Displaying publications 1 - 20 of 153 in total

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  1. Vallavan V, Krishnasamy G, Zin NM, Abdul Latif M
    Molecules, 2020 Dec 11;25(24).
    PMID: 33322256 DOI: 10.3390/molecules25245848
    Fungi are a rich source of secondary metabolites with several pharmacological activities such as antifungal, antioxidant, antibacterial and anticancer to name a few. Due to the large number of diverse structured chemical compounds they produce, fungi from the phyla Ascomycota, Basidiomycota and Muccoromycota have been intensively studied for isolation of bioactive compounds. Basidiomycetes-derived secondary metabolites are known as a promising source of antibacterial compounds with activity against Gram-positive bacteria. The continued emergence of antimicrobial resistance (AMR) poses a major challenge to patient health as it leads to higher morbidity and mortality, higher hospital-stay duration and substantial economic burden in global healthcare sector. One of the key culprits for AMR crisis is Staphylococcus aureus causing community-acquired infections as the pathogen develops resistance towards multiple antibiotics. The recent emergence of community strains of S. aureus harbouring methicillin-resistant (MRSA), vancomycin-intermediate (VISA) and vancomycin-resistant (VRSA) genes associated with increased virulence is challenging. Despite the few significant developments in antibiotic research, successful MRSA therapeutic options are still needed to reduce the use of scanty and expensive second-line treatments. This paper provides an overview of findings from various studies on antibacterial secondary metabolites from basidiomycetes, with a special focus on antistaphylococcal activity.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  2. Jafari SF, Khadeer Ahamed MB, Iqbal MA, Al Suede FS, Khalid SH, Haque RA, et al.
    J Pharm Pharmacol, 2014 Oct;66(10):1394-409.
    PMID: 25039905 DOI: 10.1111/jphp.12272
    Recently, we have isolated koetjapic acid (KA) from Sandoricum koetjape and identified its selective anticancer potentiality against colorectal carcinoma. KA is quite likely to be useful as a systemic anticancer agent against colorectal malignancy. However, with extremely low solubility, KA has to be converted into a biocompatible solubilized form without compromising the bioefficacy. Objective of this study is to enhance solubility of KA and to evaluate anticancer efficacy of potassium koetjapate in human colorectal cancer cells.
    Matched MeSH terms: Chemistry, Pharmaceutical
  3. Ngan CL, Basri M, Lye FF, Fard Masoumi HR, Tripathy M, Karjiban RA, et al.
    Int J Nanomedicine, 2014;9:4375-86.
    PMID: 25258528 DOI: 10.2147/IJN.S65689
    This research aims to formulate and to optimize a nanoemulsion-based formulation containing fullerene, an antioxidant, stabilized by a low amount of mixed surfactants using high shear and the ultrasonic emulsification method for transdermal delivery. Process parameters optimization of fullerene nanoemulsions was done by employing response surface methodology, which involved statistical multivariate analysis. Optimization of independent variables was investigated using experimental design based on Box-Behnken design and central composite rotatable design. An investigation on the effect of the homogenization rate (4,000-5,000 rpm), sonication amplitude (20%-60%), and sonication time (30-150 seconds) on the particle size, ζ-potential, and viscosity of the colloidal systems was conducted. Under the optimum conditions, the central composite rotatable design model suggested the response variables for particle size, ζ-potential, and viscosity of the fullerene nanoemulsion were 152.5 nm, -52.6 mV, and 44.6 pascal seconds, respectively. In contrast, the Box-Behnken design model proposed that preparation under the optimum condition would produce nanoemulsion with particle size, ζ-potential, and viscosity of 148.5 nm, -55.2 mV, and 39.9 pascal seconds, respectively. The suggested process parameters to obtain optimum formulation by both models yielded actual response values similar to the predicted values with residual standard error of <2%. The optimum formulation showed more elastic and solid-like characteristics due to the existence of a large linear viscoelastic region.
