Fabrication and evaluation of chitosan-coated nanostructured lipid carriers for co-delivery of paclitaxel and PD-L1 siRNA.

This study aimed to develop a nanostructured lipid carrier (NLC) capable of co-delivering paclitaxel (PTX) and programmed death-ligand 1 (PD-L1) small interfering RNA (siRNA) to enhance PTX bioavailability and bolster immunity through PD-L1 knockdown. We prepared a PTX-loaded NLC (P-NLC) and coated it with positively charged chitosan (Chi) to create P-NLC-Chi, which was subsequently conjugated to siRNA (P-NLC-Chi-siRNA). The P-NLC-Chi formulation was optimized using the Box-Behnken design.

Sialic acid-decorated liposomes enhance the anti-cancer efficacy of docetaxel in tumor-associated macrophages.

Tumor-associated macrophages (TAMs) in the tumor microenvironment potentially enhance tumor growth and invasion through various mechanisms and are thus an essential factor in tumor immunity. The highly expressed siglec-1 receptors on the surfaces of TAMs are potential targets for cancer drug delivery systems. Sialic acid (SA) is a specific ligand for siglec-1.

Sustained delivery of triamcinolone acetonide from a thermosensitive microemulsion gel system for the treatment of sensorineural hearing loss.

Intratympanic administration for the delivery of steroids has been extensively studied but limited because of low permeability of the drug through the row window membrane. Here, to effectively deliver poorly soluble triamcinolone acetonide (TA), microemulsions (ME) were prepared from Capmul MCM (oil), Cremophor RH40 (surfactant), and tetraglycol (cosurfactant) based on solubility studies, emulsifying ability test, and pseudoternary phase diagrams. Microemulsion gel (MEG) was prepared by mixing TA-ME with a poloxamer hydrogel base.

Controlled therapeutic delivery of CO from carbon monoxide-releasing molecules (CORMs).

Carbon monoxide (CO) has been regarded as a "silent killer" for its toxicity toward biological systems. However, a low concentration of endogenously produced CO has shown a number of therapeutic benefits such as anti-inflammatory, anti-proliferative, anti-apoptosis, and cytoprotective activities. Carbon monoxide-releasing molecules (CORMs) have been developed as alternatives to direct CO inhalation, which requires a specialized setting for strict dose control.

Application of supercritical fluid technology for solid dispersion to enhance solubility and bioavailability of poorly water-soluble drugs.

Many new chemical entities (NCEs) have been discovered with the development of the pharmaceutical industry. However, the main disadvantage of these drugs is their low aqueous solubility, which results in poor bioavailability, posing a challenge for pharmaceutical scientists in the field of drug development. Solid dispersion (SD) technology is one of the most successful techniques used to resolve these problems.

Local drug delivery using poly(lactic-co-glycolic acid) nanoparticles in thermosensitive gels for inner ear disease treatment.

Intratympanic (IT) therapies have been explored to address several side effects that could be caused by systemic administration of steroids to treat inner ear diseases. For effective drug delivery to the inner ear, an IT delivery system was developed using poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) and thermosensitive gels to maintain sustained release. Dexamethasone (DEX) was used as a model drug.

Docetaxel-loaded PLGA nanoparticles to increase pharmacological sensitivity in MDA-MB-231 and MCF-7 breast cancer cells.

This study aimed to develop docetaxel (DTX) loaded poly(lactic-coglycolic acid) (PLGA) nanoparticles (DTX-NPs) and to evaluate the different pharmacological sensitivity of NPs to MCF-7 and MDA-MB-231 breast cancer cells. NPs containing DTX or coumarin-6 were prepared by the nanoprecipitation method using PLGA as a polymer and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as a surfactant. The physicochemical properties of NPs were characterized.

Formulation of solid dispersion to improve dissolution and oral bioavailability of poorly soluble dexibuprofen.

Dexibuprofen (DEXI) belongs to BCS class II drug with poor aqueous solubility resulting in poor bioavailability. To enhance solubility and bioavailability of DEXI, DEXI-loaded solid dispersion (SD) was formulated. DEXI-SDs were prepared by melting method and solvent evaporation method.

Potential and Applications of Nanocarriers for Efficient Delivery of Biopharmaceuticals.

