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Article ; Online: Cetuximab-based PROteolysis targeting chimera for effectual downregulation of NSCLC with varied EGFR mutations.

Vartak, Richa / Deore, Bhavesh / Sanhueza, Carlos A / Patel, Ketan

International journal of biological macromolecules

2023 Volume 252, Page(s) 126413

Abstract: PROteolysis Targeting Chimeras (PROTACs) showed tremendous therapeutic potential in degrading several oncoproteins including undruggable proteins. PROTACs are bifunctional molecules where one-part binds to target protein while the other end recruits ... ...

Abstract	PROteolysis Targeting Chimeras (PROTACs) showed tremendous therapeutic potential in degrading several oncoproteins including undruggable proteins. PROTACs are bifunctional molecules where one-part binds to target protein while the other end recruits protein degradation machinery. With the unveiling advancements in the field of PROTACs, we explored a combinatorial approach by developing antibody-based PROTAC (ABTAC) which may effectively degrade one of the key oncoprotein driving proliferation and progression of cancer - Epidermal growth factor receptor (EGFR). The objective of current research was to synthesize and characterize an EGFR degrading ABTAC for the treatment of non-small cell lung cancer (NSCLC). Cetuximab and pomalidomide (E3 ligase recruiting ligand) were conjugated using lysine conjugation and copper free azide-alkyne cycloaddition (CuAAC) click chemistry. Analytical characterization using reverse-phase liquid chromatography and mass spectrometry suggested conjugation of five E3-ligase inhibitor molecules/antibody. Nearly 10-30 folds reduction in IC
MeSH term(s)	Humans ; Cetuximab/pharmacology ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Carcinoma, Non-Small-Cell Lung/genetics ; Carcinoma, Non-Small-Cell Lung/metabolism ; Proteolysis Targeting Chimera ; Down-Regulation ; Lung Neoplasms/drug therapy ; Lung Neoplasms/genetics ; Lung Neoplasms/metabolism ; ErbB Receptors/metabolism ; Mutation ; Proteolysis
Chemical Substances	Cetuximab (PQX0D8J21J) ; Proteolysis Targeting Chimera ; ErbB Receptors (EC 2.7.10.1) ; EGFR protein, human (EC 2.7.10.1)
Language	English
Publishing date	2023-08-19
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	282732-3
ISSN	1879-0003 ; 0141-8130
ISSN (online)	1879-0003
ISSN	0141-8130
DOI	10.1016/j.ijbiomac.2023.126413
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Article ; Online: Nanoformulation of a novel potent ebselen analog for treatment of vulvovaginal candidiasis.

Liang, Xiuyi / Menon, Suvidha / Vartak, Richa / Gaida, Radosław / Wojaczyńska, Elżbieta / Patel, Ketankumar / Billack, Blase

Nanomedicine (London, England)

2023 Volume 18, Issue 18, Page(s) 1195–1206

Abstract: Background: ...

Abstract	Background:
MeSH term(s)	Female ; Humans ; Mice ; Animals ; Candidiasis, Vulvovaginal/drug therapy ; Isoindoles ; Azoles/pharmacology ; Azoles/therapeutic use ; Candida albicans ; Antifungal Agents/pharmacology ; Antifungal Agents/therapeutic use
Chemical Substances	ebselen (40X2P7DPGH) ; Isoindoles ; Azoles ; Antifungal Agents
Language	English
Publishing date	2023-09-19
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2277839-1
ISSN	1748-6963 ; 1743-5889
ISSN (online)	1748-6963
ISSN	1743-5889
DOI	10.2217/nnm-2022-0323
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Article ; Online: Cannabidiol Inhibits

Saraswat, Aishwarya / Vartak, Richa / Patki, Manali / Patel, Ketan

Cannabis and cannabinoid research

2021 Volume 8, Issue 6, Page(s) 1008–1018

Abstract: Introduction: ...

Abstract	Introduction:
MeSH term(s)	Humans ; Cannabidiol/pharmacology ; Microsomes, Liver/metabolism ; Cytochrome P-450 CYP3A/metabolism ; Cytochrome P-450 CYP3A Inhibitors/metabolism ; SARS-CoV-2/metabolism ; COVID-19/metabolism ; Midazolam/metabolism ; Liver/metabolism
Chemical Substances	Cannabidiol (19GBJ60SN5) ; remdesivir (3QKI37EEHE) ; Cytochrome P-450 CYP3A (EC 1.14.14.1) ; Cytochrome P-450 CYP3A Inhibitors ; Midazolam (R60L0SM5BC)
Language	English
Publishing date	2021-12-16
Publishing country	United States
Document type	Journal Article
ZDB-ID	2867624-5
ISSN	2378-8763 ; 2578-5125
ISSN (online)	2378-8763
ISSN	2578-5125
DOI	10.1089/can.2021.0109
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Article: Arginine-Coated Nanoglobules for the Nasal Delivery of Insulin.

