WO2023137532A1

WO2023137532A1 - Nanostructured lipid carrier, use of the nanostructured lipid carrier, photoprotective composition and method for skin photoprotection

Info

Publication number: WO2023137532A1
Application number: PCT/BR2022/050017
Authority: WO
Inventors: Hatylas Felype Zaneti De Azevedo; Margarete MORENO DE ARAUJO; Katherine JASMINE CURO MELO; Samuel VIDAL MUSSI; Mariana SILVA DE OLIVEIRA; Flávia CHIVA CARVALHO
Original assignee: Aché Laboratórios Farmacêuticos S.A.; Laboratórios Ferring Ltda.
Priority date: 2022-01-19
Filing date: 2022-01-19
Publication date: 2023-07-27
Also published as: AR128196A1

Abstract

The present invention relates to a nanostructured lipid carrier based on vegetable sources loaded with organic or inorganic ultraviolet ﬁlters, which acts as booster in photoprotective compositions.

Description

NANOSTRUCTURED LIPID CARRIER, USE OF THE NANOSTRUCTURED LIPID CARRIER, PHOTOPROTECTIVE COMPOSITION AND METHOD FOR SKIN PHOTOPROTECTION

Field of the invention

The present invention relates to a specific nanostructured lipid carrier comprising (i) at least one specific solid natural lipid, (ii) at least one specific liquid natural lipid and (iii) at least one surfactant at particular proportions, which are combined to usefully encapsulate sunscreen filters and boost photoprotection in a sunscreen composition.

Background of the Invention

Sunscreen filters are often used as a primary defense against sun damage. These products undergo stringent safety and efficacy evaluation.

Since excessive ultraviolet (UV) radiation can cause sunburn, photoaging, and skin cancer, care products such as sunscreen usually include a classification for the specific wavelengths they filter. UV classifications include UVA (320-400 nm), UVB (290-320 nm) and UVC (200-280 nm).

Modern sunscreen products provide broad-spectrum UV protection and may contain one or several UV filters. A modern UV filter should be heat and photostable, water resistant, nontoxic, and easy to formulate. Identification of a substance that meets these criteria is as difficult as discovering a new drug; hundreds of new molecules are synthesized and screened before a lead candidate is identified. Therefore, new filter combinations of known molecules have been developed and new strategies to booster efficiency have been searched.

Organic UV filters are a group of compounds designed to absorb UV radiation and hence protect our skin against UV-induced damage. Apart from traditional sunscreens, they can be found in many other categories of personal care products. These include skin care, facial makeup, and lip care products, which are often used simultaneously, and on a regular basis. Organic filters in conventional products, can be absorbed through the skin resulting in systemic exposure with unpredicted eﬀects, so, the encapsulation could decrease the absorption of the filters by keeping them on the surface of the skin. Additionally, the encapsulation could improve the filters stability in the presence of ultraviolet radiation.

Chemical filters protect against UV radiation by absorbing, reflecting, or scattering it. Reflection and scattering are accomplished by inorganic physical UV filters. Absorption, mainly of UVB, is done by organic UV filters, which are known as chemical UV filters. The levels of UV filters in sunscreens typically vary from 0.5% to 10%, although they sometimes reach 25%.

The use of UV filters has increased recently due to growing concern about UV radiation and skin cancer, especially because of ozone depletion. Despite the continuous increase in the use of sunscreen worldwide, there is still a need to optimize sunscreen products in terms of efficiency and user experience.

Dermal absorption is not the only relevant route of exposure to organic UV filters. UV filters can also accumulate in bodies of water, such as benzophenone and chlorine byproducts derivatives that reach noticeable concentrations in rivers, lake water and at lower levels in sea (acting as coral bleaching) due to a higher dilution factor. Furthermore, small amounts of organic UV filters were found in tap, groundwater and swimming pools, suggesting that ingestion could be an additional route of exposure.

Because most UV filters are lipophilic, they tend to bioaccumulate in aquatic environments and food chains originating from them. Confirming bioaccumulation, several studies have shown the presence of UV filters in aquatic organisms, which is a major concern in the environmental and human health fields.

