Enhancing the water-solubility of curcuminoids-rich extract using a ternary inclusion complex system: Preparation, characterization, and anti-cancer activity.

Curcuminoids are known to exert diverse pharmacological effects and used in some pharmaceutical formulations. This study describes the preparation, characterization, and enhancement in the solubility and anticancer activity of a curcuminoids-rich extract (CRE) using a ternary inclusion complex system. CRE containing 88.9% w/w curcuminoids was prepared using a 'green' microwave extraction coupled with fractionation on a column of hydrophobic adsorbent resin. The ternary complex consisting of CRE, hydroxylpropyl-ß-cyclodextrin and polyvinylpyrrolidone K30 was prepared using the solvent evaporation method and thoroughly characterized using Fourier-transform infrared spectroscopy, powder X-ray diffractograms, differential scanning calorimetry and scanning electron microscopy. The ternary complex of CRE improved the water-solubility of curcuminoids (up to 70.3 µg/mL) as well as the dissolution rate when compared to those of CRE (0 µg/mL). In addition, the ternary complex exhibited significantly stronger anticancer activity against human lung adenocarcinoma (A-549), human cervical adenocarcinoma (HeLa) and human colon adenocarcinoma (HT-29) cell lines than CRE.

A Cold Process Preparation of Vetiveria zizanioides (L.) Nash Oil Lotions using Simulgel FL as an Emulsifier.

Vetiveria zizanioides (vetiver) contains viscous volatile oil, which has the ability to repel mosquitoes similar to citronella oil, a well-known mosquito repellent in tropical countries, like Thailand. The objectives of the current study were to formulate the stable oil-in-water vetiver oil lotions using Simulgel FL as a liquid emulsifier, to investigate the physicochemical properties of the prepared lotions and to evaluate the in vitro release characteristics of the stable vetiver oil lotions. In this work, the concentrations of Simulgel FL ranged from 1% to 3% weight in weight, whereas the concentrations of vetiver oil were varied: 2.5%, 5%, and 10% weight in weight. The suitable concentration of Simulgel FL was found to be 3% weight in weight. For comparison purposes, oil-in-water citronella oil lotions (10% weightin- weight citronella oil) were also prepared with similar ingredients. A mixture of vetiver oil and citronella oil (1:1 by weight) was also used as an active ingredient. By using Simulgel FL, the lotions could be prepared using a cold process (without heat). The physicochemical properties (appearance, pH, viscosity) of the stable lotions were satisfactory. All prepared lotions possessed weak acidic pH values with pseudoplastic flows. Using modified Franz diffusion cell and synthetic membrane, the release rates of vetiver oil were relatively lower than those of citronella oil.

Physicochemical properties, in vitro release and skin permeation studies of a topical formulation of standardized pomegranate rind extract.

The aim of the present study was to develop a stable formulation containing standardized pomegranate rind extracts (SPRE) for topical use in the treatment of dermal diseases. Ellagic acid (EA) as the major active constituent of SPRE (not less than 13%) was quantified by HPLC as an indicator for studies on the stability, in vitro drug release, and skin penetration/retention. The formulation prepared with polyethylene glycols (PEG 400 and PEG 4000) containing 5% SPRE has been found to be stable and provide a release rate of 36.6741±5.0072 µg/cm(2)/h that was best fitted to the zero-order kinetic model. EA from SPRE did not penetrate the full-thickness rat skin but the skin retention of EA was determined to be 2.22±0.16 µg/cm(2) with a total recovery of 95.14±5.51%. The results indicated that this 5% SPRE PEG ointment was of satisfactory physicochemical properties and worth further in vivo investigations.

Wound healing activities of standardized pomegranate rind extract and its major antioxidant ellagic acid in rat dermal wounds.

The in vivo wound healing potential of a standardized pomegranate rind extract (SPRE) and its major antioxidant constituent, ellagic acid (EA, 13 %, w/w), were investigated in three rat dermal wound models. It was found that both SPRE (5 and 2.5 %) and its equivalent amount of EA (0.65 and 0.325 %) increased the tensile strength of the incision wound by a maximum of 35.43 and 31.82 %, respectively. SPRE at 5 and 2.5 % accelerated wound contraction of the excision wound and the burn wound, while EA was effective only at 0.65 % in these two wound models. Further assays revealed that SPRE enhanced the synthesis of collagen by a maximum of 21.83 mg/g and inhibited neutrophil infiltration dose-dependently, while EA was not effective in increasing collagen accumulation and its inhibitory effect on neutrophil infiltration was milder. These results indicated that SPRE is a promising phytopharmaceutical effective in facilitating the healing of wounds and is superior to its marker compound EA.

