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Use of Magnetic Resonance Imaging for Visualization of Oral Dosage Forms in the Human Stomach: A Scoping Review (2024)
Journal Article
Akbar, T., Gershkovich, P., Stamatopoulos, K., Gowland, P. A., Stolnik, S., Butler, J., & Marciani, L. (2024). Use of Magnetic Resonance Imaging for Visualization of Oral Dosage Forms in the Human Stomach: A Scoping Review. Molecular Pharmaceutics, https://doi.org/10.1021/acs.molpharmaceut.3c01123

Oral dosage forms are the most widely and frequently used formulations to deliver active pharmaceutical ingredients (APIs), due to their ease of administration and noninvasiveness. Knowledge of intragastric release rates and gastric mixing is crucial... Read More about Use of Magnetic Resonance Imaging for Visualization of Oral Dosage Forms in the Human Stomach: A Scoping Review.

Development of lipophilic ester prodrugs of dolutegravir for intestinal lymphatic transport (2023)
Journal Article
Chu, Y., Wong, A., Chen, H., Ji, L., Qin, C., Feng, W., …Gershkovich, P. (2023). Development of lipophilic ester prodrugs of dolutegravir for intestinal lymphatic transport. European Journal of Pharmaceutics and Biopharmaceutics, 191, 90-102. https://doi.org/10.1016/j.ejpb.2023.08.015

The establishment of latent cellular and anatomical viral reservoirs is a major obstacle to achieving a cure for people infected by HIV. Mesenteric lymph nodes (MLNs) are one of the most important anatomical reservoirs of HIV. Suboptimal levels of an... Read More about Development of lipophilic ester prodrugs of dolutegravir for intestinal lymphatic transport.

Evaluation of cannabidiol nanoparticles and nanoemulsion biodistribution in the central nervous system after intrathecal administration for the treatment of pain (2023)
Journal Article
Muresan, P., Woodhams, S., Smith, F., Taresco, V., Shah, J., Wong, M., …Marlow, M. (2023). Evaluation of cannabidiol nanoparticles and nanoemulsion biodistribution in the central nervous system after intrathecal administration for the treatment of pain. Nanomedicine: Nanotechnology, Biology and Medicine, 49, Article 102664. https://doi.org/10.1016/j.nano.2023.102664

We investigated how the biodistribution of cannabidiol (CBD) within the central nervous system (CNS) is influenced by two different formulations, an oil-in-water (O/W) nanoemulsion and polymer-coated nanoparticles (PCNPs). We observed that both CBD f... Read More about Evaluation of cannabidiol nanoparticles and nanoemulsion biodistribution in the central nervous system after intrathecal administration for the treatment of pain.

Oral lipid-based formulations alter delivery of cannabidiol to different anatomical regions in the brain (2023)
Journal Article
Brookes, A., Jewell, A., Feng, W., Bradshaw, T. D., Butler, J., & Gershkovich, P. (2023). Oral lipid-based formulations alter delivery of cannabidiol to different anatomical regions in the brain. International Journal of Pharmaceutics, 635, Article 122651. https://doi.org/10.1016/j.ijpharm.2023.122651

Delivery to the brain is a challenging task due to its protection by the blood–brain barrier (BBB). Lipids and fatty acids are reported to affect the permeability of the BBB, although this has not been reported following oral administration. Cannabid... Read More about Oral lipid-based formulations alter delivery of cannabidiol to different anatomical regions in the brain.

Development of nanoparticle loaded microneedles for drug delivery to a brain tumour resection site (2022)
Journal Article
Muresan, P., McCrorie, P., Smith, F., Vasey, C., Taresco, V., Scurr, D. J., …Marlow, M. (2023). Development of nanoparticle loaded microneedles for drug delivery to a brain tumour resection site. European Journal of Pharmaceutics and Biopharmaceutics, 182, 53-61. https://doi.org/10.1016/j.ejpb.2022.11.016

Systemic drug delivery to the central nervous system (CNS) has been historically impeded by the presence of the blood brain barrier rendering many therapies inefficacious to any cancer cells residing within the brain. Therefore, local drug delivery s... Read More about Development of nanoparticle loaded microneedles for drug delivery to a brain tumour resection site.

Editorial: Lymphatic delivery and targeting of drugs, vaccines, and imaging agents (2022)
Journal Article
Han, S., Trevaskis, N., Gershkovich, P., & Kagan, L. (2022). Editorial: Lymphatic delivery and targeting of drugs, vaccines, and imaging agents. Frontiers in Pharmacology, 13, Article 1011778. https://doi.org/10.3389/fphar.2022.1011778

The lymphatic system plays a key role in the (patho) physiology of a number of diseases, including autoimmune/inflammatory disorders, cancer, infections, and metabolic syndrome. Biological pathways in the lymphatic system provide new promising treatm... Read More about Editorial: Lymphatic delivery and targeting of drugs, vaccines, and imaging agents.

