A novel snake venom-derived GPIb antagonist, anfibatide, protects mice from acute experimental ischaemic stroke and reperfusion injury.

Background And Purpose: Ischaemic stroke is a serious disease with limited therapy options. Glycoprotein (GP)Ib binding to von Willebrand factor (vWF) exposed at vascular injury initiates platelet adhesion and contributes to platelet aggregation. GPIb has been suggested as an effective target for antithrombotic therapy in stroke.

Protective effect of iridoid glycosides from Paederia scandens (LOUR.) MERRILL (Rubiaceae) on uric acid nephropathy rats induced by yeast and potassium oxonate.

Iridoid glycosides of Paederia scandens (IGPS) are an active component isolated from Chinese herb P. scandens (LOUR.) MERRILL (Rubiaceae).

Trans-resveratrol loaded chitosan nanoparticles modified with biotin and avidin to target hepatic carcinoma.

Conventional liver targeted system focuses on delivering drugs to liver, bringing toxicity on hepatic normal tissues. The purpose of this study is to construct a new system capable of specially targeting to hepatic carcinoma instead of the whole liver. Based on the fact that nanoparticles (NPs) bound with either biotin or avidin tend to accumulate in tumors and avidin-attached reagents were quickly eliminated from blood circulation and assembled in liver, trans-resveratrol loaded chitosan nanoparticles (CS-NPs), CS-NPs with the surface modified either by biotin (B-CS-NPs) or by both biotin and avidin (A-B-CS-NPs) were prepared and their physiochemical properties were investigated.

Quantification of aesculin in rabbit plasma and ocular tissues by high performance liquid chromatography using fluorescent detection: application to a pharmacokinetic study.

A simple and sensitive high performance liquid chromatography method with fluorescence detection (HPLC-FD) was described for the determination of aesculin (AL) at low concentrations in rabbit plasma and ocular tissues. After deproteinization by methanol using pazufloxacin mesilate (PM) as an internal standard (I.S.

Development of PLGA nanoparticles simultaneously loaded with vincristine and verapamil for treatment of hepatocellular carcinoma.

Hepatocellular carcinoma (HCC) is one of the malignant tumors with poor chemo-sensitivity to vincristine sulfate (VCR) due to multi-drug resistance (MDR). Combinations of encapsulated VCR and verapamil hydrochloride (VRP, a chemo-sensitizer) might be a potential strategy to improve HCC therapeutic efficacy of VCR. PLGA nanoparticles (PLGANPs) simultaneously loaded with VCR and VRP (CVn) were prepared.

Preparation, characterization, and in vivo evaluation of mitoxantrone-loaded, folate-conjugated albumin nanoparticles.

Folic acid was covalently conjugated to bovine serum albumin nanoparticles (BSANP) to target the nanoparticles to SKOV3 cells expressing folate receptors. Mitoxantrone was incorporated into the folate-conjugated albumin nanoparticles, and the final nanoparticle size was 68 nm, as measured by a laser light scattering particle analyzer. The cytotoxic activity of mitoxantrone- loaded, folate-conjugated albumin nanoparticles (MTO-BSANP-folate), which was quantitated by (3)H-thymidine incorporation, was higher than mitoxantrone-loaded BSANP (MTO-BSANP) and MTO solution, and could be inhibited by free folic acid.

Reversion of multidrug resistance by co-encapsulation of vincristine and verapamil in PLGA nanoparticles.

Multidrug resistant (MDR) cancer may be treated using combinations of encapsulated cytotoxic drugs and chemosensitizers. To optimize the effectiveness of this combinational approach, poly(d,l-lactide-co-glycolide acid) (PLGA) nanoparticles formulations capable of delivering a cytotoxic drug, vincristine, a chemosensitizer, verapamil, or their combination were prepared via combining O/W emulsion solvent evaporation and salting-out method. Moreover, this work evaluated a number of approaches for the administration of chemosensitizer-cytotoxic drug combinations in a systematic fashion.

[Studies on in vivo release of berberine hydrochloride from carboxymethyl konjac glucomannan pellets in rats].

Objective: To observe the absorption and concentration of berberine hydrochloride (BH) in gastric, entric, colonic tissue after intragastric administration of BH-containing carboxymethyl konjac glucomannan pellets for evaluating colon-specific drug delivery characteristics of the pellets.

