Core-Shell Microspheres Prepared Using Coaxial Electrostatic Spray for Local Chemotherapy of Solid Tumors.

Local chemotherapy is an alternative therapeutic strategy that involves direct delivery of drugs to the tumor site. This approach avoids adverse reactions caused by the systemic distribution of drugs and enhances the tumor-suppressing effect by concentrating the drugs at the tumor site. Drug-loaded microspheres are injectable sustained-release drug carriers that are highly suitable for local chemotherapy.

HI-6-loaded PEGylated liposomes: an on-site first-aid strategy for acute organophosphorus agent poisoning.

Organophosphorus agents, also known as nerve agents, are very dangerous chemicals that were used as chemical warfare agents. HI-6 is one of the most promising reactivators which is effective in reactivating AChE inhibited by many nerve agents. However, the fast in-vivo clearance of HI-6 became a large barrier for first aid use under some sophisticated circumstances.

Synergistic enhancement of the emergency treatment effect of organophosphate poisoning by a supramolecular strategy.

Poisoning by organophosphorus agents (OPs) is a serious public health issue across the world. These compounds irreversibly inhibit acetylcholinesterase (AChE), resulting in the accumulation of acetylcholine (ACh) and overstimulation of ACh receptors. A supramolecular detoxification system (SDS) has been designed with a view to deliver pyridine-2-aldoxime methochloride (PAM) with a synergistic inhibition effect on the ACh-induced hyperstimulation through host-guest encapsulation.

Ilomastat contributes to the survival of mouse after irradiation via promoting the recovery of hematopoietic system.

Ilomastat, a broad-spectrum inhibitor of matrix metalloproteinases (MMPs), has drawn attentions for its function in alleviating radiation damage. However, the detailed mechanisms of Ilomastat's protection from animal model remain not fully clear. In this study, the C57BL/6 mice were pre-administrated with Ilomastat or vihicle for 2 h, and then total body of mice were exposed to 6 Gy of γ-rays.

Brain-targeted delivery of obidoxime, using aptamer-modified liposomes, for detoxification of organophosphorus compounds.

Effective intracerebral delivery acetylcholinesterase (AChE) reactivator is key for the acute organophosphorus (OPs) poison treatment. However, the blood-brain barrier (BBB) restricts the transport of these drugs from blood into the brain. Herein, we developed transferrin receptor (TfR) aptamer-functionalized liposomes (Apt-LP) that could deliver AChE reactivator (obidoxime) across the BBB to act against paraoxon (POX) poisoning.

"Oil-soluble" reversed lipid nanoparticles for oral insulin delivery.

Background: In this study, we aimed to design a novel oral insulin delivery system, named "oil-soluble" reversed lipid nanoparticles (ORLN), in which a hydrophilic insulin molecule is encapsulated by a phospholipid (PC) shell and dissolved in oil to prevent the enzymatic degradation of insulin. ORLN was characterized by transmission electron microscopy and dynamic light scattering.

Results: In vitro enzymatic stability studies showed higher concentrations of insulin in cells incubated with ORLN-encapsulated insulin than in those incubated with free insulin solution in artificial intestinal fluid (pH 6.

Taste masking of water-soluble drug by solid lipid microspheres: a child-friendly system established by reversed lipid-based nanoparticle technique.

Objectives: A child-friendly taste-masking strategy using solid lipid microsphere (SLM) has been proposed to obscure the undesirable taste of some water-soluble drugs. In this study, the reversed lipid-based nanoparticle (RLBN) technique was used to encapsulate a water-soluble drug to facilitate the preparation of SLM.

Methods: The model drug used was atomoxetine hydrochloride (ATX), and a three-step method was used to prepare ATX-RLBN.

Why is glycocholic acid sodium salt better than deoxycholic acid sodium salt for the preparation of mixed micelle injections?

Classical mixed micelle systems make excellent parenteral drug carriers for lipophilic or poorly soluble drugs, but many formulations details are not fully understood and need further study. Thus, we constructed mixed micelle systems with lecithin and either glycocholic acid sodium salt or deoxycholic acid sodium salt in order to investigate the differences between the bile salts. Vitamin K, a lipid-soluble drug, was encapsulated in the mixed micelles, and the influence of bile salts on the quality and stability of the mixed micelle systems was analyzed.

Reversed Lipid-Based Nanoparticles Dispersed in Iodized Oil for Transarterial Chemoembolization.

Transarterial chemoembolization (TACE) is a promising treatment for patients suffering from unresectable liver malignancy. A coarse emulsion of doxorubicin solution and iodized oil is widely used in clinical practice. However, this coarse emulsion lacks sufficient physical stability and can split into water and oil very quickly.

