Masahiko Abe

Anti-aging efficacy of topical formulations containing niosomes entrapped with rice bran bioactive compounds

Context: Rice [Oryza sativa L. (Gramineae)] bran is a rich source of phytochemicals. Its oil also contains several bioactive components that exhibit antioxidative properties such as ferulic acid (F), γ-oryzanol (O), and phytic acid (P) which can be a new source of cosmetic raw materials. Objective: To evaluate the anti-aging effects of the gel and cream containing niosomes entrapped with the rice bran bioactive compounds. Materials and methods: The semi-purified rice bran extracts containing F, O, and P which indicated the growth stimulation of human fibroblasts and the inhibition of MMP-2 by sulforhodamine B and gelatin zymography, respectively, were entrapped in niosomes by supercritical carbon dioxide fluid (scCO2) and incorporated in gel and cream formulations. The skin hydration, elasticity, thickness and roughness, and pigmentation in human volunteers after treated with these gel and creams were investigated by corneometer, cutometer, visiometer, and mexameter, respectively. Results: Gel and cream containing the semi-purified rice bran extracts entrapped in niosomes gave no sign of erythema and edema detected within 72u2009h on the shaved rabbit skin by the closed patch test investigated by mexameter and visual observation, respectively. These formulations also demonstrated higher hydration enhancement and improvement of skin lightening, thickness, roughness, and elasticity on the skin of 30 human volunteers within the 28–day treatment not more than 9, 27, 7, 3, and 3 times, respectively. Discussion and conclusions: The formulations containing niosomes entrapped with the rice bran bioactive compounds gave superior clinical anti-aging activity which can be applied as a novel skin product.

Transfollicular enhancement of gel containing cationic niosomes loaded with unsaturated fatty acids in rice (Oryza sativa) bran semi-purified fraction

The 20mM cationic niosomes composed of Tween61/cholesterol/CTAB at 1:1:0.5M ratio which gave the best physical appearance, particle size, zeta potential and in vitro cytotoxicity were selected from six cationic niosomes prepared from various cationic lipids. The selected cationic niosomes were loaded with the semi-purified fraction 3 of Oryza sativa (OSF3) which gave the highest in vitro 5α-reductase inhibition activity. The physicochemical characteristics as well as transfollicular penetration through porcine skin by Franz diffusion cells of gel OSF3 niosomes, OSF3 niosomes, gel OSF3 and OSF3 solution were investigated. Gel containing niosomes loaded with OSF3 exhibited physical stability with 77.68% of gamma-linolenic acid, 85.34% of linoleic acid and 89.47% of oleic acid remaining for 3 months at 25 °C. In the skin, the OSF3 niosomes (120.27 ng/cm(2)) and gel OSF3 niosomes (118.17 ng/cm(2)) showed the highest cumulative amounts of the total unsaturated fatty acids (gamma-linolenic acid, linoleic acid and oleic acid) in comparing to those from the gel OSF3 (15.34 ng/cm(2)) and OSF3 solution (20.31 ng/cm(2)) of about 8 and 6 times, respectively. In the receiver compartment, the gel OSF3 niosomes (6.27 ng/cm(2)) exhibited lower cumulative amount of the total unsaturated fatty acids than that of the OSF3 niosomes (11.20 ng/cm(2)) of about 2 times. This study has suggested that gel containing OSF3 loaded in niosomes appeared to be the suitable system for topical anti-androgenic alopecia application because of the convenient use and high transfollicular penetration in the skin, but not in the receiving compartment with the advantage of low systemic effect.

Transdermal Absorption Enhancement of Rice Bran Bioactive Compounds Entrapped in Niosomes

Niosomes composed of Tween 61 and cholesterol at 1:1 molar ratio were entrapped with the mixture of the three semi-purified rice (Oryza sativa L., Family Gramineae) bran bioactive compounds [ferulic acid (F), γ-oryzanol (O), and phytic acid (P)] at 0.5%, 1.5%, and 1.5%, respectively, by the supercritical CO2 technique. The transdermal absorption by vertical Franz diffusion cells of the compounds entrapped in niosomes (Nio FOP), the unentrapped compounds (Mixed FOP), the compounds incorporated in gel and cream (Gel FOP and Cream FOP), and the compounds entrapped in niosomes and incorporated in gel and cream (Gel nio and Cream nio) was investigated. At 6xa0h, F and P from Nio FOP gave lower cumulative amount in viable epidermis and dermis (VED) than from Mixed FOP of 1.1 and 1.6 times, respectively, while O from Nio FOP exhibited higher cumulative amount in VED than from Mixed FOP of 2.4 times. The highest cumulative amount in VED of F, O, and P were from Gel nio, Cream nio, and Mixed FOP at 1.564u2009±u20090.052, 15.972u2009±u20090.273, and 25.857u2009±u20090.025xa0ng/cm2, respectively. Niosomes enhanced the transdermal absorption of the hydrophobic compound O, while retarded the hydrophilic compounds F and P indicating the less systemic risk of F and P than O when entrapped in niosomes. Thus, transdermal absorption of F, O, and P appeared to depend on niosomal size, lipophilicity of the bioactive compounds, and types of formulations. These preclinical results can be applied for the design of the clinical study of the developed rice bran niosomal topical products.

