Preparation, characterization, and antibacterial activity of plaunotol and plaunoi extracts complexed with hydroxypropyl-ß-cyclodextrin.

Croton stellatopilosus (Plaunoi) leaves accumulate several diterpenes and possess various pharmacological activities. The present study aimed to prepare, characterize and assess the antibacterial activity of inclusion complexes prepared by mixing plaunotol (PL) or plaunoi extract (PE) with cyclodextrins (CD), including α-CD, ß-CD, γ-CD, and hydroxypropyl-ß-cyclodextrin (HP-ß-CD). The inclusion complexes were characterized using SEM, XRD, DSC, and FT-IR and evaluated for aqueous solubility and thermal stability. The PL and PE lyophilized complexes with HP-ß-CD were further evaluated for their antibacterial activity against acne-causing bacteria. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) of PL, PE, and the inclusion complexes evaluated using the agar dilution method revealed that the MIC and MBC values of the inclusion complexes were lower than those of PL or PE alone. Interestingly, the complexes had a synergistic activity with clindamycin after testing with checkerboard assay. The hydrogel containing the inclusion complex and clindamycin were assessed for antibacterial activity using the agar well diffusion method. The results indicated that the hydrogels showed significant inhibition of bacterial growth. In conclusion, the prepared solid dispersion of PL or PE with HP-ß-CD could enhance antibacterial activity by increasing the drug solubility. The hydrogels containing PL or PE complex and clindamycin could be considered as a candidate for the treatment of acne vulgaris.

Influence of interfering co-appearing container peaks on the accuracy of direct quantitative Raman measurement of a sample in a plastic container.

The axially perpendicular offset (APO) scheme was previously demonstrated as a versatile scheme able to minimize or eliminate the glass background in the direct and non-sampling Raman measurement of an ethanol sample housed in a glass bottle. Alternatively, when directly analyzing a sample housed in a plastic container, another typical container yielding strong Raman peaks itself, the Raman peaks of both the container and the housed sample are unavoidably present together in a collected spectrum. Therefore, a crucial issue to investigate under this situation is how the magnitude of the co-appearing container peaks influences the accuracy for quantitative analysis of the housed sample. For the evaluation, a non-sampling Raman spectroscopic measurement of the urea concentration in a urea gel housed in a circular polypropylene (PP) container was attempted by employing two axially perpendicular offset (APO) schemes with detection windows of different sizes (25.4 and 10.0 mm, referred to as the wide-window APO (WW-APO) and narrow-window APO (NW-APO), respectively), and transmission and back-scattering schemes incorporating a 25.4 mm detection window. The intensity ratios between the container and urea peaks in the collected spectra were different depending on the adopted measurement scheme. The intensity ratio was greatest (smallest container peak) in the NW-APO measurement due to the narrowed detection window, making the generated container Raman photons at the side-wall less detectable to the bottom-positioned detector. A spectral acquisition scheme allowing the maximal suppression of the container peaks, while still maintaining the sample features, was a key requirement to secure an accurate measurement of the sample concentration. In addition, a Monte Carlo simulation was used to visualize the distributions of the container and urea photons inside the sample-housed container.

RiceSorb® as Talcum Substitute for Loose Face Powders: Formulation and Characterization.

Excessive and daily inhalation of talcum, a main ingredient of face powders, causes pulmonary talcosis, which has led to the replacement of talcum with safer natural ingredients. RiceSorb®, or Oryza sativa starch from Japanese rice, was used as an alternative owing to its nontoxic and excellent oil absorption capacity. The objectives of the present work were to formulate loose face powders from RiceSorb® and to investigate the physicochemical properties of the prepared formulations. Five formulations of loose face powders were prepared by varying the ratios between talcum and RiceSorb®: 4:0 (FT0), 3:1 (FT1), 1:1 (FT2), 1:3 (FT3), and 0:4 (FT4). The physicochemical properties were evaluated mainly based on USP 41 and NF 36 such as morphology by using a scanning electron microscope, bulk density, flow property (angle of repose), moisture content (MC), and pH. The stability of the formulations were also performed at ambient temperature and 45°C for 2 months. The formulations had pH 6.90-8.62, bulk density 0.33-0.49 g/ml, and an angle of repose 30°-41°. Overall, the formulations which contained only RiceSorb® (FT4) or higher proportion of RiceSorb® (FT3) had finer particles, lower bulk density, pH, and angle of repose than those of the formulations containing high proportion of talcum: FT0 and FT1. Under storage conditions for 2 months, the formulations containing high proportion of RiceSorb® exhibited noticeably increased MC and angle of repose. However, the other physicochemical properties were somewhat the same. The present results suggest the applicability of RiceSorb® for loose face powders.