Delivering the Acetylcholine Neurotransmitter by Nanodrugs as an Effective Treatment for Alzheimer's Disease.

The current clinical symptomatic therapy for Alzheimer's disease involves increasing acetylcholine levels in the brain by inhibiting acetylcholinesterase. However, the effectiveness of acetylcholinesterase inhibitors decreases as the disease progresses, leading to many side effects including over-inhibition of other enzymes and hepatic injury. Herein, we investigate the effects of the direct delivery of a low-dose of acetylcholine via human serum albumin nanoparticles to brain.

Creation of an assessment system for measuring the bitterness of azithromycin-containing reverse micelles.

We aimed to develop a novel method for assessing the bitterness of azithromycin-containing reverse micelles (AM-containing RMs). Azithromycin-containing reverse micelles were prepared by processing Lipoid E80 and medium chain triglycerides via a freeze-drying method. The bitterness threshold of azithromycin was determined by human taste test, and an equation was derived to correlate the azithromycin concentrations and bitterness scores of standard solutions.

A Novel Surfactant-free Lipid-based Formulation for Improving Oral Bioavailability of Loratadine Using Colloidal Silicon Dioxide as Emulsifier and Solid Carrier.

Background: The purpose of this study was to develop an innovative surfactant-free lipidbased formulation (LF) for improving oral bioavailability of loratadine based on using solid particles colloidal silicon dioxide (CSD) as emulsifier and solid carrier.

Methods: Loratadine was dissolved in oil solution with the aid of co-solvent and LF formulations were prepared by a simple adsorption and milling technique. The LF Powder was evaluated in terms of angle of repose and X-ray powder diffraction.

A novel core-shell lipid nanoparticle for improving oral administration of water soluble chemotherapeutic agents: inhibited intestinal hydrolysis and enhanced lymphatic absorption.

The oral administration of water-soluble chemotherapeutical agents is limited by their serious gastrointestinal side effects, instability at intestinal pH, and poor absorption. Aiming to solve these problems, we chose topotecan (TPT) as a model drug and developed a novel lipid formulation containing core-shell lipid nanoparticle (CLN) that makes the water-soluble drug to 'dissolve' in oil. TPT molecules can be encapsulated into nanoparticles surrounded by oil barrier while avoiding the direct contact with intestinal environment, thus easing the intestinal hydrolytic degradation and gastrointestinal (GI) irritation.

Ilomastat, a synthetic inhibitor of MMPs, prevents lung injury induced by γ-ray irradiation in mice.

Lung injury is one of the pathological features in human or animal after radiation and the main side effect for patient after lung cancer radiotherapy. The efficient protective strategy still needs to exploit and the underlying mechanisms remain to be investigated. We found that the expression and activity of matrix metalloproteinases (MMPs) significantly increased at the early stage of radiation-induced lung injury (RILI).

Reversed lipid-based nanoparticles dispersed in oil for malignant tumor treatment via intratumoral injection.

Intratumoral injection of anticancer drugs directly delivers chemotherapeutics to the tumor region, offering an alternative strategy for cancer treatment. However, most hydrophilic drugs spread quickly from the injection site into systemic circulation, leading to inferior antitumor activity and adverse effects in patients. Therefore, we developed novel reversed lipid-based nanoparticles (RLBN) as a nanoscale drug carrier.

Release Characteristics In Vitro and In Vivo of In Situ Gels for a Novel Peptide Compared with Low-Molecular-Weight Hydrophilic Drug.

Background: The thermo-sensitive in situ gels based on copolymers are attractive as an injectable drug delivery carriers for sustained releasing of hydrophilic drugs. The purposes of this work are to investigate the release behavior in vitro and pharmacokinetic profiles in vivo of peptide and lowmolecular- weight hydrophilic drug loaded in the in situ gels.

Methods: A triblock copolymer PLGA-PEG-PLGA (1402-1000-1402) 1115A (1115A) was synthesized and its rheological and gelatin properties were evaluated.

Anti-inflammatory activity of chitosan nanoparticles carrying NF-κB/p65 antisense oligonucleotide in RAW264.7 macropghage stimulated by lipopolysaccharide.

The purpose of this present study is to prepare NF-κB/p65 antisense oligonucleotide loaded chitosan nanoparticles (NPs) and evaluate their physicochemical characterization and antisense effects in RAW264.7 macrophages. Condensed nanoparticles with mean particle size of 128±16nm, average Zeta potential of 19.

The in vitro and in vivo evaluation of fenofibrate with a self- microemulsifying formulation.

