Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: Physicochemical and in vitro peculiarities important for dermal application
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2018
Authors
Nikolić, InesLunter, Dominique Jasmin
Randjelović, Danijela
Žugić, Ana
Tadić, Vanja
Marković, Bojan D.
Cekic, Nebojsa
Živković, Lada
Topalovic, Dijana
Spremo-Potparević, Biljana
Daniels, Rolf
Savić, Snežana D.
Article (Published version)
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Show full item recordAbstract
The objective of this work was to investigate and profoundly characterize low-energy nanoemulsions as multifunctional carriers, with slight reference to dermal administration. An evidence-based approach was offered for deepening the knowledge on their formation via spontaneous emulsification. Curcumin, a compound of natural origin, potentially powerful therapeutic, was chosen as a model API. Due to curcumin's demanding properties (instability, poor solubility, low permeability), its potentials remain unreached. Low-energy nanoemulsions were considered carriers capable of overcoming imposed obstacles. Formulation consisting of Polysorbate 80 and soybean lecithin as stabilizers (9:1, 10%), medium-chain triglycerides as the oil phase (10%) and ultrapure water was selected for curcumin incorporation in 3 different concentrations (1, 2 and 3 mg/mL). Physicochemical stability was demonstrated during 3 months of monitoring (mean droplet size: 111.3-146.8 nm; PDI LT 0.2; pH: 4.73-5.73). Curc...umin's release from developed vehicles followed Higuchi's kinetics. DPPH (IC50 = 0.1187 mg/ mL) and FRAP (1.19 +/- 0.02 mmol/g) assays confirmed that curcumin acts as a potent antioxidant through different mechanisms, with no alterations after incorporation in the formulation. High biocompatibility in line with antigenotoxic activity of curcumin-loaded formulations (protective and reparative) was estimated through Comet assay. A multidisciplinary approach is needed to fully characterize developed systems, directing them to more concrete application possibilities.
Keywords:
Low-energy nanoemulsions / Spontaneous emulsification / Curcumin / Atomic force microscopy / Antioxidant activity / (Anti)genotoxicitySource:
International Journal of Pharmaceutics, 2018, 550, 1-2, 333-346Publisher:
- Elsevier
Funding / projects:
- Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-MESTD-Technological Development (TD or TR)-34031)
- Republic of Serbia
- Federal Republic of Germany
- Cell Cycle Aberrations and the Impact of Oxidative Stress in Neurodegenerative Processes and Malignant Transformation of the Cell (RS-MESTD-Basic Research (BR or ON)-173034)
Note:
- The peer-reviewed version: https://cer.ihtm.bg.ac.rs/handle/123456789/3719
DOI: 10.1016/j.ijpharm.2018.08.060
ISSN: 0378-5173
PubMed: 30179702
WoS: 000445147000033
Scopus: 2-s2.0-85052734341
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Institution/Community
IHTMTY - JOUR AU - Nikolić, Ines AU - Lunter, Dominique Jasmin AU - Randjelović, Danijela AU - Žugić, Ana AU - Tadić, Vanja AU - Marković, Bojan D. AU - Cekic, Nebojsa AU - Živković, Lada AU - Topalovic, Dijana AU - Spremo-Potparević, Biljana AU - Daniels, Rolf AU - Savić, Snežana D. PY - 2018 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/2425 AB - The objective of this work was to investigate and profoundly characterize low-energy nanoemulsions as multifunctional carriers, with slight reference to dermal administration. An evidence-based approach was offered for deepening the knowledge on their formation via spontaneous emulsification. Curcumin, a compound of natural origin, potentially powerful therapeutic, was chosen as a model API. Due to curcumin's demanding properties (instability, poor solubility, low permeability), its potentials remain unreached. Low-energy nanoemulsions were considered carriers capable of overcoming imposed obstacles. Formulation consisting of Polysorbate 80 and soybean lecithin as stabilizers (9:1, 10%), medium-chain triglycerides as the oil phase (10%) and ultrapure water was selected for curcumin incorporation in 3 different concentrations (1, 2 and 3 mg/mL). Physicochemical stability was demonstrated during 3 months of monitoring (mean droplet size: 111.3-146.8 nm; PDI LT 0.2; pH: 4.73-5.73). Curcumin's