Combining several organic UV filters is a common practice to achieve broad‐spectrum UV protection (UVA and UVB) and the required sun protection factor (SPF) value for a sunscreen formulation using optimizing amounts of each compound. However, it has been noted that the photostability of organic UV filters may decrease when combining several organic filters.

Thus, there is still a need for new strategies to reduce and optimize the use of sunscreens, i.e., new composition providing improvements in efficiency, safety and sensory, reducing their concentration and, consequently, their impacts and costs.

Summary of the Invention

In one aspect, the present invention relates to a nanostructured lipid carrier ( ) comprising (i) at least one solid lipid, (ii) at least one liquid lipid and (iii) at least one surfactant useful as an ultraviolet booster to photoprotective composition.

In a second aspect, the present invention refers to the use of the nanostructured lipid carrier as an ultraviolet filter booster, particularly for the preparation of a photoprotective composition.

In a third aspect, the present invention refers to a photoprotective composition comprising the nanostructured lipid nanocarrier according to the present invention, at least one free ultraviolet filter and acceptable cosmeceutical excipients.

In a fourth aspect, the present invention refers to a method for skin photoprotection comprising applying to the skin a photoprotective composition according to the present invention.

Brief description of figures

illustrates the general structure of a nanostructured lipid carrier according to the present invention.

Figures 2 to 4 show the absorbance spectrum analysis of different raw materials (butters and oils).

shows the absorbance spectrum analysis of a nanostructured lipid carrier (NLC) according to the present invention and an equivalent nanoemulsion (NE), both without sunscreen filters.

shows the absorbance spectrum analysis of a nanostructured lipid carrier (NLC) loading sunscreen filters according to the present invention, an equivalent nanoemulsion (NE) with sunscreen filters and a formulation containing free sunscreen filters (Tinosorb S, Uvinul A plus and Uvinul T150) at the same proportions.

Description of the Invention

It was surprisingly found that the specific compounds according to the preset invention could potentiate the action of organic ultraviolet ﬁlters, demonstrating a synergic effect in terms of SPF increase.

The present invention relates to a nanostructured lipid carrier based on a combination of oil and butter of natural origin comprising:
(i) 6% to 10% of at least one solid lipid selected from refined vegetal butter comprising melting point between 50 and 70°C, palmitic acid between 50 and 70%, and oleic acid between 15 and 30%,
(ii) 2% to 4% of at least one liquid lipid selected from refined vegetal oil comprising high content in polyunsaturated and low content in saturated fat, and
(iii) 2% to 15% of at least one surfactant.

Nanostructured lipid carriers based on the combination of oil and butter of natural origin exhibited a higher absorbance at the UV absorption range than an equivalent nanoemulsion without any sunscreen filter ( ). This higher absorption potential of NLCs compared to nanoemulsions or free sunscreen filters is also seen when organic filters were encapsulated into NLCs ( ).

The (i) solid lipid is selected from the butter of bacuri (gen. platonia), cacau (gen. theobroma), cupuaçu (gen. theobroma), murumuru (gen. astrocaryum), ucuuba (gen virola), tucumã (gen. astrocaryum), karité (gen. butyrospermum) or mixtures thereof, preferably bacuri butter due to its higher absorbance alone or in combination with raspberry oil (Figures 2 and 3).

The nanostructured lipid carrier according to present invention was found to exhibit a photoprotective activity or to potentiate the photoprotective activity of sunscreen filters. In one embodiment, the (ii) liquid lipid contains oleic acid (5-35%), linoleic acid (40-65%), linolenic acid (20-35%), preferably selected from brazil nut oil (gen. bertholletia), hemp seed oil (gen. cannabis), corn oil (gen. zea), cotton seed oil (gen gossypieae), grape seed oil (gen. vitis), peanut oil (gen. arachis), sesame oil, soybean oil (gen. glycine), walnut oil (gen. juglans), sunflower oil (gen. helianthus), raspberry seed oil (gen. rubus) or mixtures thereof, more preferably raspberry seed oil.

