Displaying publications 1 - 20 of 153 in total

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  1. Fulltext Topical Lyogel Containing Corticosteroid Decreases IgE Expression and Enhances the Therapeutic Efficacy Against Atopic Eczema
    Ng SF, Anuwi NA, Tengku-Ahmad TN
    AAPS PharmSciTech, 2015 Jun;16(3):656-63.
    PMID: 25511806 DOI: 10.1208/s12249-014-0248-y
    Hydrocortisone cream intended for atopic eczema often produces unwanted side effects after long-term use. These side effects are essentially due to repeated percutaneous administration of the medication for skin dermatitis, as atopic eczema is a relapsing disorder. Hence, there is a need to develop a new hydrocortisone formulation that will deliver the drug more effectively and require a reduced dosing frequency; therefore, the side effects could be minimized. In this study, a hydroxypropyl methylcellulose (HPMC) lyogel system based on 80% organic and 20% aqueous solvents containing 1% hydrocortisone was formulated. The hydrocortisone lyogel physicochemical characteristics, rheological properties, stability profile, and in vitro Franz cell drug release properties, as well as the in vivo therapeutic efficacies and dermal irritancy in Balb/c mice were investigated. The HPMC lyogel appeared clear and soft and was easy to rub on the skin. The lyogel also showed a higher drug release profile compared with commercial hydrocortisone cream. Similar to the cream, HPMC lyogels exhibited pseudoplastic behavior. From the mouse model, the hydrocortisone lyogel showed higher inflammatory suppressive effects than the cream. However, it did not reduce the transepidermal water loss as effectively as the control did. The dermal irritancy testing revealed that the hydrocortisone lyogel caused minimal irritation. In conclusion, HPMC lyogel is a promising vehicle to deliver hydrocortisone topically, as it showed a higher drug release in vitro as well as enhanced therapeutic efficacy in resolving eczematous inflammatory reaction compared with commercial cream.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  2. Fulltext Lipid effects on expulsion rate of amphotericin B from solid lipid nanoparticles
    Tan SW, Billa N
    AAPS PharmSciTech, 2014 Apr;15(2):287-95.
    PMID: 24318197 DOI: 10.1208/s12249-013-0056-9
    We aimed to investigate the effects that natural lipids, theobroma oil (TO) and beeswax (BW), might have on the physical properties of formulated nanoparticles and also the degree of expulsion of encapsulated amphotericin B (AmB) from the nanoparticles during storage. Lecithin and sodium cholate were used as emulsifiers whilst oleic acid (OA) was used to study the influence of the state of orderliness/disorderliness within the matrices of the nanoparticles on the degree of AmB expulsion during storage. BW was found to effect larger z-average diameter compared with TO. Lecithin was found to augment the stability of the nanoparticles imparted by BW and TO during storage. An encapsulation efficiency (%EE) of 59% was recorded when TO was the sole lipid as against 42% from BW. In combination however, the %EE dropped to 39%. When used as sole lipid, TO or BW formed nanoparticles with comparatively higher enthalpies, 21.1 and 23.3 J/g respectively, which subsequently caused significantly higher degree of AmB expulsion, 81 and 83% respectively, whilst only 11.8% was expelled from a binary TO/BW mixture. A tertiary TO/BW/OA mixture registered the lowest enthalpy at 8.07 J/g and expelled 12.6% of AmB but encapsulated only 22% of AmB. In conclusion, nanoparticles made from equal concentrations of TO and BW produced the most desirable properties and worthy of further investigations.
    Matched MeSH terms: Chemistry, Pharmaceutical
  3. Fulltext Characterization of oral disintegrating film containing donepezil for Alzheimer disease
    Liew KB, Tan YT, Peh KK
    AAPS PharmSciTech, 2012 Mar;13(1):134-42.
