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Lidia Tajber
School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, College Green, Dublin 2, Ireland

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Journal article
Published: 03 August 2021 in International Journal of Pharmaceutics
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Liquid forms of active pharmaceutical ingredients, ionic liquids (ILs) and deep eutectic mixtures (DEMs), offer several potential benefits in respect to advancing pharmaceutical formulations. The aim of this study was to develop and characterise ILs/DEMs composed of two active molecules: ketoprofen (KET), as the acidic component, and a local anaesthetics (LA), lidocaine (LID), mepivacaine (MEP) or bupivacaine (BUP), which constituted the basic component. A mechanosynthetic approach was successfully applied to obtain LA-KET low melting systems. Composition/temperature phase diagrams were determined by differential scanning calorimetry. The amide LA-KET mixtures showed a eutectic behaviour during heating and formed viscous liquids upon quench cooling. Considering the quench cooled LA-KET mixtures, LA crystallisation was observed only in the LA-rich mixtures. LID, MEP and BUP formed disordered complexes with KET at an approximate 1:2 stoichiometry. Infrared spectroscopy studies revealed that the mixtures were composed mainly of hydrogen bonded acid and base molecules, but small amounts of carboxylate anions were detected. The formation of LA-KET complex not only suppressed the high crystallisation tendency of the LA molecules in the dry state, but also eliminated the crystallisation of KET and LA molecules induced by moisture, as revealed by dynamic vapour sorption studies.

ACS Style

Anita Umerska; Julija Zotova; Lidia Tajber. Formation of low melting point binary systems comprising ketoprofen and an amide local anaesthetic. International Journal of Pharmaceutics 2021, 607, 120969 .

AMA Style

Anita Umerska, Julija Zotova, Lidia Tajber. Formation of low melting point binary systems comprising ketoprofen and an amide local anaesthetic. International Journal of Pharmaceutics. 2021; 607 ():120969.

Chicago/Turabian Style

Anita Umerska; Julija Zotova; Lidia Tajber. 2021. "Formation of low melting point binary systems comprising ketoprofen and an amide local anaesthetic." International Journal of Pharmaceutics 607, no. : 120969.

Research article
Published: 11 July 2021 in Molecular Pharmaceutics
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In this work, we employed broad-band dielectric spectroscopy to determine the solubility limits of nimesulide in the Kollidon VA64 matrix at ambient and elevated pressure conditions. Our studies confirmed that the solubility of the drug in the polymer matrix decreases with increasing pressure, and molecular dynamics controls the process of recrystallization of the excess of amorphous nimesulide from the supersaturated drug–polymer solution. More precisely, recrystallization initiated at a certain structural relaxation time of the sample stops when a molecular mobility different from the initial one is reached, regardless of the temperature and pressure conditions. Finally, based on the presented results, one can conclude that by transposing vertically the results obtained at elevated pressures, one can obtain the solubility limit values corresponding to low temperatures. This approach was validated by the comparison of the experimentally determined points with the theoretically obtained values based on the Flory–Huggins theory.

ACS Style

Krzysztof Chmiel; Justyna Knapik-Kowalczuk; Ewa Kamińska; Lidia Tajber; Marian Paluch. High-Pressure Dielectric Studies—a Way to Experimentally Determine the Solubility of a Drug in the Polymer Matrix at Low Temperatures. Molecular Pharmaceutics 2021, 1 .

AMA Style

Krzysztof Chmiel, Justyna Knapik-Kowalczuk, Ewa Kamińska, Lidia Tajber, Marian Paluch. High-Pressure Dielectric Studies—a Way to Experimentally Determine the Solubility of a Drug in the Polymer Matrix at Low Temperatures. Molecular Pharmaceutics. 2021; ():1.

Chicago/Turabian Style

Krzysztof Chmiel; Justyna Knapik-Kowalczuk; Ewa Kamińska; Lidia Tajber; Marian Paluch. 2021. "High-Pressure Dielectric Studies—a Way to Experimentally Determine the Solubility of a Drug in the Polymer Matrix at Low Temperatures." Molecular Pharmaceutics , no. : 1.

Journal article
Published: 20 April 2021 in International Journal of Pharmaceutics
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The physiochemical properties of acidic or basic active pharmaceutical ingredients (APIs) can be optimised by forming salts with different counterions. The aim of this work was to synthesise a novel salt of propranolol (PRO) using sebacic acid (SEBA) as the counterion and to gain mechanistic understanding of not only the salt formation, but also its eutectic phase formation with SEBA. Thermal analysis showed a solid-state reaction occurring between PRO and SEBA leading to the formation of dipropranolol sebacate (DPS) melting at app. 170 °C and the eutectic composed of DPS and SEBA melting at app. 103 °C, comprising 0.33 mol fraction of PRO as determined by the Tammann plot. X-ray diffraction and Fourier-transform infrared spectroscopy (FTIR) confirmed the identity of the new multicomponent phases of PRO. DPS can be conveniently obtained by heat-induced crystallisation, grinding and conventional solvent crystallisation. Detailed analysis by FTIR revealed H-bond interactions between DPS and SEBA at the inter-phase in the eutectic. Bravais, Friedel, Donnay and Harker crystal morphology coupled with full interaction maps analysis allowed to understand further the nature of interactions which led to formation of the eutectic phase. This work contributes to furthering research on multicomponent pharmaceutical systems to harness their full potential.

