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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.
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 StyleAnita 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 StyleAnita 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.
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.
Hanah Mesallati; Anita Umerska; Lidia Tajber. Fluoroquinolone Amorphous Polymeric Salts and Dispersions for Veterinary Uses. Pharmaceutics 2019, 11, 268 .
AMA StyleHanah Mesallati, Anita Umerska, Lidia Tajber. Fluoroquinolone Amorphous Polymeric Salts and Dispersions for Veterinary Uses. Pharmaceutics. 2019; 11 (6):268.
Chicago/Turabian StyleHanah Mesallati; Anita Umerska; Lidia Tajber. 2019. "Fluoroquinolone Amorphous Polymeric Salts and Dispersions for Veterinary Uses." Pharmaceutics 11, no. 6: 268.
Reverse micelle-lipid nanocapsules: a novel strategy for drug delivery of the plectasin derivate AP138 antimicrobial peptide Anne-Claire Groo,1 Nada Matougui,2 Anita Umerska,2,3 Patrick Saulnier2,4 1Normandie Univ, UNICAEN, CERMN - EA 4258, FR CNRS 3038 INC3M, SF 4206 ICORE, Caen, France; 2Micro & Nanomédecines Translationelles-MINT, UNIV Angers, INSERM U1066, CNRS UMR 6021, UBL Universite Bretagne Loire, Angers, France; 3Université de Lorraine, CITHEFOR, Nancy, France; 4Angers University Hospital, Angers, France Introduction: Resistance to traditional antibiotics is an increasingly serious problem. Antimicrobial peptides (AMPs) have emerged as a new therapeutic class with great potential against infectious diseases, as they are less prone to induce resistance. Nanotechnology-based delivery strategies can improve the efficiency and stability of AMPs, particularly against proteolytic degradation. Lipid nanocapsules (LNCs) are a new generation of biomimetic nanocarriers and were used in this study to deliver peptides.Methods: AMP-loaded reverse micelles (RM) were developed and incorporated into LNCs by the phase inversion process and the antimicrobial activity of the AMPs-loaded LNC was evaluated by the minimum inhibitory concentration method. We studied the activity of AMP solutions and AMP-loaded LNCs against Gram-positive and Gram-negative bacterial strains and then evaluated the encapsulation of a new cationic AMP called AP138. Finally, we analyzed the effect of enzymatic attack on AP138 and AP138-RM-LNCs after incubation with trypsin.Results: AP138 was efficiently encapsulated in the LNCs (encapsulation efficiency = 97.8% at a drug loading of 0.151%), resulting in protection against degradation by proteases and the preservation of antimicrobial activity against Staphylococcus aureus, including methicillin-resistant Staphylococcus aureus.Conclusion: This study shows that RM-LNCs are an excellent candidate system to deliver AMPs. Keywords: nanoparticles, nanomedicine, antibacterial, AMP, methicillin-resistant Staphylococcus aureus, infection
Anne-Claire Groo; Nada Matougui; Anita Umerska; Patrick Saulnier. Reverse micelle-lipid nanocapsules: a novel strategy for drug delivery of the plectasin derivate AP138 antimicrobial peptide. International Journal of Nanomedicine 2018, ume 13, 7565 -7574.
AMA StyleAnne-Claire Groo, Nada Matougui, Anita Umerska, Patrick Saulnier. Reverse micelle-lipid nanocapsules: a novel strategy for drug delivery of the plectasin derivate AP138 antimicrobial peptide. International Journal of Nanomedicine. 2018; ume 13 ():7565-7574.
Chicago/Turabian StyleAnne-Claire Groo; Nada Matougui; Anita Umerska; Patrick Saulnier. 2018. "Reverse micelle-lipid nanocapsules: a novel strategy for drug delivery of the plectasin derivate AP138 antimicrobial peptide." International Journal of Nanomedicine ume 13, no. : 7565-7574.
The worldwide occurrence of resistance to standard antibiotics and lack of new antibacterial drugs demand new strategies to treat complicated infections. Hence, the aim of this study was to examine the antibacterial activities of an antimicrobial peptide, arenicin-3 derivative AA230, and ethylenediaminetetraacetic acid (EDTA) as well as the two compounds in combination against Gram-negative bacteria. AA230 showed strong antibacterial activity against all of the studied standard strains and clinical isolates, with minimum inhibitory concentrations ranging between 1 µg/mL and 8 µg/mL. AA230 exhibited a bactericidal mode of action. EDTA inhibited the growth of Acinetobacter baumannii at 500–1000 µg/mL. Strains of Acinetobacter baumannii were found to be more susceptible to EDTA than Pseudomonas aeruginosa or Escherichia coli. The antibacterial effects of both AA230 and EDTA were independent of the antibiotic resistance patterns. Indifference to synergistic activity was observed for AA230 and EDTA combinations using checkerboard titration. In time-kill studies, a substantial synergistic interaction between AA230 and EDTA was detected against all of the tested strains. The addition of EDTA enabled a 2–4-fold decrease in the AA230 dose. In conclusion, AA230 could have potential applications in the treatment of infections caused by Gram-negative organisms, and its effect can be potentiated by EDTA.