    PMID: 22167416 DOI: 10.1208/s12249-011-9729-4
    The aim of this study was to develop a taste-masked oral disintegrating film (ODF) containing donepezil, with fast disintegration time and suitable mechanical strength, for the treatment of Alzheimer's disease. Hydroxypropyl methylcellulose, corn starch, polyethylene glycol, lactose monohydrate and crosspovidone served as the hydrophilic polymeric bases of the ODF. The uniformity, in vitro disintegration time, drug release and the folding endurance of the ODF were examined. The in vitro results showed that 80% of donepezil hydrochloride was released within 5 minutes with mean disintegration time of 44 seconds. The result of the film flexibility test showed that the number of folding time to crack the film was 40 times, an indication of sufficient mechanical property for patient use. A single-dose, fasting, four-period, eight-treatment, double-blind study involving 16 healthy adult volunteers was performed to evaluate the in situ disintegration time and palatability of ODF. Five parameters, namely taste, aftertaste, mouthfeel, ease of handling and acceptance were evaluated. The mean in situ disintegration time of ODF was 49 seconds. ODF containing 7 mg of sucralose were more superior than saccharin and aspartame in terms of taste, aftertaste, mouthfeel and acceptance. Furthermore, the ODF was stable for at least 6 months when stored at 40°C and 75% relative humidity.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods*
  4. Formulation variables affecting drug release from xanthan gum matrices at laboratory scale and pilot scale
    Billa N, Yuen KH
    AAPS PharmSciTech, 2000;1(4):E30.
    PMID: 14727895
    The purpose of this research was to study processing variables at the laboratory and pilot scales that can affect hydration rates of xanthan gum matrices containing diclofenac sodium and the rate of drug release. Tablets from the laboratory scale and pilot scale proceedings were made by wet granulation. Swelling indices of xanthan gum formulations prepared with different amounts of water were measured in water under a magnifying lens. Granules were thermally treated in an oven at 60 degrees C, 70 degrees C, and 80 degrees C to study the effects of elevated temperatures on drug release from xanthan gum matrices. Granules from the pilot scale formulations were bulkier compared to their laboratory scale counterparts, resulting in more porous, softer tablets. Drug release was linear from xanthan gum matrices prepared at the laboratory scale and pilot scales; however, release was faster from the pilot scales. Thermal treatment of the granules did not affect the swelling index and rate of drug release from tablets in both the pilot and laboratory scale proceedings. On the other hand, the release from both proceedings was affected by the amount of water used for granulation and the speed of the impeller during granulation. The data suggest that processing variables that affect the degree of wetness during granulation, such as increase in impeller speed and increase in amount of water used for granulation, also may affect the swelling index of xanthan gum matrices and therefore the rate of drug release.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  5. Fulltext Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum)
    Meka VS, Nali SR, Songa AS, Kolapalli VR
    AAPS PharmSciTech, 2012 Dec;13(4):1451-64.
    PMID: 23090110 DOI: 10.1208/s12249-012-9873-5
    The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosage form is exposed to gastrointestinal fluids in the gastric environment. As BG was being explored for the first time for its pharmaceutical application, physicochemical, microbiological, rheological, and stability studies were carried out on this gum. In the present investigation, the physicochemical properties, such as micromeritic, rheological, melting point, moisture content, pH, swelling index, water absorption, and volatile acidity, were evaluated. The gum was characterized by scanning electron microscopy, differential scanning calorimetry (DSC), powder X-ray diffraction studies (PXRD), and Fourier transform infrared spectroscopy (FTIR). Gastroretentive floating tablets of BG were prepared with the model drug propranolol HCl by direct compression methods. The prepared tablets were evaluated for all their physicochemical properties, in vitro buoyancy, in vitro drug release, and rate order kinetics. PBG 04 was selected as an optimized formulation based on its 12-h drug release and good buoyancy characteristics. The optimized formulation was characterized with FTIR, DSC, and PXRD studies, and no interaction between the drug and BG was found. Thus, the study confirmed that BG might be used in the gastroretentive drug delivery system as a release-retarding polymer.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  6. Fulltext New film-coated tablet formulation of deferasirox is well tolerated in patients with thalassemia or lower-risk MDS: Results of the randomized, phase II ECLIPSE study
    Taher AT, Origa R, Perrotta S, Kourakli A, Ruffo GB, Kattamis A, et al.
    Am J Hematol, 2017 May;92(5):420-428.
