The effect of polysorbate 20 and polysorbate 80 on the solubility of quercetin.

Background: Quercetin acts as an antioxidant, anti-inflammatory, wound healing, and anti-aging so quercetin can be used as a topical preparation. However, it has low solubility in water at 0.01 mg/ml at 25oC. Increasing the solubility of quercetin in water was done by the addition of surfactants. Objective: This study compared the solubility of quercetin in Polysorbate 20 (P20) and Polysorbate 80 (P80) in a citrate buffer medium pH 4.5±0.2. Methods: The surfactants Polysorbate 80 and Polysorbate 20 differ in their alkyl chain length. Polysorbate 80 has an alkyl chain length of 18, while Polysorbate 20 has an alkyl chain length of 12. The concentrations of surfactant are above, below, and at the critical micelle concentration (CMC) values. The concentrations of quercetin were determined at the maximum wavelength by spectrophotometric method. Results: The results of the quercetin solubility test without surfactant were 3.89±0.59 mg/L. The results of the quercetin solubility test by adding Polysorbate 20 at a concentration of 42.0 ppm; 57.5 ppm; and 73.0 ppm were 3.62±0.72, 4.04±0.23 and 8.35±1.97 mg/L, respectively. While the solubility of quercetin by adding Polysorbate 80 at a concentration of 4.0 ppm, 11.5 ppm, and 19.0 ppm was 11.15±0.72, 11.37±1.23 and 14.17±1.96 mg/L, respectively. The solubility of quercetin is greater after the addition of surfactant Polysorbate 20 only at the concentration above the CMC value and the solubility of quercetin is greater with the addition of surfactant Polysorbate 80 at all concentrations. Surfactant Polysorbate 20 increases the solubility of quercetin in citrate buffer pH 4.5±0.2 only at concentrations above the CMC value of 2.14 times. Polysorbate 80 can increase the solubility of quercetin in citrate buffer pH 4.5±0.2 at concentrations below, at, and above CMC by 2.87, 2.92, and 3.63 times, respectively. Conclusion: Polysorbate 80 can increase the solubility of quercetin in citrate buffer pH 4.5±0.2 higher than Polysorbate 20.

The activity of candlenut oil in the nanostructured lipid carrier system on hair growth in rats.

Background: Candlenut oil (Aleurites moluccana L. Willd), which is also called Aleurites moluccana Seed (AMS) oil, is empirically effective as a hair growth agent, it is an unstable substance. Nanostructured Lipid Carrier (NLC) is a delivery system that is proven to increase the effectiveness and stability of the material, and the usage of solid lipid combination: beeswax-oleum cacao can produce good NLC characteristics. Objective: To determine the effectiveness of NLC_AMS oil with different combination of beeswax-oleum cacao (100:0; 50:50; 25:75; and 0:100) as a hair growth agent, using rats as subjects. Methods: NLC-AMS oil was made using 20% of total lipid with 5% AMS oil as liquid lipid and 15% solid lipid; combinations of beeswax-oleum cacao were of different ratios (100:0; 50:50; 25:75; and 0:100). NLC was made by High Shear Homogenization (HPH) method. Hair growth activity test carried out on male white rats using the research methods of Yoon (2010). Results: The addition of oleum cacao as a solid lipid did not affect the pH, but increased the consistency and decreased the particle size of NLC- AMS oil. There was a relationship between the characteristic of NLC and the hair growth activity test: the small particle size and low viscosity had greater hair growth activity. Conclusion: The usage of solid lipid combination: beeswaxoleum cacao can produce better NLC characteristics and had higher hair growth activity than the formulas that used single lipid.

The effect of peppermint oil addition on the physical stability, irritability, and penetration of nanostructured lipid carrier coenzyme Q10.

