Antibacterial Activity and Mechanism of Action of Osthole against .

The purpose of this study was to investigate the antibacterial activity and mechanism of action of osthole against . The antibacterial activity of osthole was evaluated by determining the minimum inhibitory concentration (MIC) and growth curve. Cell morphology, membrane permeability, membrane integrity, bacterial physiology, and metabolism were explored using different methods to elucidate the mechanism of action of osthole.

A disulfiram/copper gluconate co-loaded bi-layered long-term drug delivery system for intraperitoneal treatment of peritoneal carcinomatosis.

To develop a long-term drug delivery system for the treatment of primary and metastatic peritoneal carcinoma (PC) by intraperitoneal (IP) injection, a disulfiram (DSF)/copper gluconate (Cu-Glu)-co-loaded bi-layered poly (lactic acid-coglycolic acid) (PLGA) microspheres (Ms) - thermosensitive hydrogel system (DSF-Ms-Cu-Glu-Gel) was established. Rate and mechanisms of drug release from DSF-Ms-Cu-Glu-Gel were explored. The anti-tumor effects of DSF-Ms-Cu-Glu-Gel by IP injection were evaluated using H22 xenograft tumor model mice.

Crystallization inhibitory effects of konjac glucomannan, sodium alginate and xanthan gum on curcumin in supersaturated solution.

Supersaturating drug delivery system (SDDS) is a promising approach to enhance the solubility of hydrophobic functional components. However, SDDS is thermodynamically unstable and crystallization tends to occur. In this work, curcumin was used as a model compound, and the crystallization inhibitory effect of konjac glucomannan (KGM), sodium alginate (SA) and xanthan gum (XTG) on curcumin in supersaturated solution was investigated.

Hydrochlorothiazide/Losartan Potassium Tablet Prepared by Direct Compression.

Hydrochlorothiazide (HCTZ)/losartan potassium (LOS-K) was used as a model drug to prepare compound tablets through the investigation of the compression and mechanical properties of mixed powders to determine the formulation and preparation factors, followed by D-optimal mixture experimental design to optimize the final parameters. The type and amount of lactose monohydrate (SuperTab®14SD, 19.53−26.

Goserelin/PLGA solid dispersion used to prepare long-acting microspheres with reduced initial release and reduced fluctuation of drug serum concentration in vivo.

To prepare Goserelin (GOS) loaded long-acting microspheres with reduced initial release and prolonged drug release time of GOS, GOS/PLGA solid dispersion (by hot-melt extrusion, HME) was dissolved/dispersed in dichloromethane (DCM) to prepare microspheres by O/W method. From results of molecular dynamics simulation, PLGA and GOS molecules completely and uniformly dissolved and dispersed in DCM, respectively. In F5 microspheres (prepared by HME-O/W method), GOS existed as molecular or amorphous state, but not aggregation.

Tumor Microenvironment-Responsive Shell/Core Composite Nanoparticles for Enhanced Stability and Antitumor Efficiency Based on a pH-Triggered Charge-Reversal Mechanism.

High systemic stability and effective tumor accumulation of chemotherapeutic agents are indispensable elements that determine their antitumor efficacy. PEGylation of nanoparticles (NPs) could prolong the retention time in vivo by improving their stability in circulation, but treatment suffers reduced tumor penetration and cellular uptake of nanomedicines. The tumor microenvironment (TME)-responsive NPs maintain their stealth features during circulation and undergo a stimuli-responsive dePEGylation once exposed to the site of action, thereby achieving enhanced internalization in tumor cells.

Pharmaceutical strategies in improving anti-tumour efficacy and safety of intraperitoneal therapy for peritoneal metastasis.

: In selected patients with limited peritoneal metastasis (PM), favorable tumor biology, and a good clinical condition, there is an indication for combination of cytoreductive surgery (CRS) and subsequent intravenous (IV) or intraperitoneal (IP) chemotherapy. Compared with IV injection, IP therapy can achieve a high drug concentration within the peritoneal cavity with low systemic toxicity, however, the clinical application of IP chemotherapy is limited by the related abdominal pain, infection, and intolerance.:To improve the anti-tumor efficacy and safety of IP therapy, various pharmaceutical strategies have been developed and show promising potential.

