A combination of receptor mediated transcytosis and photothermal effect promotes BBB permeability and the treatment of meningitis using itraconazole.

Fungal infections of the central nervous system (CNS) may lead to life-threatening meningitis. Itraconazole (ITZ) is an effective antifungal agent that can be used to treat various fungal infections; however, its poor solubility along with poor permeability of the blood-brain barrier (BBB) prevents it from treating meningitis. Receptor mediated transcytosis (RMT) shows modest efficacy in BBB crossing, while affinity and saturability of interactions between ligands and receptors account for the limited efficacy of RMT in crossing the BBB.

[Pathogenesis of steroid-resistant asthma and the influence of vitamin D].

Glucocorticoid (GC) is currently the most effective drug for controlling persistent asthma; however, there is a significant difference in the response to GC among patients with asthma. Steroid-resistant asthma is one of the subtypes of asthma and has poor response to high-dose GC treatment. It may affect the quality of life of patients and even threaten their lives.

Mitochondria-targeted drug delivery system for cancer treatment.

Mitochondria are one type of the major organelles in the cell, participating in a variety of important physiological and biochemical processes, such as tricarboxylic acid cycle, fatty acid metabolism and oxidative phosphorylation. Meanwhile, it also happens to be the key regulator of apoptosis by triggering the complex cell-death processes through a variety of mechanisms. Since it plays a pivotal role in cell-death, a mitochondria-targeted treatment strategy could be promising for cancer therapy.

Conversion of mild cognitive impairment to dementia among subjects with diabetes: a population-based study of incidence and risk factors with five years of follow-up.

Type 2 diabetes mellitus (T2DM) is associated with dementia. Mild cognitive impairment (MCI) is a key determinant in this association. It is not clear whether T2DM increases the risk of conversion from MCI to dementia.

Pharmacokinetics of orally disintegrating tablets of perphenazine/hydroxypropyl-beta-cyclodextrin inclusion complex in rabbits.

We investigated the pharmacokinetic behavior of orally disintegrating tablets (ODTs) containing perphenazine/hydroxypropyl-beta-cyclodextrin inclusion complex (PPZ/HP-beta-CD) in rabbits and evaluated their bioequivalence with conventional tablets. In this study, a simple, sensitive and accurate high performance liquid chromatography method was developed for the determination of perphenazine concentration in rabbit plasma. The pharmacokinetic parameters were calculated by non-compartmental methods and the bioequivalence between PPZ/HP-beta-CD ODTs with conventional tablets was determined by calculating 90% confidence interval (CI) for the ratio of logarithmic transformed C(max), AUC(0-t), AUC(0-infinity) values.

Development of brucine-loaded microsphere/thermally responsive hydrogel combination system for intra-articular administration.

Intra-articular drug delivery system could directly deliver a drug to an affected joint and offer the possibility of reaching high drug concentrations at the site of action with limited systemic toxicity. However, depending on their chemical structure, some active compounds were rapidly cleared from the joint, thus requiring numerous injections, which could cause infection or joint disability. To control the release behavior for prolonged time periods, a novel biologically based drug delivery vehicle was designed for intra-articular using microsphere/thermally responsive hydrogel combination system in this paper.

Novel materials which possess the ability to target liver cells.

Introduction: Hepatic-targeted drug delivery systems are designed to treat diseases of the liver. However, since there are several different types of liver diseases that are caused by different cells, it is important to select the proper materials to target these different cells.

Areas Covered: This review addresses novel materials that possess the ability to target liver cells via receptor-ligand processes and offers an insight into the aspects of formulation design.

[Study on the pharmacokinetics Oxytropis falcate total flavonoids ointment in rats].

Objective: To study the pharmacokinetics of Oxytropis falcate total flavonoids ointment after transdermal administration in rats.

Methods: The content of 2',4'-dihydroxychalcone (TFC) in plasma was determined by high performance liquid chromatography. The concentration was determined at various time and the data was processed by 3P97.

[Water in oil microemulsions containing NaCl for transdermal delivery of fluorouracil].

