Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization

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Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (en)
Развој микро- и наносистема као носача за лекове са антиинфламаторним деловањем и метода за њихову карактеризацију (sr)
Razvoj mikro- i nanosistema kao nosača za lekove sa antiinflamatornim delovanjem i metoda za njihovu karakterizaciju (sr_RS)
Authors

Publications

Sustained release of alpha-lipoic acid from chitosan microbeads synthetized by inverse emulsion method

Milašinović, Nikola; Čalija, Bojan; Vidović, Bojana; Crevar-Sakač, Milkica; Vujić, Zorica; Knežević-Jugović, Zorica

(Elsevier Science Bv, Amsterdam, 2016)

TY  - JOUR
AU  - Milašinović, Nikola
AU  - Čalija, Bojan
AU  - Vidović, Bojana
AU  - Crevar-Sakač, Milkica
AU  - Vujić, Zorica
AU  - Knežević-Jugović, Zorica
PY  - 2016
UR  - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/3456
AB  - The aim of this study was to investigate the encapsulation of a-lipoic acid (LA) onto chitosan microbeads in order to achieve a sustained release. Microbeads of different compositions were synthetized by inverse emulsion method, and characterized by in vitro swelling and drug release studies, FT-IR, DSC and SEM analyses. The encapsulation of LA was performed by swelling of previously synthetized dry microbeads in LA solution. The encapsulation efficiency was determined in terms of LA concentration, using liquid chromatography tandem mass spectrometry (LC-MS/MS). The swelling of synthetized microbeads was well pronounced in the acidic media. FT-IR analysis confirmed the presence of LA in microbeads and its interactions with matrices, which was in agreement with the results revealed by DSC analysis. SEM analysis revealed the porous structure, micron-size and spherical shape of the synthetized beads. Encapsulation efficiency was in the range from 46.8 to 58.5% depending on the hydrogel composition. The microbeads exhibited sustained release of LA under conditions mimicking gastrointestinal tract. Results of antioxidant activity of released LA showed good correlation with the concentration of the released LA. The obtained results suggested that synthetized microbeads have promising potential for oral administration with reduced dosing frequency in comparison to the immediate release formulations.
PB  - Elsevier Science Bv, Amsterdam
T2  - Journal of the Taiwan Institute of Chemical Engineers
T1  - Sustained release of alpha-lipoic acid from chitosan microbeads synthetized by inverse emulsion method
EP  - 112
SP  - 106
VL  - 60
DO  - 10.1016/j.jtice.2015.10.037
ER  - 
@article{
author = "Milašinović, Nikola and Čalija, Bojan and Vidović, Bojana and Crevar-Sakač, Milkica and Vujić, Zorica and Knežević-Jugović, Zorica",
year = "2016",
abstract = "The aim of this study was to investigate the encapsulation of a-lipoic acid (LA) onto chitosan microbeads in order to achieve a sustained release. Microbeads of different compositions were synthetized by inverse emulsion method, and characterized by in vitro swelling and drug release studies, FT-IR, DSC and SEM analyses. The encapsulation of LA was performed by swelling of previously synthetized dry microbeads in LA solution. The encapsulation efficiency was determined in terms of LA concentration, using liquid chromatography tandem mass spectrometry (LC-MS/MS). The swelling of synthetized microbeads was well pronounced in the acidic media. FT-IR analysis confirmed the presence of LA in microbeads and its interactions with matrices, which was in agreement with the results revealed by DSC analysis. SEM analysis revealed the porous structure, micron-size and spherical shape of the synthetized beads. Encapsulation efficiency was in the range from 46.8 to 58.5% depending on the hydrogel composition. The microbeads exhibited sustained release of LA under conditions mimicking gastrointestinal tract. Results of antioxidant activity of released LA showed good correlation with the concentration of the released LA. The obtained results suggested that synthetized microbeads have promising potential for oral administration with reduced dosing frequency in comparison to the immediate release formulations.",
publisher = "Elsevier Science Bv, Amsterdam",
journal = "Journal of the Taiwan Institute of Chemical Engineers",
title = "Sustained release of alpha-lipoic acid from chitosan microbeads synthetized by inverse emulsion method",
pages = "112-106",
volume = "60",
doi = "10.1016/j.jtice.2015.10.037"
}
Milašinović, N., Čalija, B., Vidović, B., Crevar-Sakač, M., Vujić, Z.,& Knežević-Jugović, Z.. (2016). Sustained release of alpha-lipoic acid from chitosan microbeads synthetized by inverse emulsion method. in Journal of the Taiwan Institute of Chemical Engineers
Elsevier Science Bv, Amsterdam., 60, 106-112.
https://doi.org/10.1016/j.jtice.2015.10.037
Milašinović N, Čalija B, Vidović B, Crevar-Sakač M, Vujić Z, Knežević-Jugović Z. Sustained release of alpha-lipoic acid from chitosan microbeads synthetized by inverse emulsion method. in Journal of the Taiwan Institute of Chemical Engineers. 2016;60:106-112.
doi:10.1016/j.jtice.2015.10.037 .
Milašinović, Nikola, Čalija, Bojan, Vidović, Bojana, Crevar-Sakač, Milkica, Vujić, Zorica, Knežević-Jugović, Zorica, "Sustained release of alpha-lipoic acid from chitosan microbeads synthetized by inverse emulsion method" in Journal of the Taiwan Institute of Chemical Engineers, 60 (2016):106-112,
https://doi.org/10.1016/j.jtice.2015.10.037 . .
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Alkyl polyglucoside-stabilized emulsion as a prospective vehicle for usnea barbata CO2-supercritical extract: Assessing stability, safety and efficiency of a topical formulation