Anita Umerska; Magnus Strandh; Viviane Cassisa; Nada Matougui; Matthieu Eveillard; Patrick Saulnier. Synergistic Effect of Combinations Containing EDTA and the Antimicrobial Peptide AA230, an Arenicin-3 Derivative, on Gram-Negative Bacteria. Biomolecules 2018, 8, 122 .
AMA StyleAnita Umerska, Magnus Strandh, Viviane Cassisa, Nada Matougui, Matthieu Eveillard, Patrick Saulnier. Synergistic Effect of Combinations Containing EDTA and the Antimicrobial Peptide AA230, an Arenicin-3 Derivative, on Gram-Negative Bacteria. Biomolecules. 2018; 8 (4):122.
Chicago/Turabian StyleAnita Umerska; Magnus Strandh; Viviane Cassisa; Nada Matougui; Matthieu Eveillard; Patrick Saulnier. 2018. "Synergistic Effect of Combinations Containing EDTA and the Antimicrobial Peptide AA230, an Arenicin-3 Derivative, on Gram-Negative Bacteria." Biomolecules 8, no. 4: 122.
Catherine Fressinaud; Anita Monika Umerska; Joel Eyer; Patrick Saulnier. Effets de l’endocytose de nanocapsules lipidiques vectorisées par les oligodendrocytes. Revue Neurologique 2018, 174, S89 .
AMA StyleCatherine Fressinaud, Anita Monika Umerska, Joel Eyer, Patrick Saulnier. Effets de l’endocytose de nanocapsules lipidiques vectorisées par les oligodendrocytes. Revue Neurologique. 2018; 174 ():S89.
Chicago/Turabian StyleCatherine Fressinaud; Anita Monika Umerska; Joel Eyer; Patrick Saulnier. 2018. "Effets de l’endocytose de nanocapsules lipidiques vectorisées par les oligodendrocytes." Revue Neurologique 174, no. : S89.
Despite the promising biological and antioxidant properties of curcumin, its medical applications are limited due to poor solubility in water and low bioavailability. Polymeric nanoparticles (NPs) adapted to oral delivery may overcome these drawbacks. Properties such as particle size, zeta potential, morphology and encapsulation efficiency were assessed. Then, the possibility of storing these NPs in a solid-state form obtained by freeze-drying, in vitro curcumin dissolution and cytocompatibility towards intestinal cells were evaluated. Curcumin-loaded Eudragit® RLPO (ERL) NPs showed smaller particle diameters (245 ± 2 nm) and better redispersibility after freeze-drying than either poly(lactic-co-glycolic acid) (PLGA) or polycaprolactone (PCL) NPs. The former NPs showed lower curcumin encapsulation efficiency (62%) than either PLGA or PCL NPs (90% and 99%, respectively). Nevertheless, ERL NPs showed rapid curcumin release with 91 ± 5% released over 1 h. The three curcumin-loaded NPs proposed in this work were also compatible with intestinal cells. Overall, ERL NPs are the most promising vehicles for increasing the oral bioavailability of curcumin.
Anita Umerska; Caroline Gaucher; Felipe Oyarzun-Ampuero; Isabelle Fries-Raeth; Florence Colin; Maria Villamizar; Philippe Maincent; Anne Sapin-Minet. Polymeric Nanoparticles for Increasing Oral Bioavailability of Curcumin. Antioxidants 2018, 7, 46 .
AMA StyleAnita Umerska, Caroline Gaucher, Felipe Oyarzun-Ampuero, Isabelle Fries-Raeth, Florence Colin, Maria Villamizar, Philippe Maincent, Anne Sapin-Minet. Polymeric Nanoparticles for Increasing Oral Bioavailability of Curcumin. Antioxidants. 2018; 7 (4):46.
Chicago/Turabian StyleAnita Umerska; Caroline Gaucher; Felipe Oyarzun-Ampuero; Isabelle Fries-Raeth; Florence Colin; Maria Villamizar; Philippe Maincent; Anne Sapin-Minet. 2018. "Polymeric Nanoparticles for Increasing Oral Bioavailability of Curcumin." Antioxidants 7, no. 4: 46.
