Modified Saengmaeksan, an herbal formula containing six herbs, improves hypertension through RhoA/Rho kinase-mediated vasorelaxation.

Background: Saengmaeksan is a traditional herbal formula used in Korean medicine. We composed a modified formula based on Saengmaeksan (mSMS) with Puerariae Radix, Platycodonis Radix, Liriopis seu Ophiopogonis Tuber, Schisandrae Fructus, Coicis Semen, and Dioscoreae Rhizoma to investigate its in vivo and ex vivo antihypertensive effects and underlying mechanisms.

Methods: The antihypertensive efficacy of mSMS was assessed using l-NAME-induced hypertensive mice and spontaneously hypertensive rats (SHR).

Long-acting injectable delivery system comprising ordered mixed drug aggregates with deaggregating and uniformly embeddable viscoelastic -polysaccharide solutions.

This study aimed to construct a ready-to-use, two-syringe mixing (TM) system comprising free-flowing drug aggregates with deaggregating and uniformly embeddable polysaccharide solutions as a new approach for long-acting parenteral delivery. Rotigotine (RG) and donepezil (DP), approved for the treatment of Parkinson's and Alzheimer's diseases, respectively, were employed as model compounds. For syringe filling, free-flowing drug aggregates were engineered using ordered mixing, adhering pulverized RG (1.

Comparative analysis of novel modified drug delivery systems for improving the oral bioavailability of water-insoluble tadalafil using copovidone, TPGS and hydroxypropyl-β-cyclodextrin.

This study aims to develop novel modified drug delivery systems (MDDS) including solid dispersions, solid self-nanoemulsifying drug delivery system (S-SNEDDS) and inclusion compound (IC) of poorly water-soluble tadalafil using various biological macromolecules and compare their ability to improve solubility, dissolution and bioavailability. Ingredients of MDDS were extensively screened using SEM, DSC, and XRD. The MDDS were testified for improved solubilization, dissolution, and bioavailability and were compared with tadalafil powder and commercial product (Cialis tablets 20 mg).

Development of a Carvedilol-Loaded Solid Self-Nanoemulsifying System with Increased Solubility and Bioavailability Using Mesoporous Silica Nanoparticles.

This study developed a solid self-nanoemulsifying drug delivery system (S-SNEDDS) to improve the oral bioavailability of poorly soluble carvedilol using mesoporous silica nanoparticles (MSNs). The liquid self-nanoemulsifying drug delivery system (L-SNEDDS) consisted of carvedilol, Peceol, Tween 80, and Labrasol in a weight ratio of 10:25:50:25. The liquid SNEDDS was suspended in MSN at various ratios and spray-dried to produce S-SNEDDS.

Comparison of Solid Self-Nanoemulsifying Systems and Surface-Coated Microspheres: Improving Oral Bioavailability of Niclosamide.

Purpose: This study aimed to develop a solid self-nanoemulsifying drug delivery system (SNEDDS) and surface-coated microspheres to improve the oral bioavailability of niclosamide.

Methods: A solubility screening study showed that liquid SNEDDS, prepared using an optimized volume ratio of corn oil, Cremophor RH40, and Tween 80 (20:24:56), formed nanoemulsions with the smallest droplet size. Niclosamide was incorporated into this liquid SNEDDS and spray-dried with calcium silicate to produce solid SNEDDS.

Optimized method development and validation for determining donepezil in rat plasma: A liquid-liquid extraction, LC-MS/MS, and design of experiments approach.

Donepezil (DPZ), a piperidine-based reversible cholinesterase inhibitor, finds extensive use in treating Alzheimer's disease (AD). Originally designed as an oral formulation, DPZ encounters drawbacks such as a brief duration of action and reduced treatment effectiveness in elderly patients with memory impairment or difficulty swallowing medications. To address these issues and improve patient compliance, researchers are actively exploring alternative DPZ formulations.

Dexamethasone nanocrystals-embedded hydroxypropyl methylcellulose hydrogel increases cochlear delivery and attenuates hearing loss following intratympanic injection.

Herein, dexamethasone (DEX) nanocrystalline suspension (NS)-embedded hydrogel (NS-G) was constructed using a hydroxypropyl methylcellulose (HPMC) polymer to enhance cochlear delivery and attenuate hearing loss following intratympanic (IT) injection. Hydrophobic steroidal nanocrystals were prepared using a bead milling technique and incorporated into a polysaccharide hydrogel. The NS-G system with HPMC (average molecular weight, 86,000 g/mol; 15 mg/mL) was characterized as follows: rod-shaped drug crystalline; particle size <300 nm; and constant complex viscosity ≤1.

Injectable dual thermoreversible hydrogel for sustained intramuscular drug delivery.

Herein, we reported novel docetaxel-decorated solid lipid nanoparticle (DCT-SLN)-loaded dual thermoreversible system (DCT-DRTS) for intramuscular administration with reduced burst effect, sustained release and improved antitumor efficacy. The optimized DCT-DRTs was subjected to in-vitro and in-vivo analyses. Antitumor evaluation of the DCT-DRTS was executed and compared with DCT-hydrogel, and DCT-suspension trailed by the histopathological and immune-histochemical analyses.

Comparison of two self-nanoemulsifying drug delivery systems using different solidification techniques for enhanced solubility and oral bioavailability of poorly water-soluble celecoxib.

In this study, we aimed to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) and a solid self-nanoemulsifying granule system (S-SNEGS) to enhance the solubility and oral bioavailability of celecoxib. This process involved the preparation of a liquid SNEDDS (L-SNEDDS) and its subsequent solidification into a S-SNEDDS and a S-SNEGS. The L-SNEDDS consisted of celecoxib (drug), Captex® 355 (Captex; oil), Tween® 80 (Tween 80; surfactant) and D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS; cosurfactant) in a weight ratio of 3.

