Senem Suner 1, Orhan Yazici 2, Fereshte Rezaie 3, Elnaz Maleki Dizaj 4,5,*
1Department of Nanotechnology and Advanced Materials, Mersin University, Mersin, Turkey
2 ILKE Compony, Istanbul, Turkey
3 Faculty of Dentistry, Tabriz University of Medical Sciences, Tabriz, Iran
4 East Azerbaijan Blood Transfusion Organization, Tabriz, Iran
5 Islamic Azad University, Bonab branch, Bonab, Iran
Corresponding Author:
Elnaz Maleki Dizaj, East Azerbaijan Blood Transfusion Organization, Tabriz, Iran, Tel: +98 (41) 33353162, E-mail: emd1990biologist@yahoo.com
Abstract
The antioxidative possessions of vitamin E have introduced it as active material in many pharmaceutical and cosmetics. However, some problems like low lipophilicity, chemical instability and, poor skin diffusion lead to its low efficiency. Many efforts have been performed to use it in different drug delivery structures like lipid-based systems. In this study, we prepared vitamin E-loaded nanostructured lipid carriers (NLCs) by the hot melt homogenization technique. The results showed that vitamin E loaded NLCs possessed suitable features like high entrapment efficiency percent (EE%), small size, and narrow size distribution. We proposed that it can be used in pharmaceutical and cosmetic fields in the near future.
Keywords: Nanostructured lipid carriers, Vitamin E, Drug delivery
Introduction
Nano drug delivery systems are novel valuable aspects in pharmaceutics, cosmetics and, food areas. Delivery systems can mainly be categorized into two classes: polymer- and lipid-based structures. Nanostructure lipid carriers (NLCs) have recently more increasing attention for delivery of dermal and transdermal in biomedical studies [1-4].
The protection of the active ingredient, controlled release manner for the loaded drug as well as the physical uniformity of the colloidal system are some benefits of lipid carriers [5-7]. Furthermore, biocompatibility, as well as scalability, are other main aspects of these materials. Lipid nano-formulations specify numerous promising benefits including hydration of skin, smoothness, and ability to improve penetration of drugs in the stratum corneum. Then, they seem an appropriate choice for the cosmetic products that including fatty acids and polypeptides. Due to the outstanding properties, the NLCs are widely used for appropriate dermal and cosmetic crops [2, 8].
The antioxidative and photoprotective possessions of vitamin E have converted it to an active material in many fields. But, some issues like low lipophilicity, chemical instability, and low skin penetration lead to its low effectiveness [9, 10]. So, many efforts have been done to use it in different drug delivery classifications like lipid-based systems. In this study, we used NLCs to formulate vitamin E to improve its effectiveness as a cosmetically important material.
Materials and methods
Vitamin E was purchased from Tabriz drug stores. Poloxamer® 407 and Miglyol® 812 were attained from Sigma-Aldrich Company (USA). Glyceryl palmitostearate (Precirol® ATO-5) was purchased from Gattefossé Company (France).
Preparation of vitamin E loaded NLCs
Vitamin E-loaded NLCs were prepared by the hot melting homogenization technique [2]. Briefly, 200 mg vitamin E was dissolved in 800 mg melted Precirol® at about 50°C. Afterward, Poloxamer®’ solution was prepared in water and added dropwise into the oily solution using a homogenizer at 18000 rpm (DIAX 900 homogenizer, Heidolph, Germany) and 50°C. In the final step, the formulation was permitted to cool down at room temperature. Noticeably, in the blank NLCs Miglyol was used instead of vitamin E.
Characterization of vitamin E loaded NLCs
Size distribution
Particle size and polydispersity index (PDI) of NLCs was measured via the laser diffraction procedure (SALD 2101, Shimadzu, Japan). The volume mean diameter (VMD) was measured for the mean diameter of particles
Surface charge of NLCs
The surface charge (zeta potential (ZP)) of NLCs with and without vitamin E were measured using dynamic light scattering (Nano ZS90, Malvern). To this end, the formulations were diluted by double-distilled water before measurement.
Entrapment of vitamin E in NLCs
The entrapment of vitamin E in NLCs was studied via an ultracentrifugation technique by separating the loaded vitamin E from the free form. The formulations were precipitated by a centrifuge at 30,000 × g for 20 min. The vitamin E in the supernatant and the encapsulated vitamin E in the precipitate were analyzed by high-performance liquid chromatography to determine the entrapment efficiency percentage (EE%).
Scanning electron microscopy (SEM)
NLCs were further tested by a scanning electron microscope (MIRA3, TESCAN instrument, Czech Republic) from the morphological point of view. Samples were straddling on a metal stub using a double-sided adhesive tape and then were coated with gold under vacuum in an argon atmosphere.
Results and discussion
Preparation of vitamin E loaded NLCs
The obtained data for the formulated NLCs with and without vitamin E entrapment are summarized in Table 1. The SEM related to the prepared NLCs is also given in Figure 1.
Table 1. The size data for the formulated NLCs with and without vitamin E entrapment
| Size (nm) | ||||||||
| NMD | VMD | D90% | D50% | D10% | PDI | ZP | EE% | |
| Vitamin E-loaded NLCs | 20± 4 | 448± 11 | 1119± 41 | 430± 10 | 139± 7 | 0.5 | 12 mV | 86.6± 7 |
| Blank NLCs | 75± 3 | 189± 21 | 276± 5 | 179± 8 | 101± 9 | 0.4 | 10 mV | – |
NMD: number mean diameter, VMD: volume mean diameter, D10%, D50% and D90% show percentage of particles having 10, 50 and 90 % of the diameter lower than or equal to the given values based on volume diameter.
Figure 1. The SEM related to the prepared vitamin E loaded NLCs.
The mean diameter for NLCs without the vitamin E was 189 nm (PDI: 0.50), and that of NLCs containing vitamin E was 448 nm (PDI: 0.41). Based on the obtained data, both systems exposed stable unimodal size distribution with PDI of ≤0.60, which established a narrow size distribution model [1, 11]. Positively charged nanoparticles were achieved (10 mV) for NLCs without vitamin E. The addition of vitamin E produced a little greater ZP that may indicate its efficient entrapment into NLCs. The result exposed that EE% of vitamin E in NLCs was 86.6 ± 7 %.
Lipid-based particles with nanometric size provide close contact with the stratum corneum and, so, can increase the drug diffusion into the skin [2]. Our data exposed that the prepared vitamin E loaded NLCs showed proper size range for deep skin penetration that has also report by Patzelt et al. (643 nm, 470 nm, 300 nm, and 122 nm) resulted in a notable decrease in particle penetration depth [12].
Conclusion
Vitamin E loaded NLCs were prepared with suitable features (high EE%, small size, and narrow size distribution). We proposed that it can be open the novel way for its different applications in pharmaceutical and cosmetically fields in the near future.
Acknowledgment
The authors state that there are no financial sources for the current study.
Conflict of interests
The authors have no conflict of interest.
References
HOW TO CITE THIS ARTICLE;
Suner, S., Yazici, O., Rezaie, F., & Maleki Dizaj, E. (2019). New synthesized nanostructured lipid carriers (NLCs) for the delivery of vitamin E: production and physicochemical characterization. Journal of Advanced Chemical and Pharmaceutical Materials (JACPM), 2(1), 85-88. Retrieved from http://advchempharm.ir/journal/index.php/JACPM/article/view/79
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