Cetković, Zora

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  • Cetković, Zora (2)
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Author's Bibliography

In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems

Cetković, Zora; Cvijić, Sandra; Vasiljević, Dragana

(Taylor & Francis Ltd, Abingdon, 2018) 

TY  - JOUR
AU  - Cetković, Zora
AU  - Cvijić, Sandra
AU  - Vasiljević, Dragana
PY  - 2018
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3178
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3430
AB  - Objective: The aims of this study were to formulate simvastatin (SV)-loaded self-microemulsifying drug delivery systems (SMEDDS), and explore the potential of these drug delivery systems to improve SV solubility, and also to identify the optimal place in the gastrointestinal (GI) tract for the release of SV using coupled in vitro/in silico approach. Significance: In comparison to other published results, this study considered the extensive pre-systemic clearance of SV, which could significantly decrease its systemic and hepatic bioavailability if SV is delivered into the small intestine. Methods: SV-loaded SMEDDS were formulated using various proportions of oils (PEG 300 oleic glycerides, propylene glycol monocaprylate, propylene glycol monolaurate), surfactant (PEG 400 caprylic/capric glycerides) and cosurfactant (polysorbate 80) and subjected to characterization, and physiologically-based pharmacokinetic (PBPK) modeling. Results: According to the in vitro results, the selected SMEDDS consisted of 10.0% PEG 300 oleic glycerides, 67.5% PEG 400 caprylic/capric glycerides, and 22.5% polysorbate 80. The use of acid-resistant capsules filled with SV-loaded SMEDDS was found helpful in protecting the drug against early degradation in proximal parts of the GI tract, however, in silico simulations indicated that pH-controlled drug release system that dissolve in the distal parts of the intestine might further improve SV bioavailability (up to 7.20%). Conclusion: The obtained results suggested that combined strategy for the improvement of SV bioavailability should comprise solubility enhancement and delayed drug release. The developed SV-specific PBPK model could potentially be used to assess the influence of formulation factors on drug absorption and disposition when developing SV oral dosage forms.
PB  - Taylor & Francis Ltd, Abingdon
T2  - Drug Development and Industrial Pharmacy
T1  - In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems
VL  - 44
IS  - 5
SP  - 849
EP  - 860
DO  - 10.1080/03639045.2017.1414835
ER  - 
@article{
author = "Cetković, Zora and Cvijić, Sandra and Vasiljević, Dragana",
year = "2018",
abstract = "Objective: The aims of this study were to formulate simvastatin (SV)-loaded self-microemulsifying drug delivery systems (SMEDDS), and explore the potential of these drug delivery systems to improve SV solubility, and also to identify the optimal place in the gastrointestinal (GI) tract for the release of SV using coupled in vitro/in silico approach. Significance: In comparison to other published results, this study considered the extensive pre-systemic clearance of SV, which could significantly decrease its systemic and hepatic bioavailability if SV is delivered into the small intestine. Methods: SV-loaded SMEDDS were formulated using various proportions of oils (PEG 300 oleic glycerides, propylene glycol monocaprylate, propylene glycol monolaurate), surfactant (PEG 400 caprylic/capric glycerides) and cosurfactant (polysorbate 80) and subjected to characterization, and physiologically-based pharmacokinetic (PBPK) modeling. Results: According to the in vitro results, the selected SMEDDS consisted of 10.0% PEG 300 oleic glycerides, 67.5% PEG 400 caprylic/capric glycerides, and 22.5% polysorbate 80. The use of acid-resistant capsules filled with SV-loaded SMEDDS was found helpful in protecting the drug against early degradation in proximal parts of the GI tract, however, in silico simulations indicated that pH-controlled drug release system that dissolve in the distal parts of the intestine might further improve SV bioavailability (up to 7.20%). Conclusion: The obtained results suggested that combined strategy for the improvement of SV bioavailability should comprise solubility enhancement and delayed drug release. The developed SV-specific PBPK model could potentially be used to assess the influence of formulation factors on drug absorption and disposition when developing SV oral dosage forms.",
publisher = "Taylor & Francis Ltd, Abingdon",
journal = "Drug Development and Industrial Pharmacy",
title = "In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems",
volume = "44",
number = "5",
pages = "849-860",
doi = "10.1080/03639045.2017.1414835"
}
Cetković, Z., Cvijić, S.,& Vasiljević, D.. (2018). In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems. in Drug Development and Industrial Pharmacy
Taylor & Francis Ltd, Abingdon., 44(5), 849-860.
https://doi.org/10.1080/03639045.2017.1414835
Cetković Z, Cvijić S, Vasiljević D. In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems. in Drug Development and Industrial Pharmacy. 2018;44(5):849-860.
doi:10.1080/03639045.2017.1414835 .
Cetković, Zora, Cvijić, Sandra, Vasiljević, Dragana, "In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems" in Drug Development and Industrial Pharmacy, 44, no. 5 (2018):849-860,
https://doi.org/10.1080/03639045.2017.1414835 . .
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In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems

