Jelena R. Mitrović

Krony-PT: GPT-2 Compressed with Kronecker Products

M. Ayoub Ben Ayad, Jelena R. Mitrović, Michael Granitzer

We introduce Krony-PT, a compression technique for GPT-2 based on Kronecker products. We specifically target the feed-forward weights of each transformer block, and systematically compress the feed-forward layer matrices to various degrees. We introduce a modified Van Loan decomposition to initialize new …

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Evaluation of PEGylation efficacy of curcumin-loaded nanoemulsions using complementary methods to assess protein interactions and physicochemical properties

Jelena Đoković, Sortiria Demisli, Sanela Savić, Saša Savić et autres

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New Imidazodiazepine Analogue, 5-(8-Bromo-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole, Provides a Simplified Synthetic Scheme, High Oral Plasma and Brain Exposures, and Produces Antiseizure Efficacy in Mice, and Antiepileptogenic Activity in Neural Networks in Brain Slices from a Patient with Mesial Temporal Lobe Epilepsy

Dishary Sharmin, Branka Divović, Xingjie Ping, Rok Cerne et autres

KRM-II-81 (1) is an imidazodiazepine GABA A receptor (GABAAR) potentiator with broad antiseizure efficacy and a low sedative burden. A brominated analogue, DS-II-73 (5), was synthesized and pharmacologically characterized as a potential backup compound as KRM-II-81 moves forward into development. The synthesis …

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Freeze-dried nanocrystal dispersion of novel deuterated pyrazoloquinolinone ligand (DK-I-56-1): Process parameters and lyoprotectant selection through the stability study

Jelena R. Mitrović, Maja Bjelošević Žiberna, Aleksandar Vukadinović, Daniel E. Knutson et autres

Recently, nanocrystal dispersions have been considered as a promising formulation strategy to improve the bioavailability of the deuterated pyrazoloquinolinone ligand DK-I-56-1 (7‑methoxy-2-(4‑methoxy-d3-phenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one). In the current study, the freeze-drying process (formulation and process parameters) was investigated to improve the storage stability of the …

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Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

Jela Milić, Jelena Đoković, Ines Nikolić, Jelena R. Mitrović et autres

Contemporary trends in combinatorial chemistry and the design of pharmaceuticals targeting brain disorders have favored the development of drug candidates with increased lipophilicity and poorer water solubility, with the expected improvement in delivery across the blood-brain barrier (BBB). The growing availability of …

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High amount of lecithin facilitates oral delivery of a poorly soluble pyrazoloquinolinone ligand formulated in lipid nanoparticles: Physicochemical, structural and pharmacokinetic performances

Jelena R. Mitrović, Branka Divović, Daniel E. Knutson, Miloš Petković et autres

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Behavioural interaction of pyrazoloquinolinone positive allosteric modulators at α6GABAA receptors and diazepam in rats: Anti‐diazepam‐induced ataxia action as a structure‐dependent feature

Branka Divović, Dan Knutson, Jelena R. Mitrović, Vladimir D. Stevanović et autres

Abstract Several pyrazoloquinolinone (PQ) ligands were recently discovered as functionally selective positive modulators at the PQ site of α6‐containing GABAA receptors. PQs are also neutral modulators at the benzodiazepine site. We assessed the influence of PQ compounds from three structural groups (PZ‐II‐029 …

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The Impact of the Oil Phase Selection on Physicochemical Properties, Long-Term Stability, In Vitro Performance and Injectability of Curcumin-Loaded PEGylated Nanoemulsions

Jelena Đoković, Sotiria Demisli, Sanela Savić, Bojan Marković et autres

A nanotechnology-based approach to drug delivery presents one of the biggest trends in biomedical science that can provide increased active concentration, bioavailability, and safety compared to conventional drug-delivery systems. Nanoemulsions stand out amongst other nanocarriers for being biodegradable, biocompatible, and relatively easy …

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Overcoming the Low Oral Bioavailability of Deuterated Pyrazoloquinolinone Ligand DK-I-60-3 by Nanonization: A Knowledge-Based Approach

Jelena R. Mitrović, Branka Divović, Daniel E. Knutson, Jelena Đoković et autres

Poor water solubility of new chemical entities is considered as one of the main obstacles in drug development, as it usually leads to low bioavailability after administration. To overcome these problems, the selection of the appropriate formulation technology needs to be based …

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Curcumin Loaded PEGylated Nanoemulsions Designed for Maintained Antioxidant Effects and Improved Bioavailability: A Pilot Study on Rats

Jelena Đoković, Sanela Savić, Jelena R. Mitrović, Ines Nikolić et autres

The current study describes the experimental design guided development of PEGylated nanoemulsions as parenteral delivery systems for curcumin, a powerful antioxidant, as well as the evaluation of their physicochemical characteristics and antioxidant activity during the two years of storage. Experimental design setup …

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Nanocrystal dispersion of DK-I-56–1, a poorly soluble pyrazoloquinolinone positive modulator of α6 GABAA receptors: Formulation approach toward improved in vivo performance

Jelena R. Mitrović, Branka Divović, Daniel E. Knutson, Jelena Đoković et autres

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PEG-ylated parenteral Nanoemulsions as prospective Carriers for enhanced Brain Delivery with Diazepam as a Model Drug - Physicochemical Characterisation

Jelena Đoković, M. Konkel, Jelena R. Mitrović, Saša Savić et autres

Parenteral nanoemulsions are regarded as biocompatible drug delivery systems for lypophilic drugs. When it comes to delivering actives to the brain as a target site, prolonged circulation time is desirable. The objective of this study was to conduct physicochemical characterization of PEGylated …