Evaluation of PEGylation efficacy of curcumin-loaded nanoemulsions using complementary methods to assess protein interactions and physicochemical properties
Само за регистроване кориснике
2024
Аутори
Đoković, Jelena![](/themes/MirageFarFaR/images/orcid.png)
Demisli, Sortiria
Savić, Sanela M.
Savić, Saša R.
![](/themes/MirageFarFaR/images/orcid.png)
Randjelović, Danijela V.
Marković, Bojan
![](/themes/MirageFarFaR/images/orcid.png)
Pantelić, Ivana
![](/themes/MirageFarFaR/images/orcid.png)
Mitrović, Jelena
![](/themes/MirageFarFaR/images/orcid.png)
Stanković, Tijana
![](/themes/MirageFarFaR/images/orcid.png)
Papadimitrou, Vassiliki
Xenakis, Aristotelis
![](/themes/MirageFarFaR/images/orcid.png)
Savić, Snežana
![](/themes/MirageFarFaR/images/orcid.png)
Чланак у часопису (Објављена верзија)
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Метаподаци
Приказ свих података о документуАпстракт
Nanoemulsions (NEs) are frequently used in the food, cosmetics and pharmaceutical industries to deliver nutraceuticals, pharmaceutical or cosmetic active ingredients. When administering NEs parenterally, various stabilisers are added to prevent rapid plasma clearance and to successfully deliver the active ingredient to the target site. For this purpose, PEGylation is often used to prolong the circulation time of the droplets. However, the problem is to determine the optimal concentration of the PEGylating agent – the PEGylation efficacy – that ensures adequate surface protection. This is a particular challenge when the active ingredient is incorporated into the stabilising layer, where any changes could disrupt the stability of the droplet. For this reason, we aimed to determine the optimal concentration of PEG2000-DSPE for surface protection of curcumin-loaded NEs for parenteral administration using electron paramagnetic resonance (EPR) spectroscopy. NEs were prepared using the high p...ressure homogenisation technique with 0.1 %, 0.3 % or 0.6 % of the PEGylated phospholipid. A droplet size of approximately 100 nm and polydispersity index below 0.25 indicated suitability for parenteral application. EPR analysis showed that PEG2000-DSPE had a stabilising effect on selected NEs, which was most pronounced in the part of the stabilising layer closest to the aqueous phase. To confirm these results, protein interaction studies were carried out using dynamic light scattering, UV–Vis spectroscopy, atomic force microscopy and release studies from protein-enriched media – bovine serum albumin (BSA) or foetal bovine serum (FBS) in phosphate-buffered saline. These analyses confirmed that the addition of PEG2000-DSPE reduced protein binding to the droplets as a function of concentration, with 0.3 % providing the best protection for the droplets. Our conclusions from the EPR spectroscopy study demonstrate the usefulness of EPR in determining the optimal concentrations of PEGylating agents for surface coverage and its usefulness in the formulation development phase.
Кључне речи:
Curcumin / Bovine serum albumin / EPR spectroscopy / Foetal bovine serum / Nanoemulsion protein interactions / PEGylated nanoemulsions / PEGylation efficacyИзвор:
Journal of Molecular Liquids, 2024, 404Издавач:
- Elsevier B.V.
Финансирање / пројекти:
- NanoCellEmoCog - Neuroimmune aspects of mood, anxiety and cognitive effects of leads/drug candidates acting at GABAA and/or sigma-2 receptors: In vitro/in vivo delineation by nano- and hiPSC-based platform (RS-ScienceFundRS-Ideje-7749108)
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200161 (Универзитет у Београду, Фармацеутски факултет) (RS-MESTD-inst-2020-200161)
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200026 (Универзитет у Београду, Институт за хемију, технологију и металургију - ИХТМ) (RS-MESTD-inst-2020-200026)
Институција/група
PharmacyTY - JOUR AU - Đoković, Jelena AU - Demisli, Sortiria AU - Savić, Sanela M. AU - Savić, Saša R. AU - Randjelović, Danijela V. AU - Marković, Bojan AU - Pantelić, Ivana AU - Mitrović, Jelena AU - Stanković, Tijana AU - Papadimitrou, Vassiliki AU - Xenakis, Aristotelis AU - Savić, Snežana PY - 2024 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/5651 AB - Nanoemulsions (NEs) are frequently used in the food, cosmetics and pharmaceutical industries to deliver nutraceuticals, pharmaceutical or cosmetic active ingredients. When administering NEs parenterally, various stabilisers are added to prevent rapid plasma clearance and to successfully deliver the active ingredient to the target site. For this purpose, PEGylation is often used to prolong the circulation time of the droplets. However, the problem is to determine the optimal concentration of the PEGylating agent – the PEGylation efficacy – that ensures adequate surface protection. This is a particular challenge when the active ingredient is incorporated into the stabilising layer, where any changes could disrupt the stability of the droplet. For this reason, we aimed to determine the optimal concentration of PEG2000-DSPE for surface protection of curcumin-loaded NEs for parenteral administration using electron paramagnetic resonance (EPR) spectroscopy. NEs were prepared using the high pressure homogenisation technique with 0.1 %, 0.3 % or 0.6 % of the PEGylated