Žugić, Ana R.; Lukić, Milica Z.; Tasić-Kostov, Marija Z.; Tadić, Vanja; Arsić, Ivana A.; Mišić, Dušan; Petrović, Slobodan; Savić, Snežana D.

(Association of Chemical Engineers of Serbia, 2015)

TY  - JOUR
AU  - Žugić, Ana R.
AU  - Lukić, Milica Z.
AU  - Tasić-Kostov, Marija Z.
AU  - Tadić, Vanja
AU  - Arsić, Ivana A.
AU  - Mišić, Dušan
AU  - Petrović, Slobodan
AU  - Savić, Snežana D.
PY  - 2015
UR  - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/2883
AB  - Antimicrobial activity of Usnea barbata especially against bacteria involved in pathogenesis of various skin conditions has been well documented in literature. Nevertheless, there are no papers dealing with formulation of its isolates into topical preparations for treatment of skin infections. In present study, alkyl polyglucoside (APG)-based vehicle was developed as carrier of U. barbata CO2-supercritical extract (U-SE) that demonstrated the best anti- microbial potential in preliminary screening. For comparison, chosen extract in the same concentration and using the same procedure was incorporated into a pharmacopoeial vehicle. Comparative evaluation of physicochemical stability, efficiency and safety proved APG-based vehicle to possess certain preferential features as carrier of U-SE compared to the reference one, composing a topical formulation with potential clinical relevance in treatment of skin infections.
AB  - Antimikrobna aktivnost vrste Usnea barbata naročito protiv bakterija koje učestvuju u patogenezi različitih bolesti kože, dobro je dokumentovana u naučnoj literaturi. Uprkos tome, ne postoje radovi koji se bave formulacijom topikalnih preparata na bazi ovog lišaja namenjenih lečenju kožnih infekcija. U ovoj studiji, razvijena je podloga stablizovana alkil poliglukozidnim (APG) emulgatorom, kao potencijalni nosač za ekstrakt vrste U. barbata koji je pokazao najbolji antimikrobni potencijal u preliminarnom istraživanju nekoliko ekstrakata dobijenih upotrebom različitih ekstragenasa/postupaka. Radi poređenja, odabrani CO2-natkritični ekstrakt je inkorporiran u istoj koncentraciji (koja odgovara 2 mas.% usninske kiseline) i istim postupkom izrade u često korišćenu podlogu farmakopejskog kvaliteta, a zatim je sprovedeno uporedno istraživanje fizičko-hemijske stabilnosti, efikasnosti i bezbednosti na obe grupe uzoraka. Rezulati našeg istraživanja pokazali su da se razvijena podloga stabilizovana APG emulgatorom može smatrati pogodnim nosačem za CO2-natkritični ekstrakt vrste U. barbata, čineći topikalnu formulaciju sa potencijalnim kliničkim značajem u terapiji kožnih infekcija. Reološka istraživanja pokazala su zadovoljavajuću sposobnost emulzije stabilizovane APG emulgatorom da ostane fizički stabilna nakon dodatka CO2-natkritičnog ekstrakta vrste U. barbata, u poređenju sa farmakopejskom. Međutim, konduktometrijska merenja su pokazala određena neslaganja sa reološkim nala- zima, namećući potrebu za dodatnim istraživanjima radi konačne procene fizičke stabilnosti testiranih emulzionih sistema. Izmerene vrednosti pH tokom perioda od 90 dana čuvanja uzoraka na sobnoj temperaturi ukazale su na zadovoljavajuću preliminarnu hemijsku stabilnost svih uzoraka. Dalja istraživanja efikasnosti i bezbednosti pokazala su bolji antimikrobni potencijal uzoraka sa podlogom stabilizovanom APG emulgatorom u odnosu na tradicionalno