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, Ines
Lunter, Dominique
Ranđelović, Danijela

Žugić, Ana R.
Tadić, Vanja M.
Marković, Bojan

Cekić, Nebojša

Živković, Lada

Topalović, Dijana

Potparević, Biljana

Daniels, Rolf
Savić, Snežana

Article (Published version)

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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 Science BV, Amsterdam
Funding / projects:
- Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-34031)
- Federal Republic of Germany
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
PharmacyTY - JOUR AU - Nikolić, Ines AU - Lunter, Dominique AU - Ranđelović, Danijela AU - Žugić, Ana R. AU - Tadić, Vanja M. AU - Marković, Bojan AU - Cekić, Nebojša AU - Živković, Lada AU - Topalović, Dijana AU - Potparević, Biljana AU - Daniels, Rolf AU - Savić, Snežana PY - 2018 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3084 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 Science BV, Amsterdam 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 and Ranđelović, Danijela and Žugić, Ana R. and Tadić, Vanja M. and Marković, Bojan and Cekić, Nebojša and Živković, Lada and Topalović, Dijana and Potparević, Biljana and Daniels, Rolf and Savić, Snežana", 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 Science BV, Amsterdam", 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., Ranđelović, D., Žugić, A. R., Tadić, V. M., Marković, B., Cekić, N., Živković, L., Topalović, D., Potparević, B., Daniels, R.,& Savić, S.. (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 Science BV, Amsterdam., 550(1-2), 333-346. https://doi.org/10.1016/j.ijpharm.2018.08.060
Nikolić I, Lunter D, Ranđelović D, Žugić AR, Tadić VM, Marković B, Cekić N, Živković L, Topalović D, Potparević B, Daniels R, Savić S. 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, Ranđelović, Danijela, Žugić, Ana R., Tadić, Vanja M., Marković, Bojan, Cekić, Nebojša, Živković, Lada, Topalović, Dijana, Potparević, Biljana, Daniels, Rolf, Savić, Snežana, "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 . .