Topical anti-inflammatory potential of standardized pomegranate rind extract and ellagic acid in contact dermatitis.

The present study evaluated the topical anti-inflammatory potential of a standardized pomegranate rind extracts (SPRE) in parallel with its marker compound ellagic acid (EA, 13% w/w) against a mouse model of contact dermatitis. In the phenol-induced mouse ear edema, topical application of SPRE (5, 2.5, and 1 mg/ear) and EA (0.65, 0.325, and 0.13 mg/ear, equivalent to its content in SPRE) dose-dependently reduced the ear edema with the maximal inhibition of 79.12% and 73.63%, respectively. Triamcinolone (0.1 mg/ear) and diclofenac (1 mg/ear) as reference drugs inhibited the edema by 73.63% and 37.91%. Myeloperoxidase (MPO) activity in the mouse ear was also decreased by SPRE and EA up to 69.68% and 68.79%, respectively. Triamcinolone and diclofenac decreased the MPO activity by 76.66% and 80.14% similarly. The results indicated that topical application of SPRE and EA is promising for use in the treatment of inflammatory skin disorders.

Topical anti-inflammatory and analgesic activities of standardized pomegranate rind extract in comparison with its marker compound ellagic acid in vivo.

ETHNOPHARMACOLOGICAL RELEVANCE: In Chinese traditional medicine, the peels of Punica granatum L. have been used to treat traumatic hemorrhage, burn, and ulcers. AIMS OF THE STUDY: This study aimed to assess the topical anti-inflammatory and analgesic activities of a standardized pomegranate rind extract (SPRE) of which ellagic acid (EA) was the major antioxidant constituent and the marker compound. MATERIAL AND METHODS: The topical anti-inflammatory effects of SPRE were evaluated against acute models (croton oil-induced mouse ear edema and carrageenan-induced rat paw edema) and chronic model (complete Freund's adjuvant (CFA)-induced polyarthritis). The topical analgesic activities of SPRE were investigated in the rat punctuate mechanical hyperalgesia test and in the mouse formalin test. All studies of SPRE were carried out in parallel with its marker compound EA. RESULTS: SPRE (5%, 2.5%, and 1%, w/w) and the equivalent EA (0.65%, 0.325%, and 0.13%, w/w) dose-dependently reduced the croton oil-induced mouse ear edema with a maximal inhibition of 86.30% and 80.82%, respectively. SPRE dose-dependently attenuated the inflammatory responses in the carrageenan-induced rat paw edema and in the CFA-induced polyarthritis but the equivalent EA were effective only at the doses of 0.65% and 0.325%. Both SPRE (5%) and EA (0.65%) showed significant topical analgesic activities in the rat punctuate mechanical hyperalgesia test and in the mouse formalin test. CONCLUSIONS: SPRE was more active as an anti-inflammatory agent than EA. The anti-inflammatory and analgesic effects of SPRE were achieved through inhibiting the leukocyte infiltration and modulating the pro-inflammatory cytokines IL-ß and TNF-α. These results clearly demonstrated that SPRE is a promising phytomedicine that could find use in the treatment of inflammatory diseases.

Effects of glucam P-20, vanillin, and fixolide on mosquito repellency of citronella oil lotions.

The objective of this study was to investigate the effects of three fragrance fixatives, Glucam P-20, Vanillin, and Fixolide, on the mosquito repellent property of citronella oil lotions. In the current study, two formulae (A and B) of oil-in-water citronella oil lotions were formulated using different ingredients (emulsifiers [Cremophors or Emulwax], stiffening agents, and emollients). Citronella oil was used at 10% wt:wt. The weight ratios tested between citronella oil and each fixative were 1:0.25, 1:0.5, and 1:1. Overall, 20 formulations, including one with no fixatives for both A and B, were produced, A1-A10 and B1-B10. The repellent activities of these 20 lotions against Aedes aegypti (L.) were tested using a human-bait technique. The types and concentrations of fixatives as well as the compositions of the formulations did affect the protection time of the citronella oil lotions. The lotion containing Emulwax and 5% vanillin (B6) was the most effective repellent. It provided the longest protection time of 4.8 h, which exceeded the minimum requirement of 2 h set by the National Institute of Health, Thailand. The shortest protection time (1 h) was observed in the lotion containing Emulwax and 2.5% Glucam P-20 (B2). It could be concluded that the tested fixatives affected the repellent activity of the citronella oil lotions.