This study is to prepare the W/O microemulsion containing NaCl and fluorouracil (5-Fu) as a model drug to investigate the transdermal characteristics and skin irritation of the microemulsion in vitro. Isopropylmyristate (IPM) acting as oil phase, Aerosol-OT (AOT) as surfactant, Tween 85 as cosurfactant, NaCl solution was added dropwise to the oil phase to prepare W/O microemulsion at room temperature using magnetic stirring, and then 5-Fu powder was added. According to the area of microemulsion based on the pseudo-tertiary phase diagrams, the optimum formulation was screened initially.

[Microemulsion-based gel of fluorouracil for transdermal delivery].

This study is to prepare the microemulsion-based gel based on the W/O microemulsion and fluorouracil (5-Fu) as a model drug to study the transdermal characterization and observe its skin irritation of the microemulsion-based gel in vitro. IPM acted as oil phase, AOT as surfactant, Tween 85 as cosurfactant, water was added dropwise to the oil phase to prepare W/O microemulsion at room temperature using magnetic stirring, then 5-Fu powder was added. The gelatin was used as substrate to prepare 5-Fu microemulsion-based gel.

The studies of anti-inflammatory and analgesic activities and pharmacokinetics of Oxytropis falcate Bunge extraction after transdermal administration in rats.

The aim of this study was to evaluate the activities of anti-inflammatory and analgesic of the total flavonoids extraction from Oxytropis falcate Bunge (FEO) after transdermal administration. The pharmacokinetics and absolute bioavailability of FEO in rat, furthermore, was studied. Firstly, the anti-inflammatory and analgesic effects of the FEO were studied by xylene-induced ear edema, adjuvant-induced joint inflammation law in rats, acetic acid-induced writhing and hot-plate tests in mice.

Socioeconomic status is a critical risk factor for human rabies post-exposure prophylaxis.

The socioeconomic status of the patients is the important factor for post-exposure prophylaxis (PEP). However, few investigations were designed to study the correlation between the socioeconomic status and PEP. This study set out to determine the importance of socioeconomic status for PEP.

Comparative pharmacokinetics and bioavailability studies of quercetin, kaempferol and isorhamnetin after oral administration of Ginkgo biloba extracts, Ginkgo biloba extract phospholipid complexes and Ginkgo biloba extract solid dispersions in rats.

The aim of this study was to improve the oral bioavailability of Ginkgo biloba extract (GBE) through preparing G. biloba extract phospholipid complexes (GBP) and G. biloba extract solid dispersions (GBS).

Synthesis of a novel polymer bile salts-(polyethylene glycol)2000-bile salts and its application to the liver-selective targeting of liposomal DDB.

Purpose: The objective of this study was to achieve a sustained and targeted delivery of liposome to the liver, by modifying the phospholipid [phosphatidylcholine (PC)/cholesterol (10 : 1) liposomes with a novel polymer bile salts-(polyethylene glycol)(2000)-bile salts (BP(2)B).

Methods: First, we generated a novel BP(2)B by N,N'-dicyclohexylcarbodiimide/4-dimethylaminopyridine esterification method and confirmed by Fourier transform infraredand (1) H-NMR spectra. Second, we prepared the BP(2)B-modified liposomes (BP(2)BL) that included BP(2)B, and the effect of the weight ratios of BP(2)B/PC on entrapment efficiency was investigated and BP(2)B/PC = 3% (w/w) was determined as the optimum ratio for the 4,4'-dimethoxy-5,6,5',6'-bi (methylenedioxy)-2,2'-bicarbomethoxybiphenyl liposomes.

[The enhancing effect of borneol on the absorption of tetramethylpyrazine].

To explore the mechanism of the absorption enhancement of borneol, the effect of borneol on the intestinal absorption and the pharmacokinetics of tetramethylpyrazine phosphate after oral administration were investigated. In situ intestinal recirculation was performed to study the effect of various concentrations of borneol on the absorption of tetramethylpyrazine phosphate at duodenum, jejunum, ileum and colon. After oral administration of tetramethylpyrazine phosphate, the mixture of tetramethylpyrazine phosphate and borneol and the mixture of tetramethylpyrazine phosphate and verapamil in rats, the concentrations of tetramethylpyrazine phosphate in plasma were determined by RP-HPLC at predesigned time.

[Water in oil microemulsions for transdermal delivery of fluorouracil].

An Aersol-OT (AOT) included microemulsion containing fluorouracil was prepared by using appropriate proportion of oil, co-surfactant and water for increasing the drug transdermal delivery ability. According to the area of microemulsion basing on the pseudo-tertiary phase diagrams, the optimum formulation was screened initially. And the permeation flux of fluorouracil across excised mice skin was determined in vitro using Franz diffusion cell to optimize the formulation further.

