<Emphasis Type="BoldItalic">Leucine-Aspartic Acid-Valine</Emphasis> Sequence as Targeting Ligand and Drug Carrier for Doxorubicin Delivery to Melanoma Cells: <Emphasis Type="BoldItalic">In Vitro</Emphasis> Cellular Uptake and Cytotoxicity Studies

Purpose  

To study the feasibility of Leucine-Aspartic Acid-Valine (LDV) as targeting ligand and drug carrier for targeted delivery to integrin α₄β₁ over-expressing cancer cells.     

<Emphasis Type="Italic">In Vitro</Emphasis> Aqueous Fluid-Capacity-Limited Dissolution Testing of Respirable Aerosol Drug Particles Generated from Inhaler Products

Purpose  

To develop a unique in vitro aqueous fluid-capacity-limited dissolution system for the kinetic assessment of respirable aerosol drug particles from inhaler products.     

<Emphasis Type="Italic">In Vitro</Emphasis> and <Emphasis Type="Italic">In Vivo</Emphasis> Anticancer Activity of a Novel Nano-sized Formulation Based on Self-assembling Polymers Against Pancreatic Cancer

Purpose  

To evaluate the in vitro and in vivo pancreatic anticancer activity of a nano-sized formulation based on novel polyallylamine grafted with 5% mole cholesteryl pendant groups (CH₅-PAA).     

Fast Surface Crystallization of Amorphous Griseofulvin Below <Emphasis Type="Italic">T</Emphasis><Subscript>g</Subscript>

Purpose  

To study crystal growth rates of amorphous griseofulvin (GSF) below its glass transition temperature (T _g) and the effect of surface crystallization on the overall crystallization kinetics of amorphous GSF.     

A New <Emphasis Type="Italic">In Situ</Emphasis> Brain Perfusion Flow Correction Method for Lipophilic Drugs Based on the pH-Dependent Crone-Renkin Equation

Purpose  

To determine the flow-corrected luminal permeability, P_c, of lipophilic drugs measured by the in situ brain perfusion method under circumstances where the traditional Crone-Renkin equation (CRE) method, using diazepam as a flow marker, often fails.     

Individual differences in the improvement of cocaine-induced place preference response by the 5-HT<Subscript>2C</Subscript> receptor antagonist SB242084 in rats

Rationale and objectives  

The 5-HT_2A and 5-HT_2C receptors have been shown to be differentially involved in modulating cocaine-induced behaviors. In this study we investigated the effects of the 5-HT_2A antagonist MDL100907 (0.3 mg/kg, i.p.) and the 5-HT_2C antagonist SB242084 (0.5 mg/kg, i.p.) on development, expression, and recall of cocaine-induced conditioned place preference (CPP) in high- (HR) and low-responder (LR) rats to novelty.     

Multiclass mycotoxins in lotus seeds analysed by an isotope‐labelled internal standard‐based UPLC‐MS/MS

Objectives

This study aimed to explore the residue levels of multiclass mycotoxins in medicinal and edible lotus seeds.

Methods

A rapid and reliable isotope‐labelled internal standard‐based UPLC ‐MS /MS method was developed and validated for sensitive and accurate analysis of multiclass mycotoxins including aflatoxins (AFB ₁, AFB ₂, AFG ₁ and AFG ₂), ochratoxin A (OTA ), zearalenone (ZEN ), deoxynivalenol (DON ), fumonisins (FB ₁ and FB ₂), T‐2 and HT ‐2 toxins in lotus seeds. Some critical conditions such as extract solution with the addition of isotope‐labelled internal standard, type of mobile phase and the elution condition were scientifically optimized. The 11 mycotoxins obtained satisfactory resolution and sensitive detection in multiple reactions monitoring scanning mode combined with the ion switching technology in positive and negative ion switching mode.

Key findings

The developed isotope‐labelled internal standard‐based UPLC ‐MS /MS method exhibited an approving linearity (r  ≥  0.9984), high sensitivity (limit of detection in the range of 0.015–30.05 μg/kg), acceptable precision (RSD s ≤6.3%) and good recovery (76.0–116.0%) for 11 analytes, respectively. Ten batches of real lotus seed samples were tested, and three batches out of which were contaminated with AFB ₁, FB ₂, T‐2 and ZEN . AFB ₁ showed the highest occurrence rate (30%) with contents of 10.50 and 8.32 μg/kg in two samples over the official limit (5.0 μg/kg).