The (iii) surfactant is selected from triblock copolymer of polyethylene oxide-polypropylene oxide-polyethylene oxide (poloxamer 188), copolymer of ethylene oxide and propylene oxide blocks (poloxamer 407), steareth (brij), polysorbate 20 (tween 20), polysorbate 40 (tween 40), polysorbate 60 (tween 60), polysorbate 80 (tween 80), sodium lauryl sulfate, polyglycerol oleate (plurol oleique), lauryl glucoside (plantacare® 1200), polyoxyl-35 castor oil (kolliphor® el), polyoxyl 40 hydrogenated castor oil (kolliphor® rh40), lecithin and derivatives thereof, phospholipids and derivatives thereof, sorbitan monostearate (span) and/or C_8-10 mono- and di-glycerides (capmul mcm). In a particular embodiment, the surfactant is selected from polyglycerol oleate (plurol oleique), polysorbate 60 (tween 60) and/or copolymer of ethylene oxide and propylene oxide blocks (poloxamer 407).

The nanostructured lipid carrier according to the present invention has a particle size in a range from about 100 nm to about 300nm, a polydispersion index in a range from about 0.001 to about 0.5, a surface potential in a range from about -50mv to about +30mv, and an encapsulation efficiency greater or equal than 70%.

In a particular embodiment of the present invention, the nanostructured lipid carrier containing sunscreen filters incorporated in the nanoparticle is combined with at least one inorganic or organic ultraviolet filter, called free UV filter, that is not encapsulated in the nanostructured lipid carrier according to the present invention.

The inorganic ultraviolet filter according to the present invention is selected from at least one of titanium dioxide, zinc oxide, colloidal silicon dioxide and derivatives thereof.

The organic ultraviolet filter according to the present invention is selected from camphor benzalkonium methosulfate, terephthalylidene dicamphor sulfonic acid, methoxydibenzoylmethane, benzylidene camphor sulfonic acid, octocrylene, cinoxate, menthyl anthranilate, tea-salicylate phenylbenzimidazole sulfonic acid, ethylhexyl methoxycinnamate, benzophenone–3, benzophenone–4, benzophenone–5, paba, homosalate, polyacrylamidomethyl benzylidene camphor, peg-25 paba, ethylhexyl dimethyl paba, ethylhexyl salicylate, isoamyl p–methoxycinnamate, 4–methyl benzylidene camphor, 3-benzylidene camphor, ethylhexyl triazone, drometrizole trisiloxane, diethylhexyl butamido triazone, methylene bis-benzotriazolyl tetramethylbutylphenol, disodium phenyl dibenzimidazole tetrasulfonate, bis-ethylhexyloxyphenol methoxyphenyl triazine, polysilicone-15, diethylamino hydroxybenzoyl hexyl benzoate, tris-biphenyl triazine, bis -ethylhexylolxyphenol methoxyphenyl triazine, diethylamino hydroxybenzoyl hexyl benzoate, ethylhexyl triazone, avobenzone, octocrylene or mixtures thereof.

In a second embodiment, the present invention refers to the use of the nanostructured lipid carrier as an ultraviolet filter booster, particularly for the preparation of a photoprotective composition.

The photoprotective composition according to the present invention comprises 10% to 30% of a nanostructured lipid nanocarrier based on the total weight of the photoprotective composition; 70% to 90% of a free filter based on the total weight of the photoprotective composition; and acceptable cosmeceutical excipients.

In another embodiment, the present invention refers to a method for skin photoprotection characterized by comprising apply to the skin a photoprotective composition according to the present invention.

The present invention may improve the safety of sunscreen products by increasing the SPF, decreasing the skin penetration of organic ultraviolet filters, and decreasing the concentration of organic ultraviolet filters in a sunscreen formulation. Moreover, the lower concentration of the filters results in lower manufacturing costs while maintaining an appropriate sensory experience for the user.