Novel -Loaded Polyvinylpyrrolidone/SiO Nanofiber for Wound Dressing Prepared Using Electrospinning Method.

Electrospun nanofibers have been used as wound dressings to protect skin from infection and promote wound healing. In this study, we developed polyvinylpyrrolidone (PVP)/silicon dioxide (SD) composite nanofibers for the delivery of probiotic (SC), which potentially aids in wound healing. PVP/SD composite nanofibers were optimized through electrospinning, and bead-free nanofibers with an average diameter of 624.

Carboxymethyl cellulose-based rotigotine nanocrystals-loaded hydrogel for increased transdermal delivery with alleviated skin irritation.

Transdermal rotigotine (RTG) therapy is prescribed to manage Parkinson's disease (Neupro® patch). However, its use is suffered from application site reactions. Herein, drug nanocrystalline suspension (NS)-loaded hydrogel (NS-HG) employing polysaccharides simultaneously as suspending agent and hydrogel matrix was constructed for transdermal delivery, with alleviated skin irritation.

Modification of microenvironmental pH of nanoparticles for enhanced solubility and oral bioavailability of poorly water-soluble celecoxib.

This study aimed to develop a novel pH-modified nanoparticle with improved solubility and oral bioavailability of poorly water-soluble celecoxib by modifying the microenvironmental pH. After assessing the impact of hydrophilic polymers, surfactants and alkaline pH modifiers on the drug solubility, copovidone, sodium lauryl sulfate (SLS) and meglumine were chosen. The optimal formulation of solvent-evaporated, surface-attached and pH-modified nanoparticles composed of celecoxib/copovidone/SLS/meglumine at weight ratios of 1:1:0.

Antiangiogenic Therapeutic mRNA Delivery Using Lung-Selective Polymeric Nanomedicine for Lung Cancer Treatment.

Therapeutic antibodies that block vascular endothelial growth factor (VEGF) show clinical benefits in treating nonsmall cell lung cancers (NSCLCs) by inhibiting tumor angiogenesis. Nonetheless, the therapeutic effects of systemically administered anti-VEGF antibodies are often hindered in NSCLCs because of their limited distribution in the lungs and their adverse effects on normal tissues. These challenges can be overcome by delivering therapeutic antibodies in their mRNA form to lung endothelial cells, a primary target of VEGF-mediated pulmonary angiogenesis, to suppress the NSCLCs.

Impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system and self nano-emulsifying granule system.

The purpose of this study was to investigate the impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system (SNEDDS) and self nano-emulsifying granule system (SEGS). The mesoporous calcium silicate (Ca-silicate) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were utilised as hydrophobic carrier and hydrophilic carrier, respectively. The liquid SNEDDS formulation, composed of Tween80/Kollipohr EL/corn oil (35/50/15%) with 31% (w/w) dexibuprofen, was spray-dried and fluid-bed granulated together with Avicel using Ca-silicate or HP- β-CD as a solid carrier, producing four different solid SNEDDS and SEGS formulations.

Novel rivaroxaban-loaded microsphere systems with different surface microstructure for enhanced oral bioavailability.

This study compares rivaroxaban-loaded polymeric microsphere systems with three types of surface microstructure. Three types of polymeric microspheres loaded with rivaroxaban were fabricated using a spray-drying technique: solvent-evaporated, surface-attached, and solvent-wet microspheres, depending on whether the drug and additives used are soluble in the solvent. The solvent-evaporated and surface-attached microspheres had a rivaroxaban/polyvinylpyrrolidone/sodium lauryl sulfate (SLS) weight ratio of 1/0.

Liposomal co-delivery of toll-like receptors 3 and 7 agonists induce a hot triple-negative breast cancer immune environment.

Triple-negative breast cancer (TNBC) is highly aggressive and has no standard treatment. Although being considered as an alternative to conventional treatments for TNBC, immunotherapy has to deal with many challenges that hinder its efficacy, particularly the poor immunogenic condition of the tumor microenvironment (TME). Herein, we designed a liposomal nanoparticle (LN) platform that delivers simultaneously toll-like receptor 7 (imiquimod, IQ) and toll-like receptor 3 (poly(I:C), IC) agonists to take advantage of the different toll-like receptor (TLR) signaling pathways, which enhances the condition of TME from a "cold" to a "hot" immunogenic state.

Enhanced Oral Bioavailability of Rivaroxaban-Loaded Microspheres by Optimizing the Polymer and Surfactant Based on Molecular Interaction Mechanisms.

This study aimed to develop microspheres using water-soluble carriers and surfactants to improve the solubility, dissolution, and oral bioavailability of rivaroxaban (RXB). RXB-loaded microspheres with optimal carrier (poly(vinylpyrrolidone) K30, PVP) and surfactant (sodium lauryl sulfate (SLS)) ratios were prepared. H NMR and Fourier transform infrared (FTIR) analyses showed that drug-excipient and excipient-excipient interactions affected RXB solubility, dissolution, and oral absorption.

Hydroxypropyl-β-cyclodextrin-based solid dispersed granules: A prospective alternative to conventional solid dispersion.

The purpose of the present study was to develop hydroxypropyl-β-cyclodextrin (HP-β-CD)-based solid dispersed granules as a superior system to solid dispersion. The solid dispersed granules and solid dispersion were compared in terms of powder property improvement, solubility increment and oral bioavailability enhancement of poorly water-soluble dexibuprofen. Solid dispersion (drug/HP-β-CD/Tween80 = 1:7:0.