ACS Style

Klaudia Bialek; Zaneta Wojnarowska; Brendan Twamley; Lidia Tajber. Characterisation and fundamental insight into the formation of new solid state, multicomponent systems of propranolol. International Journal of Pharmaceutics 2021, 602, 120605 .

AMA Style

Klaudia Bialek, Zaneta Wojnarowska, Brendan Twamley, Lidia Tajber. Characterisation and fundamental insight into the formation of new solid state, multicomponent systems of propranolol. International Journal of Pharmaceutics. 2021; 602 ():120605.

Chicago/Turabian Style

Klaudia Bialek; Zaneta Wojnarowska; Brendan Twamley; Lidia Tajber. 2021. "Characterisation and fundamental insight into the formation of new solid state, multicomponent systems of propranolol." International Journal of Pharmaceutics 602, no. : 120605.

Journal article
Published: 18 January 2021 in Pharmaceutics
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The aim of this study was to characterize a 1:1 molar ratio of a pharmacologically relevant co-amorphous atorvastatin-irbesartan (ATR-IRB) system obtained by quench cooling of the crystalline ATR/IRB physical mixture for potential use in the fixed-dose combination therapy. The system was characterized by employing standard differential scanning calorimetry (DSC), Fourier transform-infrared spectroscopy (FT-IR), and intrinsic dissolution rate studies. Quantum mechanical calculations were performed to obtain information regarding intermolecular interactions in the studied co-amorphous ATR-IRB system. The co-amorphous formulation showed a significant improvement in the intrinsic dissolution rate (IDR) of IRB over pure crystalline as well as its amorphous counterpart. An unusual behavior was observed for ATR, as the IDR of ATR in the co-amorphous formulation was slightly lower than that of amorphous ATR alone. Short-term physical aging studies of up to 8 h proved that the ATR-IRB co-amorphous system remained in the amorphous form. Furthermore, no physical aging occurred in the co-amorphous system. FT-IR, density functional theory calculations, and analysis of Tg value of co-amorphous system using the Couchman–Karasz equation revealed the presence of molecular interactions between APIs, which may contribute to the increased physical stability.

ACS Style

Marcin Skotnicki; Barbara Jadach; Agnieszka Skotnicka; Bartłomiej Milanowski; Lidia Tajber; Marek Pyda; Jacek Kujawski. Physicochemical Characterization of a Co-Amorphous Atorvastatin-Irbesartan System with a Potential Application in Fixed-Dose Combination Therapy. Pharmaceutics 2021, 13, 118 .

AMA Style

Marcin Skotnicki, Barbara Jadach, Agnieszka Skotnicka, Bartłomiej Milanowski, Lidia Tajber, Marek Pyda, Jacek Kujawski. Physicochemical Characterization of a Co-Amorphous Atorvastatin-Irbesartan System with a Potential Application in Fixed-Dose Combination Therapy. Pharmaceutics. 2021; 13 (1):118.

Chicago/Turabian Style

Marcin Skotnicki; Barbara Jadach; Agnieszka Skotnicka; Bartłomiej Milanowski; Lidia Tajber; Marek Pyda; Jacek Kujawski. 2021. "Physicochemical Characterization of a Co-Amorphous Atorvastatin-Irbesartan System with a Potential Application in Fixed-Dose Combination Therapy." Pharmaceutics 13, no. 1: 118.

Research article
Published: 30 November 2020 in ACS Sustainable Chemistry & Engineering
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Mechanochemistry has been recognized as an optimal route for the synthesis of ionic liquids incorporating active pharmaceutical ingredients (API-ILs) as it eliminates the need for large volumes of solvents and purification steps, thus making it a sustainable alternative to conventional solution synthesis. In this work, a range of API-ILs incorporating lidocaine and medium-chain dicarboxylic acids as the counterions were synthesized by neat grinding, and the effect of an alkyl chain length on the phase formation was investigated. The evaluation of thermal and dynamic behaviors as well as crystallographic analysis of API-ILs was carried out in an attempt to devise a prediction tool for the structure–property relationship. Alternating trends in morphology, melting points, glass transition temperatures, and crystallographic properties of the new phases were observed across the dicarboxylic acid series. This study enhanced our understanding of the mechanisms of API-ILs formation and contributed to the current aim of the IL community to devise a systematic approach for API-IL discovery and development for pharmaceutical applications.

ACS Style

Julija Zotova; Zaneta Wojnarowska; Brendan Twamley; Marian Paluch; Lidia Tajber. Green Synthesis of Lidocaine Ionic Liquids and Salts: Mechanisms of Formation and Interactions in the Crystalline and Supercooled States. ACS Sustainable Chemistry & Engineering 2020, 8, 18266 -18276.

AMA Style

Julija Zotova, Zaneta Wojnarowska, Brendan Twamley, Marian Paluch, Lidia Tajber. Green Synthesis of Lidocaine Ionic Liquids and Salts: Mechanisms of Formation and Interactions in the Crystalline and Supercooled States. ACS Sustainable Chemistry & Engineering. 2020; 8 (49):18266-18276.

Chicago/Turabian Style

Julija Zotova; Zaneta Wojnarowska; Brendan Twamley; Marian Paluch; Lidia Tajber. 2020. "Green Synthesis of Lidocaine Ionic Liquids and Salts: Mechanisms of Formation and Interactions in the Crystalline and Supercooled States." ACS Sustainable Chemistry & Engineering 8, no. 49: 18266-18276.