Examples

Example 1 – Preparation according to the present invention

Quality by design (QbD) approaches were applied to the development of multifunctional nanostructures according to the present invention. The composition according to the present invention was prepared by hot homogenization technique followed by ultra-sonication using a sonication probe. Briefly, oil phase composed by bacuri butter, raspberry seed oil, organic ultraviolet ﬁlters, plurol and polysorbate 60 was heated to 80 °C while the aqueous phase composed by purified water was also heated separately to the same temperature. AP was gently dropped onto the OP under constant agitation, at 8000 rpm, with an Ultra Turrax™ T-25 homogenizer. The formed emulsion was homogenized for 10 minutes by sonication (with a probe and 21% amplitude). The droplets of the hot colloidal emulsion were recrystallized by cooling the emulsion to room temperature to obtain the nanoparticles. The compositions of nanoparticles are described in Table 1.
[Table 1]. Nanoparticles compositions

Components (%)	NLC 1	NE 1	NLC 2
Bacuri butter	6	-	6
Raspberry seed oil	4	15	4
Polisorbate 60 (Tween 60™)	5	5	-
Plurol	5	5	5
Poloxamer 470		-	5
Tinorsob S	2	2	-
Uvinul A	3	3	-
Uvinul T150	1	1	-
Avobenzone	-	-	3
Octocrilene	-	-	2

Example 2 - Characterizations

Particle size analysis and zeta potential analysis

The hydrodynamic diameter of the nanostructured lipid carrier according to the present invention dispersion was determined by unimodal analysis through dynamic light scattering (DLS) and the data was reported as Z-average, evaluated as the intensity. The hydrodynamic diameter, polydispersity index (PdI) and zeta potential of the nanoparticles were determined by dynamic scattering of light and electrophoretic mobility.

Encapsulation efficiency (EE%)

The encapsulation efficiency of organic ultraviolet ﬁlters into nanostructured lipid carrier according to the present invention was determined by measuring the concentration of free organic ultraviolet ﬁlters in the dispersion medium. The loaded nanostructured lipid carrier according to the present invention dispersion was uniformly mixed by gentle shaking with ethanol and then centrifuging for 20 min at 6987 g. The supernatant was filtered using a Millipore membrane. The filtrate was collected, diluted with ethanol and the concentration was measured by HPLC. The HPLC method was the same as described by Souza C, Maia Campos PMBG. Development of a HPLC method for determination of four UV filters in sunscreen and its application to skin penetration studies. Biomed Chromatogr . 2017 Dec;31. or by Bhuva C, Singh R, Sharma A. Analytical method development for simultaneous estimation of oxybenzone, octocrylene, octinoxate and avobenzone in sunscreen by high performance liquid chromatography and its validation. Pharmacophore 2012, Vol. 3 (2), 130-155.

The percentage entrapment eﬃciency (%EE) was calculated using the following equation:
[Math.] Equation

Where Ctotal is the weight of organic ultraviolet added into NLCs and Cfilt is the analyzed weight in the supernatant.

Example 3 – Initial Formulations

Several initial formulations were developed according to the compositions in Table 2. These initial examples faced issues related to large particle size and stability, which required further optimization to reach a formulation with the target profile.
[Table 2]. Initial formulations facing large particle size and stability issues

%	Bacuri Butter	Carnauba wax	Raspberry seed oil	Tween 60	Poloxamer 470	Poloxamer 188	Plurol	Capmul MCM C8	Avobenzone	Octocrylene	Tinorsob S	Uvinul A	Uvinul T150	Issues
F1	6	-	3	5	-	-	5	-	3	2	-	-	-	size > 1000 nm
F2	6	-	4	5	-	-	5	-	3	5	-	-	-	unstable (creaming)
F3	6	-	4	-	10	-	-	-	3	5	-	-	-	size > 1000 nm
F4	6	-	4	-	5	-	5	-	3	5	-	-	-	unstable (creaming)
F5	6	-	4	-	-	10	-	-	3	5	-	-	-	size > 1000 nm
F6	6	-	4	-	-	5	5	-	3	5	-	-	-	precipitated
F7	6	-	4	-	-	5	5	4	3	-	-	-	-	precipitated
F8	-	2	2	3	-	-	1	-	-	-	2	3	1	unstable (creaming)
F9	-	5	5	3	-	-	3	-	-	-	2	3	1	unstable (creaming)
F10	-	2	2	4	-	-	2	-	-	-	2	3	1	unstable (creaming)