    PMID: 28142202 DOI: 10.1002/ajh.24668
    Once-daily deferasirox dispersible tablets (DT) have a well-defined safety and efficacy profile and, compared with parenteral deferoxamine, provide greater patient adherence, satisfaction, and quality of life. However, barriers still exist to optimal adherence, including gastrointestinal tolerability and palatability, leading to development of a new film-coated tablet (FCT) formulation that can be swallowed with a light meal, without the need to disperse into a suspension prior to consumption. The randomized, open-label, phase II ECLIPSE study evaluated the safety of deferasirox DT and FCT formulations over 24 weeks in chelation-naïve or pre-treated patients aged ≥10 years, with transfusion-dependent thalassemia or IPSS-R very-low-, low-, or intermediate-risk myelodysplastic syndromes. One hundred seventy-three patients were randomized 1:1 to DT (n = 86) or FCT (n = 87). Adverse events (overall), consistent with the known deferasirox safety profile, were reported in similar proportions of patients for each formulation (DT 89.5%; FCT 89.7%), with a lower frequency of severe events observed in patients receiving FCT (19.5% vs. 25.6% DT). Laboratory parameters (serum creatinine, creatinine clearance, alanine aminotransferase, aspartate aminotransferase and urine protein/creatinine ratio) generally remained stable throughout the study. Patient-reported outcomes showed greater adherence and satisfaction, better palatability and fewer concerns with FCT than DT. Treatment compliance by pill count was higher with FCT (92.9%) than with DT (85.3%). This analysis suggests deferasirox FCT offers an improved formulation with enhanced patient satisfaction, which may improve adherence, thereby reducing frequency and severity of iron overload-related complications.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  7. Development and anti-microbial potential of topical formulations containing Cocos nucifera Linn
    Sheshala R, Ying LT, Hui LS, Barua A, Dua K
    Antiinflamm Antiallergy Agents Med Chem, 2013;12(3):253-64.
    PMID: 23746224
    In order to achieve better treatment for local wounds and bacterial infections, topical formulations containing Cocos nucifera Linn. were developed. These formulations were evaluated for their physicochemical properties and antimicrobial efficacy against various strains of microorganisms. Semisolid formulations containing 5% w/w of Cocos nucifera Linn. were prepared by employing different dermatological bases and were evaluated for their physical appearance, pH, rheological properties, FTIR-spectroscopic analysis, thermodynamic stability and stability studies. The antimicrobial activity of each prepared formulation was determined using disk-diffusion method against various strains of microorganisms. All the prepared formulations were found to be stable and exhibited suitable physicochemical characteristics including pH, viscosity and spreadability which are necessary for an ideal topical preparation, in addition to strong antimicrobial activity. Carbopol gel base was found to be the most suitable dermatological base for Cocos nucifera Linn. in comparsion to other bases. Cocos nucifera Linn. formulations showed great potential for wounds and local bacterial infections. Moreover, carbopol gel base with its aesthetic appeal was found to be a suitable dermatological base for Cocos nucifera Linn. semisolid formulation as it had demonstrated significant physicochemical properties and greater diffusion when assessed using disk- diffusion method.
    Matched MeSH terms: Chemistry, Pharmaceutical
  8. Investigation on the effect of polymer and starch on the tablet properties of lyophilized orally disintegrating tablet
    Liew KB, Peh KK
    Arch Pharm Res, 2021 Aug;44(8):1-10.
    PMID: 25579848 DOI: 10.1007/s12272-014-0542-y
    Orally disintegrating tablet (ODT) is a user friendly and convenient dosage form. The study aimed to investigate the effect of polymers and wheat starch on the tablet properties of lyophilized ODT, with dapoxetine as model drug. Three polymers (hydroxypropylmethyl cellulose, carbopol 934P and Eudragit® EPO) and wheat starch were used as matrix forming materials in preparation of lyophilized ODT. The polymeric dispersion was casted into a mould and kept in a freezer at -20 °C for 4 h before freeze dried for 12 h. It was found that increasing in HPMC and Carbopol 934P concentrations produced tablets with higher hardness and longer disintegration time. In contrast, Eudragit® EPO was unable to form tablet with sufficient hardness at various concentrations. Moreover, HPMC seems to have a stronger effect on tablet hardness compared to Carbopol 934P at the same concentration level. ODT of less friable was obtained. Wheat starch acted as binder which strengthen the hardness of ODTs and prolonged the disintegration time. ODT comprising of HPMC and wheat starch at ratio of 2:1 was found to be optimum based upon the tablet properties. The optimum formulation was palatable and 80 % of the drug was released within 30 min in the dissolution study.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  9. Fulltext Preparation and characterization of a gastric floating dosage form of capecitabine
    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*
  10. AChE inhibitor: a regio- and stereo-selective 1,3-dipolar cycloaddition for the synthesis of novel substituted 5,6-dimethoxy spiro[5.3']-oxindole-spiro-[6.3″]-2,3-dihydro-1H-inden-1″-one-7-(substituted aryl)-tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole
    Ashraf Ali M, Ismail R, Choon TS, Kumar RS, Osman H, Arumugam N, et al.
