Displaying publications 1 - 20 of 24 in total

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  1. Fulltext Effect of surfactant and surfactant blends on pseudoternary phase diagram behavior of newly synthesized palm kernel oil esters
    Mahdi ES, Sakeena MH, Abdulkarim MF, Abdullah GZ, Sattar MA, Noor AM
    Drug Des Devel Ther, 2011;5:311-23.
    PMID: 21792294 DOI: 10.2147/DDDT.S15698
    The purpose of this study was to select appropriate surfactants or blends of surfactants to study the ternary phase diagram behavior of newly introduced palm kernel oil esters.
    Matched MeSH terms: Polysorbates/chemistry*
  2. Influence of a nonionic surfactant on curcumin delivery of nanocellulose reinforced chitosan hydrogel
    Sampath Udeni Gunathilake TM, Ching YC, Chuah CH, Illias HA, Ching KY, Singh R, et al.
    Int J Biol Macromol, 2018 Oct 15;118(Pt A):1055-1064.
    PMID: 30001596 DOI: 10.1016/j.ijbiomac.2018.06.147
    Nanocellulose reinforced chitosan hydrogel was synthesized using chemical crosslinking method for the delivery of curcumin which is a poorly water-soluble drug. Curcumin extracted from the dried rhizomes of Curcuma longa was incorporated to the hydrogel via in situ loading method. A nonionic surfactant (Tween 20) was incorporated into the hydrogel to improve the solubility of curcumin. After the gas foaming process, hydrogel showed large interconnected pore structures. The release studies in gastric medium showed that the cumulative release of curcumin increased from 0.21% ± 0.02% to 54.85% ± 0.77% with the increasing of Tween 20 concentration from 0% to 30% (w/v) after 7.5 h. However, the entrapment efficiency percentage decreased with the addition of Tween 20. The gas foamed hydrogel showed higher initial burst release within the first 120 min compared to hydrogel formed at atmospheric condition. The solubility of curcumin would increase to 3.014 ± 0.041 mg/mL when the Tween 20 concentration increased to 3.2% (w/v) in simulated gastric medium. UV-visible spectra revealed that the drug retained its chemical activity after in vitro release. From these findings, it is believed that the nonionic surfactant incorporated chitosan/nanocellulose hydrogel can provide a platform to overcome current problems associated with curcumin delivery.
    Matched MeSH terms: Polysorbates/chemistry*
  3. Alginate-based emulsion template containing high oil loading stabilized by nonionic surfactants
    Ong WD, Tey BT, Quek SY, Tang SY, Chan ES
    J Food Sci, 2015 Jan;80(1):E93-E100.
    PMID: 25529579 DOI: 10.1111/1750-3841.12729
    Oil-in-water (O/W) emulsion-gel systems containing high oil payloads are of increasing interest for food applications because of the reduction in encapsulation cost, consumption frequency or volume of food products. This study shows a facile approach to prepare stable alginate-based O/W emulsions at high oil loading using a mixture of nonionic surfactants (Tween 80 and Span 20) as a template to form gelled-emulsions. The synergistic effects of alginate and surfactants on the O/W emulsion properties were evaluated in terms of oil droplet size and emulsion stability. At 2% (w/v) of alginate and 1% (w/v) of surfactants, the size distribution of oil droplets was narrow and monomodal, even at an oil loading of 70% (v/v). The emulsions formed were stable against phase separation. The oil droplet size could be further reduced to below 1 μm using a high-shear homogenizer. The emulsions formed could be easily molded and gelled into solids of different shapes via ionic gelation. The findings of this study create possible avenues for applications in food industries.
    Matched MeSH terms: Polysorbates/chemistry
  4. Effect of polyoxyethylene sorbitan esters and sodium caseinate on physicochemical properties of palm-based functional lipid nanodispersions
    Cheong JN, Mirhosseini H, Tan CP
    Int J Food Sci Nutr, 2010 Jun;61(4):417-24.
    PMID: 20151850 DOI: 10.3109/09637481003591574
    The main objective of the present study was to investigate the effect of polyoxyethylene sorbitan esters and sodium caseinate on physicochemical properties of palm-based functional lipid nanodispersions prepared by the emulsification-evaporation technique. The results indicated that the average droplet size increased significantly (P < 0.05) by increasing the chain length of fatty acids and also by increasing the hydrophile-lipophile balance value. Among the prepared nanodispersions, the nanoemulsion containing Polysorbate 20 showed the smallest average droplet size (202 nm) and narrowest size distribution for tocopherol-tocotrienol nanodispersions, while sodium caseinate-stabilized nanodispersions containing carotenoids had the largest average droplet size (386 nm), thus indicating a greater emulsifying role for Polysorbate 20 compared with sodium caseinate.