Das, Atanu / Vartak, Richa / Islam, Md Asrarul / Kumar, Sunil / Shao, Jun / Patel, Ketan

Pharmaceutics

2023 Volume 15, Issue 2

Abstract: Multiple daily injections via subcutaneous route are the primary modes of insulin delivery for patients with Diabetes Mellitus. While this process is invasive, painful and may cause patients to develop lipohypertrophy at injection site, the perception of ...

Abstract	Multiple daily injections via subcutaneous route are the primary modes of insulin delivery for patients with Diabetes Mellitus. While this process is invasive, painful and may cause patients to develop lipohypertrophy at injection site, the perception of fear surrounding this process causes patients to delay in initiation and remain persistent with insulin therapy over time. Moreover, poor glycemic control may often lead to acute complications, such as severe hypoglycemia and nocturnal hypoglycemia, especially in older patients with diabetes. To address the imperative need for a patient-convenient non-invasive insulin therapy, an insulin-loaded arginine-coated self-emulsifying nanoglobule system (INS-LANano) was developed for nasal delivery of insulin with a biodegradable cationic surfactant-Lauroyl Ethyl Arginate (LAE). Incorporation of LAE resulted in formation of positively charged nanoglobules with L-arginine oriented on the surface. LANano enabled binding of insulin molecules on the surface of nanoglobules via an electrostatic interaction between negatively charged α-helix and LAE molecules at physiological pH. INS-LANano showed a hydrodynamic diameter of 23.38 nm with a surface charge of +0.118 mV. The binding efficiency of insulin on LANano globules was confirmed by zeta potential, circular dichroism (CD) spectroscopy and centrifugal ultrafiltration studies. The attachment of insulin with permeation-enhancing nanoglobules demonstrated significantly higher in vitro permeability of insulin of 15.2% compared to insulin solution across human airway epithelial cell (Calu-3) monolayer. Upon intranasal administration of INS-LANano to diabetic rats at 2 IU/kg insulin dose, a rapid absorption of insulin with significantly higher Cmax of 14.3 mU/L and relative bioavailability (BA) of 23.3% was observed. Therefore, the INS-LANano formulation significant translational potential for intranasal delivery of insulin.
Language	English
Publishing date	2023-01-20
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics15020353
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Article ; Online: Corroborating various material-sparing techniques with hot melt extrusion for the preparation of triclabendazole amorphous solid dispersions.

Palekar, Siddhant / Mamidi, Hemanth K / Guo, Yi / Vartak, Richa / Patel, Ketan

International journal of pharmaceutics

2023 Volume 640, Page(s) 122989

Abstract: Amorphous solid dispersions (ASD) are one of the most adopted technologies for improving the solubility of novel molecules. Formulation of ASDs using solvent free methods such as hot melt extrusion (HME) has been in the spotlight off-lately. However, ... ...

Abstract	Amorphous solid dispersions (ASD) are one of the most adopted technologies for improving the solubility of novel molecules. Formulation of ASDs using solvent free methods such as hot melt extrusion (HME) has been in the spotlight off-lately. However, early-stage formulation development is tricky and a difficult bridge to pass due to limited drug availability. Material-sparing techniques (theoretical & practical) have been used for selecting suitable polymeric carriers for formulating ASDs. However, these techniques have limitations in predicting the effect of process parameters. The objective of this study is to use both theoretical and practical material-sparing techniques to optimize a polymer for the developing Triclabendazole (TBZ) ASDs. Initial screening by theoretical approaches suggested that TBZ is highly miscible with Kollidon®VA64 (VA64) and poorly miscible with Parteck®MXP (PVA). However, results from ASDs prepared using SCFe were opposite to these predictions. ASDs prepared using either technique and both VA64 and PVA showed >200x increase in solubility. Each formulation released >85% of drug in less than 15 mins. Although the thermodynamic phase diagram suggested that VA64 was the ideal polymer for TBZ-ASDs, it has certain limitations in factoring the different elements during melt-processing and hence, practical approaches like SCFe could help in predicting the drug-polymer miscibility for HME processing.
MeSH term(s)	Drug Compounding/methods ; Chemistry, Pharmaceutical/methods ; Triclabendazole ; Hot Melt Extrusion Technology/methods ; Polymers ; Solubility ; Hot Temperature
Chemical Substances	Triclabendazole (4784C8E03O) ; Polymers
Language	English
Publishing date	2023-04-28
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2023.122989
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Article ; Online: Evaluation of the antifungal activity of an ebselen-loaded nanoemulsion in a mouse model of vulvovaginal candidiasis.