Bacterial antibiotic resistance is an emerging public health problem worldwide; therefore, new therapeutic strategies are needed. Many studies have described antipsychotic compounds that present antibacterial activity. Hence, the aims of this study were to evaluate the in vitro antibacterial activity of antipsychotics belonging to different chemical families, to assess the influence of their association with lipid nanocapsules (LNCs) on their antimicrobial activity as well as drug release and to study the uptake of LNCs by bacterial cells. Antibacterial activity was evaluated against Gram-positive Staphylococcus aureus and Gram negative Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Acinetobacter baumannii by minimum inhibitory concentration (MIC) assay, and the capability of killing tested microorganisms was evaluated by time kill assay. LNCs were prepared by phase inversion method, and the antipsychotic agents were incorporated using pre-loading and post-loading strategies. Only phenothiazines and thioxanthenes showed antibacterial activity, which was independent of antibiotic-resistance patterns. Loading the nanocarriers with the drugs affected the properties of the former, particularly their zeta potential. The release rate depended on the drug and its concentration—a maximum of released drug of less than 40% over 24 hours was observed for promazine. The influence of the drug associations on the antibacterial properties was concentration-dependent since, at low concentrations (high nanocarrier/drug ratio), the activity was lost, probably due to the high affinity of the drug to nanocarriers and slow release rate, whereas at higher concentrations, the activity was well maintained for the majority of the drugs. Chlorpromazine and thioridazine increased the uptake of the LNCs by bacteria compared with blank LNCs, even below the minimum inhibitory concentration.
Hassan Nehme; Patrick Saulnier; Alyaa A. Ramadan; Viviane Cassisa; Catherine Guillet; Matthieu Eveillard; Anita Umerska. Antibacterial activity of antipsychotic agents, their association with lipid nanocapsules and its impact on the properties of the nanocarriers and on antibacterial activity. PLOS ONE 2018, 13, e0189950 .
AMA StyleHassan Nehme, Patrick Saulnier, Alyaa A. Ramadan, Viviane Cassisa, Catherine Guillet, Matthieu Eveillard, Anita Umerska. Antibacterial activity of antipsychotic agents, their association with lipid nanocapsules and its impact on the properties of the nanocarriers and on antibacterial activity. PLOS ONE. 2018; 13 (1):e0189950.
Chicago/Turabian StyleHassan Nehme; Patrick Saulnier; Alyaa A. Ramadan; Viviane Cassisa; Catherine Guillet; Matthieu Eveillard; Anita Umerska. 2018. "Antibacterial activity of antipsychotic agents, their association with lipid nanocapsules and its impact on the properties of the nanocarriers and on antibacterial activity." PLOS ONE 13, no. 1: e0189950.
Lipid nanocapsules (LNCs) are biomimetic nanocarriers used for the encapsulation of a broad variety of active ingredients. Similar to surface active compounds, LNCs contain both hydrophilic and hydrophobic parts in their structure. Moreover, the components of LNCs, macrogol 15 hydroxystearate (MHS) and lecithin, are known for their surface active properties. Therefore, the aim of this paper was to investigate the capability of the LNCs to decrease surface tension using two techniques: drop tensiometry and the Wilhelmy plate method. LNCs with diameters ranging from 30 to 100 nm were successfully obtained using a phase inversion technique. The LNCs’ properties, such as size and zeta potential, depend on the composition. LNCs exhibit a lower limiting surface tension compared to MHS (34.8–35.0 mN/m and 37.7–38.8 mN/m, respectively), as confirmed by both drop tensiometry and the Wilhelmy plate method. LNCs have exhibited a saturated interfacial concentration (SIC) that was 10-fold higher than the critical micellar concentration (CMC) of MHS or the SIC of binary and ternary mixtures of LNC ingredients. The SIC of the LNC formulations depended on the mass mixing ratio of the MHS/triglycerides but not on the presence of lecithin. The CMC/SIC values measured by the Wilhelmy plate method were higher than those obtained using drop tensiometry because of the longer duration of the tensiometry measurement. In conclusion, the surfactant-like properties of the LNCs offer new possibilities for medical and pharmaceutical applications.
Celia R. A. Mouzouvi; Anita Umerska; André K. Bigot; Patrick Saulnier. Surface active properties of lipid nanocapsules. PLoS ONE 2017, 12, e0179211 -e0179211.
AMA StyleCelia R. A. Mouzouvi, Anita Umerska, André K. Bigot, Patrick Saulnier. Surface active properties of lipid nanocapsules. PLoS ONE. 2017; 12 (8):e0179211-e0179211.
Chicago/Turabian StyleCelia R. A. Mouzouvi; Anita Umerska; André K. Bigot; Patrick Saulnier. 2017. "Surface active properties of lipid nanocapsules." PLoS ONE 12, no. 8: e0179211-e0179211.
Synergistic interactions between antimicrobial peptides derived from plectasin and lipid nanocapsules containing monolaurin as a cosurfactant against Staphylococcus aureus Anita Umerska,1 Viviane Cassisa,2 Guillaume Bastiat,1 Nada Matougui,1 Hassan Nehme,1 Florence Manero,3 Matthieu Eveillard,4 Patrick Saulnier1 1MINT, UNIV Angers, INSERM 1066, CNRS 6021, Université Bretagne Loire, Angers, Cedex, France; 2Laboratoire de bactériologie, CHU Angers, France; 3SCIAM (Service Commun dâ
Anita Umerska; Viviane Cassisa; Guillaume Bastiat; Nada Matougui; Hassan Nehme; Florence Manero; Matthieu Eveillard; Patrick Saulnier. Synergistic interactions between antimicrobial peptides derived from plectasin and lipid nanocapsules containing monolaurin as a cosurfactant against Staphylococcus aureus. International Journal of Nanomedicine 2017, ume 12, 5687 -5699.