Atomic force microscopy (AFM)
Example 4 – Nanostructured lipid carrier (NLC) formulations with target profile

Improvements in the composition of the initial formulations resulted in the NLC1 and NLC2 formulations, which exhibited particle sizes at the nanometric scale, high EE (%) and no stability issues (Table 3). The nanoemulsion 1 (NE1) was also prepared to compare against the NLC formulations.
[Table 3]. Particle Size, PdI, Zeta Potential and EE of the obtained NLC and NE

Characteristics	NLC 1	NE 1	NLC 2
Size (nm)	216 ± 19	234 ± 13	178 ± 4
PdI	0.20 ± 0.20	0.22 ± 1.2	0.19 ± 1.24
Zeta Potential (mV)	- 15 ± 1.8	-	-
EE (%) Univul A	70.0 ± 2.8	-	-
EE (%) Tinorsorb S	97.7 ± 0.12	-	-
EE (%) Univul T150	96.4 ± 0.07	-	-
EE (%) Avobenzone	-	-	84.5 ± 7.2
EE (%) Octocrilene	-	-	92.75 ± 3.8

Size and morphology of nanostructured lipid carriers according to the present invention were determined by AFM. Nanocarrier samples were prepared by depositing dilute particle dispersions on a freshly cleaved mica plate and drying with argon. Images were obtained using a Shimadzu (Scanning Probe Microscope), SPM-9600 model (Kyoto, Japan) equipped with a 100 μm tripod scanner and pyramidal cantilevers with silicon probes (force constant: 10–130 N/m) at a resonance frequency of 204 – 497 kHz. All measurements were performed in intermittent-contact mode at a scan speed of approximately 1 Hz to avoid damage of the sample surface. The average size of NLC1 was 136 nm.

In vitro photoprotective efficacy

Photoprotective efficacy was estimated in vitro by diffuse transmittance measurements in which light scattered at different angles is collected using an integrating sphere (UV-2000S Ultraviolet Transmittance Analyzer, Labsphere, USA) using polymethylmethacrylate (PMMA) plates, model HD6, Helios Cosmetic Science. Samples were weighed and uniformly applied with a glove-coated finger on a 5×5 cm PMMA plate, at a ratio of 1.3 mg/cm2 (Dario, M.F.; Oliveira, F.F.; Marins , D.S.S.; Baby, A.R.; Velasco, M.V.R.; Lobenberg , R.; Bou-Chacra, N.A. Synergistic photoprotective activity of nanocarrier containing oil of Acrocomia aculeata (Jacq.) Lodd . Ex. Martius Arecaceae . Industrial Crops And Products, v. 112, p. 305-312, 2018.). After drying at room temperature for 20 min, protected from light, the analyses were carried out in replicates of three, and nine different points per plate were measured for each sample, from 290 to 400 nm using Labsphere® (de Oliveira et al., 2016). A PMMA plate without sample was used as a reference support.

The samples consisted of a cream base (CB) SPF 22; CB+emulsion1 (emulsion with Tinisorb S, Uvinul T150 and Uvinul A plus free); CB+NLC1 (Tinisorb S, Uvinul T150 and Uvinul A plus encapsulated in nanocarriers). The emulsion and nanostructured lipid carrier according to the present invention were incorporated into the cream base in a concentration of 20% w/w.
[Table 4]. In vitro photoprotective activity

Formulation	SPF calculated by DSM simulator (sunscreen optimizer™) Theoretical SPF	SPF ± SD by Labsphere
CB 80% + 20% emulsion 1	25	17.00 ± 3.56
CB 80% + 20% NLC1 (invention)	25	42.00 ± 0.82