Method: BH-containing carboxymethyl konjac glucomannan pellets (pellets group) and BH-containing carboxymethyl cellulose suspension (control group) were intragastric administrated to rats at the dose of 50 mg x kg(-1), respectively. A high performance liquid chromatography method determinated BH concentration in rat plasma and tissue.

[Effect of several penetration enharcers on transdermal permeation and skin accumulation of artemether].

Objective: To investigate penetration characteristics of artemether and the effect of different permeation enhancer on transdermal permeation of artemether through rat skin.

Method: The permeation experiments were performed using rat skin on modified Franz diffusion cells in vitro. The concentrations of artemether in receptor compartment at specified time points were determined by HPLC.

[Preparation of self-microemusifying drug delivery system for volatile oil from rhizome of ligusticum Chuanxiong].

Objective: To search on the optimum formula for the seif-microemulsifying drug delivery system of volatile oil from rhizome of ligusticum Chuanxiong.

Methods: Through solubility experiment, orthogonal screen and drawing phase diagram, taking the degree of emulsifying, the volume of the rest oil and emulsion particle size as parameters, the appropriate proportion composed of Chuanxiong oil, nonionic surfactant and flux was screened for the optimum formulation of self-microemulsifying drug delivery system.

Results: In the formulation of self-microemulsifying drug delivery system for volatile oil from rhizome of ligusticum Chuanxiong, taking S1 as the nonionic surfactant and C1 as the co-surfactant could get the best effect of emulsifying.

[Study on drug release of gastrodin ion-activated nasal in situ gel in vitro].

Objective: To study on the drug release characteristics and mechanism of gastrodin ion-activated nasal in situ gel in vitro.

Method: Regularity and mechanism of the drug release of gastrodin nasal in situ gel were studied by using the diffusion cell model and the membrane-less dissolution model, respectively. A novel kinesis diffusion cell model was designed according to the characteristics of release environment of nasal cavity.

[In vitro dexamethasone release from nanoparticles and its pharmacokinetics in the inner ear after administration of the drug-loaded nanoparticles via the round window].

Objective: To investigate the feasibility of local drug delivery into the inner ear using solid lipid nanoparticles (SLN) and evaluate its potential for inner ear disease treatment in terms of the pharmacokinetics of the delivered drug in the inner ear.

Methods: Dexamethasone acetate (DA)-loaded SLN was prepared with Compritol 888 ATO as the matrix by means of hot dispersion-ultrasonic technique. A high-performance liquid chromatography (HPLC) was established for determining DA and dexamethasone (Dex).

[Brain targeting of gastrodin nasal in situ gel].

Objective: To investigate the biodistribution of gastrodin ion-activated nasal in situ gel in rat blood and brain tissues and to evaluate its brain targeting.

Methods: Intravenous administration of gastrodin solution or intranasal administration of gastrodin nasal in situ gel were given to 32 rats, respectively. The concentrations of gastrodin in the plasma and gastrodigenin in the brain tissues of the rats were determined by HPLC.

[Comparison of kinetic behavior in both plasma and tissue after intravenous administration of alpha-asarone in lipid emulsion and aqueous solution in rats and mice].

Objective: To compare the pharmacokinetics and tissue distribution of alpha-asarone in lipid emulsion and aqueous solution for injection and study the feasibility of lipid emulsion of alpha-asarone as the parenteral drug delivery system.

Method: HPLC was used to determine the drug concentration in rat plasma and mice tissues after intravenous (i.v.

[Study on release mechanism of berberine hydrochloride-loaded carboxymethyl konjac glucomannan pellets for colonic delivery].

Objective: To study release mechanism of berberine hydrochloride (BH) from carboxymethyl konjac glucomannan pellets for colonic delivery.

Method: The pellets were prepared by ionotropic gelation technique. The effects of the kinds of enzyme and enzyme concentration of dissolution media on the release of BH and the erosion properties of the pellets were studied.

[Study on in vitro colon-specific enzymatic degradation performance of carboxymethyl konjac glucomannan].

Objective: In vitro enzymatic degradation of carboxymethy konjac glucomannan (CMKGM) were studied to evaluate the feasibility of CMKGM used as carrier materials to prepare colon-specific drug delivery systems.