AMA StyleAnita Umerska, Viviane Cassisa, Guillaume Bastiat, Nada Matougui, Hassan Nehme, Florence Manero, Matthieu Eveillard, Patrick Saulnier. Synergistic interactions between antimicrobial peptides derived from plectasin and lipid nanocapsules containing monolaurin as a cosurfactant against Staphylococcus aureus. International Journal of Nanomedicine. 2017; ume 12 ():5687-5699.
Chicago/Turabian StyleAnita Umerska; Viviane Cassisa; Guillaume Bastiat; Nada Matougui; Hassan Nehme; Florence Manero; Matthieu Eveillard; Patrick Saulnier. 2017. "Synergistic interactions between antimicrobial peptides derived from plectasin and lipid nanocapsules containing monolaurin as a cosurfactant against Staphylococcus aureus." International Journal of Nanomedicine ume 12, no. : 5687-5699.
Ciprofloxacin (CIP) is a poorly soluble drug that also displays poor permeability. Attempts to improve the solubility of this drug to date have largely focused on the formation of crystalline salts and metal complexes. The aim of this study was to prepare amorphous solid dispersions (ASDs) by ball milling CIP with various polymers. Following examination of their solid state characteristics and physical stability, the solubility advantage of these ASDs was studied, and their permeability was investigated via parallel artificial membrane permeability assay (PAMPA). Finally, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the ASDs were compared to those of CIP. It was discovered that acidic polymers, such as Eudragit L100, Eudragit L100-55, Carbopol, and HPMCAS, were necessary for the amorphization of CIP. In each case, the positively charged secondary amine of CIP was found to interact with carboxylate groups in the polymers, forming amorphous polymeric drug salts. Although the ASDs began to crystallize within days under accelerated stability conditions, they remained fully X-ray amorphous following exposure to 90% RH at 25 °C, and demonstrated higher than predicted glass transition temperatures. The solubility of CIP in water and simulated intestinal fluid was also increased by all of the ASDs studied. Unlike a number of other solubility enhancing formulations, the ASDs did not decrease the permeability of the drug. Similarly, no decrease in antibiotic efficacy was observed, and significant improvements in the MIC and MBC of CIP were obtained with ASDs containing HPMCAS-LG and HPMCAS-MG. Therefore, ASDs may be a viable alternative for formulating CIP with improved solubility, bioavailability, and antimicrobial activity.
Hanah Mesallati; Anita Umerska; Krzysztof J. Paluch; Lidia Tajber. Amorphous Polymeric Drug Salts as Ionic Solid Dispersion Forms of Ciprofloxacin. Molecular Pharmaceutics 2017, 14, 2209 -2223.
AMA StyleHanah Mesallati, Anita Umerska, Krzysztof J. Paluch, Lidia Tajber. Amorphous Polymeric Drug Salts as Ionic Solid Dispersion Forms of Ciprofloxacin. Molecular Pharmaceutics. 2017; 14 (7):2209-2223.
Chicago/Turabian StyleHanah Mesallati; Anita Umerska; Krzysztof J. Paluch; Lidia Tajber. 2017. "Amorphous Polymeric Drug Salts as Ionic Solid Dispersion Forms of Ciprofloxacin." Molecular Pharmaceutics 14, no. 7: 2209-2223.
Novel antibiotics, such as antimicrobial peptides (AMPs), have recently attended more and more attraction. In this work, dispersed cubic liquid crystalline gel (cubosomes) was used as drug delivery vehicles for three AMPs (AP114, DPK-060 and LL-37). Association of peptides onto cubosomes was studied at two cubosome/peptide ratios using high performance liquid chromatography, ζ-potential and circular dichroism measurements. AMPs impact on the cubosome structure was investigated using small angle x-ray scattering and cryogenic transmission electron microscopy. The antimicrobial effect of the AMP loaded cubosomes was studied in vitro by minimum inhibitory concentration and time-kill assays. Proteolytic protection was investigated by incubating the formulations with two elastases and the antimicrobial effect after proteolysis was studied using radial diffusion assay. Different association efficacy onto the cubosomes was observed among the AMPs, with LL-37 showing greatest association (>60%). AP114 loaded cubosomes displayed a preserved antimicrobial effect, whereas for LL-37 the broad spectrum bacterial killing was reduced to only comprise Gram-negative bacteria. Interestingly, DPK-060 loaded cubosomes showed a slight enhanced effect against S. aureus and E. coli strains. Moreover, the cubosomes were found to protect LL-37 from proteolytic degradation, resulting in a significantly better bactericidal effect after being subjected to elastase, compared to unformulated peptide.
