Advance of hair follicle targeted drug delivery systems in the treatment of acne and hair loss / 药学学报

Hair follicle (HF), one of the skin appendages, has received a lot of attention to be a new target and pathway for drug delivery. The development of hair follicle targeted drug delivery system (HFTDDS) through percutaneous permeation is particularly important for skin diseases derived from HF such as acne, hair loss, and folliculitis for their on-site action. This review describes the structure and physiological function of HF, the microenvironment of HF, and factors affecting HF permeation. Multiple nanoformulations used to improve the HF permeation and technologies to characterize the HF permeation were introduced. The latest advance of HFTDDS based on nanoformulations were systematically summarized and analyzed in the treatment of acne and hair loss. Finally, the challenges of formulating HFTDDS were discussed. The review is expected to provide some ideas and references for developing delivery systems for treating skin diseases derived from HF.

Dexamethasone acetate microemulsions: formulation and effect on skin permeability / 药学学报

The present project was designed to optimize the microemulsion (ME) formulation of oil in water (O/W) for dexamethasone acetate (DA), and examine its impact on DA percutaneous permeation. The saturated solubility of DA in different oils, surfactants and co-surfactants was tested. The ratio of surfactant to co-surfactant was selected by constructing pseudo three phase diagrams to investigate the maximal microemulsion area. In vitro permeation studies of DA from microemulsion and suspension were performed to optimize the formulation further. Differential scanning calorimetry (DSC) and attenuated total reflection flourier transformed infrared spectroscopy (ATR-FTIR) were performed to investigate the mechanism of microemulsion action on skin. The optimized formulation was composed of oleic acid/Labrasol/propylene glycol/water with 8/45/15/32(w/w), and the DA loading was 0.75% (w/w). The permeation enhancement of microemusion was 6.00-fold as that of suspension, and the DA from microemulsion retained in the skin was 4.79-fold as that of suspension. DSC and ATR-FTIR results suggested that microemulsion could affect the intercellular lipid lamellae and keratin of the stratum corneum. The barrier function of stratum corneum was disordered by the microemulsion so that the dermal drug delivery was enhanced. Therefore, the optimized microemulsion enhanced DA percutaneous permeation significantly through the interaction of microemulsion with skin, microemulsion is a promising approach for DA percutaneous delivery.

In vitro targeting effect of lactoferrin modified PEGylated liposomes for hepatoma cells / 药学学报

A lactoferrin-containing PEGylated liposome system (Lf-PLS) was developed and tested in vitro as a hepatoma-targeting drug delivery system. PEGylated liposomes (PLS) were successfully prepared using the thin film hydration method with peglipid post insertion. Lf was covalently conjugated onto the carboxyl terminal of DSPE-PEG2000-COOH on liposomes. Coumarin-6 was used to trace Lf-PLS with fluorescence. The cellular uptake of this system was carried out in asialoglycoprotein receptor (ASGPR) positive HepG2 cells via confocal microscopy and flow cytometry. The Lf-PLS liposome was observed as spherical or oval vesicles with the particle size around 130 nm, zeta potential about -30 mV and encapsulation efficiency more than 80%. The confocal microscopy images and flow cytometry data demonstrated that Lf-PLS resulted in significantly higher cell association by ASGPR positive HepG2 cells compared to PLS. The association between Lf-PLS and cells were dependent on the concentration, time and temperature, which was inhibited by pre-incubation with excessive free Lf. The results suggest that Lf-PLS has a good targeting effect on HepG2 cells in vitro. The targeting mechanism may be related to the specific binding of Lf and ASGPR on HepG2 cells, which guides Lf-PLS to the cell surface to induce an active endocytosis process. All these results demonstrated that Lf-PLS might be a potential drug delivery system in targeting hepatocellular carcinoma, which deserves more research on its targeting ability, antitumor efficiency, and metabolism in vivo for treatment of hepatomacellular carcinoma.

Diagnostic Value of (18)F-FDG-PET/CT for Multiple Myeloma / 中国实验血液学杂志

<p><b>OBJECTIVE</b>To study the diagnostic value of (18)F-FDG-PET/CT in multiple myeloma (MM).</p><p><b>METHODS</b>A total of 66 patients, who were highly suspected of MM in our hospital from July 2012 to December 2014, were chosen as study objects. All patients were diagnosed or excluded by pathological examination. All patients were detected by (18)F-FDG-PET/CT, and its diagnostic value was analyzed. The number of focuses were counted.</p><p><b>RESULTS</b>Out of 66 patients 59 patients (89.39%) were diagnosed with multiple myeloma. The sensitivity of PET was 98.31%, the specificity of PET was 85.71%, the Youden index was 0.8402; the sensitivity of CT was 96.61%, the specificity of CT was 85.71%, the Youden index was 0.8232; the sensitivity of PET/CT was 100.00%, the specificity of PET/CT was 83.33%, the Youden index was 0.8333. In 59 MM patients, 635 focuses were detected, out of them 572 focuses (90.08%) were detected by CT, 593 focuses (93.39%) were detected by PET, 530 focuses (83.46%) were coincided on PET/CT.</p><p><b>CONCLUSION</b>(18)F-FDG-PET/CT has diagnostic value for multiple myeloma, and it can be used in locating and counting focuses, as well as in evaluating the treatment efficacy and guiding the clinical work.</p>

