Antioxidant and tyrosinase inhibitory activity of face serum containing cocoa pod husk phytosome (Theobroma cacao L.)

High polyphenol content of cocoa pod extract causing it potential to be developed as antioxidant and tyrosinaseinhibitory agent in cosmetic preparations. Phytosome system known could enhance skin penetration of phytoconstituentlike polyphenol-rich extract. The objectives of this research were to formulate phytosome containing cocoa podextract, develop phytosome complex into face serum preparation, and determine antioxidant and tyrosinase inhibitoryactivities of the extract and the formulated serum. The cocoa pod extract was developed into phytosome system bythin-layer method using soy-phosphatidylcholine. The phytosome then develop into face serum formulation usingViscolam MAC 10 as a gelling agent. The antioxidant activity was conducted by 2,2-diphenyl-1-picrylhydrazyl radicalscavenging assay and tyrosinase inhibitory activity was conducted by colorimetric enzymatic assay. The cocoa podextract has very strong antioxidant activity with inhibitory concentration (IC50) of 17.21 ppm. The extract also hastyrosinase inhibitory activity with IC50 of 199.98 ppm. The phytosome complex containing cocoa pod extract andphosphatidylcholine (1:1) has good entrapment efficiency (90.5%) with an average particle size of 672 nm. Theformulated face serum has good physical characteristic and also has antioxidant and tyrosinase inhibitory activitiesthat equal with the marketed product (Hadalabo ultimate whitening milk, Rohto, Indonesia).

Hepatoprotective effect of Phytosome Curcumin against paracetamol-induced liver toxicity in mice

Abstract Curcuma longa, which contains curcumin as a major constituent, has been shown many pharmacological effects, but it is limited using in clinical due to low bioavailability. In this study, we developed a phytosome curcumin formulation and evaluated the hepatoprotective effect of phytosome curcumin on paracetamol induced liver damage in mice. Phytosome curcumin (equivalent to curcumin 100 and 200 mg/kg body weight) and curcumin (200 mg/kg body weight) were given by gastrically and toxicity was induced by paracetamol (500 mg/kg) during 7 days. On the final day animals were sacrificed and liver function markers (ALT, AST), hepatic antioxidants (SOD, CAT and GPx) and lipid peroxidation in liver homogenate were estimated. Our data showed that phytosome has stronger hepatoprotective effect compared to curcumin-free. Administration of phytosome curcumin effectively suppressed paracetamol-induced liver injury evidenced by a reduction of lipid peroxidation level, and elevated enzymatic antioxidant activities of superoxide dismutase, catalase, glutathione peroxidase in mice liver tissue. Our study suggests that phytosome curcumin has strong antioxidant activity and potential hepatoprotective effects.

Process optimisation, characterisation and evaluation of resveratrol-phospholipid complexes using Box-Behnken statistical design.

With the advent of 21st century, researchers worldwide have extensively reviewed herbs and botanicals for their marked clinical efficacy. It has been estimated that most of the newly discovered compounds offer poor bioavailability due to their low aqueous solubility. Phospholipid complexation of the drug often helps to improve its water solubility and enhance the bioavailability. This study includes optimization of resveratrol-phospholipid complexes using a 3-factor, 3-level box-behnken design (15 batches). Three independent variables i.e. phospholipid-resveratrol ratio, refluxing temperature and reflux time were optimized for two dependent variables, i.e. yield and entrapment efficiency (EE). Complexes were prepared by refluxing stoichiometric ratio of Phospholipon 90G and resveratrol in dichloromethane and retrieved by precipitation with n-hexane. Complexation was confirmed by Fourier Transform Infra-Red (FTIR) spectroscopy. The data was suitably used to explore quadratic response surfaces and construct second order polynomial models with Design Expert®. Formulation with highest desirability (D=0.994) was selected as optimum and prepared using 1.5:1 Phospholipon 90G-resveratrol ratio (X1) at 59.4°C temperature (X2) and 4 h time (X3) to give maximum yield and entrapment efficiency. Analysis of variance (ANOVA) was also found to be significant for both the responses. Complexes were optimised for good yield and EE. The partition coefficient was lowered to 2.25 hypothesizing good passive absorption.

Physicochemical properties of baohuoside I phytosomes and its anti-tumor activity / 中国药学杂志

OBJECTIVE: To prepare baohuoside I phytosomes and study its anti-tumor activities in vitro.

Process optimisation, characterisation and evaluation of resveratrol-phospholipid complexes using Box-Behnken statistical design.

With the advent of 21st century, researchers worldwide have extensively reviewed herbs and botanicals for their marked clinical efficacy. It has been estimated that most of the newly discovered compounds offer poor bioavailability due to their low aqueous solubility. Phospholipid complexation of the drug often helps to improve its water solubility and enhance the bioavailability. This study includes optimization of resveratrol-phospholipid complexes using a 3-factor, 3-level box-behnken design (15 batches). Three independent variables i.e. phospholipid-resveratrol ratio, refluxing temperature and reflux time were optimized for two dependent variables, i.e. yield and entrapment efficiency (EE). Complexes were prepared by refluxing stoichiometric ratio of Phospholipon 90G and resveratrol in dichloromethane and retrieved by precipitation with n-hexane. Complexation was confirmed by Fourier Transform Infra-Red (FTIR) spectroscopy. The data was suitably used to explore quadratic response surfaces and construct second order polynomial models with Design Expert®. Formulation with highest desirability (D=0.994) was selected as optimum and prepared using 1.5:1 Phospholipon 90G-resveratrol ratio (X1) at 59.4°C temperature (X2) and 4 h time (X3) to give maximum yield and entrapment efficiency. Analysis of variance (ANOVA) was also found to be significant for both the responses. Complexes were optimised for good yield and EE. The partition coefficient was lowered to 2.25 hypothesizing good passive absorption.

Phytosomal Drug Delivery Systems.

Certain of the water-soluble flavonoid molecules can be converted into lipid-compatible molecular complexes, aptly called phytosomes. Phytosomes are better able to transition from a hydrophilic environment into the lipid-friendly environment of the outer cell membrane, and from there into the cell, finally reaching the blood. The term "phyto" means plant while "some" means cell-like. Phytosome is a complex of a natural active ingredient and a phospholipid. It is claimed that phytosome increases absorption of "conventional herbal extracts" or isolated active principles. The phytosome process is that combines herbal extracts and soybean phospholipids (lecithin). phytosomes are created when the standardized extract and active ingredients of a herb are bound to the phospholipids on a molecular level. The newly created Phytosome structures contain the active ingredients of the herb surrounded by the phospholipids. The phospholipid molecular structure includes a water-soluble head and two fat-soluble tails. Because of this dual solubility, the phospholipid acts as an effective emulsifier. The newly created phytosome structures contain the active ingredients of the herb surrounded by the phospholipids. The phospholipid molecular structure includes a water-soluble head and two fat-soluble tails. Because of this dual solubility, the phospholipid acts as an effective emulsifier. An emulsifier is a material that can combine two liquids that normally will not mix well together. By combining the emulsifying action of the phospholipids with the standardized botanical extracts, the phytosome form provides dramatically enhanced bioavailability and delivers faster and improved absorption of the active constituents of the herb in the intestinal tract.