upotrebljavanu farmakopejsku bazu poznatog kvaliteta. Zadovoljavajući preliminarni bezbedonosni profili su pokazani kako za uzorke stabilizovane APG emulgatorom tako i za referentne krem uzorke. Na osnovu navedenog, može se zaključiti da je istraživana podloga bazirana na APG emulgatoru pokazala određene povoljnije karakteristike kao nosač za CO2-natkritični ekstrakt vrste U. barbata u poređenju sa konvencionalno korišćenom podlogom, naročito uzimajući u obzir njene poboljšane senzorne karakteristike, kao osobinu koja je često odlučujuća za komplijansu pacijenata.
PB  - Association of Chemical Engineers of Serbia
T2  - Hemijska industrija
T1  - Alkyl polyglucoside-stabilized emulsion as a prospective vehicle for usnea barbata CO2-supercritical extract: Assessing stability, safety and efficiency of a topical formulation
T1  - Emulzija stabilizovana alkil poliglukozidnim emulgatorom kao potencijalni nosač za CO2-natkritični ekstrakt vrste Usnea barbata - procena stabilnosti, bezbednosti i efikasnosti topikalne formulacije
EP  - 712
IS  - 6
SP  - 703
VL  - 69
DO  - 10.2298/HEMIND140701002Z
ER  - 
@article{
author = "Žugić, Ana R. and Lukić, Milica Z. and Tasić-Kostov, Marija Z. and Tadić, Vanja and Arsić, Ivana A. and Mišić, Dušan and Petrović, Slobodan and Savić, Snežana D.",
year = "2015",
abstract = "Antimicrobial activity of Usnea barbata especially against bacteria involved in pathogenesis of various skin conditions has been well documented in literature. Nevertheless, there are no papers dealing with formulation of its isolates into topical preparations for treatment of skin infections. In present study, alkyl polyglucoside (APG)-based vehicle was developed as carrier of U. barbata CO2-supercritical extract (U-SE) that demonstrated the best anti- microbial potential in preliminary screening. For comparison, chosen extract in the same concentration and using the same procedure was incorporated into a pharmacopoeial vehicle. Comparative evaluation of physicochemical stability, efficiency and safety proved APG-based vehicle to possess certain preferential features as carrier of U-SE compared to the reference one, composing a topical formulation with potential clinical relevance in treatment of skin infections., Antimikrobna aktivnost vrste Usnea barbata naročito protiv bakterija koje učestvuju u patogenezi različitih bolesti kože, dobro je dokumentovana u naučnoj literaturi. Uprkos tome, ne postoje radovi koji se bave formulacijom topikalnih preparata na bazi ovog lišaja namenjenih lečenju kožnih infekcija. U ovoj studiji, razvijena je podloga stablizovana alkil poliglukozidnim (APG) emulgatorom, kao potencijalni nosač za ekstrakt vrste U. barbata koji je pokazao najbolji antimikrobni potencijal u preliminarnom istraživanju nekoliko ekstrakata dobijenih upotrebom različitih ekstragenasa/postupaka. Radi poređenja, odabrani CO2-natkritični ekstrakt je inkorporiran u istoj koncentraciji (koja odgovara 2 mas.