Menon, Suvidha / Vartak, Richa / Patel, Ketankumar / Billack, Blase

Nanomedicine : nanotechnology, biology, and medicine

2021 Volume 37, Page(s) 102428

Abstract: Vulvovaginal candidiasis (VVC), caused by Candida albicans, is a common infection in women affecting their quality of life. Standard antifungal drugs (e.g., fluconazole, itraconazole) are typically fungistatic or rendered ineffective due to drug ... ...

Abstract	Vulvovaginal candidiasis (VVC), caused by Candida albicans, is a common infection in women affecting their quality of life. Standard antifungal drugs (e.g., fluconazole, itraconazole) are typically fungistatic or rendered ineffective due to drug resistance indicating an urgent need to build an arsenal of novel antifungal agents. To surmount this issue, we tested the hypothesis that the organoselenium compound ebselen (EB) possesses antifungal efficacy in a mouse model of VVC. EB is a poorly water-soluble drug and DMSO as a vehicle has the potential to exhibit cytotoxic effects when administered in vivo. EB loaded self-nanoemulsifying preconcentrate (EB-SNEP) was developed, characterized in vitro, and tested in a mouse model of VVC. In vivo studies carried out with EB-SNEP (12.5 mg/kg) showed a remarkable decrease in infection by ~562-fold compared to control (infected, untreated animals). Taken together, EB nanoemulsion proved to be an effective and promising antifungal agent.
MeSH term(s)	Animals ; Antifungal Agents/chemistry ; Antifungal Agents/pharmacology ; Candida albicans/drug effects ; Candida albicans/pathogenicity ; Candidiasis, Vulvovaginal/drug therapy ; Candidiasis, Vulvovaginal/pathology ; Disease Models, Animal ; Emulsions/chemistry ; Emulsions/pharmacology ; Female ; Fluconazole/pharmacology ; Humans ; Isoindoles/chemistry ; Isoindoles/pharmacology ; Mice ; Microbial Sensitivity Tests ; Nanoparticles/chemistry ; Organoselenium Compounds/chemistry ; Organoselenium Compounds/pharmacology
Chemical Substances	Antifungal Agents ; Emulsions ; Isoindoles ; Organoselenium Compounds ; ebselen (40X2P7DPGH) ; Fluconazole (8VZV102JFY)
Language	English
Publishing date	2021-07-01
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2183417-9
ISSN	1549-9642 ; 1549-9634
ISSN (online)	1549-9642
ISSN	1549-9634
DOI	10.1016/j.nano.2021.102428
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Article ; Online: N

Liang, Xiuyi / Pacuła-Miszewska, Agata J / Vartak, Richa / Prajapati, Milankumar / Zheng, Haiyan / Zhao, Caifeng / Mao, Ganming / Patel, Ketankumar / Fedosova, Natalya U / Ścianowski, Jacek / Billack, Blase

Current issues in molecular biology

2024 Volume 46, Issue 3, Page(s) 2480–2496

Abstract: In the present work, we evaluated the antifungal activities of two novel ebselen analogs, ...

Abstract	In the present work, we evaluated the antifungal activities of two novel ebselen analogs,
Language	English
Publishing date	2024-03-14
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2000024-8
ISSN	1467-3045 ; 1467-3037
ISSN (online)	1467-3045
ISSN	1467-3037
DOI	10.3390/cimb46030157
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Article ; Online: Drug delivery challenges and formulation aspects of proteolysis targeting chimera (PROTACs).

Saraswat, Aishwarya L / Vartak, Richa / Hegazy, Rehab / Patel, Akanksha / Patel, Ketan

Drug discovery today

2022 Volume 28, Issue 1, Page(s) 103387

Abstract: Proteolysis targeting chimeras (PROTACs) have been extensively explored for targeted proteasomal degradation of disease-related proteins with enormous potential in the treatment of intractable diseases. However, PROTACs are poorly soluble and permeable ... ...

Abstract	Proteolysis targeting chimeras (PROTACs) have been extensively explored for targeted proteasomal degradation of disease-related proteins with enormous potential in the treatment of intractable diseases. However, PROTACs are poorly soluble and permeable bulky molecules facing several bioavailability challenges irrespective of the route of administration. Our review lays out crucial challenges in the delivery of target protein degraders and nanoformulation approaches to overcome physicochemical and biological hurdles that can aid in transporting these target-protein degraders to the disease site. We have elaborated on the current formulation approaches and further highlighted the prospective delivery strategies that could be probed for disease-specific targeted delivery of PROTACs.
MeSH term(s)	Proteolysis ; Proteolysis Targeting Chimera ; Prospective Studies ; Proteins/metabolism
Chemical Substances	Proteolysis Targeting Chimera ; Proteins
Language	English
Publishing date	2022-09-29
Publishing country	England
Document type	Journal Article ; Review ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	1324988-5
ISSN	1878-5832 ; 1359-6446
ISSN (online)	1878-5832
ISSN	1359-6446
DOI	10.1016/j.drudis.2022.103387
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Article: Vaginal Nanoformulations for the Management of Preterm Birth.