Method: The solutions with rat gastrointestinal tract (GIT) contents or with commercial enzymes were chosen to stimulate in vivo GIT environment, respectively. Enzymatic degradation of CMKGM were studied by viscometic procedure.

[Preliminary study on brain-targeted drug delivery via inner ear].

The article investigates the feasibility of delivering drugs to brain via inner ear, and provides a novel route for delivering drugs to the brain tissues. Dexamethasone acetate (DA)-loaded solid lipid nanoparticles (SLN) was prepared by using Compritol 888 ATO as material. HPLC assays for the determination of DA, dexamethasone sodium phosphate (DSP) and dexamethasone (Dex) were developed, separately.

[Transdermal and lymph targeting transfersomes of vincristine].

Vincristine (VCR) is mainly used to treat acute lymphocytic leukemia, Hodgkin and non-Hodgkin lymphoma in clinic with definite therapeutic effect. But the obvious neurotoxicity and local stimulation of which limit its clinic use. In order to increase the lymph targeting to enhance the curative effect and to lower the adverse reaction of VCR, the VCR loaded transfersomes (VCR-T) were prepared with dry-film and ultrasonic dispersing methods, and the corresponding pharmaceutical properties, pharmacokinetical characteristics and the targeting ability were studied.

[In vitro evaluation of self-emulsifying drug delivery system of volatile oil from rhizome of Ligusticum chuanxiong].

Objective: To investigate the evaluation method for self-emulsifying drug delivery system of volatile oil from rhizome of Ligusticum chuanxiong (VOC SEDDS).

Method: The self-emulsifying ability, the efficiency of self-emulsification, the properties of emulsion, the dissolution of volatile oil from Rhizome of Ligusticum Chuanxiong and the stability of the emulsion were determined.

Result: The optimized formulation can fully emulsify in 5 min and the particle sizes were around 102 nm.

Determination of aesculin in rat plasma by high performance liquid chromatography method and its application to pharmacokinetics studies.

A sensitive and reproducible high performance liquid chromatography method with UV detection was described for the determination of aesculin in rat plasma. After deproteinization by methanol using metronidazole as internal standard (I.S.

Preparation, characterization and uptake by primary cultured rat hepatocytes of liposomes surface-modified with glycyrrhetinic acid.

3-succinyl-30-stearyl glycyrrhetinic acid (Suc-GLAOSt) was synthesized as a targeting molecule, and incorporated in ordinary to liposomes (LP) to prepare a liposome surface-modified with glycyrrhetinic acid (LP-GLA), which could bind to the hepatocyte through the specific binding site of glycyrrhetinic acid (GLA) on the surface of rat cellular membrane. The maximal molar ratio of Suc-GLAOSt to total lipids in LP-GLA was 1:10. Calcein loaded liposome (Cal-LP) and calcein loaded LP-GLA (Cal-LP-GLA) were prepared by an ethanol injection method.

[Preparation and characterization of biotinylated chitosan nanoparticles].

Biotinylated chitosan nanoparticles (Bio-CS-NP) were prepared for the active delivery to cancer cells and its characterization was investigated in this study. The preparation process included two steps. First, biotinylated chitosan ( Bio-CS ) was obtained through a reaction between sulfosuccinimidobiotin and chitosan (CS).

[Study on drug release in vitro and rat intestinal absorption of resveratrol nanoliposomes].

Objective: To study the release feature of Res-nanoliposomes in vitro and clarify the difference in absorption of Res-nanoliposomes from varied intestinal segments and the absorptive mechanism in vivo.

Method: Dialytic method was used to determine resveratrol release rate of Res-nanoliposomes in vitro. An in situ rat perfusion method was used to investigate the intestinal absorption of Res-nanoliposomes.

[Preparation of liposome entrapped vincristine sulfate and mitoxantrone chlorhydric acid].

Objective: To investigate the prepation of the liposome carried with vincristine sulfate (VCR) and mitoxantrone chlorhydric acid (MTO) and to evaluate the quality of the liposome.

Method: The liposome carried with VCR and MIT was prepared by pH-gradients method and reverse evaporation technique. HPLC was employed to determine VCR and MIT entrapping efficiency of liposomal.