Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: Physicochemical and in vitro peculiarities important for dermal application

被引:29
作者
Nikolic, Ines [1 ]
Lunter, Dominique Jasmin [2 ]
Randjelovic, Danijela [3 ]
Zugic, Ana [4 ]
Tadic, Vanja [4 ]
Markovic, Bojan [5 ]
Cekic, Nebojsa [6 ]
Zivkovic, Lada [7 ]
Topalovic, Dijana [7 ]
Spremo-Potparevic, Biljana [7 ]
Daniels, Rolf [2 ]
Savic, Snezana [1 ]
机构
[1] Univ Belgrade, Fac Pharm, Dept Pharmaceut Technol & Cosmetol, Vojvode Stepe 450, Belgrade 11221, Serbia
[2] Eberhard Karts Univ, Inst Pharmazeut Technol, D-72076 Tubingen, Germany
[3] Univ Belgrade, Dept Microelect Technol, Inst Chem Technol & Met, Belgrade 11000, Serbia
[4] Inst Med Plant Res Dr Josif Pancic, Belgrade 11000, Serbia
[5] Univ Belgrade, Fac Pharm, Dept Pharmaceut Chem, Belgrade 11221, Serbia
[6] Univ Nis, Fac Technol, Leskovac 16000, Serbia
[7] Univ Belgrade, Fac Pharm, Dept Biol & Human Genet, Belgrade 11221, Serbia
关键词
Low-energy nanoemulsions; Spontaneous emulsification; Curcumin; Atomic force microscopy; Antioxidant activity; (Anti)genotoxicity; NANO-EMULSIONS; DRUG-DELIVERY; SPONTANEOUS EMULSIFICATION; ANTIOXIDANT PROPERTIES; CLINICAL-TRIALS; DIABETIC-RATS; STABILITY; CANCER; MECHANISMS; SYSTEMS;
D O I
10.1016/j.ijpharm.2018.08.060
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 < 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.
引用
收藏
页码:333 / 346
页数:14
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