All Outputs (55)

Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation (2018)
Journal Article
Citossi, F., Smith, T., Lee, J. B., Segal, J., Gershkovich, P., Stocks, M. J., Bradshaw, T. D., Kellam, B., & Marlow, M. (in press). Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation. Molecular Pharmaceutics, 15(4), https://doi.org/10.1021/acs.molpharmaceut.7b01106

Low molecular weight gelators (LMWGs) of chemotherapeutic drugs represent a valid alternative to the existing poly-mer-based formulations used for targeted delivery of anticancer drugs. Herein we report the design and development of novel self-assemb... Read More about Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation.

Oral administration of cannabis with lipids leads to high levels of cannabinoids in the intestinal lymphatic system and prominent immunomodulation (2017)
Journal Article
Zgair, A., Lee, J. B., Wong, J. C. M., Taha, D. A., Aram, J., Virgilio, D. D., McArthur, A. G., Cheng, Y.-K., Hennig, I. M., Barrett, D. A., Fischer, P. M., Constantinescu, C. S., & Gershkovich, P. (2017). Oral administration of cannabis with lipids leads to high levels of cannabinoids in the intestinal lymphatic system and prominent immunomodulation. Scientific Reports, 7, 1-12. https://doi.org/10.1038/s41598-017-15026-z

Cannabidiol (CBD) and Δ9-tetrahydrocannabinol (THC) have well documented immunomodulatory effects in vitro, but not following oral administration in humans. Here we show that oral co-administration of cannabinoids with lipids can substantially increa... Read More about Oral administration of cannabis with lipids leads to high levels of cannabinoids in the intestinal lymphatic system and prominent immunomodulation.

Development of cordycepin formulations for preclinical and clinical studies (2017)
Journal Article
Lee, J. B., Adrower, C., Qin, C., Fischer, P. M., de Moor, C. H., & Gershkovich, P. (2017). Development of cordycepin formulations for preclinical and clinical studies. AAPS PharmSciTech, 18(8), 3219-3226. https://doi.org/10.1208/s12249-017-0795-0

There is extensive literature on in vivo studies with cordycepin but these studies were generally conducted without validation of the various formulations, especially in terms of the solubility of cordycepin in the dosing vehicles used. Cordycepin is... Read More about Development of cordycepin formulations for preclinical and clinical studies.

Hyperlipidaemia alone and in combination with acidosis can increase the incidence and severity of statin-induced myotoxicity (2017)
Journal Article
Taha, D. A., Zgair, A., Lee, J. B., de Moor, C. H., Barrett, D. A., Bruce, K. D., Sungelo, M., Eckel, R. H., & Gershkovich, P. (2017). Hyperlipidaemia alone and in combination with acidosis can increase the incidence and severity of statin-induced myotoxicity. European Journal of Pharmaceutical Sciences, 100, 163-175. https://doi.org/10.1016/j.ejps.2017.01.018

The association of lipophilic statins with plasma lipoproteins in the presence of disturbed acid-base balance can modify the pharmacokinetics and tissue distribution of these drugs, resulting in alteration in their efficacy and toxicity profiles. The... Read More about Hyperlipidaemia alone and in combination with acidosis can increase the incidence and severity of statin-induced myotoxicity.

Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays (2017)
Journal Article
Lee, J. B., Zgair, A., Taha, D. A., Zang, X., Kagan, L., Kim, T. H., Kim, M. G., Yun, H.-Y., Fischer, P. M., & Gershkovich, P. (2017). Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays. European Journal of Pharmaceutics and Biopharmaceutics, 114, 38-42. https://doi.org/10.1016/j.ejpb.2016.12.027

In this study, Caco-2 permeability results from different laboratories were compared. Six different sets of apparent permeability coefficient (Papp) values reported in the literature were compared to experimental Papp obtained in our laboratory. The... Read More about Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays.

Simple and sensitive HPLC-UV method for determination of bexarotene in rat plasma (2016)
Journal Article
Lee, J. B., Zgair, A., Kim, T. H., Kim, M. G., Yoo, S. D., Fischer, P. M., & Gershkovich, P. (2017). Simple and sensitive HPLC-UV method for determination of bexarotene in rat plasma. Journal of Chromatography B, 1040, 73-80. https://doi.org/10.1016/j.jchromb.2016.11.024

Bexarotene is currently marketed for treatment of cutaneous T-cell lymphoma and there has been growing interest in its therapeutic effectiveness for other cancers. Neuroprotective effects of bexarotene have also been reported. In this study, a simple... Read More about Simple and sensitive HPLC-UV method for determination of bexarotene in rat plasma.

Linking in vitro lipolysis and microsomal metabolism for the quantitative prediction of oral bioavailability of BCS II drugs administered in lipidic formulations (2016)
Journal Article
Benito-Gallo, P., Marlow, M., Zann, V., Scholes, P., & Gershkovich, P. (in press). Linking in vitro lipolysis and microsomal metabolism for the quantitative prediction of oral bioavailability of BCS II drugs administered in lipidic formulations. Molecular Pharmaceutics, 13(10), https://doi.org/10.1021/acs.molpharmaceut.6b00597

Lipidic formulations (LFs) are increasingly utilized for the delivery of drugs that belong to class II of the Biopharmaceutics Classification System (BCS). The current work proposes, for the first time, the combination of in vitro lipolysis and micro... Read More about Linking in vitro lipolysis and microsomal metabolism for the quantitative prediction of oral bioavailability of BCS II drugs administered in lipidic formulations.