Lukas Boge; Anita Umerska; Nada Matougui; Helena Bysell; Lovisa Ringstad; Mina Davoudi; Jonny Eriksson; Katarina Edwards; Martin Andersson. Cubosomes post-loaded with antimicrobial peptides: characterization, bactericidal effect and proteolytic stability. International Journal of Pharmaceutics 2017, 526, 400 -412.
AMA StyleLukas Boge, Anita Umerska, Nada Matougui, Helena Bysell, Lovisa Ringstad, Mina Davoudi, Jonny Eriksson, Katarina Edwards, Martin Andersson. Cubosomes post-loaded with antimicrobial peptides: characterization, bactericidal effect and proteolytic stability. International Journal of Pharmaceutics. 2017; 526 (1-2):400-412.
Chicago/Turabian StyleLukas Boge; Anita Umerska; Nada Matougui; Helena Bysell; Lovisa Ringstad; Mina Davoudi; Jonny Eriksson; Katarina Edwards; Martin Andersson. 2017. "Cubosomes post-loaded with antimicrobial peptides: characterization, bactericidal effect and proteolytic stability." International Journal of Pharmaceutics 526, no. 1-2: 400-412.
Catherine Fressinaud; Anita Monika Umerska; Patrick Saulnier; Joël Eyer. Internalisation par les oligodendrocytes de nanocapsules lipidiques vectorisées. Revue Neurologique 2017, 173, S110 -S111.
AMA StyleCatherine Fressinaud, Anita Monika Umerska, Patrick Saulnier, Joël Eyer. Internalisation par les oligodendrocytes de nanocapsules lipidiques vectorisées. Revue Neurologique. 2017; 173 ():S110-S111.
Chicago/Turabian StyleCatherine Fressinaud; Anita Monika Umerska; Patrick Saulnier; Joël Eyer. 2017. "Internalisation par les oligodendrocytes de nanocapsules lipidiques vectorisées." Revue Neurologique 173, no. : S110-S111.
The aim of this work was to examine the formation and properties of chondroitin sulfate (CHON)-based nanoparticles (NPs), namely CHON/chitosan (CHIT), CHON/CHIT/calcitonin (sCT) and CHON/sCT. Both, positively and negatively charged CHON/CHIT NPs have been successfully obtained with properties that were dependent on the polymer mixing ratio, polymer concentration and molecular weight of CHIT. sCT was successfully loaded into CHON/CHIT NPs with efficiency close to 100% and notably high loading (up to 33%). A new type of NPs composed of CHON and sCT (a binary system) has been successfully developed. CHON/sCT NPs offer the advantage of a very high drug loading up to 73%. The particle size of CHON-based NPs increased in PBS, acetate buffer and in HCl solution compared to that in water, but most of them remained in the nano-range even after 24h. The media and composition of the nanocarriers were found to affect the release of sCT.
Anita Umerska; Owen I. Corrigan; Lidia Tajber. Design of chondroitin sulfate-based polyelectrolyte nanoplexes: Formation of nanocarriers with chitosan and a case study of salmon calcitonin. Carbohydrate Polymers 2017, 156, 276 -284.
AMA StyleAnita Umerska, Owen I. Corrigan, Lidia Tajber. Design of chondroitin sulfate-based polyelectrolyte nanoplexes: Formation of nanocarriers with chitosan and a case study of salmon calcitonin. Carbohydrate Polymers. 2017; 156 ():276-284.
Chicago/Turabian StyleAnita Umerska; Owen I. Corrigan; Lidia Tajber. 2017. "Design of chondroitin sulfate-based polyelectrolyte nanoplexes: Formation of nanocarriers with chitosan and a case study of salmon calcitonin." Carbohydrate Polymers 156, no. : 276-284.