Lactoferrin for the treatment of COVID-19 (Review).

The coronavirus disease 2019 (COVID-19) outbreak was caused by infection with the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The clinical outcomes of elderly individuals and those with underlying diseases affected by COVID-19 are serious, and may result in acute respiratory distress syndrome (ARDS) and even mortality. Currently, the clinical treatments for COVID-19 mostly involve symptom alleviation measures and non-specific broad spectrum antiviral drugs, as highly effective antiviral drugs and vaccines are not yet available.

The effect of polymer blends on initial release regulation and in vitro-in vivo relationship of peptides loaded PLGA-Hydrogel Microspheres.

The aim of this study was to resolve the lag time problem for peptides loaded PLGA-Hydrogel Microspheres (PLGA-gel-Ms) by blending low molecular PLGA (Mw. 1 kDa) into PLGA (Mw. 10 kDa) as an intrinsic porogen, and then assess the in vitro-in vivo relationship (IVIVR).

Ginkgolides-loaded soybean phospholipid-stabilized nanosuspension with improved storage stability and in vivo bioavailability.

The purpose of this study was to investigate the effects of soybean phospholipid, as a steric stabilizer, on improving dissolution rate, storage stability and bioavailability of ginkgolides. The ginkgolides coarse powder, hydroxypropyl methylcellulose (HPMC), soybean phospholipid and sodium dodecyl sulfate (SDS) were mixed and wet-milled to prepare nanosuspension S1. Nanosuspension S2 was obtained by the same technique except adding the soybean phospholipid.

Goserelin Acetate Loaded Poloxamer Hydrogel in PLGA Microspheres: Core-Shell Di-Depot Intramuscular Sustained Release Delivery System.

This study aimed to prepare and optimize goserelin acetate (GOS) loaded hydrogel poly(d,l-lactic acid--glycolic acid) (PLGA) microsphere that is suitable for long-acting clinical treatment, investigate its structure, and regulate the initial release manner. Here, the PLGA microsphere containing Poloxamer hydrogel loaded with ∼15% (w/w) GOS was prepared by double-emulsion-solvent evaporation method and evaluated in terms of microscopic structure, physicochemical properties, and release manner in vitro and in vivo. Raman volume imaging and scanning electron microscopy studies revealed a core-shell Di-Depot structure of the microsphere, in which multi-GOS-loaded hydrogel depots were distributed in the core region.

Effects of the multilayer structures on Exenatide release and bioactivity in microsphere/thermosensitive hydrogel system.

Traditional polypeptide-loaded PLGA microspheres (PM) using emulsion electrospray techniques often exhibit unsteady release and limited bioactivity. To solve these two problems, an Exenatide (EXT)-loaded multilayer system composed ofPM and thermosensitive hydrogel was prepared by the emulsion electrospray technique in this study. Hydrogel mixture were loaded in PLGA microspheres as Depot-hydrogel to prepare Gel/PM.

Entrapping of Nanoparticles in Yeast Cell Wall Microparticles for Macrophage-Targeted Oral Delivery of Cabazitaxel.

In this work, a nano-in-micro carrier was constructed by loading polymer-lipid hybrid nanoparticles (NPs) into porous and hollow yeast cell wall microparticles (YPs) for macrophage-targeted oral delivery of cabazitaxel (CTX). The YPs, primarily composed of natural β-1,3-d-glucan, can be recognized by the apical membrane receptor, dectin-1, which has a high expression on macrophages and intestinal M cells. By combining electrostatic force-driven self-deposition with solvent hydration/lyophilization methods, the positively charged NPs loaded with CTX or fluorescence probes were efficiently packaged into YPs, as verified by scanning electron microscope (SEM), atomic force mircoscope (AFM), and confocal laser scanning microscopy (CLSM) images.