Vegetable oils composition affects the intestinal lymphatic transport and systemic bioavailability of co-administered lipophilic drug cannabidiol (2022)
Journal Article
Feng, W., Qin, C., Abdelrazig, S., Bai, Z., Raji, M., Darwish, R., …Gershkovich, P. (2022). Vegetable oils composition affects the intestinal lymphatic transport and systemic bioavailability of co-administered lipophilic drug cannabidiol. International Journal of Pharmaceutics, 624, Article 121947. https://doi.org/10.1016/j.ijpharm.2022.121947

Although natural sesame oil has been shown to facilitate the lymphatic delivery and oral bioavailability of the highly lipophilic drug cannabidiol (CBD), considerable variability remains an unresolved challenge. Vegetable oils differ substantially in... Read More about Vegetable oils composition affects the intestinal lymphatic transport and systemic bioavailability of co-administered lipophilic drug cannabidiol.

Distribution of a highly lipophilic drug cannabidiol into different lymph nodes following oral administration in lipidic vehicle (2022)
Journal Article
Jewell, A., Brookes, A., Feng, W., Ashford, M., Gellert, P., Butler, J., …Gershkovich, P. (2022). Distribution of a highly lipophilic drug cannabidiol into different lymph nodes following oral administration in lipidic vehicle. European Journal of Pharmaceutics and Biopharmaceutics, 174, 29-34. https://doi.org/10.1016/j.ejpb.2022.03.014

Efficient delivery of highly lipophilic drugs or prodrugs to the mesenteric lymph nodes (MLN) can be achieved following oral administration with lipids. However, it remains unclear which specific MLN can be targeted and to what extent. Moreover, the... Read More about Distribution of a highly lipophilic drug cannabidiol into different lymph nodes following oral administration in lipidic vehicle.

Is oral lipid-based delivery for drug targeting to the brain feasible? (2022)
Journal Article
Brookes, A., Ji, L., Bradshaw, T. D., Stocks, M., Gray, D., Butler, J., & Gershkovich, P. (2022). Is oral lipid-based delivery for drug targeting to the brain feasible?. European Journal of Pharmaceutics and Biopharmaceutics, 172, 112-122. https://doi.org/10.1016/j.ejpb.2022.02.004

This review outlines the feasibility of oral lipid-based targeted delivery of drugs to the brain, including permeation of the central nervous system's (CNS) protective blood–brain barrier (BBB). The structure of the BBB and disruption caused by varyi... Read More about Is oral lipid-based delivery for drug targeting to the brain feasible?.

Application of In Vivo MRI Imaging to Track a Coated Capsule and Its Disintegration in the Gastrointestinal Tract in Human Volunteers (2022)
Journal Article
Sulaiman, S., Gershkovich, P., Hoad, C. L., Calladine, M., Spiller, R. C., Stolnik, S., & Marciani, L. (2022). Application of In Vivo MRI Imaging to Track a Coated Capsule and Its Disintegration in the Gastrointestinal Tract in Human Volunteers. Pharmaceutics, 14(2), Article 270. https://doi.org/10.3390/pharmaceutics14020270

Oral specially coated formulations have the potential to improve treatment outcomes of a range of diseases in distal intestinal tract whilst limiting systemic drug absorption and adverse effects. Their development is challenging, partly because of li... Read More about Application of In Vivo MRI Imaging to Track a Coated Capsule and Its Disintegration in the Gastrointestinal Tract in Human Volunteers.

Emergent SARS-CoV-2 variants: comparative replication dynamics and high sensitivity to thapsigargin (2021)
Journal Article
Al-Beltagi, S., Goulding, L. V., Chang, D. K., Mellits, K. H., Hayes, C. J., Gershkovich, P., …Chang, K. (2021). Emergent SARS-CoV-2 variants: comparative replication dynamics and high sensitivity to thapsigargin. Virulence, 12(1), 2946-2956. https://doi.org/10.1080/21505594.2021.2006960

The struggle to control the COVID-19 pandemic is made challenging by the emergence of virulent SARS-CoV-2 variants. To gain insight into their replication dynamics, emergent Alpha (A), Beta (B) and Delta (D) SARS-CoV-2 variants were assessed for thei... Read More about Emergent SARS-CoV-2 variants: comparative replication dynamics and high sensitivity to thapsigargin.

Assessing lymphatic uptake of lipids using magnetic resonance imaging: A feasibility study in healthy human volunteers with potential application for tracking lymph node delivery of drugs and formulation excipients (2021)
Journal Article
Jewell, A., Williams, H., Hoad, C. L., Gellert, P. R., Ashford, M. B., Butler, J., …Gershkovich, P. (2021). Assessing lymphatic uptake of lipids using magnetic resonance imaging: A feasibility study in healthy human volunteers with potential application for tracking lymph node delivery of drugs and formulation excipients. Pharmaceutics, 13(9), Article 1343. https://doi.org/10.3390/pharmaceutics13091343

Dietary lipids and some pharmaceutical lipid excipients can facilitate the targeted delivery of drugs to the intestinal lymphatics. Here, the feasibility of magnetic resonance imaging (MRI) for imaging lipid uptake into the intestinal lymphatics was... Read More about Assessing lymphatic uptake of lipids using magnetic resonance imaging: A feasibility study in healthy human volunteers with potential application for tracking lymph node delivery of drugs and formulation excipients.