phospholipid. A droplet size of approximately 100 nm and polydispersity index below 0.25 indicated suitability for parenteral application. EPR analysis showed that PEG2000-DSPE had a stabilising effect on selected NEs, which was most pronounced in the part of the stabilising layer closest to the aqueous phase. To confirm these results, protein interaction studies were carried out using dynamic light scattering, UV–Vis spectroscopy, atomic force microscopy and release studies from protein-enriched media – bovine serum albumin (BSA) or foetal bovine serum (FBS) in phosphate-buffered saline. These analyses confirmed that the addition of PEG2000-DSPE reduced protein binding to the droplets as a function of concentration, with 0.3 % providing the best protection for the droplets. Our conclusions from the EPR spectroscopy study demonstrate the usefulness of EPR in determining the optimal concentrations of PEGylating agents for surface coverage and its usefulness in the formulation development phase. PB - Elsevier B.V. T2 - Journal of Molecular Liquids T1 - Evaluation of PEGylation efficacy of curcumin-loaded nanoemulsions using complementary methods to assess protein interactions and physicochemical properties VL - 404 DO - 10.1016/j.molliq.2024.124888 ER -
@article{ author = "Đoković, Jelena and Demisli, Sortiria and Savić, Sanela M. and Savić, Saša R. and Randjelović, Danijela V. and Marković, Bojan and Pantelić, Ivana and Mitrović, Jelena and Stanković, Tijana and Papadimitrou, Vassiliki and Xenakis, Aristotelis and Savić, Snežana", year = "2024", abstract = "Nanoemulsions (NEs) are frequently used in the food, cosmetics and pharmaceutical industries to deliver nutraceuticals, pharmaceutical or cosmetic active ingredients. When administering NEs parenterally, various stabilisers are added to prevent rapid plasma clearance and to successfully deliver the active ingredient to the target site. For this purpose, PEGylation is often used to prolong the circulation time of the droplets. However, the problem is to determine the optimal concentration of the PEGylating agent – the PEGylation efficacy – that ensures adequate surface protection. This is a particular challenge when the active ingredient is incorporated into the stabilising layer, where any changes could disrupt the stability of the droplet. For this reason, we aimed to determine the optimal concentration of PEG2000-DSPE for surface protection of curcumin-loaded NEs for parenteral administration using electron paramagnetic resonance (EPR) spectroscopy. NEs were prepared using the high pressure homogenisation technique with 0.1 %, 0.3 % or 0.6 % of the PEGylated phospholipid. A droplet size of approximately 100 nm and polydispersity index below 0.25 indicated suitability for parenteral application. EPR analysis showed that PEG2000-DSPE had a stabilising effect on selected NEs, which was most pronounced in the part of the stabilising layer closest to the aqueous phase. To confirm these results, protein interaction studies were carried out using dynamic light scattering, UV–Vis spectroscopy, atomic force microscopy and release studies from protein-enriched media – bovine serum albumin (BSA) or foetal bovine serum (FBS) in phosphate-buffered saline. These analyses confirmed that the addition of PEG2000-DSPE reduced protein binding to the droplets as a function of concentration, with 0.3 % providing the best protection for the droplets. Our conclusions from the EPR spectroscopy study demonstrate the usefulness of EPR in determining the optimal concentrations of PEGylating agents for surface coverage and its usefulness in the formulation development phase.", publisher = "Elsevier B.V.", journal = "Journal of Molecular Liquids", title = "Evaluation of PEGylation efficacy of curcumin-loaded nanoemulsions using complementary methods to assess protein interactions and physicochemical properties", volume = "404", doi = "10.1016/j.molliq.2024.124888" }
Đoković, J., Demisli, S., Savić, S. M., Savić, S. R., Randjelović, D. V., Marković, B., Pantelić, I., Mitrović, J., Stanković, T., Papadimitrou, V., Xenakis, A.,& Savić, S.. (2024). Evaluation of PEGylation efficacy of curcumin-loaded nanoemulsions using complementary methods to assess protein interactions and physicochemical properties. in Journal of Molecular Liquids Elsevier B.V.., 404. https://doi.org/10.1016/j.molliq.2024.124888
Đoković J, Demisli S, Savić SM, Savić SR, Randjelović DV, Marković B, Pantelić I, Mitrović J, Stanković T, Papadimitrou V, Xenakis A, Savić S. Evaluation of PEGylation efficacy of curcumin-loaded nanoemulsions using complementary methods to assess protein interactions and physicochemical properties. in Journal of Molecular Liquids. 2024;404. doi:10.1016/j.molliq.2024.124888 .
Đoković, Jelena, Demisli, Sortiria, Savić, Sanela M., Savić, Saša R., Randjelović, Danijela V., Marković, Bojan, Pantelić, Ivana, Mitrović, Jelena, Stanković, Tijana, Papadimitrou, Vassiliki, Xenakis, Aristotelis, Savić, Snežana, "Evaluation of PEGylation efficacy of curcumin-loaded nanoemulsions using complementary methods to assess protein interactions and physicochemical properties" in Journal of Molecular Liquids, 404 (2024), https://doi.org/10.1016/j.molliq.2024.124888 . .