Dietary fats and pharmaceutical lipid excipients increase systemic exposure to orally administered cannabis and cannabis-based medicines (2016)
Journal Article
Zgair, A., Wong, J. C., Lee, J. B., Mistry, J., Sivak, O., Wasan, K. M., Hennig, I. M., Barrett, D. A., Constantinescu, C. S., Fischer, P. M., & Gershkovich, P. (2016). Dietary fats and pharmaceutical lipid excipients increase systemic exposure to orally administered cannabis and cannabis-based medicines. American Journal of Translational Research, 8(8), 3448-3459

There has been an escalating interest in the medicinal use of Cannabis sativa in recent years. Cannabis is often administered orally with fat-containing foods, or in lipid-based pharmaceutical preparations. However, the impact of lipids on the exposu... Read More about Dietary fats and pharmaceutical lipid excipients increase systemic exposure to orally administered cannabis and cannabis-based medicines.

Proposing the use of partial AUC as an adjunctive measure in establishing bioequivalence between deltoid and gluteal administration of long-acting injectable antipsychotics (2016)
Journal Article
Lee, L. H. N., Choi, C., Gershkovich, P., Barr, A. M., Honer, W. G., & Procyshyn, R. M. (2016). Proposing the use of partial AUC as an adjunctive measure in establishing bioequivalence between deltoid and gluteal administration of long-acting injectable antipsychotics. European Journal of Drug Metabolism and Pharmacokinetics, 41(6), 659-664. https://doi.org/10.1007/s13318-016-0348-z

The maximum plasma concentration (Cmax) and the area under the plasma concentration–time curve (AUC) are commonly used to establish bioequivalence between two formulations of the same oral medication. Similarly, these pharmacokinetic parameters have... Read More about Proposing the use of partial AUC as an adjunctive measure in establishing bioequivalence between deltoid and gluteal administration of long-acting injectable antipsychotics.

The role of acid-base imbalance in statin-induced myotoxicity (2016)
Journal Article
Taha, D. A., de Moor, C. H., Barrett, D. A., Lee, J. B., Gandhi, R. D., Hoo, C. W., & Gershkovich, P. (2016). The role of acid-base imbalance in statin-induced myotoxicity. Translational Research, The Journal of Laboratory and Clinical Medicine, 174, 140-160.e14. https://doi.org/10.1016/j.trsl.2016.03.015

Disturbances in acid-base balance, such as acidosis and alkalosis, have potential to alter the pharmacological and toxicological outcomes of statin therapy. Statins are commonly prescribed for elderly patients who have multiple co-morbidities such as... Read More about The role of acid-base imbalance in statin-induced myotoxicity.

In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B (2015)
Journal Article
Qazzaz, M. E., Raja, V. J., Lim, K.-H., Kam, T.-S., Lee, J. B., Gershkovich, P., & Bradshaw, T. D. (2016). In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B. Cancer Letters, 370(2), https://doi.org/10.1016/j.canlet.2015.10.013

Natural products play a pivotal role in medicine especially in the cancer arena. Many drugs that are currently used in cancer chemotherapy originated from or were inspired by nature. Jerantinine B (JB) is one of seven novel Aspidosperma indole alkalo... Read More about In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B.

Development of a simple and sensitive HPLC-UV method for the simultaneous determination of cannabidiol and ?(9)-tetrahydrocannabinol in rat plasma (2015)
Journal Article
Zgair, A., Wong, J., Sabri, A., Fischer, P., Barrett, D., Constantinescu, C., & Gershkovich, P. (2015). Development of a simple and sensitive HPLC-UV method for the simultaneous determination of cannabidiol and Δ(9)-tetrahydrocannabinol in rat plasma. Journal of Pharmaceutical and Biomedical Analysis, 114, 145-151. https://doi.org/10.1016/j.jpba.2015.05.019

Chain length affects pancreatic lipase activity and the extent and pH–time profile of triglyceride lipolysis (2015)
Journal Article
Benito-Gallo, P., Franceschetto, A., Wong, J. C., Marlow, M., Zann, V., Scholes, P., & Gershkovich, P. (2015). Chain length affects pancreatic lipase activity and the extent and pH–time profile of triglyceride lipolysis. European Journal of Pharmaceutics and Biopharmaceutics, 93, https://doi.org/10.1016/j.ejpb.2015.04.027

Triglycerides (TG) are one of the most common excipients used in oral lipid-based formulations. The chain length of the TG plays an important role in the oral bioavailability of the co-administered drug. Fatty acid (FA) chain-length specificity of po... Read More about Chain length affects pancreatic lipase activity and the extent and pH–time profile of triglyceride lipolysis.

Characterisation of human saliva as a platform for oral dissolution medium development (2015)
Journal Article
Gittings, S., Turnbull, N., Henry, B., Roberts, C. J., & Gershkovich, P. (2015). Characterisation of human saliva as a platform for oral dissolution medium development. European Journal of Pharmaceutics and Biopharmaceutics, 91, 16-24. https://doi.org/10.1016/j.ejpb.2015.01.007

Human saliva is a biological fluid of great importance in the field of dissolution testing. However, until now, no consensus has been reached on its key characteristics relevant to dissolution testing. As a result, it is difficult to select or develo... Read More about Characterisation of human saliva as a platform for oral dissolution medium development.

Dissolution methodology for taste masked oral dosage forms (2013)
Journal Article
Gittings, S., Turnbull, N., Roberts, C., & Gershkovich, P. (2014). Dissolution methodology for taste masked oral dosage forms. Journal of Controlled Release, 173, 32-42. https://doi.org/10.1016/j.jconrel.2013.10.030

Conventional adult dosage forms are often not suitable for the paediatric and geriatric populations due to either swallowing difficulties or patient repulsion and a requirement for tailored dosing to individual compliance or physiological needs. Alte... Read More about Dissolution methodology for taste masked oral dosage forms.