Exenatide-loaded microsphere/thermosensitive hydrogel long-acting delivery system with high drug bioactivity.

A series of mixed hydrogels of PLGA-PEG-PLGA and PCLA-PEG-PCLA were synthesized, and investigated in terms of their critical micelle concentration, stability and thermosensitive properties. Also, some mixed hydrogel was selected to prepare Depot-gel-in-Ms-in-Matrix-gel system for the treatment of type 2 diabetes mellitus. Briefly, Exenatide (EXT) loaded hydrogels was encapsulated in PLGA microspheres (Ms) and further encapsulated into blank hydrogel.

Hot-melt sub- and outercoating combined with enteric aqueous coating to improve the stability of aspirin tablets.

Aspirin is apt to hydrolyze. In order to improve its stability, a new method has been developed involving the application of hot-melt sub- and outercoating combined with enteric aqueous coating. The main aim was to investigate the influence of these factors on the stability of ASA and understand how they work.

Modified PLGA-PEG-PLGA thermosensitive hydrogels with suitable thermosensitivity and properties for use in a drug delivery system.

PLGA-PEG-PLGA (PPP) triblock copolymer is the most widely studied thermosensitive hydrogel owing to its non-toxic, biocompatible, biodegradable, and thermosensitive properties. PPP thermosensitive hydrogels are being investigated as in situ gels because, at a low temperature, PPP solutions with drugs can be injected at the target site, and converted into a gel without surgical procedures. To meet the requirements of different therapeutic applications, PPP hydrogels with different properties need to be synthesized.

Effects of Pluronic F127-PEG multi-gel-core on the release profile and pharmacodynamics of Exenatide loaded in PLGA microspheres.

Pluronic F127 and PEG as a multi-gel-core were used to prepare Exenatide-loaded microspheres and store the drug within the microspheres. Also, the sol-gel transition and novel functions of the Pluronic F127-PEG gel core were investigated.Microspheres with a multi-gel-core (GCMs) and without a multi-gel-core (Ms) were compared in terms of the rate of PLGA degradation, therelease kinetics in vitro and the efficacy in KKAy mice.

VB12-coated Gel-Core-SLN containing insulin: Another way to improve oral absorption.

To improve the oral absorption of insulin, a novel carrier of Vitamin B12 (VB12) gel core solid lipid nanopaticles (Gel-Core-SLN, GCSLN) was designed with a gel core, lipid matrix and VB12-coated surface. VB12-stearate was synthesized and characterized by infrared spectroscopy (IR), nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry (MS). Sol-gel conversion following ultrasonic heating and double emulsion technology were combined to implant the insulin-containing gel into solid lipid nanoparticles (SLN).

Investigation of a nanosuspension stabilized by Soluplus® to improve bioavailability.

The purpose of this work was to explore the feasibility of using Soluplus(®) in preparing a fenofibrate (FBT) nanosuspension adopting wet media milling technology. HPMC and Soluplus(®) were used as stabilizers to prepare FBT/HPMC nanosuspension (F1) and FBT/Soluplus(®) nanosuspension (F2), respectively. The nanosuspensions were subjected to evaluations involving particle size, dissolution, preliminary stability and pharmacokinetic behavior.

Improved dissolution rate and bioavailability of fenofibrate pellets prepared by wet-milled-drug layering.

Objective: The objective of this study is to investigate the wet-milled-drug layering process which could significantly improve the dissolution rate and oral bioavailability of fenofibrate pellets.

Methods: Fenofibrate was milled with HPMC-E5 to prepare a uniform suspension in the micrometer and nanometer range, and this suspension was then layered on to sugar spheres to form the pellets (F1, F2).

Results: The particle size was significantly reduced (from 1000 µm to 1-10 µm and 400 nm) but the fenofibrate in suspension retained its crystallinity from the results of DSC and PXRD investigations.