Lipid nanocapsules (LNCs) are a new generation of biomimetic nanocarriers obtained via a phase inversion temperature method and have an oily core of medium-chain triglycerides that is surrounded by a shelf containing a lipophilic surfactant (lecithin) and a hydrophilic surfactant macrogol 15-hydroxystearate. The aim of the present study was to produce LNCs with antibacterial activity by replacing lecithin with other lipophilic surface active compounds, namely medium-chain fatty acids and their 1-monoglycerides, which are known to have antimicrobial properties. Fatty acids and monoglycerides were found to affect the properties of LNCs, such as particle size and zeta potential. Incorporation of a co-surfactant decreased significantly particle size (p⩽0.0039). Furthermore, incorporation of either lecithin or fatty acids with at least 10 carbon atoms yielded LNCs with the zeta potential significantly more negative than that of LNCs composed solely of triglycerides and macrogol 15 hydroxystearate (p⩽0.0310). Moreover, they were capable of decreasing the phase inversion temperature. The activity of the LCNs against Gram-positive S. aureus, including a methicillin-resistant strain, increased with increases in the length of the hydrocarbon tail. Monoglyceride-LNCs were found to be more active than the corresponding fatty acids. The opposite behaviour was observed for Gram-negative bacteria, whereby only caproic acid- and caprylic acid-LNCs were found to be active against these organisms. The monoglyceride-LNCs were bactericidal, and they killed in a time-dependent manner. Fatty acid-LNCs killed in a concentration-dependent manner. A haemolysis assay was performed to obtain preliminary information on the safety of the tested LNCs. In the case of fatty acid-LNCs, the concentrations at which bacterial growth was inhibited were similar to the haemolytic concentrations. However, monoglyceride-LNCs showed antibacterial action at concentrations much lower than those at which haemolysis was observed. In conclusion, monoglyceride-LNCs are promising candidates as carriers for the encapsulation of antibacterial agents, particularly against S. aureus.
Anita Umerska; Viviane Cassisa; Nada Matougui; Marie Laure Joly-Guillou; Matthieu Eveillard; Patrick Saulnier. Antibacterial action of lipid nanocapsules containing fatty acids or monoglycerides as co-surfactants. European Journal of Pharmaceutics and Biopharmaceutics 2016, 108, 100 -110.
AMA StyleAnita Umerska, Viviane Cassisa, Nada Matougui, Marie Laure Joly-Guillou, Matthieu Eveillard, Patrick Saulnier. Antibacterial action of lipid nanocapsules containing fatty acids or monoglycerides as co-surfactants. European Journal of Pharmaceutics and Biopharmaceutics. 2016; 108 ():100-110.
Chicago/Turabian StyleAnita Umerska; Viviane Cassisa; Nada Matougui; Marie Laure Joly-Guillou; Matthieu Eveillard; Patrick Saulnier. 2016. "Antibacterial action of lipid nanocapsules containing fatty acids or monoglycerides as co-surfactants." European Journal of Pharmaceutics and Biopharmaceutics 108, no. : 100-110.
The adsorption of therapeutic molecules, e.g., peptides, onto nanocarriers is influenced by the properties of the carrier, adsorbed molecule and continuous phase. Hence, through changes in the composition of the nanocarrier and the medium, it should be possible to tune the system to make it capable of efficiently adsorbing peptides. The adsorption of calcitonin, antimicrobial peptide AP114 and polymyxin B onto lipid nanocapsules was investigated. The adsorption data were fitted to a Langmuir isotherm. Dynamic light scattering and laser Doppler velocimetry were used to investigate the changes in the hydrodynamic diameter and zeta potential, respectively, of the nanocarrier. The peptide adsorption was primarily governed by electrostatic forces; however, even without the presence of an ionisable surfactant, a significant amount of each tested molecule was adsorbed due to the enormous surface area of the nanocarriers and to peptide-nanocarrier interactions. The addition of an ionisable lipophilic surfactant, lecithin, improved the adsorption yield, which reached values of up to 100%. The adsorption yield and the properties of the nanocarrier, particularly the zeta potential, depended on the carrier and peptide concentrations and their mixing ratio. The adsorption of all tested molecules obeyed the Langmuir model over a limited concentration range.
Anita Umerska; Nada Matougui; Anne-Claire Groo; Patrick Saulnier. Understanding the adsorption of salmon calcitonin, antimicrobial peptide AP114 and polymyxin B onto lipid nanocapsules. International Journal of Pharmaceutics 2016, 506, 191 -200.
AMA StyleAnita Umerska, Nada Matougui, Anne-Claire Groo, Patrick Saulnier. Understanding the adsorption of salmon calcitonin, antimicrobial peptide AP114 and polymyxin B onto lipid nanocapsules. International Journal of Pharmaceutics. 2016; 506 (1-2):191-200.
Chicago/Turabian StyleAnita Umerska; Nada Matougui; Anne-Claire Groo; Patrick Saulnier. 2016. "Understanding the adsorption of salmon calcitonin, antimicrobial peptide AP114 and polymyxin B onto lipid nanocapsules." International Journal of Pharmaceutics 506, no. 1-2: 191-200.