    Matched MeSH terms: Chemistry, Pharmaceutical
  4. Zainol S, Basri M, Basri HB, Shamsuddin AF, Abdul-Gani SS, Karjiban RA, et al.
    Int J Mol Sci, 2012;13(10):13049-64.
    PMID: 23202937 DOI: 10.3390/ijms131013049
    Response surface methodology (RSM) was utilized to investigate the influence of the main emulsion composition; mixture of palm and medium-chain triglyceride (MCT) oil (6%-12% w/w), lecithin (1%-3% w/w), and Cremophor EL (0.5%-1.5% w/w) as well as the preparation method; addition rate (2-20 mL/min), on the physicochemical properties of palm-based nanoemulsions. The response variables were the three main emulsion properties; particle size, zeta potential and polydispersity index. Optimization of the four independent variables was carried out to obtain an optimum level palm-based nanoemulsion with desirable characteristics. The response surface analysis showed that the variation in the three responses could be depicted as a quadratic function of the main composition of the emulsion and the preparation method. The experimental data could be fitted sufficiently well into a second-order polynomial model. The optimized formulation was stable for six months at 4 °C.
    Matched MeSH terms: Chemistry, Pharmaceutical
  5. AL Azzam KM, Aboul-Enein HY
    Methods Mol Biol, 2013;919:67-78.
    PMID: 22976091 DOI: 10.1007/978-1-62703-029-8_7
    Capillary electrophoresis coupled with a capacitively coupled contactless conductivity detector (CE-C(4)D) has been employed for the determination of the β-blocker drugs (atenolol and amiloride) in pharmaceutical formulations. 150 mM acetic acid was used as background electrolyte. The influence of several factors (detector excitation voltage and frequency, buffer concentration, applied voltage, capillary temperature, and injection time) was studied. Non-UV absorbing L-valine was used as an internal standard; the analytes were all separated in less than 7 min. The separation was carried out in normal polarity mode at 28 °C, 25 kV, and using hydrodynamic injection (25 s). The separation was effected in a bare fused-silica capillary 75 μm × 52 cm. The CE-C(4)D method was validated with respect to linearity, limit of detection and quantification, accuracy, precision, and selectivity. Calibration curves were linear over the range 5-250 μg mL(-1) for the studied analytes. The relative standard deviations of intra- and inter-day precisions of migration times and corrected peak areas were less than 6.0%. The method showed good precision and accuracy and was successfully applied to the simultaneous determination of the β-blocker drugs in different pharmaceutical tablets.
    Matched MeSH terms: Chemistry, Pharmaceutical
  6. Elbashir AA, Suliman FE, Saad B, Aboul-Enein HY
    Talanta, 2009 Feb 15;77(4):1388-93.
    PMID: 19084654 DOI: 10.1016/j.talanta.2008.09.029
    A capillary electrophoretic method for the separation of the aminoglutethimide (AGT) enantiomers using methylated-beta-cyclodextrin (M-beta-CD) as chiral selector is described. Several parameters affecting the separation were studied, including the type and concentration of chiral selector, buffer pH, voltage and temperature. Good chiral separation of the racemic mixture was achieved in less than 9 min with resolution factor Rs=2.1, using a fused-silica capillary and a background electrolyte (BGE) of tris-phosphate buffer solution (50 mmol L(-1), pH 3.0) containing 30 mgm L(-1) of M-beta-CD. The separation was carried out in normal polarity mode at 25 degrees C, 16 kV and using hydrostatic injection. Acceptable validation criteria for selectivity, linearity, precision, and accuracy/recovery were included. The proposed method was successfully applied to the assay of AGT enantiomers in pharmaceutical formulations. The computational calculations for the inclusion complexes of the R- and S-AGT-M-beta-CD rationalized the reasons for the different migration times between the AGT enantiomers.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods*
  7. Samiun WS, Ashari SE, Salim N, Ahmad S
    Int J Nanomedicine, 2020;15:1585-1594.
    PMID: 32210553 DOI: 10.2147/IJN.S198914
    Background: Aripiprazole, which is a quinolinone derivative, has been widely used to treat schizophrenia, major depressive disorder, and bipolar disorder.

