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William N. Charman
BPharm, VCP; PhD, Univ. Kansas
Phone: +61 3 9903 9519
Fax: +61 3 9903 9560
email: Bill.Charman@pharm.monash.edu.au
General research interests
- Oral drug delivery and lymphatic drug transport
- Lipid-based formulation design and assessment
- Drug discovery and lead optimisation
Current research areas
- Design of formulations to enhance oral drug bioavailability
- Mechanistic evaluation of intestinal lymphatic drug transport
- Design, lead optimisation and pre-clinical development of new drug candidates
- Development of new methods for supporting rapid throughput lead optimisation
Recent significant publications
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S.A. Charman, C. Perry, F. Chiu, K. McIntosh, R. Prankerd, W.N. Charman. Alteration of the intravenous pharmacokinetics of a synthetic ozonide antimalarial in the presence of a modified cyclodextrin. (2006) Journal of Pharmaceutical Sciences 95(2): 256-267.
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Y. Dong, Y. Tang, J. Chollet, H. Matile, S. Wittlin, S.A. Charman, W.N. Charman, J.S. Tomas, C. Scheurer, C. Snyder, B. Scorneaux, S. Bajpai, S. Alexander, X. Wang, M. Padmanilayam, S. Cheruku, R. Brun, J. Vennerstrom. Effect of functional group polarity on the antimalarial activity of sprio and dispiro-1,2,4-trioxolanes. (2006) Bioorganic & Medicinal Chemistry, 14: 6368-6382.
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L. Sek, B. J. Boyd, W.N. Charman and C.J.H. Porter. Examination of the impact of a range of pluronic surfactants on the in-vitro solubilisation behaviour and oral bioavailability of pipidic formulations of atovaquone. (2006) Journal of Pharmacy and Pharmacology, 58: 809-820
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R. Holm, T. Porsgaard, C.J.H. Porter, C.E. Hoy, G.A. Edwards, A. Mullertz, H. Kristensen and W.N. Charman. Lymphatic fatty acids in canines dosed with pharmaceutical formulations containing structured triacyglycerols. (2006) European Journal of Lipid Science and Technology, 108: 714-722.
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M. Padmanilayam, B. Scorneaux, Y. Dong, J. Chollet, H. Matile, S. A. Charman, D. Creek, W.N. Charman, J.S. Tomas, C. Scheurer, S. Wittlin, R. Brun, and J. Vennerstrom. Antimalarial activity of N-Alkyl amine, carboxamide, sulphonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperdine. (2006) Bioorganic and Medicinal Chemistry Letters, 16: 5542-5545.
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N.L. Leveque, W.N. Charman and F.C.K. Chiu. Sensitive method for the quantitative determination of proguanil and its metabolites in rat blood and plasma by liquid chromatography-mass spectrometry. (2006) J. Chromatography B, 830: 314-321.
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C.S. Perry, S.A. Charman, R.J. Prankerd, F.C.K. Chiu, M.J. Scanlon, D. Chalmers and W.N. Charman. The binding interaction of synthetic ozonide antimalarials with natural and modified beta-cyclodextrins. (2006) J. Pharm. Sci., 95, 146-158.
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S.A. Charman, C.S. Perry, F.C.K. Chiu, K.A. McIntosh and W.N. Charman. Alteration of the pharmacokinetics of a new chemical entity in the presence of a substituted cyclodextrin. (2006) J. Pharm. Sci. 95: 256-267.
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C.S. Perry, S.A. Charman, R.J. Prankerd, F.C.K. Chiu, Y. Dong, J.L. Vennerstrom and W.N. Charman. Chemical kinetics and aqueous degradation pathways of a new class of synthetic ozonide antimalarials. (2006) J. Pharm. Sci., 95: 737-747.
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N.L. Trevaskis, C.J.H. Porter and W.N. Charman. The lymph lipid precursor pool is a key determinate of intestinal lymphatic drug transport. (2006) J. Pharmacol. Exp. Ther., 316: 881-891.
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N. Trevaskis, P. Tso, T. Rider, W.N. Charman, C.J.H. Porter, R. Jandacek. Tissue uptake of DDT is independent of chylomicron metabolism. (2005) Archives in Toxicology (In press)
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N.L. Leveque, W.N. Charman and F.C.K. Chiu. Sensitive method for the quantitative determination of proguanil and its metabolites in rat blood and plasma by liquid chromatography. Journal of Chromatography B (2005) 830: 314-321.
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N. Trevaskis, C.J.H. Porter and W.N. Charman. Bile increases intestinal lymphatic drug transport in the fasted rat. (2005) Pharmaceutical Research, 22(11): 1863-1870.
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T. Velkov, S. Chuang, J. Wielens, H, Sakellaris, W. N. Charman, C.J.H. Porter and M. Scanlon. The Interaction of Lipophilic Drugs with Intestinal Fatty Acid-Binding Protein. (2005) The Journal of Biological Chemistry, 280 (18): 17766 - 17769.
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Y. Dong, J. Chollet, H. Matile, S.A. Charman, F. Chiu, W.N. Charman, B. Scorneaux, H. Urwyler, J. Santo Tomas, C. Scheurer, A.D. Snyder, X. Wang, J. Karle, Y. Tang, S. Wittlin, R. Brun, J. Vennerstrom. Spiro and Dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes. (2005) J. Med. Chem. 48: 4953-4961.
