Antibacterial action and sensitization by percutaneous administration of lavender essential oil / 中国热带医学

@#Abstract: Objective To investigate the antibacterial action and skin sensitization by percutaneous administration of lavender essential oil (LEO), providing a basis for its antibacterial application of percutaneous administration. Methods The disk diffusion method was used to evaluate the antibacterial effect of LEO on five types of bacteria, and to measure its minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC); The effect of LEO on guinea pig skin irritation was observed by topical application, and its allergic reaction and allergic rate were evaluated; the levels of IgA, IgG, and IgE in the supernatant of serum and spleen tissue sensitized with dimethylbenzene and smeared with LEO were determined by the enzyme-linked immunoassay (ELISA), and the antibacterial ability, skin sensitization, and inflammation of LEO were comprehensively evaluated. Results The antibacterial circle experiment showed that LEO had an inhibitory effect on Staphylococcus epidermidis, Escherichia coli, Candida albicans, Staphylococcus aureus, and Propionibacterium acnes; the antibacterial ability from strong to weak was Staphylococcus Epidermidis (8.25 mg/mL), Escherichia coli (15.00 mg/mL), Candida albicans (16.31 mg/mL), Staphylococcus aureus (18.00 mg/mL), Propionibacterium acnes (20.78 mg/mL). The percutaneous administration of LEO did not cause skin sensitization and inflammatory reaction in guinea pigs. Compared with the blank group, the effect of topical LEO application on the weight of the guinea pig's spleen is not statistically significant (P>0.05), and the effect on the levels of IgA, IgE, IgG in the serum and spleen tissue of guinea pigs is not statistically significant (P>0.05). Conclusions LEO has a certain antibacterial effect on five common pathogenic bacteria such as Staphylococcus epidermidis, Escherichia coli, Candida albicans, Staphylococcus aureus and Propionibacterium acnes, and is safe for percutaneous administration. The results provide some reference for the development of LEO related products and their application in the field of dermatology.

Chronic Toxicity of Triptolide and Ferulic Acid Ethosomes Gel for Percutaneous Administration / 中国实验方剂学杂志

ObjectiveTo investigate the long-term safety of triptolide ferulic acid ethosome gel in percutaneous administration. MethodWe mixed triptolide with ferulic acid to make liposomes gel in different doses and then administrated the gel to SD rats of both sexes with intact skin and damaged skin for 12 weeks. The daily dosages calculated based on triptolide for the low-， middle-， and high-dose groups were 63.75， 127.50， 255.00 μg·kg-1， respectively. The body weight of each rat was measured weekly. The rats were sacrificed in the last week for the determination of serum biochemical parameters and organ indexes as well as the observation of histopathology. The toxicity was assessed based on the body weight and all the parameters and indexes. ResultAfter long-term administration， the body weight and serum biochemical parameters did not show significant difference between the gel-treated groups and the blank group with intact skin， which indicated that the percutaneous administration of triptolide and ferulic acid ethosomes gel was relatively safe. However， the rats in the high-dose group showed sparse hair and were easy to die in the case of unhairing with chloral hydrate at the late stage of the study. Comprared with the female rats with intact skin in the blank control group， the female rats with damaged skin in the middle-dose group showed decreased heart index （P<0.05）， which indicated certain cardiotoxicity. Moreover， damage appeared in skin and lung， which may be influeneced by dosage， sex， and skin state. ConclusionFerulic acid in combination with triptolide is relatively safe for percutaneous administration， whereas there are some risks of skin and lung damage in the case of long-term administration. Individualized administration scheme should be developed according to liver and kidney function and skin conditons to ensure the safety of clinical medication.

The determination of diflucortolone in rabbit plasma by liquid chromatography-tandem mass spectrometry (LC-MS/MS) / 药学学报