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

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

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

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

    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  8. Taghizadeh Davoudi E, Ibrahim Noordin M, Kadivar A, Kamalidehghan B, Farjam AS, Akbari Javar H
    Biomed Res Int, 2013;2013:495319.
    PMID: 24288681 DOI: 10.1155/2013/495319
    Gastrointestinal disturbances, such as nausea and vomiting, are considered amongst the main adverse effects associated with oral anticancer drugs due to their fast release in the gastrointestinal tract (GIT). Sustained release formulations with proper release profiles can overcome some side effects of conventional formulations. The current study was designed to prepare sustained release tablets of Capecitabine, which is approved by the Food and Drug Administration (FDA) for the treatment of advanced breast cancer, using hydroxypropyl methylcellulose (HPMC), carbomer934P, sodium alginate, and sodium bicarbonate. Tablets were prepared using the wet granulation method and characterized such that floating lag time, total floating time, hardness, friability, drug content, weight uniformity, and in vitro drug release were investigated. The sustained release tablets showed good hardness and passed the friability test. The tablets' floating lag time was determined to be 30-200 seconds, and it floated more than 24 hours and released the drug for 24 hours. Then, the stability test was done and compared with the initial samples. In conclusion, by adjusting the right ratios of the excipients including release-retarding gel-forming polymers like HPMC K4M, Na alginate, carbomer934P, and sodium bicarbonate, sustained release Capecitabine floating tablet was formulated.
    Matched MeSH terms: Chemistry, Pharmaceutical*
  9. Agatonovic-Kustrin S, Alany RG
    Pharm Res, 2001 Jul;18(7):1049-55.
    PMID: 11496944
    PURPOSE: A genetic neural network (GNN) model was developed to predict the phase behavior of microemulsion (ME), lamellar liquid crystal (LC), and coarse emulsion forming systems (W/O EM and O/W EM) depending on the content of separate components in the system and cosurfactant nature.

    METHOD: Eight pseudoternary phase triangles, containing ethyl oleate as the oil component and a mixture of two nonionic surfactants and n-alcohol or 1,2-alkanediol as a cosurfactant, were constructed and used for training, testing, and validation purposes. A total of 21 molecular descriptors were calculated for each cosurfactant. A genetic algorithm was used to select important molecular descriptors, and a supervised artificial neural network with two hidden layers was used to correlate selected descriptors and the weight ratio of components in the system with the observed phase behavior.

    RESULTS: The results proved the dominant role of the chemical composition, hydrophile-lipophile balance, length of hydrocarbon chain, molecular volume, and hydrocarbon volume of cosurfactant. The best GNN model, with 14 inputs and two hidden layers with 14 and 9 neurons, predicted the phase behavior for a new set of cosurfactants with 82.2% accuracy for ME, 87.5% for LC, 83.3% for the O/W EM, and 91.5% for the W/O EM region.

    CONCLUSIONS: This type of methodology can be applied in the evaluation of the cosurfactants for pharmaceutical formulations to minimize experimental effort.