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.

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.

In vitro probiotic properties of Lactobacillus fermentum SK5 isolated from vagina of a healthy woman.

A lactobacillus strain isolated from a vaginal tract of a healthy woman was examined in vitro for its probiotic potential. This strain, identified as Lactobacillus fermentum SK5, was able to survive at pH 3-4 and 0.1-0.2% bile, and unaffected by pepsin (3 g l(-1)) and pancreatin (1 g l(-1)), but was susceptible to all tested antibiotics except metronidazole. L. fermentum SK5 had an antimicrobial potential against gastrointestinal pathogenic Escherichia coli and vaginal pathogenic Gardnerella vaginalis. The effective substance was suspected to be a bacteriocin-like compound with a molecular weight of more than 10 kDa, but hydrogen peroxide was also detected. Further studies revealed that L. fermentum SK5 had good autoaggregation characteristic and a high surface hydrophobicity that enhanced its adhesion ability to epithelial cells and for biofilm formation. This lactobacillus showed coaggregation with E. coli and G. vaginalis to affect their adhesion and colonization. The adhesion of L. fermentum SK5 to HeLa, HT-29 and Caco-2 cells and its inhibition of E. coli and G. vaginalis adherence to these cells were demonstrated. These incidences provided evidence of the possible colonization of L. fermentum SK5 that would prevent binding and growth of E. coli and G. vaginalis onto intestinal and vaginal epithelial cells. On the basis of the ability of L. fermentum SK5 to inhibit pathogenic microorganisms through coaggregation and antimicrobial substances, it is likely that this lactobacillus strain could be a potential probiotic candidate for beneficial use in protecting against gastrointestinal and vaginal microbial infections.

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.

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.

Characterization of a novel, co-processed bio-based polymer, and its effect on mucoadhesive strength.

In this study, a biological macromolecule obtained from seeds of Manilkara zapota was co-processed with hypromellose (cop-MPH)/sodium carboxymethylcellulose (cop-MPN)/polyvinylpyrrolidone (cop-MPP) in a 1:1 ratio and characterized for powder and mucoadhesive properties. The semi-crystalline nature of co-processed excipients and physical interaction between the component molecules were confirmed by X-ray diffraction and infrared spectroscopy analysis. The morphological study by scanning electron and atomic force microscopy showed spherical and polygonal-shaped particles with predominant smooth surfaces. Thermogravimetric analysis revealed thermal stability to a temperature of 200 °C followed by depolymerization. Zeta potential measurements showed that cop-MPP was anionic, whereas cop-MPH and MPN were non-ionic. Texture analysis revealed that work of adhesion (mN·s) for both cop-MPH (390 ± 0.0018) and MPN (304 ± 0.0024) enhanced the mucoadhesion compared with the un-processed hypromellose (300 ± 0.0019) and sodium carboxymethylcellulose (280 ± 0.0012), whereas cop-MPP (240 ± 0.0028) showed mucoadhesion similar to un-processed polyvinylpyrrolidone (250 ± 0.0022). In addition, the swelling studies showed enhancement in water absorbance for all co-processed excipients. Cytotoxicity against human cells revealed >99% of cell viability. These findings demonstrate that the co-processed biological macromolecule extracted from M. zapota seed could be further explored as an effective alternative drug delivery excipient for pharmaceutical applications.

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.

Statistical optimization of bambara groundnut protein isolate-alginate matrix systems on survival of encapsulated Lactobacillus rhamnosus GG.