    Matched MeSH terms: Polysorbates/chemistry*
  5. Characterization and cytotoxicity of nanostructured lipid carriers formulated with olive oil, hydrogenated palm oil, and polysorbate 80
    How CW, Rasedee A, Abbasalipourkabir R
    IEEE Trans Nanobioscience, 2013 Jun;12(2):72-8.
    PMID: 23268387 DOI: 10.1109/TNB.2012.2232937
    Nanostructured lipid carriers (NLC) composed of solid and liquid lipids, and surfactants are potentially good colloidal drug carriers. Before NLC can be used as drug carriers, the cytotoxicity of their components must be ascertained. The cytotoxicity of solid lipids (trilaurin, palmitin, docosanoid acid, and hydrogenated palm oil [HPO]) and surfactants (Polysorbate 20, 80, and 85) were determined on BALB/c 3T3 cells. The HPO and Polysorbate 80 were least cytotoxic and used with olive oil in the formulation of NLC. The particle size, polydispersity index, zeta potential, specific surface area, and crystallinity index of the NLC were 61.14 nm, 0.461, -25.4 mV, and 49.07 m(2) and 27.12% respectively, while the melting point was 4.3 °C lower than of HPO. Unlike in serum-free, NLC incubated in fetal bovine serum-supplemented medium did not show particle growth, suggesting that serum proteins in medium inhibit nanoparticles aggregation. The study also showed that NLC was less toxic to BALB/c 3T3 cells than Polysorbate 80. Thus, NLC with olive oil, HPO, and Polysorbate 80 as components are potentially good drug carriers with minimal cytotoxicity on normal cells.
    Matched MeSH terms: Polysorbates/chemistry
  6. Fulltext Effects of selected polysorbate and sucrose ester emulsifiers on the physicochemical properties of astaxanthin nanodispersions
    Anarjan N, Tan CP
    Molecules, 2013 Jan 09;18(1):768-77.
    PMID: 23303336 DOI: 10.3390/molecules18010768
    The effects of selected nonionic emulsifiers on the physicochemical characteristics of astaxanthin nanodispersions produced by an emulsification/evaporation technique were studied. The emulsifiers used were polysorbates (Polysorbate 20, Polysorbate 40, Polysorbate 60 and Polysorbate 80) and sucrose esters of fatty acids (sucrose laurate, palmitate, stearate and oleate). The mean particle diameters of the nanodispersions ranged from 70 nm to 150 nm, depending on the emulsifier used. In the prepared nanodispersions, the astaxanthin particle diameter decreased with increasing emulsifier hydrophilicity and decreasing carbon number of the fatty acid in the emulsifier structure. Astaxanthin nanodispersions with the smallest particle diameters were produced with Polysorbate 20 and sucrose laurate among the polysorbates and the sucrose esters, respectively. We also found that the Polysorbate 80- and sucrose oleate-stabilized nanodispersions had the highest astaxanthin losses (i.e., the lowest astaxanthin contents in the final products) among the nanodispersions. This work demonstrated the importance of emulsifier type in determining the physicochemical characteristics of astaxanthin nano-dispersions.
    Matched MeSH terms: Polysorbates/chemistry*
  7. Forming a lutein nanodispersion via solvent displacement method: the effects of processing parameters and emulsifiers with different stabilizing mechanisms
    Tan TB, Yussof NS, Abas F, Mirhosseini H, Nehdi IA, Tan CP
    Food Chem, 2016 Mar 1;194:416-23.
