Layered dissolving microneedles as a need-based delivery system to simultaneously alleviate skin and joint lesions in psoriatic arthritis

Psoriatic arthritis (PsA) is a complicated psoriasis comorbidity with manifestations of psoriatic skin and arthritic joints, and tailoring specific treatment strategies for simultaneously delivering different drugs to different action sites in PsA remains challenging. We developed a need-based layered dissolving microneedle (MN) system loading immunosuppressant tacrolimus (TAC) and anti-inflammatory diclofenac (DIC) in different layers of MNs,

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.

Comparative pharmacokinetics of tetramethylpyrazine phosphate in rat plasma and extracellular fluid of brain after intranasal, intragastric and intravenous administration

The purpose of this study was to compare the pharmacokinetic profiles of tetramethylpyrazine phosphate (TMPP) in plasma and extracellular fluid of the cerebral cortex of rats via three delivery routes: intranasal (i.n.), intragastric (i.g.) and intravenous (i.v.) administration. After i.n., i.g. and i.v. administration of a single-dose at 10 mg/kg, cerebral cortex dialysates and plasma samples drawn from the carotid artery were collected at timed intervals. The concentration of TMPP in the samples was analyzed by HPLC. The area under the concentration-time curve (AUC) and the ratio of the AUCbrain to the AUCplasma (drug targeting efficiency, DTE) was calculated to evaluate the brain targeting efficiency of the drug via these different routes of administration. After i.n. administration, TMPP was rapidly absorbed to reach its peak plasma concentration within 5 min and showed a delayed uptake into cerebral cortex (t max=15 min). The ratio of the AUCbrain dialysates value between i.n. route and i.v. injection was 0.68, which was greater than that obtained after i.g. administration (0.43). The systemic bioavailability obtained with i.n. administration was greater than that obtained by the i.g. route (86.33% vs. 50.39%), whereas the DTE of the nasal route was 78.89%, close to that of oral administration (85.69%). These results indicate that TMPP is rapidly absorbed from the nasal mucosa into the systemic circulation, and then crosses the blood-brain barrier (BBB) to reach the cerebral cortex. Intranasal administration of TMPP could be a promising alternative to intravenous and oral approaches.

Optimization of Extraction Process for Yinxiejing / 中国药师

Objective:To study the optimal extraction process of Yinxiejing. Methods: An orthogonal experimental method was used with reflux time, reflux times, ethanol concentration and volume as the influencing factors, and emodin and osthole content as the indices. Results:The optimal extraction conditions for Yinxiejing were as follows:refluxing twice with 2 h every time using 8-fold 80%ethanol. Conclusion:The optimum process is stable and feasible.

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

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.

Tetrahydropalmatine's permeative properties of acupoint and non-acupoint transdermal administration of Baijiezi Tufang in vitro and in vivo / 中国中药杂志

<p><b>OBJECTIVE</b>To study tetrahydropalmatine's permeative properties of acupoint and non-adupoint transdermal administration of baijiezi tufang in vitro and in vivo.</p><p><b>METHOD</b>Taking tetrahydropalmatine as an evaluative component to assess the permeative of baijiezi tufang in acupoint skin and non-acupoint skin with the modified Franz diffusion cell method and in vivo penetration studies. The content of tetrahydropalmatine was determined by a HPLC method.</p><p><b>RESULT</b>The 24 hours cumulative permeation amount through acupoint skin was (13.53 +/- 3.92) microg x cm(-2), about 4 times higher than non-acupoint skin. The steady-state infiltration rates of tetrahydropalmatine in acupoint skin was (0.659 1 microg x cm(-2) x h(-1)), 4.5 times higher than non-acupoint skin. The content in acupoint skin was signally higher than that in non-acupoint skin (P < 0.05). An accumulation of fluorescence can be clearly seen in the four layers: stratum corneum > viable epidermis > dermis > subcutaneous.</p><p><b>CONCLUSION</b>In vitro and in vivo studies show that the permeation of baijiezi tufang in acupoint skin was better than in non-acupoint skin, following a higher cumulative amount and skin content.</p>

Clinical significance of virus infection and serum interleukin-2 levels in recurrent childhood idiopathic thrombocytopenic purpura / 中国综合临床