Antidiarrheal properties of different extracts of Chinese herbal medicine formula Bao-Xie-Ning / 中西医结合学报

<p><b>OBJECTIVE</b>Bao-Xie-Ning (BXN), a traditional Chinese herbal medicine (CHM) formula composed of Fructus Evodiae, Flos Caryophylli and Cortex Cinnamomi, and used for the treatment of infant diarrheal illness, was subject to systematic assessment for its putative multiple pharmacodynamic effects and pharmacological antidiarrheal mechanisms.</p><p><b>METHODS</b>High-performance liquid chromatography-diode array detector-electrospray ionization-mass spectrometric/mass spectrometry was developed and validated for identification and quantification of the main constituents in different extracts of BXN. Male Kunming mice weighing 20 to 25 g were used for detecting the antidiarrheal activity of the extracts. Ethanolic extract (EE), volatile oil extract (VOE), and aqueous extract (AE) of BXN were respectively subjected to pharmacodynamic and pharmacological comparison in assessing antidiarrheal effects with senna-induced diarrhea, castor oil-induced diarrhea, acetic acid-induced writhing assay, and isolated duodenum test.</p><p><b>RESULTS</b>The highest yields of three detected components of BXN, rutaecarpine, eugenol and cinnamaldehyde were observed in EE. EE showed the most remarkable antidiarrheal activity in dose-dependent and time-dependent manners in both senna- and castor oil-induced diarrhea models, and presented dose-dependent analgesic activity in acetic acid-induced algesthesia model. In addition, EE extract of BXN also exhibited strong antimobility action on the intestine and strongest depression on spontaneous contraction of isolated duodenum.</p><p><b>CONCLUSION</b>Ethanol extraction is an efficient method to extract the active constituents of BXN. BXN extract demonstrated multiple pharmacological activities affecting the main mechanisms of diarrhea, which validated BXN's usage in the comprehensive clinical treatment of diarrhea.</p>

In vivo imaging in tumor-bearing animals and pharmacokinetics of PEGylated liposomes modified with RGD cyclopeptide / 药学学报

The hydroxycamptothecin (HCPT) PEGylated liposomes (HCPT-LP) were modified with RGD cyclopeptide formed the tumor-targeting liposomes (HCPT-RGD-LP). HCPT-LP and HCPT-RGD-LP were injected intravenously with single dose of 5 mg x kg(-1) to rats. The drug concentration in plasma was determined and the pharmacokinetic behaviour was compared. The HCPT distribution in heart, liver, spleen, lung, kidney and plasma of mice was investigated following intravenous administration of HCPT-LP and HCPT injection. The nude mice implanted human hepatoma HepG2 cells were studied by in vivo imaging. The fluorescent probe was DiR and the nude mice were injected with DiR PEGylated liposomes (DiR-LP) and DiR-LP modified with RGD cyclopeptide (DiR-RGD-LP). The results showed that there was no significant difference (P > 0.05) of main pharmacokinetic parameters t1/2beta, CL, V(c), AUC(0-48 h), AUC(0-inifinity), MRT(0-48 h), MRT(0-infinity) between HCPT-RGD-LP and HCPT-LP. HCPT-LP had a remarkably better long-circulating effect than HCPT injection in mice and the concentration of HCPT was highest in liver. The DiR accumulation in tumors of DiR-RGD-LP was higher than that of DiR-LP by the visualized fluorescence of in vivo imaging. It indicated that such PEGylated liposomes modified with RGD cyclopeptide could improve the tumor targeting efficacy.

In vitro study of transdermal penetration and iontophoresis of hepatitis B vaccines through rat skin / 药学学报