    PMID: 26471574 DOI: 10.1016/j.foodchem.2015.08.045
    A solvent displacement method was used to prepare lutein nanodispersions. The effects of processing parameters (addition method, addition rate, stirring time and stirring speed) and emulsifiers with different stabilizing mechanisms (steric, electrostatic, electrosteric and combined electrostatic-steric) on the particle size and particle size distribution (PSD) of the nanodispersions were investigated. Among the processing parameters, only the addition method and stirring time had significant effects (p<0.05) on the particle size and PSD. For steric emulsifiers, Tween 20, 40, 60 and 80 were used to produce nanodispersions successfully with particle sizes below 100nm. Tween 80 (steric) was then chosen for further comparison against sodium dodecyl sulfate (SDS) (electrostatic), sodium caseinate (electrosteric) and SDS-Tween 80 (combined electrostatic-steric) emulsifiers. At the lowest emulsifier concentration of 0.1%, all the emulsifiers invariably produced stable nanodispersions with small particle sizes (72.88-142.85nm) and narrow PSDs (polydispersity index<0.40).
    Matched MeSH terms: Polysorbates/chemistry
  8. Fulltext An Artificial Neural Network Based Analysis of Factors Controlling Particle Size in a Virgin Coconut Oil-Based Nanoemulsion System Containing Copper Peptide
    Samson S, Basri M, Fard Masoumi HR, Abdul Malek E, Abedi Karjiban R
    PLoS One, 2016;11(7):e0157737.
    PMID: 27383135 DOI: 10.1371/journal.pone.0157737
    A predictive model of a virgin coconut oil (VCO) nanoemulsion system for the topical delivery of copper peptide (an anti-aging compound) was developed using an artificial neural network (ANN) to investigate the factors that influence particle size. Four independent variables including the amount of VCO, Tween 80: Pluronic F68 (T80:PF68), xanthan gum and water were the inputs whereas particle size was taken as the response for the trained network. Genetic algorithms (GA) were used to model the data which were divided into training sets, testing sets and validation sets. The model obtained indicated the high quality performance of the neural network and its capability to identify the critical composition factors for the VCO nanoemulsion. The main factor controlling the particle size was found out to be xanthan gum (28.56%) followed by T80:PF68 (26.9%), VCO (22.8%) and water (21.74%). The formulation containing copper peptide was then successfully prepared using optimum conditions and particle sizes of 120.7 nm were obtained. The final formulation exhibited a zeta potential lower than -25 mV and showed good physical stability towards centrifugation test, freeze-thaw cycle test and storage at temperature 25°C and 45°C.
    Matched MeSH terms: Polysorbates/chemistry
  9. Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment
    Asmawi AA, Salim N, Ngan CL, Ahmad H, Abdulmalek E, Masarudin MJ, et al.
    Drug Deliv Transl Res, 2019 04;9(2):543-554.
    PMID: 29691812 DOI: 10.1007/s13346-018-0526-4
    Docetaxel has demonstrated extraordinary anticancer effects on lung cancer. However, lack of optimal bioavailability due to poor solubility and high toxicity at its therapeutic dose has hampered the clinical use of this anticancer drug. Development of nanoemulsion formulation along with biocompatible excipients aimed for pulmonary delivery is a potential strategy to deliver this poorly aqueous soluble drug with improved bioavailability and biocompatibility. In this work, screening and selection of pharmaceutically acceptable excipients at their minimal optimal concentration have been conducted. The selected nanoemulsion formulations were prepared using high-energy emulsification technique and subjected to physicochemical and aerodynamic characterizations. The formulated nanoemulsion had mean particle size and ζ-potential in the range of 90 to 110 nm and - 30 to - 40 mV respectively, indicating high colloidal stability. The pH, osmolality, and viscosity of the systems met the ideal requirement for pulmonary application. The DNE4 formulation exhibited slow drug release and excellent stability even under the influence of extreme environmental conditions. This was further confirmed by transmission electron microscopy as uniform spherical droplets in nanometer range were observed after storage at 45 ± 1 °C for 3 months indicating high thermal stability. The nebulized DNE4 exhibited desirable aerosolization properties for pulmonary delivery application and found to be more selective on human lung carcinoma cell (A549) than normal cell (MRC-5). Hence, these characteristics make the formulation a great candidate for the potential use as a carrier system for docetaxel in targeting lung cancer via pulmonary delivery.
    Matched MeSH terms: Polysorbates/chemistry
  10. Characterisation of β-carotene partitioning in protein emulsions: Effects of pre-treatments, solid fat content and emulsifier type
    Wan Mohamad WAF, McNaughton D, Augustin MA, Buckow R
    Food Chem, 2018 Aug 15;257:361-367.