During the past two decades, the clinical use of biopharmaceutical products has markedly increased because of their obvious advantages over conventional small-molecule drug products. These advantages include better specificity, potency, targeting abilities, and reduced side effects. Despite the substantial clinical and commercial success, the macromolecular structure and intrinsic instability of biopharmaceuticals make their formulation and administration challenging and render parenteral delivery as the only viable option in most cases.

Use of a Spinal Thermal Massage Device for Anti-oxidative Function and Pain Alleviation.

Elderly people are vulnerable to a variety of diseases, including chronic pain, which reduces their levels of physical fitness. Thermal massage has been shown to relieve pain and activate antioxidant enzymes. The objective of this study was to determine whether thermal massaging of the spinal column can reduce muscle pain and induce antioxidant function.

Therapeutic effects of celecoxib polymeric systems in rat models of inflammation and adjuvant-induced rheumatoid arthritis.

The incidence of rheumatoid arthritis (RA), an autoimmune inflammatory disease, is rapidly increasing in aging societies. In the current study, celecoxib (CXB) micelles were developed to improve the oral absorption and anti-inflammatory effects of CXB in cell studies and λ-carrageenan rat models, and to enhance the therapeutic effects of CXB on RA in complete Freund's adjuvant (CFA)-induced RA rat models. Moreover, CXB micelles and previously developed solid dispersion (SD6) formulations were evaluated.

Chitosan-coated nanostructured lipid carriers of fenofibrate with enhanced oral bioavailability and efficacy.

Fenofibrate is frequently used to lower cholesterol levels in cardiovascular disease. Owing to its poor solubility and high gastrointestinal permeability, it is classified as a Biopharmaceutics Classification System class II compound. The aim of this study was to improve the solubility and bioavailability of fenofibrate by formulating it as fenofibrate-loaded nanostructured lipid carriers (FFB-NLCs) and coating it with a biodegradable polymer to allow controlled drug release.

Design and evaluation of the anticancer activity of paclitaxel-loaded anisotropic-poly(lactic-co-glycolic acid) nanoparticles with PEGylated chitosan surface modifications.

This study aimed to evaluate the anticancer activity of paclitaxel-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (PNPs) based on their shapes and surface modifications in breast cancer cells. We hypothesized that anisotropic-PNPs (AT-PNPs) with PEGylated chitosan (CP) surface modifications and high aspect ratios exhibit higher anticancer activity than PNPs and AT-PNPs with CP surface modifications and low aspect ratios. Six types of PNPs and AT-PNPs with different shapes and surface modifications were successfully prepared.

Design of Coenzyme Q10 solid dispersion for improved solubilization and stability.

Solubilization and stabilization of poorly soluble drugs are important issues in the pharmaceutical industry. Herein, a Coenzyme Q10 (CQ10) solid dispersion (SD) formulation was designed to enhance CQ10 solubility, dissolution (%), and stability. CQ10 SD formulations were prepared with a dual polymer system using a melting method.

Optimization of Polyarginine-Conjugated PEG Lipid Grafted Proliposome Formulation for Enhanced Cellular Association of a Protein Drug.

The purpose of this study was to develop an oral proliposomal powder of protein using poly-l-arginine-conjugated 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol) (DSPE-PEG) (PLD) for enhancing cellular association upon reconstitution and to compare its effects with a non-grafted and PEGylated formulation. Cationic proliposome (CATL), PLD-grafted CATL (PLD-CATL), PEGylated CATL (PEG CATL), and PLD grafted-PEG CATL (PLD-PEG CATL) were prepared and compared. Successful conjugation between poly-l-arginine and DSPE-PEG was confirmed by H NMR and FT-IR.

Antibacterial effect of traditional food ingredients for healthcare on Helicobacter pylori.

Background: The development of antibacterial materials using various traditional food ingredients will be valuable to inhibit Helicobacter pylori in the future. The vegetables and herbs used in this study were food ingredients that normal people eat every day. This paper can be used as a resource for healthcare.

Improvement of the dissolution rate and bioavailability of fenofibrate by the supercritical anti-solvent process.

The purpose of this study was to improve solubility and oral bioavailability of fenofibrate via solid dispersion (SD) using a supercritical anti-solvent (SAS) process with amphipathic polymers P407 and TPGS. Solid dispersion techniques have been widely used to enhance the solubility and dissolution profiles of poorly soluble drugs. Fenofibrate is classified as a Biopharmaceutics Classification System class II compound because of its low solubility and high gastrointestinal permeability.