% usninske kiseline) i istim postupkom izrade u često korišćenu podlogu farmakopejskog kvaliteta, a zatim je sprovedeno uporedno istraživanje fizičko-hemijske stabilnosti, efikasnosti i bezbednosti na obe grupe uzoraka. Rezulati našeg istraživanja pokazali su da se razvijena podloga stabilizovana APG emulgatorom može smatrati pogodnim nosačem za CO2-natkritični ekstrakt vrste U. barbata, čineći topikalnu formulaciju sa potencijalnim kliničkim značajem u terapiji kožnih infekcija. Reološka istraživanja pokazala su zadovoljavajuću sposobnost emulzije stabilizovane APG emulgatorom da ostane fizički stabilna nakon dodatka CO2-natkritičnog ekstrakta vrste U. barbata, u poređenju sa farmakopejskom. Međutim, konduktometrijska merenja su pokazala određena neslaganja sa reološkim nala- zima, namećući potrebu za dodatnim istraživanjima radi konačne procene fizičke stabilnosti testiranih emulzionih sistema. Izmerene vrednosti pH tokom perioda od 90 dana čuvanja uzoraka na sobnoj temperaturi ukazale su na zadovoljavajuću preliminarnu hemijsku stabilnost svih uzoraka. Dalja istraživanja efikasnosti i bezbednosti pokazala su bolji antimikrobni potencijal uzoraka sa podlogom stabilizovanom APG emulgatorom u odnosu na tradicionalno upotrebljavanu farmakopejsku bazu poznatog kvaliteta. Zadovoljavajući preliminarni bezbedonosni profili su pokazani kako za uzorke stabilizovane APG emulgatorom tako i za referentne krem uzorke. Na osnovu navedenog, može se zaključiti da je istraživana podloga bazirana na APG emulgatoru pokazala određene povoljnije karakteristike kao nosač za CO2-natkritični ekstrakt vrste U. barbata u poređenju sa konvencionalno korišćenom podlogom, naročito uzimajući u obzir njene poboljšane senzorne karakteristike, kao osobinu koja je često odlučujuća za komplijansu pacijenata.",
publisher = "Association of Chemical Engineers of Serbia",
journal = "Hemijska industrija",
title = "Alkyl polyglucoside-stabilized emulsion as a prospective vehicle for usnea barbata CO2-supercritical extract: Assessing stability, safety and efficiency of a topical formulation, Emulzija stabilizovana alkil poliglukozidnim emulgatorom kao potencijalni nosač za CO2-natkritični ekstrakt vrste Usnea barbata - procena stabilnosti, bezbednosti i efikasnosti topikalne formulacije",
pages = "712-703",
number = "6",
volume = "69",
doi = "10.2298/HEMIND140701002Z"
}
Žugić, A. R., Lukić, M. Z., Tasić-Kostov, M. Z., Tadić, V., Arsić, I. A., Mišić, D., Petrović, S.,& Savić, S. D.. (2015). Alkyl polyglucoside-stabilized emulsion as a prospective vehicle for usnea barbata CO2-supercritical extract: Assessing stability, safety and efficiency of a topical formulation. in Hemijska industrija
Association of Chemical Engineers of Serbia., 69(6), 703-712.
https://doi.org/10.2298/HEMIND140701002Z
Žugić AR, Lukić MZ, Tasić-Kostov MZ, Tadić V, Arsić IA, Mišić D, Petrović S, Savić SD. Alkyl polyglucoside-stabilized emulsion as a prospective vehicle for usnea barbata CO2-supercritical extract: Assessing stability, safety and efficiency of a topical formulation. in Hemijska industrija. 2015;69(6):703-712.
doi:10.2298/HEMIND140701002Z .
Žugić, Ana R., Lukić, Milica Z., Tasić-Kostov, Marija Z., Tadić, Vanja, Arsić, Ivana A., Mišić, Dušan, Petrović, Slobodan, Savić, Snežana D., "Alkyl polyglucoside-stabilized emulsion as a prospective vehicle for usnea barbata CO2-supercritical extract: Assessing stability, safety and efficiency of a topical formulation" in Hemijska industrija, 69, no. 6 (2015):703-712,
https://doi.org/10.2298/HEMIND140701002Z . .
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A new class of emulsion systems - Fast inverted o/w emulsions: Formulation approach, physical stability and colloidal structure