    Bioorg Med Chem Lett, 2012 Jan 1;22(1):508-11.
    PMID: 22142546 DOI: 10.1016/j.bmcl.2011.10.087
    Pyrrolothiazolyloxindole analogues share vital pharmacological properties, considered useful in Alzheimer's disease (AD). The aim of this study was synthesis and evaluate pyralothiazolyloxindole analogues if possess acetyl cholinesterase (AChE) inhibitory activity. The easily accessible one-pot synthesis of these compounds resulted to be significantly less difficult and expensive than that of donepezil. Several compounds possess anti-cholinesterase activity in the order of micro and sub-micromolar. Particularly, compound was the most potent inhibitors of the series against acetyl cholinesterase enzyme with IC(50) 0.11μmol/L.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  11. Characterization and effect on skin hydration of engkabang-based emulsions
    Abd Gani SS, Basri M, Rahman MB, Kassim A, Abd Rahman RN, Salleh AB, et al.
    Biosci Biotechnol Biochem, 2010;74(6):1188-93.
    PMID: 20530909
    Formulations containing engkabang fat and engkabang fat esters, F10 and E15 respectively were prepared using a high-shear homogenizer, followed by a high-pressure homogenizer. Both formulations were stable at room temperature, at 45 degrees C, and after undergoing freeze-thaw cycles. The particle sizes of F10 and E15 after high pressure were 115.75 nm and 148.41 nm respectively. The zeta potentials of F10 and E15 were -36.4 mV and -48.8 mV respectively, while, the pH values of F10 and E15 were 5.59 and 5.81 respectively. The rheology of F10 and E15 showed thixotropy and pseudoplastic behavior respectively. There were no bacteria or fungal growths in the samples. The short-term moisturizing effect on 20 subjects analyzed by analysis of variance (ANOVA), gave p-values of 7.35 x 10(-12) and 2.77 x 10(-15) for F10 and E15 respectively. The hydration of the skins increased after application of F10 and E15 with p-value below 0.05.
    Matched MeSH terms: Chemistry, Pharmaceutical
  12. Coatless alginate pellets as sustained-release drug carrier for inflammatory bowel disease treatment
    Md Ramli SH, Wong TW, Naharudin I, Bose A
    Carbohydr Polym, 2016 Nov 05;152:370-381.
    PMID: 27516284 DOI: 10.1016/j.carbpol.2016.07.021
    Conventional alginate pellets underwent rapid drug dissolution and failed to exert colon targeting unless subjected to complex coating. This study designed coatless delayed-release oral colon-specific alginate pellets for ulcerative colitis treatment. Alginate pellets, formulated with water-insoluble ethylcellulose and various calcium salts, were prepared using solvent-free melt pelletization technique which prevented reaction between processing materials during agglomeration and allowed reaction to initiate only in dissolution. Combination of acid-soluble calcium carbonate and highly water-soluble calcium acetate did not impart colon-specific characteristics to pellets due to pore formation in fragmented matrices. Combination of moderately water-soluble calcium phosphate and calcium acetate delayed drug release due to rapid alginate crosslinking by soluble calcium from acetate salt followed by sustaining alginate crosslinking by calcium phosphate. The use of 1:3 ethylcellulose-to-alginate enhanced the sustained drug release attribute. The ethylcellulose was able to maintain the pellet integrity without calcium acetate. Using hydrophobic prednisolone as therapeutic, hydrophilic alginate pellets formulated with hydrophobic ethylcellulose and moderately polar calcium phosphate exhibited colon-specific in vitro drug release and in vivo anti-inflammatory action. Coatless oral colon-specific alginate pellets can be designed through optimal formulation with melt pelletization as the processing technology.