Chemosensitization of temozolomide-resistant pediatric diffuse midline glioma using potent nanoencapsulated forms of a N(3)-propargyl analogue (2021)
Journal Article
Heravi Shargh, V., Luckett, J., Bouzinab, K., Paisey, S., Turyanska, L., Singleton, W. G., …Coyle, B. (2021). Chemosensitization of temozolomide-resistant pediatric diffuse midline glioma using potent nanoencapsulated forms of a N(3)-propargyl analogue. ACS Applied Materials and Interfaces, 13(30), 35266-35280. https://doi.org/10.1021/acsami.1c04164

The lack of clinical response to the alkylating agent temozolomide (TMZ) in pediatric diffuse midline/intrinsic pontine glioma (DIPG) has been associated with O6-methylguanine-DNA-methyltransferase (MGMT) expression and mismatch repair deficiency. He... Read More about Chemosensitization of temozolomide-resistant pediatric diffuse midline glioma using potent nanoencapsulated forms of a N(3)-propargyl analogue.

Oral administration of tipranavir with long-chain triglyceride results in moderate intestinal lymph targeting but no efficient delivery to HIV-1 reservoir in mesenteric lymph nodes (2021)
Journal Article
Sheriston, C., Medrano-Padial, C., Qin, C., Fischer, P. M., Feng, W., Chu, Y., …Ling, B. (2021). Oral administration of tipranavir with long-chain triglyceride results in moderate intestinal lymph targeting but no efficient delivery to HIV-1 reservoir in mesenteric lymph nodes. International Journal of Pharmaceutics, 602, Article 120621. https://doi.org/10.1016/j.ijpharm.2021.120621

The introduction of combination antiretroviral therapy (cART) led to substantial improvement in mortality and morbidity of HIV-1 infection. However, the poor penetration of antiretroviral agents to HIV-1 reservoirs limit the ability of the antiretrov... Read More about Oral administration of tipranavir with long-chain triglyceride results in moderate intestinal lymph targeting but no efficient delivery to HIV-1 reservoir in mesenteric lymph nodes.

Natural sesame oil is superior to pre-digested lipid formulations and purified triglycerides in promoting the intestinal lymphatic transport and systemic bioavailability of cannabidiol (2021)
Journal Article
Feng, W., Qin, C., Chu, Y. J., Berton, M., Lee, J. B., Zgair, A., …Gershkovich, P. (2021). Natural sesame oil is superior to pre-digested lipid formulations and purified triglycerides in promoting the intestinal lymphatic transport and systemic bioavailability of cannabidiol. European Journal of Pharmaceutics and Biopharmaceutics, 162, 43-49. https://doi.org/10.1016/j.ejpb.2021.02.013

© 2021 Elsevier B.V. Lipid-based formulations play a significant role in oral delivery of lipophilic drugs. Previous studies have shown that natural sesame oil promotes the intestinal lymphatic transport and oral bioavailability of the highly lipophi... Read More about Natural sesame oil is superior to pre-digested lipid formulations and purified triglycerides in promoting the intestinal lymphatic transport and systemic bioavailability of cannabidiol.

Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents (2021)
Journal Article
Shao, H., Foley, D. W., Huang, S., Abbas, A. Y., Lam, F., Gershkovich, P., …Wang, S. (2021). Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents. European Journal of Medicinal Chemistry, 214, Article 113244. https://doi.org/10.1016/j.ejmech.2021.113244

Cyclin-dependent kinases (CDKs) are a family of Ser/Thr kinases involved in cell cycle and transcriptional regulation. CDK9 regulates transcriptional elongation and this unique property has made it a potential target for several diseases. Due to the... Read More about Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.

Thapsigargin Is a Broad-Spectrum Inhibitor of Major Human Respiratory Viruses: Coronavirus, Respiratory Syncytial Virus and Influenza A Virus (2021)
Journal Article
Al-Beltagi, S., Preda, C. A., Goulding, L. V., James, J., Pu, J., Skinner, P., …Chang, K. (2021). Thapsigargin Is a Broad-Spectrum Inhibitor of Major Human Respiratory Viruses: Coronavirus, Respiratory Syncytial Virus and Influenza A Virus. Viruses, 13(2), Article 234. https://doi.org/10.3390/v13020234

The long-term control strategy of SARS-CoV-2 and other major respiratory viruses needs to in-clude antivirals to treat acute infections, in addition to the judicious use of effective vaccines. Whilst COVID-19 vaccines are being rolled out for mass va... Read More about Thapsigargin Is a Broad-Spectrum Inhibitor of Major Human Respiratory Viruses: Coronavirus, Respiratory Syncytial Virus and Influenza A Virus.

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., 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.