List of works - William N. Charman

50years of oral lipid-based formulations: Provenance, progress and future perspectives

scientific article published on 15 April 2016

A conscious dog model for assessing the absorption, enterocyte-based metabolism, and intestinal lymphatic transport of halofantrine.

scientific article published in October 2001

A mouse model to evaluate the impact of species, sex, and lipid load on lymphatic drug transport

scientific article

A novel cubic phase of medium chain lipid origin for the delivery of poorly water soluble drugs.

scientific article published in September 2004

A physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine

scientific article published on 01 May 1996

A simplified liquid chromatography assay for the quantitation of halofantrine and desbutylhalofantrine in plasma and identification of a degradation product of desbutylhalofantrine formed under alkaline conditions

article

Acute hypertriglyceridemia promotes intestinal lymphatic lipid and drug transport: a positive feedback mechanism in lipid and drug absorption.

scientific article

Alteration of the intravenous pharmacokinetics of a synthetic ozonide antimalarial in the presence of a modified cyclodextrin

scientific article published in February 2006

An Acute and Coincident Increase in FABP Expression and Lymphatic Lipid and Drug Transport Occurs During Intestinal Infusion of Lipid-Based Drug Formulations to Rats

scientific article published on 01 August 2006

An examination of the interplay between enterocyte-based metabolism and lymphatic drug transport in the rat.

scientific article published on 7 February 2006

An in vitro examination of the impact of polyethylene glycol 400, Pluronic P85, and vitamin E d-alpha-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine.

scientific article published on January 2002

Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp. ⬇️

scientific article

Bile increases intestinal lymphatic drug transport in the fasted rat.

scientific article published on 16 August 2005

Characterisation and quantification of medium chain and long chain triglycerides and their in vitro digestion products, by HPTLC coupled with in situ densitometric analysis.

scientific article published in June 2001

Computational prediction of drug solubility in lipid based formulation excipients.

scientific article published on 15 June 2013

Computational prediction of formulation strategies for beyond-rule-of-5 compounds

scientific article

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.

scientific article

Correction to "targeted drug delivery to lymphocytes: a route to site-specific immunomodulation?"

scientific article published on 13 October 2011

Degradation of berenil (diminazene aceturate) in acidic aqueous solution

scientific article published in October 2004

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity.

scientific article published in May 2018

Does stereoselective lymphatic absorption contribute to the enantioselective pharmacokinetics of halofantrine In Vivo?

scientific article published in May 2003

Drug solubilization behavior during in vitro digestion of simple triglyceride lipid solution formulations

scientific article published in February 2004

Drug solubilization behavior during in vitro digestion of suspension formulations of poorly water-soluble drugs in triglyceride lipids

scientific article published in February 2004

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H receptor antagonists

article

Effect of Altered Serum Lipid Concentrations on the IC50 of Halofantrine against Plasmodium Falciparum ⬇️

scientific article published on February 1, 1998

Evaluation of the impact of altered lipoprotein binding conditions on halofantrine induced QTc interval prolongation in an anaesthetized rabbit model

scientific article published in January 2004

Examination of oral absorption and lymphatic transport of halofantrine in a triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides.

scientific article

Examination of the impact of a range of Pluronic surfactants on the in-vitro solubilisation behaviour and oral bioavailability of lipidic formulations of atovaquone

scientific article published on 01 June 2006

High throughput, quantitative analysis of human osteoclast differentiation and activity

scientific article published on 14 December 2016

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice

scientific article published on April 2009

Identification of an antimalarial synthetic trioxolane drug development candidate

scientific article

Influence of physicochemical properties on the patterns of association of a series of aliphatic esters of halofantrine with plasma lipoproteins

scientific article published in March 2004

Influence of the intermediate digestion phases of common formulation lipids on the absorption of a poorly water-soluble drug.

scientific article published in March 2005

Intestinal bile secretion promotes drug absorption from lipid colloidal phases via induction of supersaturation

scientific article published on 27 March 2013

Intestinal lymphatic transport enhances the post-prandial oral bioavailability of a novel cannabinoid receptor agonist via avoidance of first-pass metabolism.

scientific article published on 12 March 2009

Intestinal lymphatic transport of halofantrine occurs after oral administration of a unit-dose lipid-based formulation to fasted dogs

scientific article published on September 1, 2003

Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: implications for lymphatic transport and absolute bioavailability studies.

scientific article published on 23 May 2012

Isoform-Specific Biased Agonism of Histamine H3 Receptor Agonists

scientific article published on 18 November 2016

Kinetics of iron-mediated artemisinin degradation: effect of solvent composition and iron salt

scientific article published in August 2005

Label-Free Kinetics: Exploiting Functional Hemi-Equilibrium to Derive Rate Constants for Muscarinic Receptor Antagonists

scientific article published on 4 August 2015

Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice

scientific article

Lymphatic fatty acids in canines dosed with pharmaceutical formulations containing structured triacylglycerols

Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target

scientific article

Murine GPRC6A Mediates Cellular Responses to L-Amino Acids, but Not Osteocalcin Variants

scientific article published on 19 January 2016

Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin

scientific article published in March 2004

Partitioning of halofantrine hydrochloride between water, micellar solutions, and soybean oil: Effects on its apparent ionization constant.

scientific article published in November 2003

Probing drug solubilization patterns in the gastrointestinal tract after administration of lipid-based delivery systems: a phase diagram approach.

scientific article

Professor Valentino J. Stella: scientist, mentor, entrepreneur, family man, and giant in pharmaceutical chemistry

scientific article published on 30 May 2012

Self-association of nicotinamide in aqueous solution: mass transport, freezing-point depression, and partition coefficient studies

scientific article published on September 1, 1991

Self-micellization of gemfibrozil 1-O-beta acyl glucuronide in aqueous solution

scientific article

Sensitive method for the quantitative determination of proguanil and its metabolites in rat blood and plasma by liquid chromatography-mass spectrometry

scientific article published on 23 November 2005

Separation and characterization 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.

scientific article published in March 2003

Stability of peroxide antimalarials in the presence of human hemoglobin

scientific article published on June 2009

Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

scientific article

Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation.

scientific article

Synthesis, structure-activity relationships and brain uptake of a novel series of benzopyran inhibitors of insulin-regulated aminopeptidase.

scientific article published on 7 February 2014

Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria

scientific article

Targeted delivery of a model immunomodulator to the lymphatic system: comparison of alkyl ester versus triglyceride mimetic lipid prodrug strategies

scientific article published on 05 January 2014

Targeted drug delivery to lymphocytes: a route to site-specific immunomodulation?

scientific article published on 12 November 2010

The Role of the Intestinal Lymphatics in the Absorption of Two Highly Lipophilic Cholesterol Ester Transfer Protein Inhibitors (CP524,515 and CP532,623)

scientific article published on 11 March 2010

The binding interaction of synthetic ozonide antimalarials with natural and modified beta-cyclodextrins

scientific article published in January 2006

The impact of P-glycoprotein efflux on enterocyte residence time and enterocyte-based metabolism of verapamil.

scientific article published in December 2001

The interaction of lipophilic drugs with intestinal fatty acid-binding protein.

scientific article

The lymph lipid precursor pool is a key determinant of intestinal lymphatic drug transport.

scientific article

The mechanism of lymphatic access of two cholesteryl ester transfer protein inhibitors (CP524,515 and CP532,623) and evaluation of their impact on lymph lipoprotein profiles

scientific article published on 16 July 2010

The role of lecithin degradation on the pH dependent stability of halofantrine encapsulated fat nano-emulsions

scientific article published on 12 June 2017

The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).

scientific article

Tissue uptake of DDT is independent of chylomicron metabolism

scientific article published in April 2006

Transport and absorption of drugs via the lymphatic system

scientific article published on 01 August 2001

Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity

scientific article published on 13 April 2009

Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: studies with halofantrine.

scientific article

List of works by William N. Charman

50years of oral lipid-based formulations: Provenance, progress and future perspectives

A conscious dog model for assessing the absorption, enterocyte-based metabolism, and intestinal lymphatic transport of halofantrine.

A mouse model to evaluate the impact of species, sex, and lipid load on lymphatic drug transport

A novel cubic phase of medium chain lipid origin for the delivery of poorly water soluble drugs.

A physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine

A simplified liquid chromatography assay for the quantitation of halofantrine and desbutylhalofantrine in plasma and identification of a degradation product of desbutylhalofantrine formed under alkaline conditions

Acute hypertriglyceridemia promotes intestinal lymphatic lipid and drug transport: a positive feedback mechanism in lipid and drug absorption.

Alteration of the intravenous pharmacokinetics of a synthetic ozonide antimalarial in the presence of a modified cyclodextrin

An Acute and Coincident Increase in FABP Expression and Lymphatic Lipid and Drug Transport Occurs During Intestinal Infusion of Lipid-Based Drug Formulations to Rats

An examination of the interplay between enterocyte-based metabolism and lymphatic drug transport in the rat.

An in vitro examination of the impact of polyethylene glycol 400, Pluronic P85, and vitamin E d-alpha-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine.

Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp. ⬇️

Bile increases intestinal lymphatic drug transport in the fasted rat.

Characterisation and quantification of medium chain and long chain triglycerides and their in vitro digestion products, by HPTLC coupled with in situ densitometric analysis.