Comparison of paclitaxel solid dispersion and polymeric micelles for improved oral bioavailability and in vitro anti-cancer effects.

The purpose of this study was to develop paclitaxel (PTX) formulations with solid dispersion (SD) and micelles (M) in order to improve solubility and oral absorption in rats. In addition, the enhanced anti-cancer effects of PTX formulations were compared in various breast cancer cell lines. The SD formulations with various copolymers were prepared using a solvent evaporation method, and micelles with Soluplus® mixed with d-α-tocopheryl polyethylene glycol-1000-succinate (TPGS) were prepared using a film hydration method.

Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs.

Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic anticancer drugs) based on effectiveness and safety profile. Biologic drugs are administered by intravenous (IV) injection due to their large molecular weight, while small molecule drugs are preferentially administered by gastrointestinal route.

Design of novel proliposome formulation for antioxidant peptide, glutathione with enhanced oral bioavailability and stability.

To develop proliposome formulations to improve the oral bioavailability of l-glutathione (GSH), GSH-loaded proliposomes were prepared using the granule method. Mannitol was selected as an effective excipient to achieve the desired particle size, entrapment efficiency (EE), and solubility for oral delivery of the final formulation. To evaluate the effect of surface charge of proliposomes on the oral bioavailability of GSH, negative (F1-F4) and positive proliposomes (F5-F9) were prepared.

Naftopidil-fumaric acid interaction in a solid dispersion system: Improving the dissolution rate and oral absorption of naftopidil in rats.

The aim of this study was to improve the dissolution rate and oral absorption of naftopidil (NAF) in rats via solid dispersion (SD) with a weak acid and copolymer. We hypothesized that the dissolution rate and oral bioavailability of NAF would increase through hydrogen bonding between NAF and weak acids/hydrophilic polymers. d‑α‑Tocopherol polyethylene glycol 1000 succinate (TPGS) and fumaric acid were selected as the hydrophilic polymer and weak acid based on their apparent solubility and pre-dissolution test results, respectively.

Amorphous multi-system of celecoxib improves its anti-inflammatory activity in vitro and oral absorption in rats.

In the present study, a multi-system for solid dispersion (SD) of celecoxib (CXB) was designed to improve its solubility and anti-inflammatory effects in vitro as well as oral absorption in rats. The SD formulations were prepared by a solvent evaporation with a multi-system as the solubilizer; an alkalizer; and fumed silica (Aerosil 200). The physicochemical properties of the SD formulations were evaluated.

Comparison of adsorption and conjugation of Herceptin on poly(lactic-co-glycolic acid) nanoparticles - Effect on cell internalization in breast cancer cells.

Surfaces of nanoparticles with are commonly modified to enhance the targeting effect. In this study, we performed surface modifications of docetaxel (DTX)-loaded poly(lactic-co-glycolic acid) nanoparticles (PNPs) with Herceptin® (HCT) to improve the internalization and cytotoxicity in breast cancer cells. The PNPs were prepared with surfactant, poly(ethylene-alt-maleic anhydride) (PEMA), including a number of carboxyl groups for conjugation.

Solid dispersion of dutasteride using the solvent evaporation method: Approaches to improve dissolution rate and oral bioavailability in rats.

The aim of this study was to develop a dutasteride (DUT) solid dispersion (SD) using hydrophilic substances to enhance its dissolution (%) and oral bioavailability in rats. DUT-SD formulations were prepared with various co-polymers using a solvent evaporation method. The physical properties of DUT-SD formulations were confirmed using field emission scanning electron microscopy (FE-SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and attenuated total reflectance Fourier transform infrared (ATR-FT-IR) spectroscopy.

Alleviation of ascorbic acid-induced gastric high acidity by calcium ascorbate and .

Ascorbic acid is one of the most well-known nutritional supplement and antioxidant found in fruits and vegetables. Calcium ascorbate has been developed to mitigate the gastric irritation caused by the acidity of ascorbic acid. The aim of this study was to compare calcium ascorbate and ascorbic acid, focusing on their antioxidant activity and effects on gastric juice pH, total acid output, and pepsin secretion in an rat model, as well as pharmacokinetic parameters.