Journal article
Published: 07 August 2020 in European Journal of Pharmaceutical Sciences
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Direct compression remains one of the most favourable methods available to produce tablet compacts due to its simplicity, efficiency and cost effectiveness however, the technique still remains unsuitable for the majority of formulations due to materials exhibiting poor physical properties such as inadequate compressibility and deformation mechanisms. Whereas crystallo-co-spray drying of various blends has shown to improve the tabletting properties of poorly processable materials, the role of the solvent feed composition in altering the soluble fraction ratio of the excipient to the drug in a crystallo-co-spray dried agglomerate is not well understood. The aim of this work was to investigate the role of the soluble fraction of a drug (paracetamol) and an excipient (α-lactose monohydrate) on the tabletting properties of their crystallo-co-spray dried agglomerates produced via co-spray drying using various inlet feed solvent compositions in order to vary the soluble fraction of the excipient in the feed. It was found that an increase in excipient soluble fraction in the inlet feed resulted in a greater degree of intimate mixing in the final spray dried powder blend, which in turn led to an improvement in tabletting properties of the poorly processable drug.

ACS Style

Alan F. McDonagh; Bronagh Duff; Lorna Brennan; Lidia Tajber. The impact of the degree of intimate mixing on the compaction properties of materials produced by crystallo-co-spray drying. European Journal of Pharmaceutical Sciences 2020, 154, 105505 .

AMA Style

Alan F. McDonagh, Bronagh Duff, Lorna Brennan, Lidia Tajber. The impact of the degree of intimate mixing on the compaction properties of materials produced by crystallo-co-spray drying. European Journal of Pharmaceutical Sciences. 2020; 154 ():105505.

Chicago/Turabian Style

Alan F. McDonagh; Bronagh Duff; Lorna Brennan; Lidia Tajber. 2020. "The impact of the degree of intimate mixing on the compaction properties of materials produced by crystallo-co-spray drying." European Journal of Pharmaceutical Sciences 154, no. : 105505.

Journal article
Published: 06 August 2020 in Pharmaceutics
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The crystallization of poorly soluble drug molecules with an excipient into new solid phases called cocrystals has gained a considerable popularity in the pharmaceutical field. In this work, the cocrystal approach was explored for a very poorly water soluble antifungal active, itraconazole (ITR), which was, for the first time, successfully converted into this multicomponent solid using an aromatic coformer, terephthalic acid (TER). The new cocrystal was characterized in terms of its solid-state and structural properties, and a panel of pharmaceutical tests including wettability and dissolution were performed. Evidence of the cocrystal formation was obtained from liquid-assisted grinding, but not neat grinding. An efficient method of the ITR–TER cocrystal formation was ball milling. The stoichiometry of the ITR–TER phase was 2:1 and the structure was stabilized by H-bonds. When comparing ITR–TER with other cocrystals, the intrinsic dissolution rates and powder dissolution profiles correlated with the aqueous solubility of the coformers. The rank order of the dissolution rates of the active pharmaceutical ingredient (API) from the cocrystals was ITR–oxalic acid > ITR–succinic acid > ITR–TER. Additionally, the ITR–TER cocrystal was stable in aqueous conditions and did not transform to the parent drug. In summary, this work presents another cocrystal of ITR that might be of use in pharmaceutical formulations.

ACS Style

Ricardo Machado Cruz; Tereza Boleslavská; Josef Beránek; Eszter Tieger; Brendan Twamley; Maria Santos-Martinez; Ondřej Dammer; Lidia Tajber. Identification and Pharmaceutical Characterization of a New Itraconazole Terephthalic Acid Cocrystal. Pharmaceutics 2020, 12, 741 .

AMA Style

Ricardo Machado Cruz, Tereza Boleslavská, Josef Beránek, Eszter Tieger, Brendan Twamley, Maria Santos-Martinez, Ondřej Dammer, Lidia Tajber. Identification and Pharmaceutical Characterization of a New Itraconazole Terephthalic Acid Cocrystal. Pharmaceutics. 2020; 12 (8):741.

Chicago/Turabian Style

Ricardo Machado Cruz; Tereza Boleslavská; Josef Beránek; Eszter Tieger; Brendan Twamley; Maria Santos-Martinez; Ondřej Dammer; Lidia Tajber. 2020. "Identification and Pharmaceutical Characterization of a New Itraconazole Terephthalic Acid Cocrystal." Pharmaceutics 12, no. 8: 741.

Journal article
Published: 18 May 2020 in Pharmaceutics
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The main purpose of this paper was to evaluate the impact of both high- and low-Tg polymer additives on the physical stability of an amorphous drug, sildenafil (SIL). The molecular mobility of neat amorphous SIL was strongly affected by the polymeric excipients used (Kollidon VA64 (KVA) and poly(vinylacetate) (PVAc)). The addition of KVA slowed down the molecular dynamics of amorphous SIL (antiplasticizing effect), however, the addition of PVAc accelerated the molecular motions of the neat drug (plasticizing effect). Therefore, in order to properly assess the effect of the polymer on the physical stability of SIL, the amorphous samples at both: isothermal (at constant temperature—353 K) and isochronal (at constant relaxation time—τα = 1.5 ms) conditions were compared. Our studies showed that KVA suppressed the recrystallization of amorphous SIL more efficiently than PVAc. KVA improved the physical stability of the amorphous drug, regardless of the chosen concentration. On the other hand, in the case of PVAc, a low polymer content (i.e., 25 wt.%) destabilized amorphous SIL, when stored at 353 K. Nevertheless, at high concentrations of this excipient (i.e., 75 wt.%), its effect on the amorphous pharmaceutical seemed to be the opposite. Therefore, above a certain concentration, the PVAc presence no longer accelerates the SIL recrystallization process, but inhibits it.