    PMID: 29622223 DOI: 10.1016/j.foodchem.2018.03.027
    Understanding the bioactive partitioning between the phases of an emulsion system underpins strategies for improving the efficiency of bioactive protection against degradation. We analysed partitioning of β-carotene in emulsions with various formulations in-situ using confocal Raman microscopy (CRM). The partitioning of β-carotene into the aqueous phase of emulsions increased when whey protein isolate (WPI) was heat or high pressure-treated prior to emulsion formation. However, increasing the concentration of high pressure-treated WPI reduced the β-carotene partitioning into the aqueous phase. Increasing the solid fat content in the carrier oil favoured the migration of β-carotene into the aqueous phase. The use of WPI as the emulsifier resulted in a greater partitioning of β-carotene into the aqueous phase compared to when Tween 40 was the emulsifier. This study demonstrates that partitioning of β-carotene between the aqueous and oil phase is dependent on the characteristics of the oil phase, emulsifier type and processing.
    Matched MeSH terms: Polysorbates/chemistry
  11. Stability of Bioactive Compounds and Antioxidant Activities of Kenaf Seed Oil-in-Water Nanoemulsions under Different Storage Temperatures
    Cheong AM, Tan CP, Nyam KL
    J Food Sci, 2018 Oct;83(10):2457-2465.
    PMID: 30178877 DOI: 10.1111/1750-3841.14332
    Kenaf seed oil-in-water nanoemulsions (NANO) stabilized by sodium caseinate (SC), beta-cyclodextrin (β-CD), and Tween 20 (T20) have been optimized and shown to improve in vitro bioaccessibility and physicochemical stability in the previous study. The main objective of this study was to evaluate the stability of bioactive compounds and antioxidants in the NANO during storage at different temperatures (4 °C, 25 °C, and 40 °C). An evaluation of the antioxidant activities of each emulsifier showed that SC had good scavenging capability with 97.6% ABTS radical scavenging activity. Therefore, SC which was used as one of the main emulsifiers could further enhanced the antioxidant activity of NANO. At week 8 of storage, NANO that stored at 4 °C had maintained the best bioactive compounds stability and antioxidant activities with 90% retention of vitamin E and 65% retention of phytosterols. These results suggested that 4 °C would be the most suitable storage temperature for NANO containing naturally present vitamin E and phytosterols. From the accelerated storage results at 40 °C, NANO containing vitamin E and phytosterols had maintained half of its initial concentration until week 4 and week 2 of storage, which is equivalent to 16 weeks and 8 weeks of storage at room temperature, respectively.

    PRACTICAL APPLICATION: The results of this study provide a better understanding on the stability of bioactive compounds and antioxidant activities in oil-in-water nanoemulsions that stabilized by similar ternary emulsifiers during storage at different temperatures. In addition, this study could be used as a predictive model to estimate the shelf life of bioactive compounds encapsulated in the form of nanoemulsions.

    Matched MeSH terms: Polysorbates/chemistry
  12. Fulltext Molecular dynamics simulation of palmitate ester self-assembly with diclofenac
    Abedi Karjiban R, Basri M, Abdul Rahman MB, Salleh AB
    Int J Mol Sci, 2012;13(8):9572-9583.
    PMID: 22949816 DOI: 10.3390/ijms13089572
    Palm oil-based esters (POEs) are unsaturated and non-ionic esters with a great potential to act as chemical penetration enhancers and drug carriers for transdermal drug nano-delivery. A ratio of palmitate ester and nonionic Tween80 with and without diclofenac acid was chosen from an experimentally determined phase diagram. Molecular dynamics simulations were performed for selected compositions over a period of 15 ns. Both micelles showed a prolate-like shape, while adding the drug produced a more compact micellar structure. Our results proposed that the drug could behave as a co-surfactant in our simulated model.
    Matched MeSH terms: Polysorbates/chemistry
  13. Cellular uptake of Nigella sativa oil-PLGA microparticle by PC-12 cell line
    Doolaanea AA, Mansor N', Mohd Nor NH, Mohamed F
    J Microencapsul, 2014;31(6):600-8.