The number of antibiotic-resistant bacteria is increasing worldwide, and the demand for novel antimicrobials is constantly growing. Antimicrobial peptides (AMPs) could be an important part of future treatment strategies of various bacterial infection diseases. However, AMPs have relatively low stability, because of proteolytic and chemical degradation. As a consequence, carrier systems protecting the AMPs are greatly needed, to achieve efficient treatments. In addition, the carrier system also must administrate the peptide in a controlled manner to match the therapeutic dose window. In this work, lyotropic liquid crystalline (LC) structures consisting of cubic glycerol monooleate/water and hexagonal glycerol monooleate/oleic acid/water have been examined as carriers for AMPs. These LC structures have the capability of solubilizing both hydrophilic and hydrophobic substances, as well as being biocompatible and biodegradable. Both bulk gels and discrete dispersed structures (i.e., cubosomes and hexosomes) have been studied. Three AMPs have been investigated with respect to phase stability of the LC structures and antimicrobial effect: AP114, DPK-060, and LL-37. Characterization of the LC structures was performed using small-angle X-ray scattering (SAXS), dynamic light scattering, ζ-potential, and cryogenic transmission electron microscopy (Cryo-TEM) and peptide loading efficacy by ultra performance liquid chromatography. The antimicrobial effect of the LCNPs was investigated in vitro using minimum inhibitory concentration (MIC) and time-kill assay. The most hydrophobic peptide (AP114) was shown to induce an increase in negative curvature of the cubic LC system. The most polar peptide (DPK-060) induced a decrease in negative curvature while LL-37 did not change the LC phase at all. The hexagonal LC phase was not affected by any of the AMPs. Moreover, cubosomes loaded with peptides AP114 and DPK-060 showed preserved antimicrobial activity, whereas particles loaded with peptide LL-37 displayed a loss in its broad-spectrum bactericidal properties. AMP-loaded hexosomes showed a reduction in antimicrobial activity.
Lukas Boge; Helena Bysell; Lovisa Ringstad; David Wennman; Anita Umerska; Viviane Cassisa; Jonny Eriksson; Marie-Laure Joly-Guillou; Katarina Edwards; Martin Andersson. Lipid-Based Liquid Crystals As Carriers for Antimicrobial Peptides: Phase Behavior and Antimicrobial Effect. Langmuir 2016, 32, 4217 -4228.
AMA StyleLukas Boge, Helena Bysell, Lovisa Ringstad, David Wennman, Anita Umerska, Viviane Cassisa, Jonny Eriksson, Marie-Laure Joly-Guillou, Katarina Edwards, Martin Andersson. Lipid-Based Liquid Crystals As Carriers for Antimicrobial Peptides: Phase Behavior and Antimicrobial Effect. Langmuir. 2016; 32 (17):4217-4228.
Chicago/Turabian StyleLukas Boge; Helena Bysell; Lovisa Ringstad; David Wennman; Anita Umerska; Viviane Cassisa; Jonny Eriksson; Marie-Laure Joly-Guillou; Katarina Edwards; Martin Andersson. 2016. "Lipid-Based Liquid Crystals As Carriers for Antimicrobial Peptides: Phase Behavior and Antimicrobial Effect." Langmuir 32, no. 17: 4217-4228.
Nanoformulations have attracted a lot of attention because of their size-dependent properties. Among the array of nanoformulations, lipid nanoformulations (LNFs) have evoked increasing interest because of the advantages of their high degree of biocompatibility and versatility. The performance of lipid nanoformulations is greatly influenced by their composition and structure. Therapeutic peptides represent a growing share of the pharmaceutical market. However, the main challenge for their development into commercial products is their inherent physicochemical and biological instability. Important peptides such as insulin, calcitonin and cyclosporin A have been incorporated into LNFs. The association or encapsulation of peptides within lipid-based carriers has shown to protect the labile molecules against enzymatic degradation. This review describes strategies used for the formulation of peptides and some methods used for the assessment of association efficiency. The advantages and drawbacks of such carriers are also described.
Nada Matougui; Lukas Boge; Anne-Claire Groo; Anita Umerska; Lovisa Ringstad; Helena Bysell; Patrick Saulnier. Lipid-based nanoformulations for peptide delivery. International Journal of Pharmaceutics 2016, 502, 80 -97.
AMA StyleNada Matougui, Lukas Boge, Anne-Claire Groo, Anita Umerska, Lovisa Ringstad, Helena Bysell, Patrick Saulnier. Lipid-based nanoformulations for peptide delivery. International Journal of Pharmaceutics. 2016; 502 (1-2):80-97.
Chicago/Turabian StyleNada Matougui; Lukas Boge; Anne-Claire Groo; Anita Umerska; Lovisa Ringstad; Helena Bysell; Patrick Saulnier. 2016. "Lipid-based nanoformulations for peptide delivery." International Journal of Pharmaceutics 502, no. 1-2: 80-97.
Anita Umerska; Celia R.A. Mouzouvi; André Bigot; Patrick Saulnier. Formulation and nebulization of fluticasone propionate-loaded lipid nanocarriers. International Journal of Pharmaceutics 2015, 493, 224 -232.
AMA StyleAnita Umerska, Celia R.A. Mouzouvi, André Bigot, Patrick Saulnier. Formulation and nebulization of fluticasone propionate-loaded lipid nanocarriers. International Journal of Pharmaceutics. 2015; 493 (1-2):224-232.