    Matched MeSH terms: Chemistry, Pharmaceutical
  10. Sultana S, Hossain MAM, Naquiah NNA, Ali ME
    PMID: 30028648 DOI: 10.1080/19440049.2018.1500719
    Gelatin is widely used in pharmaceuticals as a protective coating, such as soft and hard capsule shells. However, the animal source of gelatin is a sensitive issue because certain gelatins such as porcine and bovine gelatins are not welcome in Halal, Kosher and Hindus' consumer goods. Recently, we have documented DNA barcoding and multiplex PCR platforms for discriminating porcine, bovine and fish gelatins in various fish and confectionary products; but those assays were not self-authenticating and also not tested in highly refined pharmaceutical products. To address this knowledge gap, here we report a self-authenticating multiplex PCR-restriction fragment length polymorphism (RFLP) assay to identify animal sources of various gelatin in pharmaceutical capsules. Three different restriction enzymes, BsaAI, Hpy188I and BcoDI were used to yield distinctive RFLP patterns for gelatin-based bovine (26, 94 bp), fish (97, 198 bp) and porcine (17, 70 bp) DNA in control experiments. The specificity was cross-tested against 16 non-target species and the optimised assay was used to screen gelatin sources in 30 halal-branded pharmaceuticals capsule shells. Bovine and porcine DNA was found in 27 and 3 of the 30 different capsules products. The assay was suitable for detecting 0.1 to 0.01 ng total DNA extracted from pure and mixed gelatins. The study might be useful to authenticate and monitor halal, kosher, vegetarian and Hindu compliant pharmaceuticals, foods and cosmetics.
    Matched MeSH terms: Chemistry, Pharmaceutical
  11. Ho WY, Yeap S, Liang WS, Beh BK, Mohamad N, Alitheen NB
    Pak J Pharm Sci, 2015 Jan;28(1):15-22.
    PMID: 25553678
    Vernonia amygdalina is a strong natural antioxidant that possessed various medicinal properties. In this study, the spray-dried water extract of V. amygdalina was evaluated for its in vitro antioxidant capacity and in vivo hepatoprotective effect against alcoholic-mediated liver damage. Total phenolic and flavonoid content of spray-dried V. amygdalina water extract were determined. Liver enzyme profiles, liver antioxidant level and nitric oxide level were evaluated in alcohol-induced liver injured mice or co-supplement with spray-dried V. amydalina. Water extract of spray-dried V. amygalina that contained phenolic content of 24.8±1.5 mg/g gallic acid equivalent and total flavonoid content of 25.7±1.3 mg/g catechin equivalent was able to inhibit 50% of xanthine and tyrosinase oxidation at 170 μg/ml and 2 mg/mL, respectively. On the other hand, extracts at both 10 and 50 mg/kg body weight were able to reduce the levels of Alanine transaminase (ALT), Alkaline phosphatase (ALP), Aspartate transaminase (AST), triglyceride and total bilirubin content inthe alcohol-mediated liver injury in mice. Furthermore, it also helped to increase levels of Superoxide dismutase (SOD), Ferric reducing ability of plasma (FRAP) and reduce the levels of Nitric oxide (NO) and Malondialdehyde (MDA) in the liver of the treated mice. These resultssuggestedthat water extract of spray-dried V. amygdalina exhibited liver protective effect, which could be contributed by its antioxidant properties.
    Matched MeSH terms: Chemistry, Pharmaceutical
  12. Greco G, Di Piazza S, Chan J, Zotti M, Hanna R, Gheno E, et al.
    Photodiagnosis Photodyn Ther, 2020 Mar;29:101575.
    PMID: 31614222 DOI: 10.1016/j.pdpdt.2019.10.010
    BACKGROUND: A large number of systemic diseases can be linked to oral candida pathogenicity. The global trend of invasive candidiasis has increased progressively and is often accentuated by increasing Candida albicans resistance to the most common antifungal medications. Photodynamic therapy (PDT) is a promising therapeutic approach for oral microbial infections. A new formulation of 5-aminolevulinic acid (5%ALA) in a thermosetting gel (t) (5%ALA-PTt) was patented and recently has become available on the market. However, its antimicrobial properties, whether mediated or not by PDT, are not yet known. In this work we characterised them.

    METHODS: We isolated a strain of C. albicans from plaques on the oral mucus membrane of an infected patient. Colonies of this strain were exposed for 1 24 h, to 5%ALA-PTt, 5%ALA-PTt buffered to pH 6.5 (the pH of the oral mucosa) (5%ALA-PTtb) or not exposed (control). The 1 h-exposed samples were also irradiated at a wavelength of 630 nm with 0.14 watts (W) and 0.37 W/cm2 for 7 min at a distance of <1 mm.

    RESULTS AND CONCLUSION: The 5% ALA-PTt preparation was shown to be effective in reducing the growth of biofilm and inoculum of C. albicans. This effect seems to be linked to the intrinsic characteristics of 5%ALA-TPt, such acidic pH and the induction of free radical production. This outcome was significantly enhanced by the effect of PDT at relatively short incubation and irradiation times, which resulted in growth inhibition of both treated biofilm and inoculum by ∼80% and ∼95%, respectively.