ACS Style

Justyna Knapik-Kowalczuk; Krzysztof Chmiel; Justyna Pacułt; Klaudia Bialek; Lidia Tajber; Marian Paluch. Enhancement of the Physical Stability of Amorphous Sildenafil in a Binary Mixture, with either a Plasticizing or Antiplasticizing Compound. Pharmaceutics 2020, 12, 460 .

AMA Style

Justyna Knapik-Kowalczuk, Krzysztof Chmiel, Justyna Pacułt, Klaudia Bialek, Lidia Tajber, Marian Paluch. Enhancement of the Physical Stability of Amorphous Sildenafil in a Binary Mixture, with either a Plasticizing or Antiplasticizing Compound. Pharmaceutics. 2020; 12 (5):460.

Chicago/Turabian Style

Justyna Knapik-Kowalczuk; Krzysztof Chmiel; Justyna Pacułt; Klaudia Bialek; Lidia Tajber; Marian Paluch. 2020. "Enhancement of the Physical Stability of Amorphous Sildenafil in a Binary Mixture, with either a Plasticizing or Antiplasticizing Compound." Pharmaceutics 12, no. 5: 460.

Journal article
Published: 17 April 2020 in Pharmaceutics
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Ionic liquids (ILs) and deep eutectic mixtures (DEMs) are potential solutions to the problems of low solubility, polymorphism, and low bioavailability of drugs. The aim of this work was to develop and investigate ketoprofen (KET)-based ILs/DEMs containing an ester local anesthetic (LA): benzocaine (BEN), procaine (PRO) and tetracaine (TET) as the second component. ILs/DEMs were prepared via a mechanosynthetic process that involved the mixing of KET with an LA in a range of molar ratios and applying a thermal treatment. After heating above the melting point and quench cooling, the formation of supercooled liquids with Tgs that were dependent on the composition was observed for all KET-LA mixtures with exception of that containing 95 mol% of BEN. The KET-LA mixtures containing either ≥ 60 mol% BEN or 95 mol% of TET showed crystallization to BEN and TET, respectively, during either cooling or second heating. KET decreased the crystallization tendency of BEN and TET and increased their glass-forming ability. The KET-PRO systems showed good glass-forming ability and did not crystallize either during the cooling or during the second heating cycle irrespective of the composition. Infrared spectroscopy and molecular modeling indicated that KET and LAs formed DEMs, but in the KET-PRO systems small quantities of carboxylate anions were present.

ACS Style

Anita Umerska; Klaudia Bialek; Julija Zotova; Marcin Skotnicki; Lidia Tajber. Anticrystal Engineering of Ketoprofen and Ester Local Anesthetics: Ionic Liquids or Deep Eutectic Mixtures? Pharmaceutics 2020, 12, 368 .

AMA Style

Anita Umerska, Klaudia Bialek, Julija Zotova, Marcin Skotnicki, Lidia Tajber. Anticrystal Engineering of Ketoprofen and Ester Local Anesthetics: Ionic Liquids or Deep Eutectic Mixtures? Pharmaceutics. 2020; 12 (4):368.

Chicago/Turabian Style

Anita Umerska; Klaudia Bialek; Julija Zotova; Marcin Skotnicki; Lidia Tajber. 2020. "Anticrystal Engineering of Ketoprofen and Ester Local Anesthetics: Ionic Liquids or Deep Eutectic Mixtures?" Pharmaceutics 12, no. 4: 368.

Journal article
Published: 07 April 2020 in Langmuir
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ACS Style

Anita Umerska; Anne Sapin-Minet; Marianne Parent; Lidia Tajber; Philippe Maincent; Ariane Boudier. Understanding the Thermodynamic Mechanisms Leading to the Binding of Albumin to Lipid Nanocapsules. Langmuir 2020, 1 .

AMA Style

Anita Umerska, Anne Sapin-Minet, Marianne Parent, Lidia Tajber, Philippe Maincent, Ariane Boudier. Understanding the Thermodynamic Mechanisms Leading to the Binding of Albumin to Lipid Nanocapsules. Langmuir. 2020; ():1.

Chicago/Turabian Style

Anita Umerska; Anne Sapin-Minet; Marianne Parent; Lidia Tajber; Philippe Maincent; Ariane Boudier. 2020. "Understanding the Thermodynamic Mechanisms Leading to the Binding of Albumin to Lipid Nanocapsules." Langmuir , no. : 1.

