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Full-Text Articles in Other Pharmacy and Pharmaceutical Sciences

Preclinical Development Of Novel Chemotherapeutic Agent Ac1lpszg: Formulation Optimization, In Vitro Characterization, And In Vivo Pharmacokinetics, Ritu Gupta Aug 2022

Preclinical Development Of Novel Chemotherapeutic Agent Ac1lpszg: Formulation Optimization, In Vitro Characterization, And In Vivo Pharmacokinetics, Ritu Gupta

Dissertations (2016-Present)

Preclinical development of novel chemotherapeutic agent AC1LPSZG, a mammalian target of rapamycin (mTOR) inhibitor, involved development of sensitive reverse-phase ultra-performance liquid chromatography (UPLC) and LC-MS/MS methods for quantification of AC1LPSZG in in vitro study samples and rat plasma, respectively. Pharmacokinetic studies were done in SD rats after intravenous injection of cosolvent formulations. The resulting pharmacokinetic parameters were analyzed using non-compartmental analysis (NCA) and two-compartmental modeling. Poly (D, L-lactic-co-glycolic acid) (PLGA) is most used biodegradable synthetic polymer for nano drug delivery due to its non-toxic and biodegradable nature, and tunable release properties. PLGA nanoparticles (NPs) were prepared by ‘nanoprecipitation’ technique using …


Preclinical Development Of A Novel Antileishmanial Agent Ojt007: Bioanalytical Assay, In Vitro Studies And Pharmacokinetics, Maria Eugenia Rincon-Nigro May 2022

Preclinical Development Of A Novel Antileishmanial Agent Ojt007: Bioanalytical Assay, In Vitro Studies And Pharmacokinetics, Maria Eugenia Rincon-Nigro

Dissertations (2016-Present)

Current treatments for cutaneous leishmaniasis suffer from toxic side effects, high cost, parenteral administration, and drug resistance. Thus, there is a critical need to develop oral drugs for the treatment of leishmaniasis. OJT007 is a novel class of drug with potent antiproliferative effects against Leishmania Major. The purpose of this project is to conduct preclinical drug development studies for OJT007 including bioanalytical assay development, pre-formulation studies, in vitro hepatic drug metabolism and in vivo pharmacokinetics. A sensitive, specific, and reproducible ultra-high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated. The separation was achieved on a UPLC BEH …


Discovery Of Ojt008 As A Novel Inhibitor Of Mycobacterium Tuberculosis, Collins Chidi Onyenaka May 2022

Discovery Of Ojt008 As A Novel Inhibitor Of Mycobacterium Tuberculosis, Collins Chidi Onyenaka

Dissertations (2016-Present)

Despite recent progress in the diagnosis of Tuberculosis (TB), the chemotherapeutic management of TB is still challenging. Mycobacterium tuberculosis (Mtb) is the etiological agent of TB, and TB is classified as the 13th leading cause of death globally [WHO 2021]. 558,000 people were reported to develop multi-drug resistant TB globally [WHO 2020]. Our research focuses on targeting Methionine Aminopeptidase (MetAP), an essential protein for the viability of Mtb. MetAP is a metalloprotease that catalyzes the removal of N-terminal methionine (NME) during translation of protein [Giglione et al., 2003]. This essential role of MetAPs makes this enzyme an auspicious target for …


Discovery Of Ojt010 As A Novel Inhibitor Of Severe Acute Respiratory Syndrome Coronavirus 2, Manvir Kaur May 2022

Discovery Of Ojt010 As A Novel Inhibitor Of Severe Acute Respiratory Syndrome Coronavirus 2, Manvir Kaur

Dissertations (2016-Present)

The current pandemic of coronavirus disease (COVID-19) caused by the highly infectious pathogen, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), represents a global public health challenge. The emergence of deadly SARS-CoV-2 variants with mutations on the viral genes has made it more imperative to discover therapeutics that target the host receptors for COVID-19 treatment. Therefore, our research has targeted the critical host entry receptors: Angiotensin-converting enzyme-2 (ACE2) for SARS-CoV-2 entry into the human cells. SARS-CoV-2 is an enveloped RNA beta coronavirus that infects human cells via interaction with the ACE2 receptor, followed by viral replication and virus dissemination. Spike protein …