Conclusions

The monitoring of multiclass mycotoxins in Chinese herbal medicines is in great urgency to ensure the security of consumers. The proposed method could be further utilized for simple, sensitive and rapid detection of more mycotoxins in other complex matrices to compensate for matrix effects.

     

The effects of PRX-07034, a novel 5-HT<Subscript>6</Subscript> antagonist,on cognitive flexibility and working memory in rats

Rationale  

Accumulating evidence indicates that schizophrenia and autism spectrum disorder patients are marked by cognitive deficits in working memory and strategy switching. There is accumulating evidence that 5-hydroxytryptamine (5-HT)₆ receptors may serve as a useful target to improve cognitive functioning.     

Fe<Subscript>3</Subscript>O<Subscript>4</Subscript>-PEI-RITC Magnetic Nanoparticles with Imaging and Gene Transfer Capability: Development of a Tool for Neural Cell Transplantation Therapies

Purpose  

To develop Fe₃O₄-PEI-RITC magnetic nanoparticles with multimodal MRI-fluorescence imaging and transfection capability, for use in neural cell replacement therapies.     

Pharmacokinetic-Pharmacodynamic Modeling of the Inhibitory Effects of Naproxen on the Time-Courses of Inflammatory Pain,Fever, and the <Emphasis Type="Italic">Ex Vivo</Emphasis> Synthesis of TXB<Subscript>2</Subscript> and PGE<Subscript>2</Subscript> in Rats

Purpose  

To quantify and compare the time-course and potency of the analgesic and antipyretic effects of naproxen in conjunction with the inhibition of PGE₂ and TXB₂.     

A Semi-mechanistic Modeling Strategy to Link <Emphasis Type="Italic">In Vitro</Emphasis> and <Emphasis Type="Italic">In Vivo</Emphasis> Drug Release for Modified Release Formulations

Purpose  

To develop a semi-mechanistic model linking in vitro to in vivo drug release.     

Immunodensity and mRNA expression of A<Subscript>2A</Subscript> adenosine,D<Subscript>2</Subscript> dopamine,and CB<Subscript>1</Subscript> cannabinoid receptors in postmortem frontal cortex of subjects with schizophrenia: effect of antipsychotic treatment

Rationale  

Dopamine D₂ receptors are the main target of antipsychotic drugs. In the brain, D₂ receptors coexpress with adenosine A_2A and CB₁ cannabinoid receptors, leading to functional interactions.     

Short circuit: Disaggregation of adrenocorticotropic hormone and cortisol levels in HIV‐positive,methamphetamine‐using men who have sex with men

Objective

This study examined if methamphetamine use alone (METH + HIV?) and methamphetamine use in combination with HIV (METH + HIV+) were associated with hypothalamic‐pituitary‐adrenal (HPA) axis dysregulation as well as insulin resistance relative to a nonmethamphetamine‐using, HIV‐negative comparison group (METH‐HIV?).

Methods

Using an intact groups design, serum levels of HPA axis hormones in 46 METH + HIV? and 127 METH + HIV+ men who have sex with men (MSM) were compared to 136 METH‐HIV? men.

Results

There were no group differences in prevailing adrenocorticotropic hormone (ACTH) or cortisol levels, but the association between ACTH and cortisol was moderated by METH + HIV+ group (β = ?0.19, p < .05). Compared to METH‐HIV? men, METH + HIV+ MSM displayed 10% higher log₁₀ cortisol levels per standard deviation lower ACTH. Both groups of methamphetamine‐using MSM had lower insulin resistance and greater syndemic burden (i.e., sleep disturbance, severe depression, childhood trauma, and polysubstance use disorder) compared to METH‐HIV? men. However, the disaggregated functional relationship between ACTH and cortisol in METH + HIV+ MSM was independent of these factors.

Conclusions

Further research is needed to characterize the bio‐behavioral pathways that explain dysregulated HPA axis functioning in HIV‐positive, methamphetamine‐using MSM.     