Journal article
Published: 02 April 2020 in International Journal of Pharmaceutics
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Rutin is one of the most important flavonoids with poor bioavailability. This work aimed at addressing the issue of poor biopharmaceutical performance of rutin by applying a combination of complexation with secondary processing into tablets. Mechanical activation was the most suitable method of rutin complex formation with (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD), while the β-cyclodextrin (β-CD) complex successfully formed by kneading with an ethanol/water mixture. Complexation was confirmed by thermal analysis, powder X-ray diffraction and vibrational spectroscopy. Dynamic vapour sorption showed that stability of powders at high humidity conditions was satisfactory, however, the β-CD complex retained around 8% of moisture. The complexes were compacted with or without tricalcium phosphate (TRI-CAFOS) filler at a range of compression pressures (19–113 MPa). The best tabletability was determined for rutin/HP-β-CD, compressibility for the TRI-CAFOS blends with complexes and compactibility for the rutin/HP-β-CD + TRI-CAFOS mix. Dissolution studies showed quicker and more complete dissolution (pH 1.2) of rutin/HP-β-CD tablets, however the compacts comprising the filler were superior than pure complexes. The tablets manufactured in this study appear to be promising delivery systems of rutin and it is recommended to combine rutin/HP-β-CD with TRI-CAFOS and compact at 38–76 MPa.

ACS Style

Magdalena Paczkowska; Alan F. McDonagh; Klaudia Bialek; Lidia Tajber; Judyta Cielecka-Piontek. Mechanochemical activation with cyclodextrins followed by compaction as an effective approach to improving dissolution of rutin. International Journal of Pharmaceutics 2020, 581, 119294 .

AMA Style

Magdalena Paczkowska, Alan F. McDonagh, Klaudia Bialek, Lidia Tajber, Judyta Cielecka-Piontek. Mechanochemical activation with cyclodextrins followed by compaction as an effective approach to improving dissolution of rutin. International Journal of Pharmaceutics. 2020; 581 ():119294.

Chicago/Turabian Style

Magdalena Paczkowska; Alan F. McDonagh; Klaudia Bialek; Lidia Tajber; Judyta Cielecka-Piontek. 2020. "Mechanochemical activation with cyclodextrins followed by compaction as an effective approach to improving dissolution of rutin." International Journal of Pharmaceutics 581, no. : 119294.

Journal article
Published: 31 March 2020 in Journal of Medical Science
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Open Research Biopharmaceutical Internships Support (ORBIS) is an international, Horizon 2020 project funded by Maria Skłodowska-Curie Actions, Research and Innovation Staff Exchange (RISE) programme. Six academic institutions and four pharmaceutical companies from seven countries cooperate with the aim to improve the preclinical pathway of medicine development through increased Research and Development (R&D) productivity, especially focusing on processes and technologies which address the challenge of poor drug bioavailability. The RISE scheme supports secondments, meaning that early stage and experienced researchers are sent to consortium partner institutions to advance studies on pharmaceutical preformulation, dosage forms and drug delivery systems and methods of biopharmaceutical evaluation. The ORBIS project enables secondees to gain news skills and develop their competences in an international and intersectoral environment, strengthening the human capital and knowledge synergy in the European pharmaceutical R&D sector.

ACS Style

Janina Lulek; Emilia Jakubowska; Sharon Davin; Aleksandra Dumicic Dumicic; Grzegorz Garbacz; Bożena Michniak-Kohn; Piotr J. Rudzki; Wojciech Smułek; Anne Juppo; Clare Strachan; Oleg Syarkevych; Lidia Tajber. ORBIS (Open Research Biopharmaceutical Internships Support) – building bridges between academia and pharmaceutical industry to improve drug development. Journal of Medical Science 2020, 89, e419 -e419.

AMA Style

Janina Lulek, Emilia Jakubowska, Sharon Davin, Aleksandra Dumicic Dumicic, Grzegorz Garbacz, Bożena Michniak-Kohn, Piotr J. Rudzki, Wojciech Smułek, Anne Juppo, Clare Strachan, Oleg Syarkevych, Lidia Tajber. ORBIS (Open Research Biopharmaceutical Internships Support) – building bridges between academia and pharmaceutical industry to improve drug development. Journal of Medical Science. 2020; 89 (1):e419-e419.

Chicago/Turabian Style

Janina Lulek; Emilia Jakubowska; Sharon Davin; Aleksandra Dumicic Dumicic; Grzegorz Garbacz; Bożena Michniak-Kohn; Piotr J. Rudzki; Wojciech Smułek; Anne Juppo; Clare Strachan; Oleg Syarkevych; Lidia Tajber. 2020. "ORBIS (Open Research Biopharmaceutical Internships Support) – building bridges between academia and pharmaceutical industry to improve drug development." Journal of Medical Science 89, no. 1: e419-e419.

Journal article
Published: 12 March 2020 in Pharmaceutics
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The use of nanocarriers is being researched to achieve oral peptide delivery. Insulin-associated anionic polyelectrolyte nanoparticle complexes (PECs) were formed that comprised hyaluronic acid and chitosan in an optimum mass mixing ratio of 5:1 (MR 5), followed by coating with a pH-dependent polymer. Free insulin was separated from PECs by size exclusion chromatography and then measured by HPLC. The association efficiency of insulin in PECs was >95% and the loading was ~83 µg/mg particles. Dynamic light scattering and nanoparticle tracking analysis of PECs revealed low polydispersity, a negative zeta potential range of −40 to −50 mV, and a diameter range of 95–200 nm. Dissolution studies in simulated small intestinal fluid (FaSSIF-V2) revealed that the PECs were colloidally stable. PECs that were coated with Eudragit® L-100 delayed insulin release in FaSSIF-V2 and protected insulin against pancreatin attack more than uncoated PECs. Uncoated anionic PECs interacted weakly with mucin in vitro and were non-cytotoxic to Caco-2 cells. The coated and uncoated PECs, both concentrated further by ultrafiltration, permitted dosing of 50 IU/kg in rat jejunal instillations, but they failed to reduce plasma glucose or deliver insulin to the blood. When ad-mixed with the permeation enhancer (PE), sucrose laurate (100 mM), the physicochemical parameters of coated PECs were relatively unchanged, however blood glucose was reduced by 70%. In conclusion, the use of a PE allowed for the PEC-released bioactive insulin to permeate the jejunum. This has implications for the design of orally delivered particles that can release the payload when formulated with enhancers.