A sensitive and efficient liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for quantitative determination of diflucortolone in rabbit plasma after dermal administration of diflucortolone valerate cream to rabbits. After extraction with ethyl acetate, the chromatographic separation was performed on Zorbax Eclipse XDB-C18 (50 mm×4.6 mm, 5 μm) with a gradient mobile phase consisting of 50% acetonitrile-50% methanol and 0.1% formic acid-5% methanol-5 mmol·L-1 ammonium formate at a flow rate of 0.35 mL·min-1. The quantitative analysis was carried out using multiple reaction monitoring (MRM) at specific ion transitions of m/z [M+H]+ 395.2→m/z 355.2 for diflucortolone and m/z [M+H]+ 258.1→m/z 120.9 for ethoxyphenylethylamine (internal standard) in positive ion mode with electrospray ionization (ESI) source. This validated LC-MS/MS method had a linearity over the concentration range of 0.01-10 ng·mL-1 with the lower limit of quantification (LLOQ) at 0.01 ng·mL-1. At level of LLOQ, the inter and intra-assay precision (RSD) were no greater than 9.82% and 11.0%, respectively. The main pharmacokinetic parameters of the diflucortolone including tmax, Cmax, AUC0-72 h, and t1/2 were as follows: (6.33±1.21) h, (0.168±0.080 0) ng·mL-1, (3.15±0.834) h·ng·mL-1, (32.0±17.4) h. The method was validated in the pharmacokinetic study of diflucortolone in rabbit following dermal administration of diflucortolone valerate cream at dose of 0.01 g·cm-2. In this study, the program of animal testing had been approved by Committee on the management and usage of experimental animal in the Evaluation Company of Innovative Drug, Tianjin Institute of Pharmaceutical Research.

Percutaneous ethanol injection versus conservative treatment for benign cystic and mixed thyroid nodules

ABSTRACT Objective To evaluate the efficacy and safety of percutaneous ethanol injection (PEI) in reducing the volume of cystic and mixed thyroid nodules. Materials and methods A total of 36 patients with nodules treated with PEI and 13 individuals who declined PEI and were followed clinically or received other non surgical treatment (control group). Assessments were performed at baseline (immediately before treatment in the PEI group or evaluation of the nodule on ultrasonography in the control group) at short-term (on average 30 days after the last injection in the PEI group), and long-term (on average 14 months after baseline in the PEI group or 26 months after baseline in the control group). Results In the PEI group, the mean baseline volume of 10.4 ± 9.8 cm3 reduced at short-term follow-up to 2.9 ± 3.1 cm3 (67.7 ± 19.9%, p < 0.001) and at long-term follow-up to 2.0 ± 2.5 cm3 (78.2 ± 19.5%, p < 0.01 versus baseline and p = 0.009 versus short-term follow-up). Both types of nodules showed similar degrees of reduction. In the control group, mean volume was 5.8 ± 3.4 cm3 at baseline and 6.2 ± 3.0 cm3 at long-term follow-up (p = 0.507). Compared with the control group, the PEI group showed larger reduction (p < 0.001). Conclusions PEI is effective in reducing the volume of cystic and mixed benign thyroid nodules, with sustained long-term efficacy and better outcome when compared with conservative therapies. Treatment with PEI is a safe alternative, with minimal, transient and self-limited adverse events.

Analysis of pharmacokinetic characteristics of low molecular weight heparin gel after transdermal adminstration by in vivo microdialysis technique combined with colorimetric method / 中国药学杂志

OBJECTIVE: To determine the concentrations of low molecular weight heparin (LMWH) in dermal and plasma of rats after administration of LMWH gel to evaluate its pharmacokinetic characteristics. METHODS: The rats were treated with abdominal hair removal, followed by administrating LMWH gel. The concentrations of LMWH in the dermal of rats at different time points were measured by microdialysis technique combined with colorimetric method, and the concentrations of LMWH in the blood of rats at different time points were measured by cutting-tail method and Coatest Heparin Kit. RESULTS: The LMWH tmax in dermis was 270 min, tmax was (4.40 ± 0.54) IU · mL-1, t1/2 was (137.04 ± 87.98) min, AUC0-t, was (911.76 ± 330.69) IU · mL · min-1, MRT0-t was (322.67 ± 40.94) min; the LMWH tmax in plasma was 540 min, cmax was (2.23 ± 0.40) IU · mL-1, t1/2 was (294.99 ± 183.74) min, AUC0-t was (110.59 ± 212.41) IU · mL · min, MRT0-t, was (422.48 ± 52.96) min after LMWH gel was percutaneous administrated. CONCLUSION: In vivo microdialysis technique combined with colorimetric method can be used for the evaluation of pharmacokinetic characteristics of LMWH gel. The method has the advantages of simple operation with high sensitivity and specificity. LMWH gel have the characteristics of slow transdermal penetration speed and stabilized concentration.