The SPF results demonstrated that the incorporation of sunscreen agents into the nanostructured lipid carrier according to the present invention has altered their overall UV attenuation characteristics (Table 4). Moreover, the limited variability of the SPF value measured for the cream containing the encapsulated UV filter (relative standard deviation, 0.82%) indicated a uniform UV protection and hence a homogeneous distribution of the nanoparticles. The formulation according to the present invention surprisingly showed an SPF ± SD of 42.00 ± 0.82 measured in the Labsphere equipment.
Example 5 – Combination of NLC-loading filters and free chemical filters

To further investigate the SPF increase of incorporating NLC-loaded filters into different formulations, several combinations of NLC-loaded and free filters were tested in terms of SPF and UVA-PF in vitro and in vivo (Table 5). Group I was tested with a prior art product containing an SPF of 30 and UVA-PF of 10. The components of this prior art product are described below: 61.3% water, 12.15% of organic filters [ethylhexyl methoxycinnamate (and) bht, ethylhexyl triazone, diethylamino hydroxybenzoyl hexyl benzoate, bis-ethylhexyloxyphenol methoxyphenyl triazine] and 26.55% of other excipients.
[Table 5]. Evaluation of the combination of free chemical filters + nanoencapsulated filters (NLCs) in vitro and in vivo

Groups		Total amount of sunscreens (%) in the analyzed final formulation	Percentage reduction of the total amount of filters compared to group I	SPF		UVA-PF
Groups				In vitro	In vivo	In vitro	In vivo
I	Emulsion containing free filters at the same proportion of the prior art product	13.5	-	27.7	30	15.7	10
II	Emulsion containing free filters in the same proportion as NLCs	6	-	6.3	NA	7.3	NA
III	NLC (100% Encapsulated Filters)	6	-	5.3	NA	5	NA
IV	Free filters (90%) + Encapsulated filters -NLC (10%)	12.75	5.56	-	35.2 ± 9.5	-	9.3 ± 1.4
V	Free filters (80%) + Encapsulated filters -NLC (20%)	12	11.11	42	31 ± 5.8	13.3	11.1 ± 2
VI	Free filters (80%) + Free filters-group II (20%)	12	11.11	17	23.8 ± 4.1	14	8.4 ± 2.1
VII	Free filters (70%) + Encapsulated filters -NLC (30%)	11.25	16.67	-	25.8 ± 4.9	-	8.7 ± 2.2

In Table 5, NA means “not analyzed”, i.e. the analysis was not carried out due to the results from the in vitro tests. Groups IV to VII were tested with a mixture of free filters + encapsulated filters (NLCs) in different proportions.

The rationale for the inclusion of specific groups in the experiment is detailed below:

Group I and Group II have different total amounts of sunscreen filters and were included to assess emulsions containing either the same proportion of a prior art product (Group 1) or the proportion included in the NLCs;
Group II and III have the same amount of chemical filters. Group III was included to verify the SPF of the formulation containing only encapsulated filters according to the present invention;
Different mixtures varying the proportion between Group I with the nanostructured lipid carrier according to the present invention were tested (Groups IV, V and VII);
Group VI corresponds to a mixture between Group I (80%) and Group II (20%) that was included as a comparator against Group V to verify whether NLC encapsulated filters in Group V increase SPF when combined with free filters.

The analysis of the results included in Table 5 indicated that the combination of NLC-loaded and free filters provides SPF values within the same SPF range of free filters, but with lower amounts of organic filters in the composition:

Comparing Group V with Group VI, an increase in the SPF value was verified, which is due to the synergistic effect between free and encapsulated filters;
Group V maintained the same in vivo SPF value than Group I, but with a smaller amount of chemical filters, demonstrating a surprising synergistic effect with direct impact in the total amount of filter used (cost and safety);
Group IV has a similar in vivo SPF value than Group I but with a smaller amount of chemical filters;

The nanostructured lipid carriers according to the present invention based on vegetable resources had relatively high loading levels and reduced size. Moreover, these NLC can be combined with free organic UV filters as boosters of photoprotection, allowing the reduction of the amounts of sunscreen filters, while providing natural and innovative agents in cosmetics products, with low cost, and biocompatibility.