Background: Coenzyme Q10 is formulated into Nanostructured Lipid Carrier (NLC) added with peppermint oil (PO) 0% (F1), 1% (F2), 1.5% (F3) and 2% (F4) to increase its penetration. Objective: This study aims to determine the effect of PO addition on the irritability, stability, and penetration of Coenzyme Q10 in the NLC. Methods: Coenzyme Q10 NLC was prepared using the High Shear Homogenization method. Furthermore, physical characterization was carried out. Physical stability testing was carried out for 90 days at a temperature of 25±5oC and an RH of 60±10%. The in vivo irritation test was observed for mice's back skin after 24 hours while the penetration study was further evaluated at 2 hours of the sample application. Results: Increasing the PO amount into Coenzyme Q10 NLC reduced the viscosity which was 329.1±15.5 cps for PO 0% to 219.9±2.9 cps for 2% addition. The observation of particle morphology showed that all NLC Coenzyme Q10 has a spherical particle shape with particle size between 188.25±13.22 to 197.80±14.19 nm. All formulas had high entrapment efficiency (>80%). PO addition did not cause changes in physical characteristics during 90 days of storage. The 24 hours' irritation test showed that F2 and F3 are non-irritating. By PO addition skin penetration improved at 2 hours' penetration study. Conclusion: PO addition up to 2% reduced viscosity, but did not affect particle size and morphology of Coenzyme Q10 NLC. Addition of PO up to 1.5% increased entrapment efficiency, did not irritate and increased the penetration of Coenzyme Q10 NLC.

The effect of surfactant type on characteristics, skin penetration and anti-aging effectiveness of transfersomes containing amniotic mesenchymal stem cells metabolite products in UV-aging induced mice.

Transfersome has been developed to enhance dermal delivery of amniotic mesenchymal stem cell metabolite products (AMSC-MP). AMSC-MP contains many growth factors for managing skin aging, thus improving the quality of an adjusted life year. This study aims to determine the effect of surfactant types acting as the edge activator on transfersome-loading AMSC-MP. Transfersome was prepared by thin-layer hydration method and composed of l-α-phosphatidylcholine as a phospholipid and three types of surfactants, namely; cationic (stearylamine), anionic (sodium cholate), and nonionic surfactant (Tween 80) at a weight ratio of 85:15, respectively. Transfersomes were evaluated for physical characteristics, penetration, effectiveness, and safety. The results showed that sodium cholate, an anionic surfactant, produced the smallest transfersome particle size, i.e., 144.2 ± 3.2 nm, among all formulas. Trans-SA containing stearylamine had a positive charge of 41.53 ± 6.03 mV compared to Trans-SC and Trans-TW, whose respective charges were -56.9 ± 0.55 mV and -41.73 ± 0.86 mV. The small particle size and low negative value of zeta potential enabled high dermal penetration by transfersomes containing AMSC-MP, while the positive charge of stearylamine hindered its penetration of deeper skin layers. Trans-SC and Trans-TW produced higher collagen density values at 77.11 ± of 4.15% and 70.05 ± of 6.95%, than that of Trans-SA. All the AMSC-MP transfersomes were relatively safe with 0.5-1.0 macrophage cell numbers invaded the dermis per field of view. In conclusion, sodium cholate, an anionic surfactant, demonstrated considerable capacity as the edge activator of transfersome-loading AMSC-MP for skin anti-aging therapy.

Optimization of microspheres containing virgin coconut oil and hydrolyzed virgin coconut oil as antimicrobial.

Virgin Coconut Oil (VCO) with potential fatty acid content has a strong antibacterial effect for drug and cosmetics. VCO was hydrolyzed as hydrolyzed VCO (HVCO) to increase its activity. This study aims to optimize VCO and HVCO microspheres. Examination was included fatty acid content, density, and organoleptic. VCO and HVCO microspheres were characterized by yield, moisture content (MC), morphology, and size. Fatty acid content was done through gas chromatography mass spectrometry whereas for microspheres, effect of alginate concentration (1%-2%), and addition of poly ethylene glycol (PEG) were studied. VCO and HVCO microspheres formulas showed that an increase in polymer concentration, increasing yield, and improving MC. The most optimal 2% alginate with the addition of PEG increased yield up to 59% and reduced size. F4 microspheres resulted the highest yield, low MC, and high fatty acids. Morphology was spherical and smooth with small size. Optimization of HVCO microspheres showed its potential which recommend for antibacterial and antifungal activity.

Characterization and in vitro release of inhalation quercetin solid lipid microparticles: Effect of lipid.