    Matched MeSH terms: Chemistry, Pharmaceutical
  13. Wong TW, Wahab S, Anthony Y
    Drug Dev Ind Pharm, 2007 Jul;33(7):737-46.
    PMID: 17654022
    The drug release behavior of beads made of poly(methyl vinyl ether-co-maleic acid) was investigated with respect to the influence of microwave irradiation. The beads were prepared by an extrusion method with sodium diclofenac as a model water-soluble drug. The beads were subjected to microwave irradiation at 80 W for 5 and 20 min, and at 300 W for 1 min 20 s and 5 min 20 s. The profiles of drug dissolution, drug content, drug-polymer interaction, and polymer-polymer interaction were determined by using dissolution testing, drug content assay, differential scanning calorimetry, and Fourier transform infra-red spectroscopy. Keeping the level of supplied irradiation energy identical, treatment of beads by microwave at varying intensities of irradiation did not bring about similar drug release profiles. The extent and rate of drug released from beads were markedly enhanced through treating the samples by microwave at 80 W as a result of loss of polymer-polymer interaction via the (CH(2))(n) moiety, but decreased upon treating the beads by microwave at 300 W following polymer-polymer interaction via the O-H, COOH, and COO(-) moieties as well as drug-polymer interaction via the N-H, O-H, COO(-), and C-O moieties. The beads treated by microwave at 300 W exhibited a higher level of drug release retardation capacity than those that were treated by microwave at 80 W in spite of polymer-polymer interaction via the (CH(2))(n) moiety was similarly reduced in the matrix. The mechanism of drug release of both microwave-treated and untreated beads tended to follow zero order kinetics. The drug release was markedly governed by the state of polymer relaxation of the matrix and was in turn affected by the state of polymer-polymer and/or drug-polymer interaction in beads.
    Matched MeSH terms: Chemistry, Pharmaceutical
  14. Hasnain MS, Nayak AK, Singh M, Tabish M, Ansari MT, Ara TJ
    Int J Biol Macromol, 2016 Feb;83:71-7.
    PMID: 26608007 DOI: 10.1016/j.ijbiomac.2015.11.044
    Alginate-based bipolymeric-nanobioceramic composite matrices for sustained drug release were developed through incorporation of nano-hydroxyapatite [nHAp] powders within ionotropically-gelled calcium ion-induced alginate-poly (vinyl pyrrolidone) blends polymeric systems. nHAp powders were synthesized by precipitation technique using calcium hydroxide [Ca(OH)2] and orthophosphoric acid [H3PO4] as raw materials. The average particle size of these was synthesized. nHAp powders was found as 19.04 nm and used to prepare nHAp-alginate-PVP beads containing DS. These beads exhibited drug entrapment efficiency (%) of 65.82±1.88 to 94.45±3.72% and average bead sizes of 0.98±0.07 to 1.23±0.15 mm. These beads were characterized by scanning electron microscopy (SEM) and Fourier transform-infra red (FTIR) spectroscopy analyses. Various nHAp-alginate-PVP beads containing DS exhibited prolonged sustained drug release and followed the Koresmeyer-Peppas model of drug release (R2=0.9908-0.9978) with non-Fickian release (anomalous transport) mechanism (n=0.73-0.84) for drug release over 8 h.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  15. Salam NA, Naeem MA, Malik NS, Riaz M, Shahiq-Uz-Zaman -, Masood-Ur-Rehman -, et al.
    Pak J Pharm Sci, 2020 Jan;33(1(Supplementary)):269-279.
    PMID: 32122858
    The main objective of the present study was to explore the potential of matrix tablets as extended release dosage form of tianeptine, using HMPC K100 as a polymer. HPMC K100 extended the release of the drug from formulation due to the gel-like structure. Direct compression method was adopted to compress the tablets using different concentrations of polymer. Tablets were evaluated for pre-compression and post-compression parameters. Drug release study showed that tablet extends the release of drug with the increasing concentration of polymer. Drug, polymers and tablets were analyzed and/or characterized for compatibility, degradation, thermal stability, amorphous or crystalline nature via FTIR, DSC, TGA, XRD studies. SEM study predicted that tablets had a uniform structure. HPMC K100 based tablets were similar to that of the reference product. Acute toxicity study conducted on Swiss albino mice showed that matrix tablets were safe and non-toxic, as no changes in physical activity and functions of organs were observed. Biochemical and histopathological study revealed lack of any kind of abnormality in liver and renal function. Moreover, necrotic changes were absent at organ level.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods*
  16. Khoo YS, Aziz Z
    J Clin Pharm Ther, 2009 Apr;34(2):133-45.
    PMID: 19250134 DOI: 10.1111/j.1365-2710.2008.00998.x
    Prevention of cardiovascular disease by modifying its major risk factors, including serum cholesterol levels, is an important strategy. Regular intake of garlic has been suggested, but its impact on cholesterol levels has been inconsistent.
