All Outputs (53)

Strawberry decreases intraluminal and intestinal wall hydrolysis of testosterone undecanoate (2021)
Journal Article
Zgair, A., Dawood, Y., Ibrahem, S. M., Lee, J. B., Feng, W., Fischer, P. M., & Gershkovich, P. (2021). Strawberry decreases intraluminal and intestinal wall hydrolysis of testosterone undecanoate. Molecules, 26(1), Article 233. https://doi.org/10.3390/molecules26010233

Male hypogonadism is often treated by testosterone (T) replacement therapy such as oral administration of the ester prodrug, testosterone undecanoate (TU). However, the systemic exposure to T following oral TU is very low due to esterase-mediated met... Read More about Strawberry decreases intraluminal and intestinal wall hydrolysis of testosterone undecanoate.

Targeted delivery of lopinavir to HIV reservoirs in the mesenteric lymphatic system by lipophilic ester prodrug approach (2020)
Journal Article
Qin, C., Chu, Y., Feng, W., Fromont, C., He, S., Ali, J., …Gershkovich, P. (2021). Targeted delivery of lopinavir to HIV reservoirs in the mesenteric lymphatic system by lipophilic ester prodrug approach. Journal of Controlled Release, 329, 1077-1089. https://doi.org/10.1016/j.jconrel.2020.10.036

© 2020 Elsevier B.V. The combined antiretroviral therapy (cART) can efficiently suppress HIV replication, but the cessation of cART usually results in viral rebound, mostly due to the presence of viral reservoirs. The mesenteric lymphatic system, inc... Read More about Targeted delivery of lopinavir to HIV reservoirs in the mesenteric lymphatic system by lipophilic ester prodrug approach.

Predicting intestinal and hepatic first-pass metabolism of orally administered testosterone 3 undecanoate 4 (2020)
Journal Article
Zgair, A., Dawood, Y., Ibrahim, S. M., Back, H.-M., Kagan, L., Gershkovich, P., & Lee, J. B. (2020). Predicting intestinal and hepatic first-pass metabolism of orally administered testosterone 3 undecanoate 4. Applied Sciences, 10(20), Article 7283. https://doi.org/10.3390/app10207283

The bioavailability of orally administered drugs could be impacted by intestinal and 12 hepatic first-pass metabolism. Testosterone undecanoate (TU), an orally administered ester prodrug 13 of testosterone, is significantly subjected to first-pass me... Read More about Predicting intestinal and hepatic first-pass metabolism of orally administered testosterone 3 undecanoate 4.

The Interplay Between Liver First-Pass Effect and Lymphatic Absorption of Cannabidiol and Its Implications for Cannabidiol Oral Formulations (2020)
Journal Article
Franco, V., Gershkovich, P., Perucca, E., & Bialer, M. (2020). The Interplay Between Liver First-Pass Effect and Lymphatic Absorption of Cannabidiol and Its Implications for Cannabidiol Oral Formulations. Clinical Pharmacokinetics, 59(12), 1493-1500. https://doi.org/10.1007/s40262-020-00931-w

For highly lipophilic drugs, passage into the intestinal lymphatic system rather than the portal vein following oral administration may represent a major alternative route of delivery into the general circulation. Increasing intestinal lymphatic tran... Read More about The Interplay Between Liver First-Pass Effect and Lymphatic Absorption of Cannabidiol and Its Implications for Cannabidiol Oral Formulations.

Development and validation of a cost-effective and sensitive bioanalytical HPLC-UV method for determination of lopinavir in rat and human plasma (2020)
Journal Article
Qin, C., Feng, W., Chu, Y. J., Lee, J. B., Berton, M., Bettonte, S., …Gershkovich, P. (2020). Development and validation of a cost-effective and sensitive bioanalytical HPLC-UV method for determination of lopinavir in rat and human plasma. Biomedical Chromatography, 34(11), Article e4934. https://doi.org/10.1002/bmc.4934

© 2020 The Authors. Biomedical Chromatography published by John Wiley & Sons Ltd A simple, sensitive and cost-effective HPLC-UV bioanalytical method for determination of lopinavir (LPV) in rat and human plasma was developed and validated. The plasm... Read More about Development and validation of a cost-effective and sensitive bioanalytical HPLC-UV method for determination of lopinavir in rat and human plasma.