Fenofibrate is virtually insoluble in water and is highly lipophilic, which leads to poor oral bioavailability. The purpose of this approach is to develop self-microemulsifying drug delivery system (SMEDDS) for oral bioavailability enhancement of fenofibrate. The in vitro dissolution test and pharmacokinetic behavior in beagle dogs were conducted to assess the formulation of fenofibrate in selfmicroemulsifying systems.

Effect of composite SiO₂@AuNPs on wound healing: in vitro and vivo studies.

Recently gold nanomaterials have been widely applied in the biomedical field, but their biosafety is still controversial. We immobilized small gold nanoparticles (AuNPs) on a large silica substrate to form silica-gold core-shell materials (SiO2@AuNPs) via classical seed-mediated growth. In vitro, 500 nm-SiO2@AuNPs could promote the proliferation of mouse embryonic fibroblast cells (NIH/3T3).

The In vitro and In vivo Evaluation of Fenofibrate with a Self-microemulsifying Formulation.

Fenofibrate is virtually insoluble in water and is highly lipophilic, which leads to poor oral bioavailability. The purpose of this approach is to develop self-microemulsifying drug delivery system (SMEDDS) for oral bioavailability enhancement of fenofibrate. The in vitro dissolution test and pharmacokinetic behavior in beagle dogs were conducted to assess the formulation of fenofibrate in self-microemulsifying systems.

Dissolution evaluation in vitro and bioavailability in vivo of self-microemulsifying drug delivery systems for pH-sensitive drug loratadine.

The aim of this study was to improve the oral absorption of loratadine, a pH-sensitive drug, by self-microemulsifying drug delivery systems (SMEDDSs). The optimal SMEDDS was analysed and evaluated after emulsification in distilled water with diameter of 26.57 ± 0.

Oil-based formulation as a sustained-released injection for a novel synthetic peptide.

In this study, sustained-release of GnRH antagonist peptide LXT-101 was realized through oil formulation, and their releasing characteristics in vitro and in vivo were investigated. In this formulation, the static interaction between cationic charged peptide LXT-101 and the negative charged phospholipid led to the formation of the phospholipid-peptide complex, by which LXT-101 was completely dissolved in oils. This formulation was prepared by mixing an aqueous solution of LXT-101 and empty SUV (small unilamellar liposomes) containing EPC (phosphatidylcholine) and DPPG (1, 2-dipalmitog-sn-glycero-3- phosphoglycerol) at an appropriate ratio, the mixture was subsequently lyophilized, and the resultant was dissolved in the oil to form a clear oily solution containing solubilized peptide LXT-101.

Determination of iodate by HPLC-UV after on-line electrochemical reduction to iodide.

In this study, a novel on-line pre-column electrochemical instrument (PECI) coupled with high-performance liquid chromatography (HPLC) was developed, and a novel method based on PEC-HPLC-UV for amplifying the ultraviolet (UV) response of iodate (IO₃⁻) was studied. Iodate undergoes reduction in the PECI, and the resulting I(-) was injected to an HPLC system and detected by a UV detector. For IO₃⁻ analysis, conditions that can influence the reduction efficiency, including applied potential, pH value and salt concentration, were investigated in detail.

Morphology of nanostructures and their long-acting properties in vivo for a novel synthetic peptide of gonadotropin-releasing hormone antagonist.

Objectives: To demonstrate the correlation between the nanostructure formation and the long duration of action in vivo of peptides, the morphology of nanostructures of LXT-101, a novel synthetic amphiphilic peptide of gonadotropin-releasing hormone antagonist were observed when dissolved in different solvents, and their long-acting properties in vivo were investigated in this study.

Methods: The morphology of nanostructures of LXT-101 was observed by transmission electron microscopy when dissolved in different solvents, and the plasma concentrations of LXT-101 and testosterone levels were also assayed for different solutions after intramuscular injection administration in beagle dogs.

Key Findings: TEM data suggest that LXT-101 in pure water can form fibres, while in mannitol, dextrose or sodium chloride solution, they tend to form vesicles.

Oral delivery of oil-based formulation for a novel synthetic cationic peptide of GnRH (gonadotropin-releasing hormone) antagonist for prostate cancer treatment.

LXT-101, a cationic peptide is a novel antagonist of gonadotropin-releasing hormone (GnRH) for prostate cancer treatment. However, effective delivery of peptide drugs into the body by the oral route remains a major challenge due to their origin properties with high molecular weights, strong polarity and low stability in the gastrointestinal (GI) tract. In this study, we have developed a novel oral delivery of oil-based formulation in which therapeutic peptide LXT-101 are solubilized in oils and with this solution as oil phase, an optimum formulation of self-microemulsifying drug delivery system (SMEDDS) was developed.