    Matched MeSH terms: Chemistry, Pharmaceutical
  17. Sakeena MH, Elrashid SM, Munavvar AS, Azmin MN
    J Oleo Sci, 2011;60(4):155-8.
    PMID: 21427510
    Aim of the present work is to study the effects of oil and drug concentrations on droplets size of a nanoemulsion. Newly introduced oil, palm oil esters (POEs) by Universiti Putra Malaysia researchers was selected for the oil phase of the nanoemulsion, because the oil was reported to be a good vehicle for pharmaceutical use. Nanoemulsions were prepared with different concentrations of oil and drug and their effects on droplets size were studied by laser scattering spectroscopy (Nanophox). The results of droplets size analysis shows the droplets size increase with increasing concentration of oil and drug concentrations. It can be concluded from this study, that oil and drug concentrations have an effect on the droplets size of POEs nanoemulsion system.
    Matched MeSH terms: Chemistry, Pharmaceutical
  18. Sakeena MH, Muthanna FA, Ghassan ZA, Kanakal MM, Elrashid SM, Munavvar AS, et al.
    J Oleo Sci, 2010;59(4):223-8.
    PMID: 20299769
    The aim of the present study is to formulate and investigate the potential of nanoemulsion formulation for topical delivery of ketoprofen. In this study, Palm Oil Esters (POEs) a newly introduced oil by Universiti Putra Malaysia researchers was chosen for the oil phase of the nanoemulsion, because the oil was reported to be a good vehicle for pharmaceutical use. Oil-in-water nanoemulsion was prepared by spontaneous emulsification method. The droplets size was studied by laser scattering spectroscopy (Nanophox) and Transmission Electron Microscopy (TEM). Franz diffusion cells were used, to determine the drug release and drug transferred through methyl acetate cellulose membrane (artificial membrane). The results of droplets size analysis shows the droplets are in the range of nanoemulsion which is below than 500 nm. The in vitro release profile shows a sufficient percentage of drugs released through the methyl acetate cellulose membrane. This initial study showed that the nanoemulsion formulated using POEs has great potential for topical delivery of ketoprofen.
    Matched MeSH terms: Chemistry, Pharmaceutical
  19. Al-Edresi S, Baie S
    Int J Pharm, 2009 May 21;373(1-2):174-8.
    PMID: 19429303 DOI: 10.1016/j.ijpharm.2009.02.011
    Virgin coconut oil (VCO)-in-water, nano-emulsion in the form of cream stabilized by Emulium Kappa as an emulsifier, was prepared by using the Emulsion Inversion Point method. A nano-emulsion with droplet size <300 nm was then obtained. VCO has recently become a more popular new material in the cosmetic industries. Emulium Kappa is an ionic emulsifier that contains sodium stearoyl lactylate, the active whitening ingredient was Kojic Dipalmitate. Ostwald ripening is the main destabilizing factor for the nano-emulsion. This decline can be reduced by adding non-soluble oil, namely squalene, to the virgin coconut oil. We tested VCO:squalene in the ratios of 10:0, 9.8:0.2, 9.6:0.4, 9.4:0.6, 9.2:0.8, 9:1 and 8:2 and discovered that squalene's higher molecular weight (above critical molecular weight) resulted in low polarity and insolubility in the continuous phase. The continuous partitioning between the droplets results in the decline of Ostwald ripening. Furthermore, flocculation may occur due to the instability of nano-emulsion, especially for the preparations with little or no squalene at all. The stability of the nano-emulsion was evaluated by the electrophoretic properties of the emulsion droplets. The zeta potential values for the emulsion increased as the percentage of squalene oil increased.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  20. Tan SL, Stanslas J, Basri M, Abedi Karjiban RA, Kirby BP, Sani D, et al.
    Curr Drug Deliv, 2015;12(6):795-804.
    PMID: 26324229
    Carbamzepine (CBZ) was encapsulated in a parenteral oil-in-water nanoemulsion, in an attempt to improve its bioavailability. The particle size, polydispersity index and zeta potential were measured using dynamic light scattering. Other parameters such as pH, osmolality, viscosity, drug loading efficiency and entrapment efficiency were also recorded. Transmission electron microscopy revealed that emulsion droplets were almost spherical in shape and in the nano-range. The in vitro release profile was best characterized by Higuchi's equation. The parenteral nanoemulsion of CBZ showed significantly higher AUC0→5, AUC0→∞, AUMC0→5, AUMC0→∞, Cmax and lower clearance than that of CBZ solution in plasma. Additionally, parenteral nanoemulsion of CBZ showed significantly higher AUC0→∞, AUMC0→∞ and Cmaxthan that of CBZ solution in brain. The parenteral nanoemulsion of CBZ could therefore use as a carrier, worth exploring further for brain targeting.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
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