    PMID: 24697178 DOI: 10.3109/02652048.2014.898709
    The aim of this study is to investigate the cell uptake of Nigella sativa oil (NSO)-PLGA microparticle by neuron-like PC-12 cells in comparison to surfactants; hydrophilic (Tween 80 & Triton X100) and hydrophobic (Span 80). Solvent evaporation was used to precisely control the size, zeta potential and morphology of the particle. The results revealed varying efficiencies of the cell uptake by PC-12 cells, which may be partially attributed to the surface hydrophobicity of the microparticles. Interestingly, the uptake efficiency of PC-12 cells was higher with the more hydrophilic microparticle. NSO microparticle showed evidence of being preferably internalised by mitotic cells. Tween 80 microparticle showed the highest cell uptake efficiency with a concentration-dependent pattern suggesting its use as uptake enhancer for non-scavenging cells. In conclusion, PC-12 cells can take up NSO-PLGA microparticle which may have potential in the treatment of neurodegenerative disease.
    Matched MeSH terms: Polysorbates/chemistry
  14. Fulltext Preparation of Tween 80-Zn/Al-levodopa-layered double hydroxides nanocomposite for drug delivery system
    Kura AU, Hussein-Al-Ali SH, Hussein MZ, Fakurazi S
    ScientificWorldJournal, 2014;2014:104246.
    PMID: 24782658 DOI: 10.1155/2014/104246
    We incorporated anti-Parkinsonian drug, levodopa (dopa), in Zn/Al-LDH by coprecipitation method to form dopa-LDH nanocomposite. Further coating of Tween-80 on the external surfaces of dopa-LDH nanocomposite was achieved through the oxygen of C=O group of Tween-80 with the layer of dopa-LDH nanocomposite. The final product is called Tween-dopa-LDH nanocomposite. The X-ray diffraction indicates that the Tween-dopa-LDH nanocomposite was formed by aggregation structure. From the TGA data, the Tween-80 loading on the surface of LDH and dopa-LDH was 8.6 and 7.4%, respectively. The effect of coating process on the dopa release from Tween-dopa-LDH nanocomposite was also studied. The release from Tween-dopa-LDH nanocomposite shows slower release compared to the release of the drug from dopa-LDH nanocomposite as done previously in our study, presumably due to the retarding shielding effect. The cell viability study using PC12 showed improved viability with Tween-80 coating on dopa-LDH nanocomposite as studied by mitochondrial dehydrogenase activity (MTT assay).
    Matched MeSH terms: Polysorbates/chemistry*
  15. Effect of Emulsification Method and Particle Size on the Rate of in vivo Oral Bioavailability of Kenaf (Hibiscus cannabinus L.) Seed Oil
    Cheong AM, Tan CP, Nyam KL
    J Food Sci, 2018 Jul;83(7):1964-1969.
    PMID: 29802733 DOI: 10.1111/1750-3841.14191
    Kenaf (Hibiscus cannabinus L.) seed oil-in-water nanoemulsions stabilized by complexation of beta-cyclodextrin with sodium caseinate and Tween 20 have been shown to have higher bioaccessibility of vitamin E and total phenolic content than nonemulsified kenaf seed oil in the previous in vitro gastrointestinal digestion study. However, its oral bioavailability was unknown. Therefore, the aim of this study was to evaluate the rate of in vivo oral bioavailability of kenaf seed oil-in-water nanoemulsions in comparison with nonemulsified kenaf seed oil and kenaf seed oil macroemulsions during the 180 min of gastrointestinal digestion. Kenaf seed oil macroemulsions were produced by using conventional method. Kenaf seed oil-in-water nanoemulsions had shown improvement in the rate of absorption. At 180 min of digestion time, the total α-tocopherol bioavailability of kenaf seed oil nanoemulsions was increased by 1.7- and 1.4-fold, compared to kenaf seed oil and macroemulsion, respectively. Kenaf seed oil-in-water nanoemulsions were stable in considerably wide range of pH (>5 and <3), suggesting that it can be fortified into beverages within this pH range PRACTICAL APPLICATION: The production of kenaf seed oil-in-water nanoemulsions had provided a delivery system to encapsulate the kenaf seed oil, as well as enhanced the bioaccessibility and bioavailability of kenaf seed oil. Therefore, kenaf seed oil-in-water nanoemulsions exhibit a great potential application in nutraceutical fields.
    Matched MeSH terms: Polysorbates/chemistry
  16. Fulltext Optimization of process parameters in preparation of tocotrienol-rich red palm oil-based nanoemulsion stabilized by Tween80-Span 80 using response surface methodology
    Chong WT, Tan CP, Cheah YK, B Lajis AF, Habi Mat Dian NL, Kanagaratnam S, et al.
    PLoS One, 2018;13(8):e0202771.
