pH-activatable oxidative stress amplifying dissolving microneedles for combined chemo-photodynamic therapy of melanoma.

Photodynamic therapy (PDT)-mediated oxidation treatment is extremely attractive for skin melanoma ablation, but the strong hydrophobicity and poor tumor selectivity of photosensitizers, as well as the oxygen-consuming properties of PDT, leading to unsatisfactory therapeutic outcomes. Herein, a tumor acidic microenvironment activatable dissolving microneedle (DHA@HPFe-MN) was developed to realize controlled drug release and excellent chemo-photodynamic therapy of melanoma via oxidative stress amplification. The versatile DHA@HPFe-MN was fabricated by crosslinking a self-synthesized protoporphyrin (PpIX)-ADH-hyaluronic acid (HA) conjugate HA-ADH-PpIX with "iron reservoir" PA-Fe complex in the needle tip via acylhydrazone bond formation, and dihydroartemisinin (DHA) was concurrently loaded in the hydrogel network.

Tumor-targeted hyaluronic acid-based oxidative stress nanoamplifier with ROS generation and GSH depletion for antitumor therapy.

Tumor cells with innate oxidative stress are more susceptible to exogenous ROS-mediated oxidative damage than normal cells. However, the generated ROS could be scavenged by the overexpressed GSH in cancer cells, thus causing greatly restricted efficiency of ROS-mediated antitumor therapy. Herein, using cinnamaldehyde (CA) as a ROS generator while β-phenethyl isothiocyanate (PEITC) as a GSH scavenger, we designed a tumor-targeted oxidative stress nanoamplifier to elevate intracellular ROS level and synchronously suppress antioxidant systems, for thorough redox imbalance and effective tumor cells killing.

pH-responsive hyaluronic acid-based nanoparticles for targeted curcumin delivery and enhanced cancer therapy.

Curcumin (CUR) display promising antitumor effects, however, the poor water solubility severely limited its clinical application. To overcome this problem, polymeric nanocarriers have been adopted for targeted CUR delivery and enhanced cancer therapy. In this paper, utilizing an acid-labile hydrazone linkage, hydrophobic CUR was conjugated with hydrophilic hyaluronic acid (HA) to form amphiphilic HA-ADH-CUR conjugates, which could subsequently self-assemble to form nanoparticles (HA@CUR NPs) in aqueous.

Calcium phosphate nanoparticles functionalized with alendronate-conjugated polyethylene glycol (PEG) for the treatment of bone metastasis.

Because of the peculiarity of the bone microstructure, the uptake of chemotherapeutics often happens at non-targeted sites, which induces side effects. In order to solve this problem, we designed a bone-targeting drug delivery system that can release drug exclusively in the nidus of the bone. Alendronate (ALN), which has a high ability to target to hydroxyapatite, was used to fabricate double ALN-conjugated poly (ethylene glycol) 2000 material (ALN-PEG-ALN).

Novel Galactosylated Poly(ethylene glycol)-Cholesterol for Liposomes as a Drug Carrier for Hepatocyte-Targeting.

In this study, three types of galactosylated cholesterol (i.e., gal-PEG194-chol, gal-PEG1000-chol and gal-PEG2000-chol) were synthesized with one terminal of polyethylene glycol of various chain lengths conjugated to the galactoside moiety, and the other terminal conjugated to the cholesterol.

Improvement of pharmacokinetic and antitumor activity of layered double hydroxide nanoparticles by coating with PEGylated phospholipid membrane.

Layered double hydroxide (LDH) has attracted considerable attention as a drug carrier. However, because of its poor in vivo behavior, polyethylene glycolylated (PEGylated) phospholipid must be used as a coformer to produce self-assembled core-shell nanoparticles. In the present study, we prepared a PEGylated phospholipid-coated LDH (PLDH) (PEG-PLDH) delivery system.

[Determination of vitexin in plasma by HPLC-MS/MS method and its pharmacokinetics in rats].

Objective: To establish a HPLC-MS/MS method for the determination of vitexin in rat plasma and its pharmacokinetics.

Methods: The HPLC-MS/MS method used Capcell Pak C18 column (50 mm x 2.0 mm I.