Enhanced glucose synthesis in three-dimensional hepatocyte collagen matrix.

Three-dimensional (3D) cell culture model offers a unique opportunity to study hepatocytes that require extracellular matrix to keep the cells at the differentiated state. In this report, we cultured isolated mouse hepatocytes in a 3D collagen matrix system and developed a protocol to measure glucose production at 3h, 6h, 18h and 24h after culture. The results demonstrated that hepatocytes cultured under 3D collagen matrix condition consistently produced glucose at 240-290 mg/10(6) cells for up to 24h.

A simple gas chromatographic method for the simultaneous determination and pharmacokinetic study of tetramethylpyrazine phosphate and borneol in mouse plasma and brain tissue after oral administration of the fufang tetramethylpyrazine phosphate tablets.

A rapid, sensitive, and simple gas chromatographic method with flame ionization detection is developed for the simultaneous determination of tetramethylpyrazine phosphate (TMPP) and borneol in mouse plasma and brain tissue. Sample preparations are carried out by deproteinization with an internal standard solution in methanol. The analytes and internal standard (dimethyl sulfoxide) are well-separated on an HP-5 MS capillary column.

A simple HPLC method for the determination of bifendate: application to a pharmacokinetic study of bifendate liposome.

A rapid, sensitive and simple high-performance liquid chromatographic (HPLC) method with ultraviolet detector (UV) has been developed for the determination of bifendate in 100 microl plasma of rats. Sample preparation was carried out by deproteinization with 100 microl of acetonitrile. A 20 microl of supernatant was directly injected into the HPLC system with methanol-double distilled water (65/35, v/v) as the mobile phase at a flow rate of 1.

The enhancing effect of synthetical borneol on the absorption of tetramethylpyrazine phosphate in mouse.

The main purpose of this study was to illustrate the effect of synthetical borneol (SB) on the plasma and brain concentration profile of tetramethylpyrazine phosphate (TMPP) in mice after oral administration of TMPP without or with different amounts of SB. The concentrations of TMPP on the plasma and brain in mice were determined by GC-FID. The pharmacokinetic parameters were computed by software program 3p97.

[Preparation of verapamil hydrochloride controlled-onset extended-release pellets and its pharmacokinetics in dogs].

Aim: To prepare verapamil hydrochloride controlled-onset extended-release pellets (VH-COERP) and study its release behavior in vitro. To compare the pharmacokinetic characteristics and bioavailability in six Beagle dogs after oral administration of VH-COERP and verapamil hydrochloride delayed-release pellets (VH-DRP) as reference.

Methods: The core of VH-COERP were prepared in the fluidized bed (mini-glatt) by spraying water solution containing drugs onto sucrose-starch pellets with hydroroxy propyl methyl cellulose (HPMC) as the inner coating swelling layer and ethylcellulouse aqueous dispersion as the outer coating controlled layer.

Preparation of silymarin proliposome: a new way to increase oral bioavailability of silymarin in beagle dogs.

The aim of the present study was to find a method to increase oral bioavailability of silymarin, that is to say, by the preparation of silymarin proliposome and to compare the pharmacokinetic characteristics and bioavailability after oral administration of silymarin proliposome and silymarin in beagle dogs. Silymarin proliposome was prepared by the film-deposition on carriers. After the proliposome was contacted with water, the silymarin liposome suspensions formed automatically.

[Preparation of silymarin proliposomes and its pharmacokinetics in rats].

Aim: To study the preparation of silymarin proliposomes. To study its physicochemic properties, its pharmacokinetical characteristics and bioavailability in rats after oral administration.

Methods: Silymarin proliposomes were prepared by film-deposition on carriers.

[Preparation of silybin-phospholipid complex and its bioavailability in rats].

Aim: To prepare silybin-phospholipid complex and study its physicochemical properties. To compare the pharmacokinetic characteristics and bioavailability after oral administration of silybinphospholipid complex and silybin material in rats.

Methods: Using acetone as a reaction medium, silybin and phospholipid were resolved into the medium, when the organic solvent was clear, then removed under vacuum evaporation, silybin-phospholipid complex was obtained.