    Matched MeSH terms: Chemistry, Pharmaceutical
  13. Functional properties of dually modified sago starch/κ-carrageenan films: An alternative to gelatin in pharmaceutical capsules
    Oladzadabbasabadi N, Ebadi S, Mohammadi Nafchi A, Karim AA, Kiahosseini SR
    Carbohydr Polym, 2017 Mar 15;160:43-51.
    PMID: 28115099 DOI: 10.1016/j.carbpol.2016.12.042
    The aim of this study was development a composite film based on sago starch and κ-carrageenan to find a gelatin alternative in the pharmaceutical capsules processing. Hydrolyzed-Hydroxypropylated (dually modified) sago starch was mixed with κ-carrageenan (0.25, 0.5, 0.75, and 1%). The drying kinetics, thermomechanical, physicochemical, and barrier properties of composite films were estimated and compared with bovine gelatin. Results show that drying kinetics and mechanical properties of the composite films were comparable to those of gelatin. The water vapor permeability and moisture content of the composite films were lower than those of gelatin. The solubility of the composite films was higher than that of gelatin, and the composite films were more stable at higher relative humidity than were the gelatin films. These results show that dually modified sago starch in combination with κ-carrageenan has properties similar to those of gelatin, thus proposed system can be used in pharmaceutical capsules processes.
    Matched MeSH terms: Chemistry, Pharmaceutical*
  14. Phytochemical survey of Malaysian plants preliminary chemical and pharmacological screening
    Nakanishi K, Sasaki S, Kiang AK, Goh J, Kakisawa H, Ohashi M, et al.
    Chem Pharm Bull (Tokyo), 1965 Jul;13(7):882-90.
    PMID: 5867816
    Matched MeSH terms: Chemistry, Pharmaceutical*
  15. 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: Chemistry, Pharmaceutical
  16. Fulltext Design, synthesis and biological potential of heterocyclic benzoxazole scaffolds as promising antimicrobial and anticancer agents
    Kakkar S, Kumar S, Narasimhan B, Lim SM, Ramasamy K, Mani V, et al.
    Chem Cent J, 2018 Sep 19;12(1):96.
    PMID: 30232633 DOI: 10.1186/s13065-018-0464-8
    BACKGROUND: Benzoxazole is the most important class of heterocyclic compound in medicinal chemistry. It has been incorporated in many medicinal compounds making it a versatile heterocyclic compound that possess a wide spectrum of biological activities.

    RESULTS: The molecular structures of synthesized benzoxazole derivatives were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity against selected microbial species using tube dilution method and antiproliferative activity against human colorectal carcinoma (HCT 116) cancer cell line by Sulforhodamine B assay.

    CONCLUSION: In vitro antimicrobial results demonstrated that compounds 4, 5, 7 and 16 showed promising antimicrobial potential. The in vitro anticancer activity indicated that compounds 4 and 16 showed promising anticancer activity against human colorectal cancer cell line (HCT 116) when compared to standard drug and these compounds may serve as lead compound for further development of novel antimicrobial and anticancer agents.

    Matched MeSH terms: Chemistry, Pharmaceutical
  17. Fulltext Synthesis, biological evaluation and corrosion inhibition studies of transition metal complexes of Schiff base
    Kashyap S, Kumar S, Ramasamy K, Lim SM, Shah SAA, Om H, et al.
    Chem Cent J, 2018 Nov 20;12(1):117.
    PMID: 30460466 DOI: 10.1186/s13065-018-0487-1
    BACKGROUND: The transition metal complexes formed from Schiff base is regarded as leading molecules in medicinal chemistry. Because of the preparative availability and diversity in the structure of central group, the transition metals are important in coordination chemistry. In the present work, we have designed and prepared Schiff base and its metal complexes (MC1-MC4) and screened them for antimicrobial, anticancer and corrosion inhibitory properties.

    METHODOLOGY: The synthesized metal complexes were characterized by physicochemical and spectral investigation (UV, IR, 1H and 13C-NMR) and were further evaluated for their antimicrobial (tube dilution) and anticancer (SRB assay) activities. In addition, the corrosion inhibition potential was determined by electrochemical impedance spectroscopy (EIS) technique.