<Emphasis Type="Italic">In Vitro</Emphasis> and <Emphasis Type="Italic">In Vivo</Emphasis> Effects of Water Extract of White Cocoa Tea (<Emphasis Type="Italic">Camellia ptilophylla</Emphasis>) Against Human Prostate Cancer

Purpose  

We evaluated the chemotherapeutic effect of water extract of white cocoa tea (WCTE) against human prostate cancer (PCa) in vitro and in vivo.     

Population <Emphasis Type="Italic">In Vitro</Emphasis>-<Emphasis Type="Italic">In Vivo</Emphasis> Correlation Model for Pramipexole Slow-Release Oral Formulations

Purpose  

To establish an in vitro-in vivo level A correlation (IVIVC) for pramipexole slow-release formulations.     

Silibinin Suppresses Spontaneous Tumorigenesis in <Emphasis Type="BoldItalic">APC</Emphasis><Superscript>min/+</Superscript> Mouse Model by Modulating Beta-Catenin Pathway

Purpose  

Here we assessed whether silibinin, a nontoxic chemopreventive agent, inhibits spontaneous intestinal tumorigenesis in APC ^min/+ mouse model, a genetically predisposed animal model of human familial adenomatous polyposis (FAP).     

Higher serotonin transporter availability in early‐onset obsessive–compulsive disorder patients undergoing escitalopram treatment: A [11C]DASB PET study

Objective

Early‐onset obsessive–compulsive disorder (EOCD) and late‐onset obsessive–compulsive disorder (LOCD) are distinct subtypes of obsessive–compulsive disorder (OCD). OCD patients are treated with serotonin reuptake inhibitors, but the difference in serotonin transporter (SERT) availability between medicated EOCD and LOCD is unexplored yet.

Methods

Six EOCD and 6 LOCD patients were enrolled. They underwent serial [¹¹C]DASB positron emission tomography scans during maintenance therapy with escitalopram, and their plasma concentration of escitalopram was measured simultaneously with the scan. Then, the drug‐free binding potential of SERT was calculated by pharmacokinetic–pharmacodynamic modelling.

Results

In comparison with LOCD patients, SERT availability was significantly higher in the putamen of EOCD patients (U = 4, p = .026), but not in the caudate nucleus (U = 14, p = .589), thalamus (U = 16, p = .818), and dorsal raphe nucleus (U = 7, p = .093). Binding potential of putamen showed a negative correlation (r = ?.580, p = .048) with age of onset of the disease, but not with the Yale–Brown Obsessive Compulsive Scale scores.

Conclusions

These findings indicate that the earlier the age of onset of OCD, the less serotonergic pathology there is and that this difference remains even after long‐term serotonin reuptake inhibitor treatment. Clinically, it might suggest that nonserotonergic treatments would be a better option for EOCD patients.     

Development of New Localized Drug Delivery System Based on Ceftriaxone-Sulbactam Composite Drug Impregnated Porous Hydroxyapatite: A Systematic Approach for <Emphasis Type="Italic">In Vitro</Emphasis> and <Emphasis Type="Italic">In Vivo</Emphasis> Animal Trial

Purpose  

Present investigation deals with an extensive approach incorporating in vitro and in vivo experimentation to treat chronic osteomyelitis, using hydroxyapatite porous scaffolds.     

Enhanced Bioavailability of L-Carnitine After Painless Intradermal Delivery <Emphasis Type="BoldItalic">vs.</Emphasis> Oral Administration in Rats

Purpose  

In vitro and in vivo permeation studies were conducted to evaluate the characteristic of percutaneous administration of high hydrophilic drug L-carnitine (LC) by Functional MicroArray (FMA) painless intradermal delivery system.     

Bioadhesive Films Containing Benzocaine: Correlation Between <Emphasis Type="Italic">In Vitro</Emphasis> Permeation and <Emphasis Type="Italic">In Vivo</Emphasis> Local Anesthetic Effect

Purpose  

The aim of this work was to develop anesthetic bioadhesive films containing benzocaine and study their in vitro skin permeation and in vivo performance, in comparison with commercial formulations.