Dr PAVEL GERSHKOVICH's Outputs (55)

Novel Use of Manganese Gluconate as a Marker for Visualization of Tablet Dissolution in the Fed Human Stomach Using Magnetic Resonance Imaging (2024)
Journal Article
Akbar, T., Gershkovich, P., Stamatopoulos, K., Gowland, P., Stolnik, S., Butler, J., & Marciani, L. (2025). Novel Use of Manganese Gluconate as a Marker for Visualization of Tablet Dissolution in the Fed Human Stomach Using Magnetic Resonance Imaging. Molecular Pharmaceutics, 22(1), 594-598. https://doi.org/10.1021/acs.molpharmaceut.4c00854

Magnetic resonance imaging (MRI) of dry or solid materials in the gastrointestinal (GI) tract requires the use of contrast agents to enhance visualisation of the dosage forms. In this study, we explore the novel use of manganese gluconate added to ta... Read More about Novel Use of Manganese Gluconate as a Marker for Visualization of Tablet Dissolution in the Fed Human Stomach Using Magnetic Resonance Imaging.

Rapeseed oleosomes facilitate intestinal lymphatic delivery and oral bioavailability of cannabidiol (2024)
Journal Article
Ji, L., Feng, W., Chen, H., Chu, Y., Wong, A., Zhu, Y., Sinatra, G., Bramante, F., Carrière, F., Stocks, M. J., di Bari, V., Gray, D. A., & Gershkovich, P. (2025). Rapeseed oleosomes facilitate intestinal lymphatic delivery and oral bioavailability of cannabidiol. International Journal of Pharmaceutics, 668, Article 124947. https://doi.org/10.1016/j.ijpharm.2024.124947

Due to high lipophilicity and extensive first-pass metabolic loss, cannabidiol (CBD) has low oral bioavailability. Co-administration of CBD and long-chain lipids facilitates the intestinal lymphatic delivery, resulting in higher systemic bioavailabil... Read More about Rapeseed oleosomes facilitate intestinal lymphatic delivery and oral bioavailability of cannabidiol.

Delivery of imiquimod to intestinal lymph nodes following oral administration (2024)
Journal Article
Chen, H., Ji, L., Wong, A., Chu, Y., Feng, W., Zhu, Y., Wang, J., Comeo, E., Kim, D.-H., Stocks, M. J., & Gershkovich, P. (2024). Delivery of imiquimod to intestinal lymph nodes following oral administration. International Journal of Pharmaceutics, 667, Article 124895. https://doi.org/10.1016/j.ijpharm.2024.124895

Intestinal lymph nodes are involved in the progression of colorectal cancer (CRC). Tumours suppress the activation of dendritic cells (DCs) in draining lymph nodes, diminishing anti-cancer immune response. Imiquimod (IMQ) facilitates DCs activation v... Read More about Delivery of imiquimod to intestinal lymph nodes following oral administration.

Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents (2024)
Journal Article
Brookes, A., Kindon, N., Scurr, D. J., Alexander, M. R., Gershkovich, P., & Bradshaw, T. (2024). Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents. BJC Reports, 2, Article 67. https://doi.org/10.1038/s44276-024-00088-0

Background
Glioblastoma multiforme (GBM) is an aggressive cancer with poor prognosis, partly due to resistance to the standard chemotherapy treatment, temozolomide (TMZ). Phytocannabinoid cannabidiol (CBD) has exhibited anti-cancer effects against G... Read More about Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents.

Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents (2024)
Journal Article
Brookes, A., Kindon, N., Scurr, D., Alexander, M., Gershkovich, P., & BRADSHAW, T. (2024). Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents. British Journal of Cancer, 2, Article 67. https://doi.org/10.1038/s44276-024-00088-0

Background
Glioblastoma multiforme (GBM) is an aggressive cancer with poor prognosis, partly due to resistance to the standard chemotherapy treatment, temozolomide (TMZ). Phytocannabinoid cannabidiol (CBD) has exhibited anti-cancer effects against G... Read More about Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents.

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, 21(4), 1553-1562. 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., Stocks, M. J., & 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., Chapman, V., Smith, S., Hathway, G., Rahman, R., Gershkovich, P., & 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., Kern, S., Smith, S., Gershkovich, P., Rahman, R., & 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., Chu, Y., Ji, L., Gray, D. A., Stocks, M. J., Constantinescu, C. S., Barrett, D. A., Fischer, P. M., & 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., Fischer, P. M., Scurr, D. J., Stocks, M. 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., Coleman, C. M., & Chang, K.-C. (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., Stolnik, S., Scurr, D., Stocks, M. J., Marciani, L., Gowland, P. A., & 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., Lowis, S., Gershkovich, P., Bradshaw, T. D., Stevens, M. F., Bienemann, A., & 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., Jane Khor, Y., Chan, T., Watson, B. E., Gershkovich, P., Stocks, M. J., & 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., Bettonte, S., Stocks, M. J., Constantinescu, C. S., Barrett, D. A., Fischer, P. M., & 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.