    PMID: 30142164 DOI: 10.1371/journal.pone.0202771
    Red palm oil (RPO) is a natural source of Vitamin E (70-80% tocotrienol). It is a potent natural antioxidant that can be used in skin-care products. Its antioxidant property protects skin from inflammation and aging. In our work, a tocotrienol-rich RPO-based nanoemulsion formulation was optimized using response surface methodology (RSM) and formulated using high pressure homogenizer. Effect of the concentration of three independent variables [surfactant (5-15 wt%), co-solvent (10-30 wt%) and homogenization pressure (500-700 bar)] toward two response variables (droplet size, polydispersity index) was studied using central composite design (CCD) coupled to RSM. RSM analysis showed that the experimental data could be fitted into a second-order polynomial model and the coefficients of multiple determination (R2) is 0.9115. The optimized formulation of RPO-based nanoemulsion consisted of 6.09 wt% mixed surfactant [Tween 80/Span 80 (63:37, wt)], 20 wt% glycerol as a co-solvent via homogenization pressure (500 bar). The optimized tocotrienol-rich RPO-based nanoemulsion response values for droplet size and polydispersity index were 119.49nm and 0.286, respectively. The actual values of the formulated nanoemulsion were in good agreement with the predicted values obtained from RSM, thus the optimized compositions have the potential to be used as a nanoemulsion for cosmetic formulations.
    Matched MeSH terms: Polysorbates/chemistry
  17. Fulltext The preparation and evaluation of self-nanoemulsifying systems containing Swietenia oil and an examination of its anti-inflammatory effects
    Eid AM, El-Enshasy HA, Aziz R, Elmarzugi NA
    Int J Nanomedicine, 2014;9:4685-95.
    PMID: 25336948 DOI: 10.2147/IJN.S66180
    There is an increasing trend among pharmaceutical industries to use natural bioactive materials as medicinal agents and to use new technologies such as self-nanoemulsifying systems. The solubility and bioavailability of poorly soluble drugs can be enhanced by self-nanoemulsifying systems. Swietenia oil is frequently used because of its antimicrobial, antimutagenic, and anticancer bioactive medical properties. This study was conducted to develop self-nanoemulsifying systems for Swietenia oil that will enhance the anti-inflammatory activity of the oil. The self-emulsifying systems developed for Swietenia oil in this study were constructed using ternary phase diagrams and contained the nonionic surfactants Labrasol(®), Tween 20, Capmul(®), and Labrafil(®). The effect of these surfactants on the formulation was examined. The mean droplet size of Swietenia oil as well as their distribution, appearance, viscosity, and spreading times were studied to find the optimum formula, which contained droplets that were less than 200 nm. The next step was to test the anti-inflammatory properties of the optimum formula using a carrageenan-induced rat paw edema test. The results from this test were compared to the oil solution. Different oil/surfactants mixtures had various emulsification properties that were related to the size of their droplets. Tween 20 is a good surfactant to use in self-emulsifying systems because it produces droplets of nano-size. Mixtures of Capmul/Labrasol at a ratio of 2:1 and Labrafil/Tween 20 at a ratio of 1:2 were able to produce self-nanoemulsifying formulations containing Swietenia oil concentrations that ranged from 20%-50%. Nanoemulsion occurred when the size of the droplets fell below 200 nm with low size distribution (<0.3) after being gently mixed with water. It was found that the hydrophilic/lipophilic balance value affected the ternary phase diagram behavior of Swietenia oil and surfactants. In addition, the anti-inflammatory properties of Swietenia oil were greater in the self-nanoemulsifying systems than in the oil solution.
    Matched MeSH terms: Polysorbates/chemistry
  18. Fulltext Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
    Lim WM, Rajinikanth PS, Mallikarjun C, Kang YB
    Int J Nanomedicine, 2014;9:2117-26.