This study purposes to develop solid lipid microparticles (SLM) inhalation delivery system for respiratory diseases with Quercetin as the active agent. Quercetin has various functions, such as for antioxidant, anti-inflammatory, immunomodulator, and antivirus. SLM is formed from a mixture of lipids and surfactants, namely, Glyceryl Behenate as solid lipid, Poloxamer 188 as the surfactant, and production of SLM using the melt o/w emulsification technique and was dried using freeze dryer. The effect of lipid concentration was studied in this research. Quercetin SLM was characterized by moisture content, Fourier transform infrared, particle size, yield, drug loading, and encapsulation efficiency. The SLM particles produced were spherical in shape and had a smooth surface with sizes of F1, F2, and F3 were 1.79 µm, 1.88 µm, and 1.91 µm, respectively. According to the target particle size of inhalation, Quercetin SLM had good flowability according to Carr's Index (F1 = 12.73% ± 0.38, F2 = 14.28% ± 0.65, F3 = 14.65% ± 0.62), in which the highest drug loading and EE of F3 were 10.94% and 88.48%, respectively. In vitro release study showed that in 630 min about 31%-33% Quercetin released indicated sustained release following Higuchi kinetics and quercetin release rate was not affected by the amount of lipid. To sum up, quercetin SLM demonstrates its potential as an inhalation delivery system and it is recommended to study its stability.

Improving the anti-ageing activity of coenzyme Q10 through protransfersome-loaded emulgel.

Coenzyme Q10 (CoQ10) is a naturally produced organic molecule which acts as an antioxidant agent, including in skin anti-ageing, and plays a major role in the social determinants of health. However, its level in the body will decrease during ageing. Therefore, an external supplement is required to repair damaged skin, especially the skin dermis layer. This study aims to evaluate the use of a protransfersomal emulgel to improve the skin delivery and stability of CoQ10 which demonstrates low water solubility, poor permeability and instability. CoQ10 was initially dissolved in oleic acid at a weight ratio of 1:56. Protransfersome was then loaded with CoQ10 (Protransf-CoQ10) and prepared using a composition of L-α-Phosphatidylcholine and Tween 80 at a molar ratio of 85:15. The Protransf-CoQ10 was dispersed in an emulgel base consisting of Tween 80 and Span 80 to produce Protransf-CoQ10 emulgel. The in vivo studies of anti-aging activity and irritability were further evaluated by applying daily 200 mg of emulgels twice a day to a 4 cm2 section on the back of a UV-ray aging-induced male Balb/c mouse 20 min before irradiation. The results showed that Protransf-CoQ10 could transform into transfersomal vesicles with particle sizes of approximately 201.5 ± 6.1 nm and a zeta potential of - 11.26 ± 5.14 mV. The dispersion of Protransf-CoQ10 into emulgel base resulted in stable Protransf-CoQ10 Emulgel during 28 days of observation at low temperatures. Moreover, the in vivo study revealed that Protransf-CoQ10 Emulgel successfully increases the collagen density and number of fibroblast cells in UV radiation skin-aged induced-mice which reflects its potential for repairing the skin ageing process. In addition, the 24-h topical application of Protransf-CoQ10 Emulgel showed that no erythema or skin rash was observed during the study. In conclusion, loading CoQ10 into protransfersomal Emulgel successfully enhanced the stability and anti-ageing efficacy enabling its potential use as anti-ageing cosmetics.

Coenzyme Q10 nanostructured lipid carriers as an inducer of the skin fibroblast cell and its irritability test in a mice model.

Background Coenzyme Q10 is a fat-soluble antioxidant that can help to prevent collagen and elastin damage and avoid wrinkles. Coenzyme Q10 has several disadvantages to be formulated in topical dosage forms, such as low water solubility and large molecular weight. These make coenzyme Q10 retained in the stratum corneum and cause low skin penetration, so proper formulation is required to get products that can penetrate the skin layer. A nanostructured lipid carrier (NLC) consists of a matrix of solid lipids and liquid lipids in a certain amount with nanoparticle size; it may help increase the penetration of active ingredients. Methods For the antiaging activity test, mice were grouped into four treatment groups and killed on the 14th day; then the back of the skin was stained with Masson trichrome staining. For the irritation test, the mice were grouped into three groups and killed after 24 h; then the back of the mice was stained with hematoxylin-eosin staining. Results The number of fibroblasts in mice with NLC coenzyme Q10 is highest from all test groups. The irritation test results after 24 h of application preparation showed that NLC coenzyme Q10 did not irritate the skin of the back of male mice. Conclusions One percent coenzyme Q10 loaded in NLC induced the number of fibroblast cells in the mice model and showed no irritability effect in histopathology preparations.