In vitro percutaneous delivery of hepatitis B vaccines was investigated in order to assess the penetration of vaccine under passive diffusion and iontophoresis conditions. The study was carried out using Franz vertical diffusion cell through the hairless abdominal skin of Sprague-Dawley (SD) rats. Enzyme-linked immunosorbent assay (ELISA) was used to determine the cumulative amount of permeation and the retention amount of drug in skin. Passive diffusion alone resulted in less skin permeation and retention of hepatitis B vaccines, only (2.1 +/- 0.1) ng x cm(-2) and (2.3 +/- 0.1) ng x cm(-2) after 24 h when the initial concentration of vaccine in the donor compartment was 23 microg x mL(-1) and 46 microg x mL(-1), respectively. After removing the stratum corneum, the permeation and retention amount of hepatitis B vaccines increased to (383.7 +/- 86.2) ng x cm(-2) and (16.8 +/- 4.6) ng x cm(-2), respectively, 171.6-folds and 2.1-folds more than that from its intact skin with the drug loaded at 46 microg x mL(-1). Iontophoresis induced a significant increase of cumulative and retention amount of hepatitis B vaccines through the skin (P < 0.05). Application of iontophoresis significantly enhanced the permeation of hepatitis B vaccines (P < 0.05) by 2.7-folds and 6.6-folds for the intact skin, and by 1.6-folds and 1.8-folds for the tape-stripped skin with initial drug loading of 23 microg x mL(-1) and 46 microg x mL(-1), respectively. Iontophoresis also significantly increased the amount of drug retained in the skin. After applying iontophoresis for 6 h, the amount of skin retention was nearly the same as passive diffusion for 24 h both from intact skin [(16.8 +/- 4.6) ng x cm(-2) vs (13.3 +/- 5.4) ng x cm(-2)] (P > 0.05) and tape-stripped skin [(36.7 +/- 14.1) ng x cm(-2) vs (26.8 +/- 11.2) ng x cm(-2)] (P > 0.05). Overall, these findings revealed that the transportation efficiency of bioactive substance like hepatitis B vaccines may be improved by iontophoresis, which can be potentially used in the field of transcutaneous immunization.

Effect of composite salvia injection on platelet parameters in children with anaphylactoid purpura / 中国结合医学杂志

<p><b>OBJECTIVE</b>To explore the effect of composite salvia injection (CSI) on platelet parameters in children with anaphylactoid purpura (AP) and its clinical significance.</p><p><b>METHODS</b>One hundred and fifty children with AP were assigned to two groups, 80 in Group A and 70 in Group B. They were treated, respectively, with conventional therapy only or conventional therapy combined with CSI. Their platelet parameters, including blood platelet count (BPC), mean platelet volume (MPV), platelet distribution width (PDW) and plateletcrit (PCT) were determined at the acute stage and convalescent stage, respectively.</p><p><b>RESULTS</b>At the acute stage, the BPC in AP children of both groups was in the normal range, but significant abnormality was shown in the levels of MPV, PDW and PCT. As for comparisons of these parameters at the convalescent stage, significant difference between the two groups was also shown in terms of MPV, PDW and PCT (P<0.05 or P<0.01).</p><p><b>CONCLUSION</b>Although platelet shows no quantitative change in the pathogenic process of AP, important functional changes are surely existent. CSI could promote the normalization of platelet function.</p>

Significance of Changes of Serum Beta 2-Microglobulin,Cytocine Levels in Childhood Idiopathic Thrombocytopenic Purpura / 实用儿科临床杂志

Objective To study the changes and significance of serum beta 2-microglobulin(?2-MG),cytocine interleukin-2(IL-2) in the clinical progress of childhood idiopathic thrombocytopenic purpura(ITP).Methods One hundred and ten patients of childhood ITP were chosen for the test group(70 cases of primary ITP and 40 cases of recurrent ITP),and 110 normal children for the control group.Levels of serum ?2-MG and IL-2 were determined by radioimmunoassay kit and analysed with two sample t-test.Results Among the patients,the serum IL-2 levels were significantly lower and serum ?2-MG levels were significantly higher than those in control group(P0.05).Conclusion Determining serum IL-2 and ?2-MG levels has important significance to reflect the progress of disease and direct treatment.

Solubilization on cryptotanshinone by hydroxypropyl-beta-cyclodextrin and preparation of their inclusion compound / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare cryptotanshinone (CT)-cyclodextrin inclusion compound and improve dissolution of CT.</p><p><b>METHOD</b>Inclusion ratio was determined by plotting the phase solubility curve of CT versus hydroxypropyl-beta-cyclodextrin (HPCD). CT-cyclodextrin inclusion compound was made by wet grinding method. Properties of the inclusion compound was investigated by in vitro dissolution test, DTA and IR spectrum.</p><p><b>RESULT</b>Inclusion ratio of CT versus HPCD was 1:1. Dissolution of CT-HPCD inclusion compound at 45 min was 21.6 times of material drug.</p><p><b>CONCLUSION</b>Dissolution of CT was improved remarkably in CT-HPCD inclusion compound. The complexation force of the inclusion compound was hydrogen bond formed by carbonyl group of CT and hydroxyl group of HPCD.</p>

Review and analysis of present status of the micronization of Chinese traditional medicine / 中国中药杂志

Micronization is one of the methods to improve the solubility and bioavailability of drug, the micronization of TCM is a new techonology of TCM mordenization. status in quo of TCM micronization was reviewed and analyzed. Effects of micronization on the dissolution of active ingredients and pharmacological action were widely studied, however some fundmental aspects, such as engineering factors of superfine powder preparation, stability of them and the optimal particle size, are urgently to be studied.