    PMID: 24833900 DOI: 10.2147/IJN.S57565
    The objectives of this study were to develop and characterize itraconazole (ITZ)-loaded nanostructured lipid carriers (NLCs) and to study their potential for drug delivery into the brain. Precirol(®) ATO 5 and Transcutol(®) HP were selected as the lipid phase, and Tween(®) 80 and Solutol(®) HS15 as surfactants. The ITZ-NLCs were prepared by a hot and high-pressure homogenization method. The entrapment efficiency for the best formulation batch was analyzed using high-performance liquid chromatography and was found to be 70.5%±0.6%. The average size, zeta potential, and polydispersity index for the ITZ-NLCs used for animal studies were found to be 313.7±15.3 nm, -18.7±0.30 mV, and 0.562±0.070, respectively. Transmission electron microscopy confirmed that ITZ-NLCs were spherical in shape, with a size of less than 200 nm. Differential scanning calorimetry and X-ray diffractometry analysis showed that ITZ was encapsulated in the lipid matrix and present in the amorphous form. The in vitro release study showed that ITZ-NLCs achieved a sustained release, with cumulative release of 80.6%±5.3% up to 24 hours. An in vivo study showed that ITZ-NLCs could increase the ITZ concentration in the brain by almost twofold. These results suggest that ITZ-NLCs can be exploited as nanocarriers to achieve sustained release and brain-targeted delivery.
    Matched MeSH terms: Polysorbates/chemistry
  19. Particle size analysis of nanocrystals: improved analysis method
    Keck CM
    Int J Pharm, 2010 May 5;390(1):3-12.
    PMID: 19733647 DOI: 10.1016/j.ijpharm.2009.08.042
    The influence of optical parameters, additional techniques (e.g. PIDS technology) and the importance of light microscopy were investigated by comparing laser diffraction data obtained via the conventional method and an optimized analysis method. Also the influence of a possible dissolution of nanocrystals during a measurement on the size result obtained was assessed in this study. The results reveal that dissolution occurs if unsaturated medium or microparticle saturated medium is used for the measurements. The dissolution is erratic and the results are not reproducible. Dissolution can be overcome by saturating the measuring medium prior to the measurement. If nanocrystals are analysed the dispersion medium should be saturated with the nanocrystals, because the solubility is higher than for coarse micro-sized drug material. The importance of using the optimized analysis method was proven by analysing 40 different nanosuspensions via the conventional versus the optimized sizing method. There was no large difference in the results obtained for the 40 nanosuspensions using the conventional method. This would have led to the conclusion, that all the 40 formulations investigated are physically stable. However, the analysis via the optimized method revealed that from 40 formulations investigated only four were physically stable. In conclusion an optimized analysis saves time and money and avoids misleading developments, because discrimination between "stable" and "unstable" can be done reliably at a very early stage of the development.
    Matched MeSH terms: Polysorbates/chemistry
  20. Fulltext Optimization of nanoemulsion containing gemcitabine and evaluation of its cytotoxicity towards human fetal lung fibroblast (MRC5) and human lung carcinoma (A549) cells
    Wahgiman NA, Salim N, Abdul Rahman MB, Ashari SE
    Int J Nanomedicine, 2019;14:7323-7338.
    PMID: 31686809 DOI: 10.2147/IJN.S212635
    Background: Gemcitabine (GEM) is a chemotherapeutic agent, which is known to battle cancer but challenging due to its hydrophilic nature. Nanoemulsion is water-in-oil (W/O) nanoemulsion shows potential as a carrier system in delivering gemcitabine to the cancer cell.

    Methods: The behaviour of GEM in MCT/surfactants/NaCl systems was studied in the ternary system at different ratios of Tween 80 and Span 80. The system with surfactant ratio 3:7 of Tween 80 and Span 80 was chosen for further study on the preparation of nanoemulsion formulation due to the highest isotropic region. Based on the selected ternary phase diagram, a composition of F1 was chosen and used for optimization by using the D-optimal mixture design. The interaction variables between medium chain triglyceride (MCT), surfactant mixture Tween 80: Span 80 (ratio 3:7), 0.9 % sodium chloride solution and gemcitabine were evaluated towards particle size as a response.

    Results: The results showed that NaCl solution and GEM gave more effects on particle size, polydispersity index and zeta potential of 141.57±0.05 nm, 0.168 and -37.10 mV, respectively. The optimized nanoemulsion showed good stability (no phase separation) against centrifugation test and storage at three different temperatures. The in vitro release of gemcitabine at different pH buffer solution was evaluated. The results showed the release of GEM in buffer pH 6.5 (45.19%) was higher than GEM in buffer pH 7.4 (13.62%). The cytotoxicity study showed that the optimized nanoemulsion containing GEM induced cytotoxicity towards A549 cell and at the same time reduced cytotoxicity towards MRC5 when compared to the control (GEM solution).

    Matched MeSH terms: Polysorbates/chemistry
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