    RESULTS AND DISCUSSION: Antimicrobial screening results found complexes (MC1-MC4) to exhibit less antibacterial activity against the tested bacterial species compared to ofloxacin while the complex MC1 exhibited greater antifungal activity than the fluconazole. The anticancer activity results found the synthesized Schiff base and its metal complexes to elicit poor cytotoxic activity than the standard drug (5-fluorouracil) against HCT116 cancer cell line. Metal complex MC2 showed more corrosion inhibition efficiency with high Rct values and low Cdl values.

    CONCLUSION: From the results, we can conclude that complexes MC1 and MC2 may be used as potent antimicrobial and anticorrosion agents, respectively.

    Matched MeSH terms: Chemistry, Pharmaceutical
  18. A bioequivalence comparison of two formulations of rifampicin (300- vs 150-mg capsules): An open-label, randomized, two-treatment, two-way crossover study in healthy volunteers
    Chik Z, Basu RC, Pendek R, Lee TC, Mohamed Z
    Clin Ther, 2010 Sep;32(10):1822-31.
    PMID: 21194606 DOI: 10.1016/j.clinthera.2010.09.006
    Rifampicin is a semisynthetic antibiotic derivative of rifamycin used worldwide for the treatment of various forms of tuberculosis.
    Matched MeSH terms: Chemistry, Pharmaceutical
  19. Tamoxifen-loaded nanostructured lipid carrier as a drug delivery system: characterization, stability assessment and cytotoxicity
    How CW, Rasedee A, Manickam S, Rosli R
    Colloids Surf B Biointerfaces, 2013 Dec 1;112:393-9.
    PMID: 24036474 DOI: 10.1016/j.colsurfb.2013.08.009
    Cancer nanotherapeutics is beginning to overwhelm the global research and viewed to be the revolutionary treatment regime in the medical field. This investigation describes the development of a stable nanostructured lipid carrier (NLC) system as carrier for Tamoxifen (TAM). The TAM-loaded NLC (TAM-NLC) developed with 200mg of TAM showed a spherical particle with the size of 46.6nm, polydispersity index of 0.267, entrapment efficiency of 99.74% and with the zeta potential of -23.78mV. Besides, the equivalent cytotoxicity of TAM and TAM-NLC to human (MCF-7) and mice (4T1) mammary breast cancer cell lines were observed. Incubating the formulation at the physiological pH resulted into reduced Ostwald ripening rate but without any significant change in the absorptivity. When coupled with the measurements of zeta potential and Ostwald ripening rate, the absorbance assay may be used to predict the long-term stability of drug-loaded nanoparticle formulations. The results of the study also suggest that TAM-NLC is a promising drug delivery system for breast cancer therapy. This is the first encouraging report on the in vitro effect of TAM-NLC against human and mouse mammary adenocarcinoma cell lines.
    Matched MeSH terms: Chemistry, Pharmaceutical
  20. Formulation optimization of palm kernel oil esters nanoemulsion-loaded with chloramphenicol suitable for meningitis treatment
    Musa SH, Basri M, Masoumi HR, Karjiban RA, Malek EA, Basri H, et al.
    Colloids Surf B Biointerfaces, 2013 Dec 1;112:113-9.
    PMID: 23974000 DOI: 10.1016/j.colsurfb.2013.07.043
    Palm kernel oil esters nanoemulsion-loaded with chloramphenicol was optimized using response surface methodology (RSM), a multivariate statistical technique. Effect of independent variables (oil amount, lecithin amount and glycerol amount) toward response variables (particle size, polydispersity index, zeta potential and osmolality) were studied using central composite design (CCD). RSM analysis showed that the experimental data could be fitted into a second-order polynomial model. Chloramphenicol-loaded nanoemulsion was formulated by using high pressure homogenizer. The optimized chloramphenicol-loaded nanoemulsion response values for particle size, PDI, zeta potential and osmolality were 95.33nm, 0.238, -36.91mV, and 200mOsm/kg, respectively. The actual values of the formulated nanoemulsion were in good agreement with the predicted values obtained from RSM. The results showed that the optimized compositions have the potential to be used as a parenteral emulsion to cross blood-brain barrier (BBB) for meningitis treatment.
    Matched MeSH terms: Chemistry, Pharmaceutical
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