altering the physical integrity of the lipid bases.
    Matched MeSH terms: Solubility
  14. Formulation and optimization of orally disintegrating tablets of sumatriptan succinate
    Sheshala R, Khan N, Darwis Y
    Chem Pharm Bull (Tokyo), 2011;59(8):920-8.
    PMID: 21804234
    The aims of the present research were to mask the intensely bitter taste of sumatriptan succinate and to formulate orally disintegrating tablets (ODTs) of the taste masked drug. Taste masking was performed by coating sumatriptan succinate with Eudragit EPO using spray drying technique. The resultant microspheres were evaluated for thermal analysis, yield, particle size, entrapment efficiency and in vitro taste masking. The tablets were formulated by mixing the taste masked microspheres with different types and concentrations of superdisintegrants and compressed using direct compression method followed by sublimation technique. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. All the tablet formulations disintegrated in vitro within 37-410 s. The optimized formulation containing 5% Kollidon CL-SF released more than 90% of the drug within 15 min and the release was comparable to that of commercial product (Suminat®). In human volunteers, the optimized formulation was found to have a pleasant taste and mouth feel and disintegrated in the oral cavity within 41 s. The optimized formulation was found to be stable and bioequivalent with Suminat®.
    Matched MeSH terms: Solubility
  15. Formulation and in vivo evaluation of ondansetron orally disintegrating tablets using different superdisintegrants
    Sheshala R, Khan N, Chitneni M, Darwis Y
    Arch Pharm Res, 2011 Nov;34(11):1945-56.
    PMID: 22139694 DOI: 10.1007/s12272-011-1115-y
    The aim of this study was to formulate cost effective taste-masked orally disintegrating tablets of ondansetron, a bitter drug using different superdisintegrants by a wet granulation technique. Microcrystalline cellulose (Avicel) as a diluent and disintegrant in addition to aspartame as a sweetener were used in all formulations. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. The tablets' hardness was maintained in the range of 2-3 kg and friability was <1% for all batches. All tablet formulations disintegrated rapidly in vitro within 5.83 to 33.0 sec. The optimized formulation containing 15% Polyplasdone XL-10 released more than 90% of drug within 5 min and the release was comparable to that of a commercial product. In human volunteers, optimized formulation was found to have a pleasant taste and mouth feel and they disintegrated in the oral cavity within 12 sec. The stability results were also satisfactory. A pharmacokinetic study with the optimized formulation was performed in comparison with a reference (Zofer MD 8®) and they were found to be bioequivalent. In conclusion, a cost effective ondansetron orally disintegrating tablet was successfully prepared with acceptable hardness, desirable taste and rapid disintegration in the oral cavity.
    Matched MeSH terms: Solubility
  16. Preparation, characterization, and in vivo evaluation of insulin-loaded PLA-PEG microspheres for controlled parenteral drug delivery
    Sheshala R, Peh KK, Darwis Y
    Drug Dev Ind Pharm, 2009 Nov;35(11):1364-74.
    PMID: 19832637 DOI: 10.3109/03639040902939213
    AIM: The aim of this study was to prepare insulin-loaded poly(lactic acid)-polyethylene glycol microspheres that could control insulin release at least for 1 week and evaluate their in vivo performance in a streptozotocin-induced diabetic rat model.
    METHODS: The microspheres were prepared using a water-in-oil-in-water double emulsion solvent evaporation technique. Different formulation variables influencing the yield, particle size, entrapment efficiency, and in vitro release profiles were investigated. The pharmacokinetic study of optimized formulation was performed with single dose in comparison with multiple dose of Humulin 30/70 as a reference product in streptozotocin-induced diabetic rats.
    RESULTS: The optimized formulation of insulin microspheres was nonporous, smooth-surfaced, and spherical in structure under scanning electron microscope with a mean particle size of 3.07 microm and entrapment efficiency of 42.74% of the theoretical amount incorporated. The in vitro insulin release profiles was characterized by a bimodal behavior with an initial burst release because of the insulin adsorbed on the microsphere surface, followed by slower and continuous release corresponding to the insulin entrapped in polymer matrix.
    CONCLUSIONS: The optimized formulation and reference were comparable in the extent of absorption. Consequently, these microspheres can be proposed as new controlled parenteral delivery system.
    Matched MeSH terms: Solubility
  17. Solid Lipid Nanoparticles of Atovaquone Based on 2(4) Full-Factorial Design
    Mohtar N, A K Khan N, Darwis Y
    Iran J Pharm Res, 2015;14(4):989-1000.