[Effect of verapamil on pharmacokinetics of puerarin in rats].

Objective: To investigate the effect of verapamil on the pharmacokinetics of puerarin in rats.

Method: Puerarin with or without verapamil was administered intravenously or orally to rats. The concentration of puerarin in serum was determined by HPLC.

[Preparation of self-microemulsifying soft capsule and investigation of dissolution for Duyiwei].

Objective: To prepare the self-microemulsifying soft capsule (SMESC) of Duyiwei and investigate its dissolution property.

Methods: Through solubility experiment, self-microemulsification in vitro, drawing phase diagram and investigating the stability of solution, the optimum formulation was determined for Duyiwei. The dissolution of SMESC was measured, taking the commercial capsule as reference.

[Assessment of Pueraria lobata isoflavone with self-microemulsifying drug delivery systems in vitro and in vivo].

Objective: To evaluate the self-microemulsifying ability and dissolution behavior of pueraria lobata isoflavone in vitro and the pharmacokinetic behavior in rats.

Methods: The self-microemulsifying rate was evaluated by the self-microemulsifying time and the self-microemulsifying efficiency was evaluated by the particle size of resultant microemulsions. The plasma concentrations were evaluated by HPLC and dissolution and pharmacokinetic behavior of self-microemulsifying drug delivery systems were evaluated by comparison with commercial tablets.

Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma.

Aim: To study the intravenous and oral pharmacokinetic behavior of oridonin and its extent of absolute oral bioavailability in rats.

Methods: Oridonin was administered to rats via iv (5, 10 and 15 mg/kg), po (20, 40 and 80 mg/kg) or ip administration (10 mg/kg). The concentrations of oridonin in rat plasma were determined by a high performance liquid chromatography with electrospray ionization mass spectrometric detection (HPLC/ESI-MS) method and the pharmacokinetic parameters were determined by non-compartmental analysis.

Quantitative structure-retention relationship studies using immobilized artificial membrane chromatography I: amended linear solvation energy relationships with the introduction of a molecular electronic factor.

Linear solvation energy relationships (LSERs) amended by the introduction of a molecular electronic factor were employed to establish quantitative structure-retention relationships using immobilized artificial membrane (IAM) chromatography, in particular ionizable solutes. The chromatographic indices, log k(IAM), were determined by HPLC on an IAM.PC.

Self-microemulsifying drug delivery systems (SMEDDS) for improving in vitro dissolution and oral absorption of Pueraria lobata isoflavone.

The aim of our investigation was to develop and characterize self-microemulsifying drug delivery systems (SMEDDS) of Pueraria lobata isoflavone to improve its in vitro dissolution and oral absorption in beagle dogs. SMEDDS consisted of oil (ethyl oleate), a surfactant (Tween 80), and a cosurfactant (Transcutol P). In all the SMEDDS, the level of Pueraria lobata isoflavone was fixed at 20% w/w of the vehicle.

Study on the bioavailability of puerarin from Pueraria lobata isoflavone self-microemulsifying drug-delivery systems and tablets in rabbits by liquid chromatography-mass spectrometry.

To evaluate the bioavailability of puerarin from Pueraria lobata isoflavone self-microemulsifying drug delivery systems (SMEDDS) and Yufengningxin tablets, a rapid and specific liquid chromatography--mass spectrometric method was developed and validated to determine puerarin in rabbit serum. The analyte was extracted from serum samples by precipitating the serum proteins, separated on a Diamonsil C(18) column and detected by mass spectrometry with an electrospray ionization interface. 4-Hydroxybenzaldehyde was used as the internal standard.

Determination of 3-n-butylphthalide in rabbit plasma by HPLC with fluorescence detection and its application in pharmacokinetic study.

A rapid, sensitive and specific reversed-phase high-performance liquid chromatographic method was developed for the determination of 3-n-butylphthalide, a drug currently being developed for treatment of stroke, in rabbit plasma. Fluorescence detection at an excitation wavelength of 280 nm and an emission wavelength of 304 nm was used for quantification of 3-n-butylphthalide. Ibuprofen was used as internal standard.