Encapsulation may protect viable probiotic cells. This study aims at the evaluation of a bambara groundnut protein isolate (BGPI)-alginate matrix designed for encapsulating a probiotic Lactobacillus rhamnosus GG. The response surface methodology was employed to gain the optimal concentrations of BGPI and alginate on encapsulation efficiency and survival of encapsulated cells. The capsules were prepared at the optimal combination by the traditional extrusion method composed of 8.66% w/v BGPI and 1.85% w/v alginate. The encapsulation efficiency was 97.24%, whereas the survival rates in an acidic condition and after the freeze-drying process were 95.56% and 95.20%, respectively-higher than those using either BGPI or alginate as the encapsulating agent individually. The designed capsules increased the probiotic L. rhamnosus GG survival relative to free cells in a simulated gastric fluid by 5.00 log cfu/ml after 3 h and in a simulated intestinal fluid by 8.06 log cfu/ml after 4 h. The shelf-life studies of the capsules over 6 months at 4 °C and 30 °C indicated that the remaining number of viable cells in a BGPI-alginate capsule was significantly higher than that of free cells in both temperatures. It was demonstrated that the BGPI-alginate capsule could be utilized as a new probiotic carrier for enhanced gastrointestinal transit and storage applied in food and/or pharmaceutical products.

Characterization, Antioxidant and Antibacterial Potentials of Tamarindus indica L. Fruit Pulp Extract Loaded O/W Nanoemulsions

Abstract The main purposes of the current study were to formulate o/w nanoemulsions as a carrier for Tamarindus indica (tamarind) fruit pulp extract and to study the antioxidant and antibacterial potentials of nanoemulsions containing tamarind extract, focusing on cosmetic/hygiene applications. The o/w nanoemulsions using a mixture of Tween 80 and Span 80 as an emulsifier (5%w/w) were prepared by a high pressure homogenization process. Two concentrations of sweet tamarind extract, 3.3 and 6.6%w/w, based on the bioactivity study, were incorporated into the blank nanoemulsions to produce loaded nanoemulsions, F1-3.3TE (3.3%) and F1- 6.6TE (6.6%). As compared with the unloaded nanoemulsion, both tamarind extract loaded nanoemulsions showed reduced pH and significantly increased viscosity. Overall, the loaded nanoemulsions had droplet sizes of approximately 130 nm, zeta potential around -38 mV and polydispersity index (PDI) values less than 0.2. The nanoemulsion F1-3.3TE had better stability (e.g. significantly greater % tartaric acid content and lesser PDI value) than the nanoemulsion F1-6.6TE did. The antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl assay revealed that the nanoemulsions F1-3.3TE and F1-6.6TE had scavenging activities of 81.66 ± 0.77% and 63.80 ± 0.79%, respectively. However, antioxidant activity of these two formulations decreased under stress conditions (heating-cooling cycles). Such incidence did not occur for their antibacterial properties investigated by agar well diffusion technique. The two formulations exhibited inhibition zones of approximately 24.0-27.7 mm against Staphylococcus aureus and Staphylococcus epidermidis, responsible for malodor of underarms. The results suggest the potential of using sweet tamarind pulp extract loaded nanoemulsions as hygiene products.

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 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.

Characterization of mefenamic acid-guaiacol ester: stability and transport across Caco-2 cell monolayers.

PURPOSE: Prodrug of non-steroidal anti-inflammatory drugs (NSAIDs) or NSAIDs linked with guaiacol have been reported to suppress gastrointestinal (GI) toxicity or induce GI protective effect. In this study. mefenamic-guaiacol ester was synthesized and its physicochemical properties. stability, and transport across Caco-2 monolayers were investigated. METHODS: Synthesis of the ester was carried out using mefenamic acid, guaiacol. N. N'-dimethylaminopyridine, and N,N'dicyclohexylcarbodiimide. The hydrolysis of the ester was investigated in aqueous buffer solutions pH 1-12 as well as in Caco-2 homogenate, human plasma, and porcine liver esterase. Caco-2 cell monolayers were utilized for transport studies. Due to the high lipophilicity of the ester with a calculated logP of 6.15, bovine serum albumin (BSA, 4%) was included in the receiver compartment to obtain a good in vitro-in vivo correlation. Permeation of the ester was assessed with or without the exposure of cells to PMSF, an inhibitor of esterase. RESULTS: The ester was stable at a wide pH range from 1-10. However, it was hydrolyzed by enzymes from porcine liver esterase and Caco-2 homogenate. With the PMSF exposure on the apical (AP) side and in the presence of 4% BSA on the basolateral (BL) side, the transported amount of the ester from AP-to-BL direction was 14.63% after 3 hr with a lag time of 23 min. The Papp for the ester was 4.72 x 10(-6) cm s(-1). CONCLUSION: The results from hydrolysis studies indicate that this ester is a prodrug. The Papp value suggests the moderate absorption characteristic of the compound. The accumulation of this highly lipophilic ester in Caco-2 cells is reduced in the presence of BSA.