Cetković, Zora; Cvijić, Sandra; Vasiljević, Dragana

(Taylor & Francis Ltd, Abingdon, 2018) 

TY  - JOUR
AU  - Cetković, Zora
AU  - Cvijić, Sandra
AU  - Vasiljević, Dragana
PY  - 2018
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3178
AB  - Objective: The aims of this study were to formulate simvastatin (SV)-loaded self-microemulsifying drug delivery systems (SMEDDS), and explore the potential of these drug delivery systems to improve SV solubility, and also to identify the optimal place in the gastrointestinal (GI) tract for the release of SV using coupled in vitro/in silico approach. Significance: In comparison to other published results, this study considered the extensive pre-systemic clearance of SV, which could significantly decrease its systemic and hepatic bioavailability if SV is delivered into the small intestine. Methods: SV-loaded SMEDDS were formulated using various proportions of oils (PEG 300 oleic glycerides, propylene glycol monocaprylate, propylene glycol monolaurate), surfactant (PEG 400 caprylic/capric glycerides) and cosurfactant (polysorbate 80) and subjected to characterization, and physiologically-based pharmacokinetic (PBPK) modeling. Results: According to the in vitro results, the selected SMEDDS consisted of 10.0% PEG 300 oleic glycerides, 67.5% PEG 400 caprylic/capric glycerides, and 22.5% polysorbate 80. The use of acid-resistant capsules filled with SV-loaded SMEDDS was found helpful in protecting the drug against early degradation in proximal parts of the GI tract, however, in silico simulations indicated that pH-controlled drug release system that dissolve in the distal parts of the intestine might further improve SV bioavailability (up to 7.20%). Conclusion: The obtained results suggested that combined strategy for the improvement of SV bioavailability should comprise solubility enhancement and delayed drug release. The developed SV-specific PBPK model could potentially be used to assess the influence of formulation factors on drug absorption and disposition when developing SV oral dosage forms.
PB  - Taylor & Francis Ltd, Abingdon
T2  - Drug Development and Industrial Pharmacy
T1  - In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems
VL  - 44
IS  - 5
SP  - 849
EP  - 860
DO  - 10.1080/03639045.2017.1414835
ER  - 
@article{
author = "Cetković, Zora and Cvijić, Sandra and Vasiljević, Dragana",
year = "2018",
abstract = "Objective: The aims of this study were to formulate simvastatin (SV)-loaded self-microemulsifying drug delivery systems (SMEDDS), and explore the potential of these drug delivery systems to improve SV solubility, and also to identify the optimal place in the gastrointestinal (GI) tract for the release of SV using coupled in vitro/in silico approach. Significance: In comparison to other published results, this study considered the extensive pre-systemic clearance of SV, which could significantly decrease its systemic and hepatic bioavailability if SV is delivered into the small intestine. Methods: SV-loaded SMEDDS were formulated using various proportions of oils (PEG 300 oleic glycerides, propylene glycol monocaprylate, propylene glycol monolaurate), surfactant (PEG 400 caprylic/capric glycerides) and cosurfactant (polysorbate 80) and subjected to characterization, and physiologically-based pharmacokinetic (PBPK) modeling. Results: According to the in vitro results, the selected SMEDDS consisted of 10.0% PEG 300 oleic glycerides, 67.5% PEG 400 caprylic/capric glycerides, and 22.5% polysorbate 80. The use of acid-resistant capsules filled with SV-loaded SMEDDS was found helpful in protecting the drug against early degradation in proximal parts of the GI tract, however, in silico simulations indicated that pH-controlled drug release system that dissolve in the distal parts of the intestine might further improve SV bioavailability (up to 7.20%). Conclusion: The obtained results suggested that combined strategy for the improvement of SV bioavailability should comprise solubility enhancement and delayed drug release. The developed SV-specific PBPK model could potentially be used to assess the influence of formulation factors on drug absorption and disposition when developing SV oral dosage forms.",
publisher = "Taylor & Francis Ltd, Abingdon",
journal = "Drug Development and Industrial Pharmacy",
title = "In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems",
volume = "44",
number = "5",
pages = "849-860",
doi = "10.1080/03639045.2017.1414835"
}
Cetković, Z., Cvijić, S.,& Vasiljević, D.. (2018). In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems. in Drug Development and Industrial Pharmacy
Taylor & Francis Ltd, Abingdon., 44(5), 849-860.
https://doi.org/10.1080/03639045.2017.1414835
Cetković Z, Cvijić S, Vasiljević D. In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems. in Drug Development and Industrial Pharmacy. 2018;44(5):849-860.
doi:10.1080/03639045.2017.1414835 .
Cetković, Zora, Cvijić, Sandra, Vasiljević, Dragana, "In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems" in Drug Development and Industrial Pharmacy, 44, no. 5 (2018):849-860,
https://doi.org/10.1080/03639045.2017.1414835 . .
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