ACS Style

Svenja Sladek; Fiona McCartney; Mena Eskander; David J. Dunne; Maria Jose Santos-Martinez; Federico Benetti; Lidia Tajber; David J. Brayden. An Enteric-Coated Polyelectrolyte Nanocomplex Delivers Insulin in Rat Intestinal Instillations When Combined with a Permeation Enhancer. Pharmaceutics 2020, 12, 259 .

AMA Style

Svenja Sladek, Fiona McCartney, Mena Eskander, David J. Dunne, Maria Jose Santos-Martinez, Federico Benetti, Lidia Tajber, David J. Brayden. An Enteric-Coated Polyelectrolyte Nanocomplex Delivers Insulin in Rat Intestinal Instillations When Combined with a Permeation Enhancer. Pharmaceutics. 2020; 12 (3):259.

Chicago/Turabian Style

Svenja Sladek; Fiona McCartney; Mena Eskander; David J. Dunne; Maria Jose Santos-Martinez; Federico Benetti; Lidia Tajber; David J. Brayden. 2020. "An Enteric-Coated Polyelectrolyte Nanocomplex Delivers Insulin in Rat Intestinal Instillations When Combined with a Permeation Enhancer." Pharmaceutics 12, no. 3: 259.

Journal article
Published: 11 February 2020 in Powder Technology
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This study proposes lipid nanocapsules (LNCs)-based Trojan particles made by entrapping 59 ± 3 nm LNCs in carbohydrate-based microparticles via spray drying. This work focused on optimisation of maintenance of the nanocarrier colloidal properties, solid state properties and suitability of Trojan particles for pulmonary deposition. The properties of Trojan particles were evaluated as a function of the nature of carbohydrate, the feed concentration and LNC loading. The presence of nanocapsules had a significant impact on the size and morphology of microparticles and their solid state properties. Spray drying did not destroy the LNCs and their size after reconstitution varied between 78 ± 1 and 121 ± 1 nm. The lactose, trehalose and raffinose-based Trojan particles were readily dispersed as aerosols with mass median aerodynamic diameters between 5.3 ± 0.1 and 6.2 ± 0.1 μm using a dry powder inhaler. In conclusion, LNC-Trojan particles were shown to successfully not only to encapsulate the lipid nanocapsules but also to release them.

ACS Style

Anita Umerska; Naila A. Mugheirbi; Agnieszka Kasprzak; Patrick Saulnier; Lidia Tajber. Carbohydrate-based Trojan microparticles as carriers for pulmonary delivery of lipid nanocapsules using dry powder inhalation. Powder Technology 2020, 364, 507 -521.

AMA Style

Anita Umerska, Naila A. Mugheirbi, Agnieszka Kasprzak, Patrick Saulnier, Lidia Tajber. Carbohydrate-based Trojan microparticles as carriers for pulmonary delivery of lipid nanocapsules using dry powder inhalation. Powder Technology. 2020; 364 ():507-521.

Chicago/Turabian Style

Anita Umerska; Naila A. Mugheirbi; Agnieszka Kasprzak; Patrick Saulnier; Lidia Tajber. 2020. "Carbohydrate-based Trojan microparticles as carriers for pulmonary delivery of lipid nanocapsules using dry powder inhalation." Powder Technology 364, no. : 507-521.

Journal article
Published: 22 January 2020 in International Journal of Pharmaceutics
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The novel process of crystallo-co-spray drying of paracetamol and α-lactose monohydrate was investigated by varying the spray dryer inlet temperature and inlet feed solvent composition. A crystalline agglomerate was obtained with no change to the physical structure of either component throughout both investigations and with possible interactions between the hydroxyl groups of the α-lactose monohydrate and the amide and hydroxyl groups of the paracetamol detected. The percentage soluble fraction of the components in the inlet feed had the largest influence on the morphology of the final dried agglomerate. Low excipient soluble fraction resulted in an increase in paracetamol surface coating and high excipient soluble fraction produced agglomerates of highly mixed components. The use of crystallo-co-spray drying can serve as a method of producing an agglomerated blend of crystalline co-spray dried components leading to possible opportunities for process intensification with the reduction of process steps such as blending, agglomeration, drying and milling into one single stage.

ACS Style

Alan F. McDonagh; Lidia Tajber. Crystallo-co-spray drying as a new approach to manufacturing of drug/excipient agglomerates: Impact of processing on the properties of paracetamol and lactose mixtures. International Journal of Pharmaceutics 2020, 577, 119051 .

AMA Style

Alan F. McDonagh, Lidia Tajber. Crystallo-co-spray drying as a new approach to manufacturing of drug/excipient agglomerates: Impact of processing on the properties of paracetamol and lactose mixtures. International Journal of Pharmaceutics. 2020; 577 ():119051.