Claims

A nanostructured lipid carrier characterized by comprising:
(i) At least one solid lipid selected from a refined vegetal butter comprising a melting point between 50 and 70°C, palmitic acid between 50 and 70%, and oleic acid between 15 and 30%,
(ii) At least one liquid lipid selected from a refined vegetal oil comprising high levels of polyunsaturated and low levels of saturated fat, and
(iii) at least one surfactant.
The nanostructured lipid carrier according to claim 1 characterized by (i) the solid lipid selected from the butter of Bacuri (Gen. Platonia), Cacau (Gen. Theobroma), Cupuaçu (Gen. Theobroma), Murumuru (Gen. Astrocaryum), Ucuuba (Gen Virola), Tucumã (Gen. Astrocaryum), Karité (Gen. Butyrospermum) or mixtures thereof.
The nanostructured lipid carrier according to claim 2 characterized by (i) the solid lipid is selected from bacuri butter.
The nanostructured lipid carrier according to claim 1 characterized by (ii) the liquid lipid comprises oleic acid (5-35%), linoleic acid (40-65%), linolenic acid (20-35%).
The nanostructured lipid carrier according to claim 4 characterized by (ii) the liquid lipid is selected from Brazil nut oil (Gen. Bertholletia), Hemp seed oil (gen. Cannabis), corn oil (Gen. Zea), cotton seed oil (Gen Gossypieae), grape seed oil (gen. Vitis), peanut oil (Gen. Arachis), sesame oil, soybean oil (Gen. Glycine), walnut oil (Gen. Juglans), sunflower oil (Gen. Helianthus), raspberry seed oil (gen. Rubus) or mixtures thereof.
The nanostructured lipid carrier according to claim 5 characterized by (ii) the liquid lipid is selected from raspberry seed oil.
The nanostructured lipid carrier according to claim 1 characterized by the vegetable oil has photoprotective activity or potentiates photoprotective activity, or combinations thereof.
The nanostructured lipid carrier according to claim 1 characterized by all vegetable sources have anti-inflammatory, antioxidant and moisturizing activity or potentiates anti-inflammatory, antioxidant and moisturizing activity, or combinations thereof.
The nanostructured lipid carrier according to claim 1 characterized by the (iii) surfactant is selected from triblock copolymer of polyethylene oxide-polypropylene oxide-polyethylene oxide, copolymer of ethylene oxide and propylene oxide blocks, steareth, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, sodium lauryl sulfate, polyglycerol oleate, lauryl glucoside, polyoxyl-35 castor oil, polyoxyl 40 hydrogenated castor oil, lecithin and derivatives thereof, phospholipids and derivatives thereof, sorbitan monostearate and/or C_8-10 mono- and di-glycerides.
The nanostructured lipid carrier according to claim 9 characterized by (iii) the surfactant is selected from polyglycerol oleate, polysorbate 60 and/or copolymer of ethylene oxide and propylene oxide blocks.
The nanostructured lipid carrier according to any of claims 1 to 10 characterized by comprising:
(i) 6% to 10% of refined vegetal butter;
(ii) 2% to 4% of refined vegetal oil;
(iii) 2% to 15% of surfactant.
The nanostructured lipid carrier according to any of claims 1 to 11, characterized by the carrier has a particle size in a range from about 100 nm to about 300nm.
The nanostructured lipid carrier according to any of claims 1 to 11, characterized by the carrier has a polydispersion index in a range from about 0.001 to about 0.5.
The nanostructured lipid carrier according to any of claims 1 to 11, characterized by the carrier has a surface potential in a range from about -50mV to about +30mV.
The nanostructured lipid carrier according to any of claims 1 to 14, characterized by the carrier has an encapsulation efficiency greater or equal than 70%.
The nanostructured lipid carrier according to any of claims 1 to 15 characterized by further comprising at least one inorganic or organic ultraviolet filter.