Objective To study the clinical significance of vires infection and serum interleukin-2 (IL-2)Ievels in recurrent childhood idiopathic thrombocytopenic purpura(ITP).Methods The cytomegalovirus(CMV),epstein-Barrvirus(EBV)-adenovirus(ADV),herpesvirus(HSV)antibodies ISM and IL-2 levels were determined in the serum of 4 childhood with recurrent childhood ITP as well as in 40 normal controls with ELISA and RIA.Re-sults The CMV-lgM positive cases were 18,EBV-IgM were 14-ADV-IgM were 5,HSV-lgM were 3.In the controls,those were 3,2,1,and 0 respectively(P<0.05 or P<0.01).The serum IL-2(0.35±0.12)μg/L levels were sig-nificantly lower than those in the controls[(0.61±0.17)μ/L,P<0.05].Conclusion DNA virus antibodies and IL-2 levels can reflect virus infection and immune condition of diseases in recurrent childhood ITP.It is impor-rant to comprehend the mechanism of recurrent childhood ITP for guiding clinical treatment.

Preparation and evaluation of self-microemulsifying drug delivery systems with tanshinone Ⅱ_A / 中草药

Objective The self-microemulsifying drug delivery system(SMEDDS) with tanshinone ⅡA was prepared in order to develop its new dosage forms.Methods Pseudo ternary phase diagrams were used to evaluate the self-microemulsification existence area under emulsifier,coemulsifer,and oil phase.The HPLC analysis in vitro was set up.Solubility in various vehicles was determined.The self-microemulsification efficiency was assessed,such as stability,particle size,and Zeta potential.Results The solubi-lity of tanshinone ⅡA in SMEDDS was about 2.5 mg/g,droplet size was within 20 nm,and the absolute value of Zeta potential was over 60 mV.The stability of SMEDDS with tanshinone ⅡA was better in centrifugal condition with high temperature but not good enough to the light.Conclusion The SMEDDS can make tanshinone ⅡA solublized in water,and is an optimum vehicle in new dosage forms of tanshinone ⅡA.

Permeability of integerrimine in vitro / 中草药

Object The permeability of integerrimine was studied in vitro to design its anticancer preparations Methods Vilia Chien diffusion cells were adopted as apparatus for in vitro skin permeation, nude mouse skins were used as permeation barrier and permeation coefficient (P) was calculated The concentrations of integerrimine in samples were measured by RP HPLC, and the effects of Azone, 4% Tween 80, 8% propylene glycol on it were studied Results Its P is 1 184?10 -2 cm/h with water solution as donor and pH 6 8 PBS as receptor Its enhancement rate (ER) of 2% Azone and 8% propylene glycol is 2 8 and 1 5, while Tween 80 inhibits its penetration Conclusion Integerrimine is a good candidate of antiskin cancer for transdermal drug delivery, and the optimal formulation can be designed according to the experiments

Influence of gel vehicles on release in vitro and transdermal resorption of integerrimine / 中成药

AIM: The gel vehicle was optimized by release and transdermal resorption of integerrimine in vitro in order to design its anti-cancer transdermal drug delivery system. METHODS: The releasing rate was detected by dissolution Vilia-Chien diffusion cells, nude mouse skin were used as permeation barrier, the concentration of integerrimine in samples was measured by RP-HPLC. RESULTS: Integerrimine releases of three different vehicles conformed to Higuchi equation, the releasing rate of CMC-Na gel is faster than that of HPMC gel, and that of Carbopol gel is the slowest in three, and corresponded with zero kinetic equation. CONCLUSION: HPMC is an drug vehicle of choice.

Effect of micronization on the powder characteristic of Angelica Sinennsis and extraction of ferulic acid / 中成药

AIM: The powder characteristic, water and ethanol extraction amount, extraction amount of active ingredient ferulic acid were comparatively studied between crude powder and micronized powder to explore the application of micronization technology to Angelica Sinennsis. METHODS: Angelica Sinennsis powder was characterized by laser diffraction analyzer and scanning electron microscopy, the angle of repose and bulk density were measured, the water and ethanol extraction were quantified by cooled and heated extraction, the active ingredient ferulic acid was detected by RP HPLC after it released from Angelica Sinennsis. RESULTS: The differences of particle characteristic and surface morphology between the crude and superfine powder were significant, however, water and enthanol extraction amount were not increased markedlky, the dissolution amount of ferulic acid was almost the same. CONCLUSION: Pharmaceutical characteristic of Angelica Sinennsis powder is affected by micronization, but its bioavailability is not improved. Micronization technology is not suitable to Angelica Sinennsis.