Mir, Asad / Vartak, Richa V / Patel, Ketan / Yellon, Steven M / Reznik, Sandra E

Pharmaceutics

2022 Volume 14, Issue 10

Abstract: Preterm birth (PTB) is a leading cause of infant morbidity and mortality in the world. In 2020, 1 in 10 infants were born prematurely in the United States. The World Health Organization estimates that a total of 15 million infants are born prematurely ... ...

Abstract	Preterm birth (PTB) is a leading cause of infant morbidity and mortality in the world. In 2020, 1 in 10 infants were born prematurely in the United States. The World Health Organization estimates that a total of 15 million infants are born prematurely every year. Current therapeutic interventions for PTB have had limited replicable success. Recent advancements in the field of nanomedicine have made it possible to utilize the vaginal administration route to effectively and locally deliver drugs to the female reproductive tract. Additionally, studies using murine models have provided important insights about the cervix as a gatekeeper for pregnancy and parturition. With these recent developments, the field of reproductive biology is on the cusp of a paradigm shift in the context of treating PTB. The present review focuses on the complexities associated with treating the condition and novel therapeutics that have produced promising results in preclinical studies.
Language	English
Publishing date	2022-09-23
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics14102019
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Article ; Online: Susceptibility of Lung Carcinoma Cells to Nanostructured Lipid Carrier of ARV-825, a BRD4 Degrading Proteolysis Targeting Chimera.

Vartak, Richa / Saraswat, Aishwarya / Yang, Yuqi / Chen, Zhe-Sheng / Patel, Ketan

Pharmaceutical research

2022 Volume 39, Issue 11, Page(s) 2745–2759

Abstract: The present work was aimed at developing an optimized and modified nanostructured lipid carrier of BRD4 protein degrading Proteolysis Targeting Chimera (PROTAC) against non-small cell lung carcinoma. PROTACs are an emerging class of anticancer molecules ... ...

Abstract	The present work was aimed at developing an optimized and modified nanostructured lipid carrier of BRD4 protein degrading Proteolysis Targeting Chimera (PROTAC) against non-small cell lung carcinoma. PROTACs are an emerging class of anticancer molecules with nanomolar activity but associated with significant solubility challenges. Lipid-based colloidal systems like nanostructured lipid carriers are widely explored for such highly lipophilic molecules. ARV-825, a cereblon-based PROTAC was investigated for its anticancer efficacy in vitro in 2D and 3D lung cancer models. ARV-825 loaded PEGylated nanostructured lipid carriers (AP-NLC) was prepared using melt emulsification technique. ARV-825 was stabilized using Precirol® ATO5 and Captex® 300 EP/NF as the solid and liquid lipid, respectively. However, hydrophobic ion-pairing with medium chain fatty acid was required to improve drug loading and stability. A hydrodynamic diameter and polydispersity index of 56.33 ± 0.42 nm and 0.16 respectively with zeta potential of -21 ± 1.24 mV was observed. In vitro migration and colony formation assay confirmed the anticancer activity of ARV-825 alone and AP-NLC. Nearly 38% and 50% apoptotic cell population were observed after ARV-825 and AP-NLC treatment. Immunoblotting assay showed complete suppression of BRD4 and c-Myc protein expression for AP-NLC. Most importantly, significant reduction in the growth of multicellular 3D spheroid of A549 cells confirmed the effectiveness of BRD4 PROTAC and its lipid nanoparticle in non-small cell lung cancer (NSCLC). AP-NLC. Higher amount of red fluorescence throughout the spheroid surface further confirmed superior efficacy of AP-NLC in tumor penetration and cell killing.
MeSH term(s)	Humans ; Carcinoma ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Drug Carriers/chemistry ; Excipients/chemistry ; Lipids/chemistry ; Lung/metabolism ; Lung Neoplasms/drug therapy ; Nanostructures/chemistry ; Nuclear Proteins/metabolism ; Particle Size ; Proteolysis ; Transcription Factors/metabolism
Chemical Substances	ARV-825 ; BRD4 protein, human ; Drug Carriers ; Excipients ; Lipid Nanoparticles ; Lipids ; Nuclear Proteins ; Transcription Factors
Language	English
Publishing date	2022-02-10
Publishing country	United States
Document type	Journal Article
ZDB-ID	843063-9
ISSN	1573-904X ; 0724-8741 ; 0739-0742
ISSN (online)	1573-904X
ISSN	0724-8741 ; 0739-0742
DOI	10.1007/s11095-022-03184-3
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