Korać, Radava; Krajišnik, Danina; Savić, Snežana; Pantelić, Ivana; Jovancić, Petar; Cekić, Nebojša; Milić, Jela

(Elsevier Science BV, Amsterdam, 2014)

TY  - JOUR
AU  - Korać, Radava
AU  - Krajišnik, Danina
AU  - Savić, Snežana
AU  - Pantelić, Ivana
AU  - Jovancić, Petar
AU  - Cekić, Nebojša
AU  - Milić, Jela
PY  - 2014
UR  - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/5751
AB  - The fast inverted oil-in-water (o/w) emulsions named SWOP (SWitch Oil Phase) emulsions have been investigated with particular reference to physicochemical characteristics. Emulsions (oil-in-water (o/w) and water-in-oil (w/o)) are widely used in cosmetic and pharmaceutical formulations. Fast inverted o/w emulsions have been introduced as an alternative. The combination of appropriate w/o emulsifiers, anionic surfactants and polymeric stabilizers is essential for the formation of these emulsions. Samples of investigated, fast inverted o/w emulsion were prepared by hot-hot emulsification procedure using the combination of a w/o polymeric emulsifier (polyglyceryl-2 dipolyhydroxystearate) with a mild surfactant (sodium lauryl glucoside carboxylate (and) lauryl glucoside) in ratio 4:1.5 with addition of a stabilizing polymer (sodium polyacrylate). In the same manner, reference o/w and w/o emulsions were prepared. Investigated and reference emulsions were compared according to their physicochemical characteristics, structural characteristics, and their stability under the foreseen storage conditions and under the stress conditions employing the centrifugation test, pH, conductivity, rheological and contact angle measurements, microscopic observation, differential scanning calorimetry and thermogravimetric analysis. The samples of investigated and reference o/w emulsions were stable during three months storage at room temperature, while the samples of reference w/o emulsion showed phase separation. Only the samples of investigated emulsion remained stable in centrifugation test taken after the six freeze-thaw cycles. Oscillatory rheology indicated that the elastic modulus was dominant for both the investigated and the reference o/w emulsions due to the presence of gel structures, but the values of maximal apparent viscosity of the investigated emulsion which increased due to the temperature changes and the higher yield stress values that were obtained for the reference o/w emulsion indicated that the reference o/w emulsion had a stronger gel structure. Analysis of all the emulsions using polarization microscopy showed that the reference o/w emulsion had a more regular and a more rigid structure than the investigated emulsion. Obtained DSC and TGA results indicated that the SWOP emulsion showed a much faster evaporation of the water than the reference o/w emulsion which is in fine agreement with results from the contact angle measurements, i.e., the inversion point for the SWOP emulsion was attained in less than 15 min in comparison with the reference o/w emulsion. Generally, the fast inverted, SWOP emulsion showed better characteristics in comparison with the reference o/w and w/o emulsions making it suitable for the wide range of applications.
PB  - Elsevier Science BV, Amsterdam
T2  - Colloids and Surfaces A: Physicochemical and Engineering Aspects
T1  - A new class of emulsion systems - Fast inverted o/w emulsions: Formulation approach, physical stability and colloidal structure
EP  - 278
SP  - 267
VL  - 461
DO  - 10.1016/j.colsurfa.2014.08.005
ER  - 
@article{
author = "Korać, Radava and Krajišnik, Danina and Savić, Snežana and Pantelić, Ivana and Jovancić, Petar and Cekić, Nebojša and Milić, Jela",
year = "2014",