Chicago/Turabian Style

Alan F. McDonagh; Lidia Tajber. 2020. "Crystallo-co-spray drying as a new approach to manufacturing of drug/excipient agglomerates: Impact of processing on the properties of paracetamol and lactose mixtures." International Journal of Pharmaceutics 577, no. : 119051.

Journal article
Published: 06 November 2019 in Advanced Powder Technology
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The parameters governing the crystallisation of paracetamol using various conventional techniques has been extensively studied, however the factors influencing the drug crystallisation using spray drying is not as well understood. The aim of this work was to investigate the crystallisation of an active pharmaceutical ingredient through evaporative crystallisation using a spray dryer to study the physicochemical properties of the drug and to use semi-empirical equations to gain insight into the morphology and particle size of the dried powder. Paracetamol solutions were spray dried at various inlet temperatures ranging from 60 °C to 120 °C and also from a series of inlet feed solvent compositions ranging from 50/50% v/v ethanol/water to 100% ethanol and solid-state characterisation was done. The size and morphology of the dried materials were altered with a change in spray drying parameters, with an increase in inlet temperature leading to an increase in particle Sauter mean diameter (from 3.0 to 4.4 µm) and a decrease in the particle size with an increase in ethanol concentration in the feed (from 4.6 to 4.4 µm) as a result of changes in particle density and atomised droplet size. The morphology of the dried particles consisted of agglomerates of individual crystallites bound together into larger semi-spherical agglomerates with a higher tendency for particles having crystalline ridges to form at higher ethanol concentrations of the feed.

ACS Style

Alan F. McDonagh; Lidia Tajber. The control of paracetamol particle size and surface morphology through crystallisation in a spray dryer. Advanced Powder Technology 2019, 31, 287 -299.

AMA Style

Alan F. McDonagh, Lidia Tajber. The control of paracetamol particle size and surface morphology through crystallisation in a spray dryer. Advanced Powder Technology. 2019; 31 (1):287-299.

Chicago/Turabian Style

Alan F. McDonagh; Lidia Tajber. 2019. "The control of paracetamol particle size and surface morphology through crystallisation in a spray dryer." Advanced Powder Technology 31, no. 1: 287-299.

Journal article
Published: 18 October 2019 in European Journal of Pharmaceutical Sciences
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One of the greatest problems of pre-clinical development of new chemical entities is their poor aqueous solubility. Herein, we focus our attention on MD20 – a novel calcium channel blocker that selectively blocks T-type calcium channel (Cav3.2) over L-type calcium channel (Cav1.2). To avoid future problems with limited solubility of this compound, an amorphous form of MD20 was obtained and thoroughly investigated by various experimental techniques. The thermal properties of both crystalline and amorphous MD20 were examined by differential scanning calorimetry and thermogravimetry. Dielectric spectroscopy studies of MD20 at T < Tg revealed that this compound possesses as many as four secondary relaxation processes. The molecular dynamics of the supercooled sample was investigated by dielectric and mechanical spectroscopies. In this paper, a comparison of the relaxation dynamics of supercooled MD20 obtained from both of these experimental techniques is presented. On the basis of the dielectric studies, the time of physical stability of the investigated material (at T = 298 K) was predicted as 150 years. Finally, we have performed experimental long-term stability tests, which showed that amorphous MD20 did not reveal any signs of re-crystallization for at least 260 days.

ACS Style

Justyna Knapik-Kowalczuk; Miyase Gözde Gündüz; Krzysztof Chmiel; Karolina Jurkiewicz; Mateusz Kurek; Lidia Tajber; Renata Jachowicz; Marian Paluch. Molecular dynamics, viscoelastic properties and physical stability studies of a new amorphous dihydropyridine derivative with T-type calcium channel blocking activity. European Journal of Pharmaceutical Sciences 2019, 141, 105083 .

AMA Style

Justyna Knapik-Kowalczuk, Miyase Gözde Gündüz, Krzysztof Chmiel, Karolina Jurkiewicz, Mateusz Kurek, Lidia Tajber, Renata Jachowicz, Marian Paluch. Molecular dynamics, viscoelastic properties and physical stability studies of a new amorphous dihydropyridine derivative with T-type calcium channel blocking activity. European Journal of Pharmaceutical Sciences. 2019; 141 ():105083.

Chicago/Turabian Style

Justyna Knapik-Kowalczuk; Miyase Gözde Gündüz; Krzysztof Chmiel; Karolina Jurkiewicz; Mateusz Kurek; Lidia Tajber; Renata Jachowicz; Marian Paluch. 2019. "Molecular dynamics, viscoelastic properties and physical stability studies of a new amorphous dihydropyridine derivative with T-type calcium channel blocking activity." European Journal of Pharmaceutical Sciences 141, no. : 105083.

Journal article
Published: 04 September 2019 in European Journal of Pharmaceutics and Biopharmaceutics
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Itraconazole (ITR) is a broad-spectrum antifungal drug with a very low solubility. In this work, the application of a heat induced evaporative antisolvent nanoprecipitation process yielded disordered nanoparticles (NPs) of ITR. The inclusion of different types of poly(ethylene glycol) (PEG) allowed PEGylation of NPs by adsorption to be achieved. The NP dispersions were composed of monodispersed particles in a nanometric size range (<290 nm) and although PEGylation had no impact on the average particle size, the surface potential was partially neutralised in the modified NPs. The solid state analysis using powder X-ray diffraction and thermal analysis revealed a disordered, liquid crystalline smectic organisation of the non-PEGylated NPs, while some of the PEGylated NPs were more crystalline. The PEGylated NPs exhibited mucoadhesive potential in stationary conditions (dynamic light scattering analysis) but when flow conditions were applied (nanoparticle tracking analysis and quartz crystal microbalance with dissipation) the particles had mucopenetrative properties. The non-PEGylated ITR NPs did not interact with mucin and therefore, this system was considered as having mucopenetrative character. This study demonstrates that the properties of NPs made of organic drug molecules can be modified by polymers, which may impact on their interaction with mucin and therefore on their potential systemic absorption.