release from developed vehicles followed Higuchi's kinetics. DPPH (IC50 = 0.1187 mg/ mL) and FRAP (1.19 +/- 0.02 mmol/g) assays confirmed that curcumin acts as a potent antioxidant through different mechanisms, with no alterations after incorporation in the formulation. High biocompatibility in line with antigenotoxic activity of curcumin-loaded formulations (protective and reparative) was estimated through Comet assay. A multidisciplinary approach is needed to fully characterize developed systems, directing them to more concrete application possibilities. PB - Elsevier T2 - International Journal of Pharmaceutics T1 - Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: Physicochemical and in vitro peculiarities important for dermal application VL - 550 IS - 1-2 SP - 333 EP - 346 DO - 10.1016/j.ijpharm.2018.08.060 ER -
@article{ author = "Nikolić, Ines and Lunter, Dominique Jasmin and Randjelović, Danijela and Žugić, Ana and Tadić, Vanja and Marković, Bojan D. and Cekic, Nebojsa and Živković, Lada and Topalovic, Dijana and Spremo-Potparević, Biljana and Daniels, Rolf and Savić, Snežana D.", year = "2018", abstract = "The objective of this work was to investigate and profoundly characterize low-energy nanoemulsions as multifunctional carriers, with slight reference to dermal administration. An evidence-based approach was offered for deepening the knowledge on their formation via spontaneous emulsification. Curcumin, a compound of natural origin, potentially powerful therapeutic, was chosen as a model API. Due to curcumin's demanding properties (instability, poor solubility, low permeability), its potentials remain unreached. Low-energy nanoemulsions were considered carriers capable of overcoming imposed obstacles. Formulation consisting of Polysorbate 80 and soybean lecithin as stabilizers (9:1, 10%), medium-chain triglycerides as the oil phase (10%) and ultrapure water was selected for curcumin incorporation in 3 different concentrations (1, 2 and 3 mg/mL). Physicochemical stability was demonstrated during 3 months of monitoring (mean droplet size: 111.3-146.8 nm; PDI LT 0.2; pH: 4.73-5.73). Curcumin's release from developed vehicles followed Higuchi's kinetics. DPPH (IC50 = 0.1187 mg/ mL) and FRAP (1.19 +/- 0.02 mmol/g) assays confirmed that curcumin acts as a potent antioxidant through different mechanisms, with no alterations after incorporation in the formulation. High biocompatibility in line with antigenotoxic activity of curcumin-loaded formulations (protective and reparative) was estimated through Comet assay. A multidisciplinary approach is needed to fully characterize developed systems, directing them to more concrete application possibilities.", publisher = "Elsevier", journal = "International Journal of Pharmaceutics", title = "Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: Physicochemical and in vitro peculiarities important for dermal application", volume = "550", number = "1-2", pages = "333-346", doi = "10.1016/j.ijpharm.2018.08.060" }
Nikolić, I., Lunter, D. J., Randjelović, D., Žugić, A., Tadić, V., Marković, B. D., Cekic, N., Živković, L., Topalovic, D., Spremo-Potparević, B., Daniels, R.,& Savić, S. D.. (2018). Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: Physicochemical and in vitro peculiarities important for dermal application. in International Journal of Pharmaceutics Elsevier., 550(1-2), 333-346. https://doi.org/10.1016/j.ijpharm.2018.08.060
Nikolić I, Lunter DJ, Randjelović D, Žugić A, Tadić V, Marković BD, Cekic N, Živković L, Topalovic D, Spremo-Potparević B, Daniels R, Savić SD. Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: Physicochemical and in vitro peculiarities important for dermal application. in International Journal of Pharmaceutics. 2018;550(1-2):333-346. doi:10.1016/j.ijpharm.2018.08.060 .
Nikolić, Ines, Lunter, Dominique Jasmin, Randjelović, Danijela, Žugić, Ana, Tadić, Vanja, Marković, Bojan D., Cekic, Nebojsa, Živković, Lada, Topalovic, Dijana, Spremo-Potparević, Biljana, Daniels, Rolf, Savić, Snežana D., "Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: Physicochemical and in vitro peculiarities important for dermal application" in International Journal of Pharmaceutics, 550, no. 1-2 (2018):333-346, https://doi.org/10.1016/j.ijpharm.2018.08.060 . .