abstract = "The fast inverted oil-in-water (o/w) emulsions named SWOP (SWitch Oil Phase) emulsions have been investigated with particular reference to physicochemical characteristics. Emulsions (oil-in-water (o/w) and water-in-oil (w/o)) are widely used in cosmetic and pharmaceutical formulations. Fast inverted o/w emulsions have been introduced as an alternative. The combination of appropriate w/o emulsifiers, anionic surfactants and polymeric stabilizers is essential for the formation of these emulsions. Samples of investigated, fast inverted o/w emulsion were prepared by hot-hot emulsification procedure using the combination of a w/o polymeric emulsifier (polyglyceryl-2 dipolyhydroxystearate) with a mild surfactant (sodium lauryl glucoside carboxylate (and) lauryl glucoside) in ratio 4:1.5 with addition of a stabilizing polymer (sodium polyacrylate). In the same manner, reference o/w and w/o emulsions were prepared. Investigated and reference emulsions were compared according to their physicochemical characteristics, structural characteristics, and their stability under the foreseen storage conditions and under the stress conditions employing the centrifugation test, pH, conductivity, rheological and contact angle measurements, microscopic observation, differential scanning calorimetry and thermogravimetric analysis. The samples of investigated and reference o/w emulsions were stable during three months storage at room temperature, while the samples of reference w/o emulsion showed phase separation. Only the samples of investigated emulsion remained stable in centrifugation test taken after the six freeze-thaw cycles. Oscillatory rheology indicated that the elastic modulus was dominant for both the investigated and the reference o/w emulsions due to the presence of gel structures, but the values of maximal apparent viscosity of the investigated emulsion which increased due to the temperature changes and the higher yield stress values that were obtained for the reference o/w emulsion indicated that the reference o/w emulsion had a stronger gel structure. Analysis of all the emulsions using polarization microscopy showed that the reference o/w emulsion had a more regular and a more rigid structure than the investigated emulsion. Obtained DSC and TGA results indicated that the SWOP emulsion showed a much faster evaporation of the water than the reference o/w emulsion which is in fine agreement with results from the contact angle measurements, i.e., the inversion point for the SWOP emulsion was attained in less than 15 min in comparison with the reference o/w emulsion. Generally, the fast inverted, SWOP emulsion showed better characteristics in comparison with the reference o/w and w/o emulsions making it suitable for the wide range of applications.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "Colloids and Surfaces A: Physicochemical and Engineering Aspects",
title = "A new class of emulsion systems - Fast inverted o/w emulsions: Formulation approach, physical stability and colloidal structure",
pages = "278-267",
volume = "461",
doi = "10.1016/j.colsurfa.2014.08.005"
}
Korać, R., Krajišnik, D., Savić, S., Pantelić, I., Jovancić, P., Cekić, N.,& Milić, J.. (2014). A new class of emulsion systems - Fast inverted o/w emulsions: Formulation approach, physical stability and colloidal structure. in Colloids and Surfaces A: Physicochemical and Engineering Aspects
Elsevier Science BV, Amsterdam., 461, 267-278.
https://doi.org/10.1016/j.colsurfa.2014.08.005
Korać R, Krajišnik D, Savić S, Pantelić I, Jovancić P, Cekić N, Milić J. A new class of emulsion systems - Fast inverted o/w emulsions: Formulation approach, physical stability and colloidal structure. in Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2014;461:267-278.
doi:10.1016/j.colsurfa.2014.08.005 .
Korać, Radava, Krajišnik, Danina, Savić, Snežana, Pantelić, Ivana, Jovancić, Petar, Cekić, Nebojša, Milić, Jela, "A new class of emulsion systems - Fast inverted o/w emulsions: Formulation approach, physical stability and colloidal structure" in Colloids and Surfaces A: Physicochemical and Engineering Aspects, 461 (2014):267-278,
https://doi.org/10.1016/j.colsurfa.2014.08.005 . .
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