Synthesis of micellar-like terpolymer nanoparticles with reductively-cleavable cross-links and evaluation of efficacy in 2D and 3D models of triple negative breast cancer (2020)
Journal Article
Monteiro, P. F., Gulfam, M., Monteiro, C. J., Travanut, A., Abelha, T. F., Pearce, A. K., …Alexander, C. (2020). Synthesis of micellar-like terpolymer nanoparticles with reductively-cleavable cross-links and evaluation of efficacy in 2D and 3D models of triple negative breast cancer. Journal of Controlled Release, 323, 549-564. https://doi.org/10.1016/j.jconrel.2020.04.049

© 2020 Elsevier B.V. Triple negative or basal-like breast cancer (TNBC) is characterised by aggressive progression, lack of standard therapies and poorer overall survival rates for patients. The bad prognosis, high rate of relapse and resistance agai... Read More about Synthesis of micellar-like terpolymer nanoparticles with reductively-cleavable cross-links and evaluation of efficacy in 2D and 3D models of triple negative breast cancer.

Delivery of temozolomide and N3-propargyl analog to brain tumors using an apoferritin nanocage (2020)
Journal Article
Bouzinab, K., Summers, H., Stevens, M. F., Moody, C. J., Thomas, N. R., Gershkovich, P., …Turyanska, L. (2020). Delivery of temozolomide and N3-propargyl analog to brain tumors using an apoferritin nanocage. ACS Applied Materials and Interfaces, 12(11), 12609-12617. https://doi.org/10.1021/acsami.0c01514

Glioblastoma multiforme (GBM) is a grade IV astrocytoma, which is the most aggressive form of brain tumor. The standard of care for this disease includes surgery, radiotherapy and temozolomide (TMZ) chemotherapy. Poor accumulation of TMZ at the tumor... Read More about Delivery of temozolomide and N3-propargyl analog to brain tumors using an apoferritin nanocage.

Is rat a good model for assessment of particulate-based taste-masked formulations? (2019)
Journal Article
Ali, J., Chiang, M., Lee, J. B., Voronin, G. O., Bennett, J., Cram, A., …Gershkovich, P. (2020). Is rat a good model for assessment of particulate-based taste-masked formulations?. European Journal of Pharmaceutics and Biopharmaceutics, 146, 1-9. https://doi.org/10.1016/j.ejpb.2019.11.001

Recently there has been an increased interest to develop specialised dosage forms that are better suited to specific patient populations, such as paediatrics and geriatrics. In these patient populations the acceptability of the oral dosage form can b... Read More about Is rat a good model for assessment of particulate-based taste-masked formulations?.

A novel nucleoside rescue metabolic pathway may be responsible for therapeutic effect of orally administered cordycepin (2019)
Journal Article
Lee, J. B., Radhi, M., Cipolla, E., Gandhi, R. D., Sarmad, S., Zgair, A., …Gershkovich, P. (2019). A novel nucleoside rescue metabolic pathway may be responsible for therapeutic effect of orally administered cordycepin. Scientific Reports, 9, Article 15760. https://doi.org/10.1038/s41598-019-52254-x

Although adenosine and its analogues have been assessed in the past as potential drug candidates due to the important role of adenosine in physiology, only little is known about their absorption following oral administration. In this work, we have st... Read More about A novel nucleoside rescue metabolic pathway may be responsible for therapeutic effect of orally administered cordycepin.

Solid lipid nanoparticles self-assembled from spray dried microparticles (2019)
Journal Article
Sanchez-Vazquez, B., Lee, J. B., Strimaite, M., Buanz, A., Bailey, R., Gershkovich, P., …Williams, G. R. (2019). Solid lipid nanoparticles self-assembled from spray dried microparticles. International Journal of Pharmaceutics, 572, Article 118784. https://doi.org/10.1016/j.ijpharm.2019.118784

We report the self-assembly of drug-loaded solid lipid nanoparticles (SLNs) from spray dried microparticles comprising poly(vinylpyrrolidone) (PVP) loaded with glyceryl tristearate (GTS) and either indomethacin (IMC) or 5-fluorouracil (5-FU). When th... Read More about Solid lipid nanoparticles self-assembled from spray dried microparticles.

In search of effective therapies to overcome resistance to Temozolomide in brain tumours (2019)
Journal Article
Grundy, R., Bouzinab, K., Summers, H., Zhang, J., Stevens, M. F. G., Moody, C. J., …Bradshaw, T. D. (2019). In search of effective therapies to overcome resistance to Temozolomide in brain tumours. Cancer Drug Resistance, 2(4), 1018-1031. https://doi.org/10.20517/cdr.2019.64

Glioblastoma multiforme is the most common and lethal brain tumour-type. The current standard of care includes Temozolomide (TMZ) chemotherapy. However, inherent and acquired resistance to TMZ thwart successful treatment. The direct repair protein me... Read More about In search of effective therapies to overcome resistance to Temozolomide in brain tumours.

Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer (2019)
Journal Article
Garces, A. E., Al-Hayali, M., Lee, J. B., Li, J., Gershkovich, P., Bradshaw, T. D., & Stocks, M. J. (2020). Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer. ACS Medicinal Chemistry Letters, 11(3), 316-321. https://doi.org/10.1021/acsmedchemlett.9b00378

We report on the synergistic effect of PI3K inhibition with ALK inhibition for the possible treatment of EML4-ALK positive lung cancer. We have brought together ceritinib (ALK inhibitor) and pictilisib (PI3K inhibitor) into a single bivalent molecule... Read More about Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer.

Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition (2019)
Journal Article
Hossan, M. S., Chan, Z. Y., Collins, H. M., Shipton, F. N., Butler, M. S., Rahmatullah, M., …Bradshaw, T. D. (2019). Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition. Cancer Letters, 453, 57-73. https://doi.org/10.1016/j.canlet.2019.03.034

Natural products possess a significant role in anticancer therapy and many currently-used anticancer drugs are of natural origin. Cerberin (CR), a cardenolide isolated from the fruit kernel of Cerbera odollam, was found to potently inhibit cancer cel... Read More about Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition.

Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine (2018)
Journal Article
Ali, J., Zgair, A., Hameed, G. S., Garnett, M. C., Roberts, C. J., Burley, J. C., & Gershkovich, P. (2019). Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine. International Journal of Pharmaceutics, 555, 228-236. https://doi.org/10.1016/j.ijpharm.2018.11.051

The oral cavity is of great importance to the performance of orally retained formulations, including: orally disintegrating tablets, taste-masked formulations, and buccal/sublingual delivery systems. With regards to in vitro dissolution assessment of... Read More about Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine.

Quantitative prediction of oral bioavailability of a lipophilic antineoplastic drug bexarotene administered in lipidic formulation using a combined in vitro lipolysis/microsomal metabolism approach (2018)
Journal Article
Lee, J. B., Kim, T. H., Feng, W., Choi, H. G., Zgair, A., Shin, S., …Shin, B. S. (2019). Quantitative prediction of oral bioavailability of a lipophilic antineoplastic drug bexarotene administered in lipidic formulation using a combined in vitro lipolysis/microsomal metabolism approach. Pharmaceutical Sciences, 108(2), 1047-1052. https://doi.org/10.1016/j.xphs.2018.09.025

For performance assessment of the lipid-based drug delivery systems (LBDDS), in vitro lipolysis is commonly applied because traditional dissolution tests do not reflect the complicated in vivo micellar formation and solubilisation processes. Much of... Read More about Quantitative prediction of oral bioavailability of a lipophilic antineoplastic drug bexarotene administered in lipidic formulation using a combined in vitro lipolysis/microsomal metabolism approach.

Analytical ultracentrifugation in saliva research: Impact of green tea astringency and its significance on the in-vivo aroma release (2018)
Journal Article
Dinu, V., Liu, C., Ali, J., Ayed, C., Gershkovich, P., Adams, G. G., Harding, S. E., & Fisk, I. (2018). Analytical ultracentrifugation in saliva research: Impact of green tea astringency and its significance on the in-vivo aroma release. Scientific Reports, 8, 1-9. https://doi.org/10.1038/s41598-018-31625-w

Current saliva testing methods rely on cutting edge yet expensive techniques for the detection and analysis of genetic material, proteins and biomarkers for clinical use. However, these techniques are limited in scope and often cannot be used with co... Read More about Analytical ultracentrifugation in saliva research: Impact of green tea astringency and its significance on the in-vivo aroma release.

Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system (2018)
Journal Article
Lee, J. B., Zgair, A., Malec, J., Kim, T. H., Kim, M. G., Ali, J., Qin, C., Feng, W., Chiang, M., Gao, X., Voronin, G., Garces, A., Lau, C. L., Chan, T.-H., Hume, A., McIntosh, T. M., Soukarieh, F., Al-Hayali, M., Cipolla, E., Collins, H. M., …Gershkovich, P. (2018). Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system. Journal of Controlled Release, 286, 10-19. https://doi.org/10.1016/j.jconrel.2018.07.022

The intestinal lymphatic system plays an important role in the pathophysiology of multiple diseases including lymphomas, cancer metastasis, autoimmune diseases, and human immunodeficiency virus (HIV) infection. It is thus an important compartment for... Read More about Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system.

Therapeutic cannabinoids in multiple sclerosis: immunomodulation revisited (2018)
Journal Article
Constantinescu, C. S., & Gershkovich, P. (2018). Therapeutic cannabinoids in multiple sclerosis: immunomodulation revisited. European Journal of Neurology, 25(7), 905-906. https://doi.org/10.1111/ene.13658

Cannabinoids are compounds with pleiotropic properties that act on the cannabinoid receptors, CB1 and CB2, and are divided into endocannabinoids, the endogenous ligands of these receptors, synthetic cannabinoids and phytocannabinoids. The latter are... Read More about Therapeutic cannabinoids in multiple sclerosis: immunomodulation revisited.

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., …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.