Characteristics of niosomes entrapped with rice bran bioactive compounds prepared by supercritical carbon dioxide

Bioactive compounds [ferulic acid(F), γ-oryzanol(O) and phytic acid(P)] in rice bran are unstable antioxidants. Niosomes composed of Tween61 mixed with cholesterol at 1:1 molar ratio which gave the highest physical stability at 4, 30 and 45 °C for 3 months, were selected to entrap the semi-purified rice bran extracts containing F, O and P at 0.5, 1.5 and 1.5%w/w, respectively as well as their combination by supercritical carbon dioxide (scCO2) or chloroform film with sonication. The entrapment efficiency of F, O and P in niosomes was determined by gel filtration. The characteristics including vesicular size, morphology, dispersibility, phase transition temperature (Tc) and microviscosity of the niosomal dispersion were also investigated by dynamic light scattering (DLS) apparatus, freeze-fracture transmission electron microscope (FF-TEM), visual observation, differential scanning calorimeter (DSC) and the fluorescence polarization technique, respectively. The niosomes entrapped and not entrapped with the semi-purified rice bran extracts by both scCO2 and the chloroform film technique were stable vesicles with the size of 300–1500 nm. The morphology of all niosomes prepared by scCO2 and chloroform film technique were in large unilamellar vesicles (LUVs) and the mixture of unilamellar and multilameller vesicles (MLVs), respectively. The Tc of all niosomes prepared by both methods was 75 to 81 °C with the AH of +0.337 to +0.661 kJ/mol. The LUV niosomes by scCO2 gave higher entrapment efficiencies of the hydrophilic bioactive compounds, F (64.47±1.17%) and P (54.85±0.11%) and lower entrapment efficiencies of the hydrophobic bioactive compound, O (47.54±2.31%) than niosomes by the chloroform film which gave at 53.56±1.76 (F), 60.79±0.65 (P), 53.48±0.15 (O) %, respectively, of about 1.3 times. This study has indicated that the rice bran bioactive compounds did not only not interfere with the Tc and microviscosity of niosomes prepared by both methods, but also the niosomes prepared by scCO2 technique can enhance the entrapment efficiency of these bioactive compounds.

Potent in vivo anticancer activity and stability of liposomes encapsulated with semi-purified Job’s tear (Coix lacryma-jobi Linn.) extracts on human colon adenocarcinoma (HT-29) xenografted mice

Abstract The in vivo anticancer activity and stability of liposomes encapsulated with semi-purified Job’s tear (Coix lacryma-jobi Linn.) extracts (S5L), prepared by supercritical carbon dioxide fluid technique, on human colon adenocarcinoma (HT29) xenografted mice were investigated. For the stability and the physicochemical characteristics, S5L showed a high stability of pH, good dispersibility, small particle size and stable zeta potential. Liposomes can protect linoleic acid in the extract comparing with the free S5. S5L kept at 4u2009°C for 3 months showed the highest linoleic acid content of 63.50%, whereas at 45u2009°C, the lowest linoleic acid content of 42.66% was observed. The anticancer activity and toxicity on xenografted mice were observed for 14 days. At the end of the experiment, the relative tumor volume (RTV) in the S5L-treated xenografted mice showed a significant RTV reduction. The high dose of S5 and S5L were potent with the highest inhibition of tumor growth of 48.67 and 54.75%, which was 86.94% and 97.81% of 5-fluorouracil, respectively. The apoptotic activity was shown in xenografted mice treated with S5 at medium and high dose, S5L, 5-fluorouracil and commercial product. All treated xenografted mice showed no toxic signs and symptoms, abnormality of internal organs histopathology and blood chemistry. This study has demonstrated the high physicochemical stability of liposomes encapsulated with semi-purified Job’s tear extract and their potent anticancer activity on human colon adenocarcinoma xenografted model with the potential for further development to anticolon cancer drug.