Computational prediction of drug solubility in lipid based formulation excipients.

Computational prediction of formulation strategies for beyond-rule-of-5 compounds

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.

Correction to "targeted drug delivery to lymphocytes: a route to site-specific immunomodulation?"

Degradation of berenil (diminazene aceturate) in acidic aqueous solution

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity.

Does stereoselective lymphatic absorption contribute to the enantioselective pharmacokinetics of halofantrine In Vivo?

Drug solubilization behavior during in vitro digestion of simple triglyceride lipid solution formulations

Drug solubilization behavior during in vitro digestion of suspension formulations of poorly water-soluble drugs in triglyceride lipids

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H receptor antagonists

Effect of Altered Serum Lipid Concentrations on the IC50 of Halofantrine against Plasmodium Falciparum ⬇️

Evaluation of the impact of altered lipoprotein binding conditions on halofantrine induced QTc interval prolongation in an anaesthetized rabbit model

Examination of oral absorption and lymphatic transport of halofantrine in a triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides.

Examination of the impact of a range of Pluronic surfactants on the in-vitro solubilisation behaviour and oral bioavailability of lipidic formulations of atovaquone

High throughput, quantitative analysis of human osteoclast differentiation and activity

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice

Identification of an antimalarial synthetic trioxolane drug development candidate

Influence of physicochemical properties on the patterns of association of a series of aliphatic esters of halofantrine with plasma lipoproteins

Influence of the intermediate digestion phases of common formulation lipids on the absorption of a poorly water-soluble drug.

Intestinal bile secretion promotes drug absorption from lipid colloidal phases via induction of supersaturation

Intestinal lymphatic transport enhances the post-prandial oral bioavailability of a novel cannabinoid receptor agonist via avoidance of first-pass metabolism.

Intestinal lymphatic transport of halofantrine occurs after oral administration of a unit-dose lipid-based formulation to fasted dogs

Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: implications for lymphatic transport and absolute bioavailability studies.

Isoform-Specific Biased Agonism of Histamine H3 Receptor Agonists

Kinetics of iron-mediated artemisinin degradation: effect of solvent composition and iron salt

Label-Free Kinetics: Exploiting Functional Hemi-Equilibrium to Derive Rate Constants for Muscarinic Receptor Antagonists

Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice

Lymphatic fatty acids in canines dosed with pharmaceutical formulations containing structured triacylglycerols

Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target

Murine GPRC6A Mediates Cellular Responses to L-Amino Acids, but Not Osteocalcin Variants

Orally active antimalarials: hydrolytically stable derivatives of 10-trifluoromethyl anhydrodihydroartemisinin

Partitioning of halofantrine hydrochloride between water, micellar solutions, and soybean oil: Effects on its apparent ionization constant.

Probing drug solubilization patterns in the gastrointestinal tract after administration of lipid-based delivery systems: a phase diagram approach.

Professor Valentino J. Stella: scientist, mentor, entrepreneur, family man, and giant in pharmaceutical chemistry

Self-association of nicotinamide in aqueous solution: mass transport, freezing-point depression, and partition coefficient studies

Self-micellization of gemfibrozil 1-O-beta acyl glucuronide in aqueous solution

Sensitive method for the quantitative determination of proguanil and its metabolites in rat blood and plasma by liquid chromatography-mass spectrometry

Separation and characterization 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.

Stability of peroxide antimalarials in the presence of human hemoglobin

Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation.

Synthesis, structure-activity relationships and brain uptake of a novel series of benzopyran inhibitors of insulin-regulated aminopeptidase.

Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria

Targeted delivery of a model immunomodulator to the lymphatic system: comparison of alkyl ester versus triglyceride mimetic lipid prodrug strategies

Targeted drug delivery to lymphocytes: a route to site-specific immunomodulation?

The Role of the Intestinal Lymphatics in the Absorption of Two Highly Lipophilic Cholesterol Ester Transfer Protein Inhibitors (CP524,515 and CP532,623)

The binding interaction of synthetic ozonide antimalarials with natural and modified beta-cyclodextrins

The impact of P-glycoprotein efflux on enterocyte residence time and enterocyte-based metabolism of verapamil.

The interaction of lipophilic drugs with intestinal fatty acid-binding protein.

The lymph lipid precursor pool is a key determinant of intestinal lymphatic drug transport.

The mechanism of lymphatic access of two cholesteryl ester transfer protein inhibitors (CP524,515 and CP532,623) and evaluation of their impact on lymph lipoprotein profiles

The role of lecithin degradation on the pH dependent stability of halofantrine encapsulated fat nano-emulsions

The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).

Tissue uptake of DDT is independent of chylomicron metabolism

Transport and absorption of drugs via the lymphatic system

Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity

Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: studies with halofantrine.