ACS Style

Ricardo Machado Cruz; Maria Jose Santos-Martinez; Lidia Tajber. Impact of polyethylene glycol polymers on the physicochemical properties and mucoadhesivity of itraconazole nanoparticles. European Journal of Pharmaceutics and Biopharmaceutics 2019, 144, 57 -67.

AMA Style

Ricardo Machado Cruz, Maria Jose Santos-Martinez, Lidia Tajber. Impact of polyethylene glycol polymers on the physicochemical properties and mucoadhesivity of itraconazole nanoparticles. European Journal of Pharmaceutics and Biopharmaceutics. 2019; 144 ():57-67.

Chicago/Turabian Style

Ricardo Machado Cruz; Maria Jose Santos-Martinez; Lidia Tajber. 2019. "Impact of polyethylene glycol polymers on the physicochemical properties and mucoadhesivity of itraconazole nanoparticles." European Journal of Pharmaceutics and Biopharmaceutics 144, no. : 57-67.

Protocol
Published: 25 July 2019 in Methods in Molecular Biology
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In recent years, nanoparticle tracking analysis (NTA) has emerged as an alternative tool for particle size characterization. Especially when examining polydisperse systems, individual particle to particle tracking allows for higher peak resolution than dynamic light scattering techniques. However, NTA requires an experienced user with a good insight into how the different settings can affect the determination of particle size and size distributions. This chapter provides a guideline for protein aggregation studies using the example of temperature-induced aggregation of IgG at low concentration.

ACS Style

Svenja Sladek; Kate McComiskey; Anne Marie Healy; Lidia Tajber. Nanoparticle Tracking Analysis to Examine the Temperature-Induced Aggregation of Proteins. Methods in Molecular Biology 2019, 2039, 131 -139.

AMA Style

Svenja Sladek, Kate McComiskey, Anne Marie Healy, Lidia Tajber. Nanoparticle Tracking Analysis to Examine the Temperature-Induced Aggregation of Proteins. Methods in Molecular Biology. 2019; 2039 ():131-139.

Chicago/Turabian Style

Svenja Sladek; Kate McComiskey; Anne Marie Healy; Lidia Tajber. 2019. "Nanoparticle Tracking Analysis to Examine the Temperature-Induced Aggregation of Proteins." Methods in Molecular Biology 2039, no. : 131-139.

Journal article
Published: 09 June 2019 in Pharmaceutics
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Enrofloxacin (ENRO) is a poorly soluble drug used in veterinary medicine. It differs from the more widely used fluoroquinolone ciprofloxacin (CIP) by the presence of an ethyl substituent on its piperazine amino group. While a number of recent studies have examined amorphous composite formulations of CIP, little research has been conducted with ENRO in this area. Therefore, the main purpose of this work was to produce amorphous solid dispersions (ASDs) of ENRO. The solid-state properties of these samples were investigated and compared to those of the equivalent CIP ASDs, and their water uptake behavior, solubility, dissolution, and antibacterial activity were assessed. Like CIP, X-ray amorphous solid dispersions were obtained when ENRO was ball milled with acidic polymers, whereas the use of neutral polymers resulted in semi-crystalline products. Proton transfer from the carboxylic acids of the polymers to the tertiary amine of ENRO’s piperazine group appears to occur in the ASDs, resulting in an ionic bond between the two components. Therefore, these ASDs can be referred to as amorphous polymeric salts (APSs). The glass transition temperatures of the APSs were significantly higher than that of ENRO, and they were also resistant to crystallization when exposed to high humidity levels. Greater concentrations were achieved with the APSs than the pure drug during solubility and dissolution studies, and this enhancement was sustained for the duration of the experiments. In addition, the antimicrobial activity of ENRO was not affected by APS formation, while the minimum inhibitory concentrations and minimum bactericidal concentrations obtained with the APS containing hydroxypropyl methylcellulose acetate succinate grade MG (HPMCAS-MG) were significantly lower than those of the pure drug. Therefore, APS formation is one method of improving the pharmaceutical properties of this drug.

ACS Style

Hanah Mesallati; Anita Umerska; Lidia Tajber. Fluoroquinolone Amorphous Polymeric Salts and Dispersions for Veterinary Uses. Pharmaceutics 2019, 11, 268 .

AMA Style

Hanah Mesallati, Anita Umerska, Lidia Tajber. Fluoroquinolone Amorphous Polymeric Salts and Dispersions for Veterinary Uses. Pharmaceutics. 2019; 11 (6):268.

Chicago/Turabian Style

Hanah Mesallati; Anita Umerska; Lidia Tajber. 2019. "Fluoroquinolone Amorphous Polymeric Salts and Dispersions for Veterinary Uses." Pharmaceutics 11, no. 6: 268.