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D.J. Creek, F. Chiu, R. Prankerd, S.A. Charman, W.N. Charman. Kinetics of iron-mediated artemisinin degradation: effect of solvent composition and iron salt.(2005) J. Pharm. Sci. 94: 1820-1829.
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G.A. Kossena, W.N. Charman, B.J. Boyd, C.J.H. Porter. Influence of the intermediate digestion phases of common formulation lipids on the absorption of a poorly water-soluble drug (2005) J. Pharm. Res. 94(3): 481-492.
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J.L.Vennerstrom, S. Arbe-Barnes, R. Brun, S.A. Charman, F.C.K. Chiu, J. Chollet, Y. Dong, A. Dorn, D. Hunziker, H. Matile, K.A. McIntosh, M. Padmanilayam, J. Santo Tomas, C. Scheurer, B. Scorneaux, Y. Tang, H. Urwyler, S. Wittlin, W.N. Charman. Identification of an antimalarial synthetic trioxolane drug development candidate.(2004) Nature, 430: 900-904.
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C.J.H. Porter, A.M. Kaukonen, B.J. Boyd, G.A. Edwards, W.N. Charman.Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol administered as a medium-chain lipid-based microemulsion formulation. (2004) Pharm. Res., 21: 1405-1412.
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G.A. Kossena, W.N. Charman, B.J. Boyd, C.J.H. Porter. A novel cubic phase of medium chain formulation lipid origin for the delivery of poorly water soluble drugs.(2004) J. Controlled Release, 99: 217-229.
- M.P. McIntosh, A.J. Batey, S.J. Coker, C.J.H. Porter, W.N. Charman.Evaluation of the impact of altered lipoprotein binding conditions on halofantrine induced QTc interval prolongation in an anesthetised rabbit model. (2004) J. Pharm. Pharmacol., 56: 69-77.
- G.A. Kossena, W.N. Charman, B.J. Boyd, D.E. Dunstan, C.J.H. Porter.Probing drug solubilisation patterns in the gastrointestinal tract after administration of lipid based delivery systems: A phase diagram approach. (2004) J. Pharm. Sci., 93:332-348.
- A.M. Kaukonen, B.J. Boyd, W.N. Charman, C.J.H. Porter. Drug solubilisation behaviour during in vitro digestion of suspension formulations of poorly water soluble drugs in triglyceride lipids. (2004) Pharm. Res., 21:254-260.
- S-M Khoo, D.M. Shackleford, C.J.H. Porter, G.A. Edwards, W.N. Charman. Intestinal lymphatic transport of halofantrine occurs after oral administration of a unit dose lipid-based formulation to fasted dogs. (2003) Pharm. Res., 20:1460-1465.
- D.M. Shackleford, W.A. Fassen, N. Houwing, H. Lass, G.A. Edwards, C.J.H. Porter, W.N. Charman. The contribution of lymphatically transported testosterone undecanoate to the systemic exposure of testosterone after oral administration of two Andriol formulations in conscious lymph-duct cannulated dogs (2003) J. Pharmacol. Exp. Ther., 306:925-933.
- B.M. Johnson, W.N. Charman, C.J.H. Porter. Application of compartmental modelling to an examination of in vitro permeability data: Assessing the impact of tissue uptake, P-glycoprotein, and CYP3A. (2003) Drug Metab. Dispos., 31:1151-1160.
- B.M. Johnson, W. Chen, R.T. Borchardt, W.N. Charman, C.J.H. Porter. A kinetic evaluation of the absorption, efflux and metabolism of verapamil in the autoperfused rat jejunum. (2003) J. Pharmacol. Exp. Ther., 305:151-158.
- G.A. Kossena, B.J. Boyd, C.J.H. Porter, W.N Charman. Separation and characterisation of the colloidal phases produced on digestion of common formulation lipids and assessment of their impact on the apparent solubility of selected poorly water-soluble drugs. (2003) J. Pharm. Sci., 92: 634-648.
- L. Sek, C.J.H. Porter, A.M. Kaukonen, W.N. Charman. Evaluation of the in vitro digestion profiles of long and medium chain glycerides and the phase behaviour of their lipolytic products. (2002) J. Pharm. Pharmacol., 54:29-41.
- S-M Khoo, R.J. Prankerd, G.A. Edwards, C.J.H. Porter, W.N. Charman. A physicochemical basis for the extensive intestinal lymphatic transport of a poorly lipid soluble antimalarial, halofantrine hydrochloride, after post-prandial administration to dogs.(2002). J. Pharm. Sci., 91:647-659.
- S-M Khoo, G.A. Edwards, C.J.H. Porter, W.N. Charman. A conscious dog model for assessing the absorption, enterocyte-based metabolism and intestinal lymphatic transport of halofantrine.(2001) J. Pharm. Sci., 90:1599-1607.
- W.N. Charman. Lipids, lipophilic drugs, and oral drug delivery - some emerging concepts.(2000) J. Pharm. Sci., 89: 967-978.
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