    PMID: 26664366
    Solid lipid nanoparticles of atovaquone (ATQ-SLN) were prepared by high shear homogenization method using tripalmitin, trilaurin, and Compritol 888 ATO as the lipid matrices and Phospholipon 90H, Tween 80, and poloxamer 188 as the surfactants. Optimization of the formulations was conducted using 6 sets of 2(4) full-factorial design based on four independent variables that were the number of homogenizing cycles, concentration of the lipid, concentration of the co-surfactant, and concentration of the main surfactant. The dependent variables were particle size and polydispersity index (PdI). The homogenizing cycles showed a negative influence on the dependent variables which reduced both the particle size and the PdI value. Moreover, a combination of certain percentages of the main surfactant and co-surfactant also showed a negative influence that reduced both the particle size and PdI value. Selected formulations from each design were further characterized for the entrapment efficiency and yield. The optimised formulation of ATQ-SLN consisted of trilaurin, Phospholipon 90H and Tween 80 with a particle size of 89.4 ± 0.2 nm and entrapment efficiency of 83.0 ± 1.7%. The in-vitro release evaluation of the formulation showed a complete and immediate release of ATQ from the SLN that could be a solution to improve the poor aqueous solubility and hence poor bioavailability of the drug.
    Matched MeSH terms: Solubility
  18. Development and characterization of lecithin stabilized glibenclamide nanocrystals for enhanced solubility and drug delivery
    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: Solubility
  19. Water-Soluble Dioxidovanadium(V) Complexes of Aroylhydrazones: DNA/BSA Interactions, Hydrophobicity, and Cell-Selective Anticancer Potential
    Sahu G, Banerjee A, Samanta R, Mohanty M, Lima S, Tiekink ERT, et al.
    Inorg Chem, 2021 Oct 18;60(20):15291-15309.
    PMID: 34597028 DOI: 10.1021/acs.inorgchem.1c01899
    Five new anionic aqueous dioxidovanadium(V) complexes, [{VO2L1,2}A(H2O)n]α (1-5), with the aroylhydrazone ligands pyridine-4-carboxylic acid (3-ethoxy-2-hydroxybenzylidene)hydrazide (H2L1) and furan-2-carboxylic acid (3-ethoxy-2-hydroxybenzylidene)hydrazide (H2L2) incorporating different alkali metals (A = Na+, K+, Cs+) as countercation were synthesized and characterized by various physicochemical techniques. The solution-phase stabilities of 1-5 were determined by time-dependent NMR and UV-vis, and also the octanol/water partition coefficients were obtained by spectroscopic techniques. X-ray crystallography of 2-4 confirmed the presence of vanadium(V) centers coordinated by two cis-oxido-O atoms and the O, N, and O atoms of a dianionic tridentate ligand. To evaluate the biological behavior, all complexes were screened for their DNA/protein binding propensity through spectroscopic experiments. Finally, a cytotoxicity study of 1-5 was performed against colon (HT-29), breast (MCF-7), and cervical (HeLa) cancer cell lines and a noncancerous NIH-3T3 cell line. The cytotoxicity was cell-selective, being more active against HT-29 than against other cells. In addition, the role of hydrophobicity in the cytotoxicity was explained in that an optimal hydrophobicity is essential for high cytotoxicity. Moreover, the results of wound-healing assays indicated antimigration in case of HT-29 cells. Remarkably, 1 with an IC50 value of 5.42 ± 0.15 μM showed greater activity in comparison to cisplatin against the HT-29 cell line.
    Matched MeSH terms: Solubility
  20. Cellulose acetate from oil palm empty fruit bunch via a one step heterogeneous acetylation
    Wan Daud WR, Djuned FM
    Carbohydr Polym, 2015 Nov 5;132:252-60.
    PMID: 26256348 DOI: 10.1016/j.carbpol.2015.06.011
    Acetone soluble oil palm empty fruit bunch cellulose acetate (OPEFB-CA) of DS 2.52 has been successfully synthesized in a one-step heterogeneous acetylation of OPEFB cellulose without necessitating the hydrolysis stage. This has only been made possible by the mathematical modeling of the acetylation process by manipulating the variables of reaction time and acetic anhydride/cellulose ratio (RR). The obtained model was verified by experimental data with an error of less than 2.5%. NMR analysis showed that the distribution of the acetyl moiety among the three OH groups of cellulose indicates a preference at the C6 position, followed by C3 and C2. XRD revealed that OPEFB-CA is highly amorphous with a degree of crystallinity estimated to be ca. 6.41% as determined from DSC. The OPEFB-CA films exhibited good mechanical properties being their tensile strength and Young's modulus higher than those of the commercial CA.
    Matched MeSH terms: Solubility
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