The nanostructured lipid carrier according to claim 16 characterized by the inorganic ultraviolet filter is selected from at least one of titanium dioxide, zinc oxide, colloidal silicon dioxide and derivatives thereof.
The nanostructured lipid carrier according to claim 16 characterized by the organic ultraviolet filter is selected from camphor benzalkonium methosulfate, terephthalylidene dicamphor sulfonic acid, methoxydibenzoylmethane, benzylidene camphor sulfonic acid, octocrylene, cinoxate, menthyl anthranilate, tea-salicylate phenylbenzimidazole sulfonic acid, ethylhexyl methoxycinnamate, benzophenone–3, benzophenone–4, benzophenone–5, paba, homosalate, polyacrylamidomethyl benzylidene camphor, peg-25 paba, ethylhexyl dimethyl paba, ethylhexyl salicylate, isoamyl p–methoxycinnamate, 4–methyl benzylidene camphor, 3-benzylidene camphor, ethylhexyl triazone, drometrizole trisiloxane, diethylhexyl butamido triazone, methylene bis-benzotriazolyl tetramethylbutylphenol, disodium phenyl dibenzimidazole tetrasulfonate, bis-ethylhexyloxyphenol methoxyphenyl triazine, polysilicone-15, diethylamino hydroxybenzoyl hexyl benzoate, tris-biphenyl triazine, bis -ethylhexylolxyphenol methoxyphenyl triazine, diethylamino hydroxybenzoyl hexyl benzoate, ethylhexyl triazone, avobenzone, octocrylene or mixtures thereof.
Use of the nanostructured lipid carrier as defined in one of claims 1 to 18 characterized by being an ultraviolet filter booster.
The use of the nanostructured lipid carrier as defined in one of claims 1 to 18 characterized by being for the preparation of a photoprotective composition.
A photoprotective composition characterized by comprising:
(i) nanostructured lipid nanocarrier as defined in any of claims 1 to 18;
(ii) at least one free ultraviolet filter;
(iii) acceptable cosmeceutical excipients.
The photoprotective composition, according to claim 21, characterized by comprising:
(i) 10% to 30% of a nanostructured lipid nanocarrier as defined in one of claims 1 to 18 based on the total weight of the photoprotective composition;
(ii) 70% to 90% of a free filter based on the total weight of the photoprotective composition;
(iii) acceptable cosmeceutical excipients.
The photoprotective composition, according to claim 23, characterized by the free ultraviolet filter is selected from inorganic or organic ultraviolet filters.
The photoprotective composition, according to claim 25, characterized by the inorganic ultraviolet filter is selected from at least one of titanium dioxide, zinc oxide, colloidal silicon dioxide and derivatives thereof.
The photoprotective composition, according to claim 25, characterized by the organic ultraviolet filter is selected from camphor benzalkonium methosulfate, terephthalylidene dicamphor sulfonic acid, methoxydibenzoylmethane, benzylidene camphor sulfonic acid, octocrylene, cinoxate, menthyl anthranilate, tea-salicylate phenylbenzimidazole sulfonic acid, ethylhexyl methoxycinnamate, benzophenone–3, benzophenone–4, benzophenone–5, paba, homosalate, polyacrylamidomethyl benzylidene camphor, peg-25 paba, ethylhexyl dimethyl paba, ethylhexyl salicylate, isoamyl p–methoxycinnamate, 4–methyl benzylidene camphor, 3-benzylidene camphor, ethylhexyl triazone, drometrizole trisiloxane, diethylhexyl butamido triazone, methylene bis-benzotriazolyl tetramethylbutylphenol, disodium phenyl dibenzimidazole tetrasulfonate, bis-ethylhexyloxyphenol methoxyphenyl triazine, polysilicone-15, diethylamino hydroxybenzoyl hexyl benzoate, tris-biphenyl triazine, bis -ethylhexylolxyphenol methoxyphenyl triazine, diethylamino hydroxybenzoyl hexyl benzoate, ethylhexyl triazone, avobenzone, octocrylene or mixtures thereof.
A method for skin photoprotection characterized by comprising apply to the skin a photoprotective composition according to any of claims 21 to 25.