Aristolactam BIII, a naturally derived DYRK1A inhibitor, rescues Down syndrome-related phenotypes.

Background: Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a significant pathogenic factor in Down syndrome (DS), wherein DYRK1A is overexpressed by 1.5-fold because of trisomy of human chromosome 21. Thus, DYRK1A inhibition is considered a therapeutic strategy to modify the disease.

Bacteria-Targeted Clindamycin Loaded Polymeric Nanoparticles: Effect of Surface Charge on Nanoparticle Adhesion to MRSA, Antibacterial Activity, and Wound Healing.

Adhesion of nanoparticles (NPs) to the bacterial cell wall by modifying their physicochemical properties can improve the antibacterial activity of antibiotic. In this study, we prepared positively charged clindamycin-loaded poly (lactic-co-glycolic acid)-polyethylenimine (PLGA-PEI) nanoparticles (Cly/PPNPs) and negatively charged clindamycin-loaded PLGA NPs (Cly/PNPs) and investigated the effect of NP adhesion to bacteria on the treatment of methicillin-resistant (MRSA)-infected wounds. The Cly/PPNPs and Cly/PNPs were characterized according to particle size, polydispersity index, surface charge, and drug loading.

An injectable liquid crystal system for sustained delivery of entecavir.

Liquid crystal (LC) technology has attracted much interest for new injectable sustained-release (SR) formulations. In this study, an injectable liquid crystal-forming system (LCFS) including entecavir was prepared for the treatment of hepatitis B. In particular, an anchoring effect was introduced because LCFSs are relatively hydrophobic while entecavir is a slightly charged drug.

Chitosan-based hybrid nanocomplex for siRNA delivery and its application for cancer therapy.

Purpose: Chitosan, a natural and biocompatible cationic polymer, is an attractive carrier for small interfering RNA (siRNA) delivery. The purpose of this study was to develop a chitosan-based hybrid nanocomplex that exhibits enhanced physical stability in the bloodstream compared with conventional chitosan complexes. Hybrid nanocomplexes composed of chitosan, protamine, lecithin, and thiamine pyrophosphate were prepared for systemic delivery of survivin (SVN) siRNA.

A new injectable liquid crystal system for one month delivery of leuprolide.

An injectable liquid crystal-forming system (LCFS) was prepared by using sorbitan monooleate (SMO) as a new liquid crystal-forming material for injections, and its potential use of clinically available sustained-release formulation was evaluated. LCFS was prepared using SMO mixed with phosphatidyl choline and tocopherol acetate, and contained 3.75 mg of leuprolide acetate as a monthly dose in 90 μl in liquid form.

Pharmacokinetic properties and bioequivalence of 2 formulations of valsartan 160-mg tablets: A randomized, single-dose, 2-period crossover study in healthy Korean male volunteers.

Background: The solubility of valsartan is dependent on pH and thus may cause patient variability in drug absorption and failure in bioequivalence studies; thus, increasing the solubility and release of valsartan at low pH has been suggested for a more favorable pharmacokinetic profile. However, due to this pH dependence, the change in the formulation process could alter the disintegration and/or dissolution profile of the drug, possibly making the results of bioequivalence studies misleading.

Objective: The aim of this study was to assess the bioavailability and tolerability of a newly developed oral formulation of valsartan 160 mg (wet-granulation tablet) in healthy Korean male volunteers.

Sustained delivery of human growth hormone using a polyelectrolyte complex-loaded thermosensitive polyphosphazene hydrogel.

A combined system of polyelectrolyte complex (PEC) and injectable, biodegradable and thermosensitive poly(organophosphazene) hydrogel has been suggested as an injectable depot for a controlled and sustained delivery of human growth hormone (hGH) to improve patient compliance. PEC was prepared by mixing polycations with hGH to suppress diffusion of hGH from the hydrogel through an enlargement of the hydrodynamic size of hGH. Among the polycations, poly-L-arginine (PLA) formed a large complex with hGH and its size increased as the amount of PLA increased.

Evaluation of the Clinical Data Dictionary (CiDD).

Objectives: The purpose of the study was to evaluate content coverage and data quality of the Clinical Data Dictionary (CiDD) developed by the Center for Interoperable EHR (CiEHR).

Methods: A total of 12,994 terms were collected from 98 clinical forms of a tertiary cancer center hospital with 500 beds. After data cleaning, 9,418 terms were mapped with the data items of the CiDD by the research team, and validated by 30 doctors and nurses at the research hospital.

Cationic and thermosensitive protamine conjugated gels for enhancing sustained human growth hormone delivery.

Thermosensitive and cationic poly(organophosphazenes) were designed and synthesized for the sustained delivery of human growth hormone (hGH) charged negatively at the physiological conditions to enhance greatly patient convenience and to improve efficacy and stability. Protamine for a complex formation with hGH was chosen and conjugated to carboxylic acid-terminated poly(organophosphazenes) by a covalent amide linkage. The aqueous solution of the cationic polymer conjugates formed a gel at 37 degrees C regardless of hGH presence.

The efficacy and safety of clopidogrel resinate as a novel polymeric salt form of clopidogrel.

A novel polymeric salt of clopidogrel, clopidogrel resinate, was prepared as a anticoagulant drug. To prove the feasibility as a new active substance, clopidogrel resinate was evaluated for its efficacy and safety. In accelerated stability tests, the clopidogrel resinate tablet (Pregrel) showed less brown discoloration and fewer impurities than the clopidogrel bisulfate tablets under open and closed conditions.

Development of parenteral formulation for a novel angiogenesis inhibitor, CKD-732 through complexation with hydroxypropyl-beta-cyclodextrin.

The effect of hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) on the aqueous solubility and chemical stability of O-(4-Dimethylaminoethoxycinnamoyl)fumagillol (CKD-732), a new angiogenesis inhibitor, was investigated with an aim of preparing a stable and effective parenteral formulation. The CKD-732/HP-beta-CyD inclusion complex was obtained in solid state by freeze-drying and characterized in solution by proton nuclear magnetic resonance (1H NMR). Then, the pharmacokinetic profile in rats and the in vivo tumor growth inhibitory activity in mice following the parenteral administration of aqueous CKD-732/HP-beta-CyD complex were compared to those of CKD-732.