Chicago/Turabian StyleAnita Umerska; Celia R.A. Mouzouvi; André Bigot; Patrick Saulnier. 2015. "Formulation and nebulization of fluticasone propionate-loaded lipid nanocarriers." International Journal of Pharmaceutics 493, no. 1-2: 224-232.
A new type of self-assembled polyelectrolyte complex nanocarrier composed of chondroitin (CHON) and protamine (PROT) was designed and the ability of the carriers to bind salmon calcitonin (sCT) was examined. The response of sCT-loaded CHON/PROT NPs to a change in the properties of the liquid medium, e.g. its pH, composition or ionic strength was studied and in vitro peptide release was assessed. The biocompatibility of the NPs was evaluated in Caco-2 cells. CHON/PROT NPs were successfully obtained with properties that were dependent on the concentration of the polyelectrolytes and their mixing ratio. X-ray diffraction determined the amorphous nature of the negatively charged NPs, while those with the positive surface potential were semi-crystalline. sCT was efficiently associated with the nanocarriers (98-100%) and a notably high drug loading (13-38%) was achieved. The particles had negative zeta potential values and were homogenously dispersed with sizes between 60 and 250nm. CHON/PROT NPs released less than 10% of the total loaded peptide in the first hour of the in vitro release studies. The enthalpy of the decomposition exotherm correlated with the amount of sCT remaining in NPs after the release experiments. The composition of medium and its ionic strength was found to have a considerable influence on the release of sCT from CHON/PROT NPs. Complexation to CHON markedly reduced the toxic effects exerted by PROT and the NPs were compatible and well tolerated by Caco-2 cells.
Anita Umerska; Krzysztof Jan Paluch; Maria Jose Santos-Martinez; Carlos Medina; Owen I. Corrigan; Lidia Tajber. Chondroitin-based nanoplexes as peptide delivery systems – Investigations into the self-assembly process, solid-state and extended release characteristics. European Journal of Pharmaceutics and Biopharmaceutics 2015, 93, 242 -253.
AMA StyleAnita Umerska, Krzysztof Jan Paluch, Maria Jose Santos-Martinez, Carlos Medina, Owen I. Corrigan, Lidia Tajber. Chondroitin-based nanoplexes as peptide delivery systems – Investigations into the self-assembly process, solid-state and extended release characteristics. European Journal of Pharmaceutics and Biopharmaceutics. 2015; 93 ():242-253.
Chicago/Turabian StyleAnita Umerska; Krzysztof Jan Paluch; Maria Jose Santos-Martinez; Carlos Medina; Owen I. Corrigan; Lidia Tajber. 2015. "Chondroitin-based nanoplexes as peptide delivery systems – Investigations into the self-assembly process, solid-state and extended release characteristics." European Journal of Pharmaceutics and Biopharmaceutics 93, no. : 242-253.
This work investigates a new type of polyelectrolyte complex nanocarrier composed of hyaluronic acid (HA) and protamine (PROT). Small (approximately 60 nm) and negatively charged nanoparticles (NPs) with a polydispersity index of less than 0.2 were obtained with properties that were dependent on the mixing ratio, concentration of polyelectrolytes and molecular weight of HA. Salmon calcitonin (sCT) was efficiently (up to 100%) associated with the NPs, and the drug loading (9.6-39% w/w) was notably high, possibly due to an interaction between HA and sCT. The NPs released -70-80% of the sCT after 24 hours, with the estimated total amount of released sCT depending on the amount of HA and PROT present in the NPs. The isoelectric point of the NPs was close to pH 2, and the negative surface charge was maintained above this pH. The HA/PROT nanoplexes protected the sCT from enzymatic degradation and showed low toxicity to intestinal epithelial cells, and thus may be a promising oral delivery system for peptides.
Anita Umerska; Krzysztof J. Paluch; Maria-Jose Santos Martinez; Owen I. Corrigan; Carlos Medina; Lidia Tajber. Self-assembled hyaluronate/protamine polyelectrolyte nanoplexes: synthesis, stability, biocompatibility and potential use as peptide carriers. Journal of Biomedical Nanotechnology 2014, 10, 3658 -3673.
AMA StyleAnita Umerska, Krzysztof J. Paluch, Maria-Jose Santos Martinez, Owen I. Corrigan, Carlos Medina, Lidia Tajber. Self-assembled hyaluronate/protamine polyelectrolyte nanoplexes: synthesis, stability, biocompatibility and potential use as peptide carriers. Journal of Biomedical Nanotechnology. 2014; 10 (12):3658-3673.
Chicago/Turabian StyleAnita Umerska; Krzysztof J. Paluch; Maria-Jose Santos Martinez; Owen I. Corrigan; Carlos Medina; Lidia Tajber. 2014. "Self-assembled hyaluronate/protamine polyelectrolyte nanoplexes: synthesis, stability, biocompatibility and potential use as peptide carriers." Journal of Biomedical Nanotechnology 10, no. 12: 3658-3673.