Bifunctional Oxaliplatin (IV) Prodrug Based pH-Sensitive PEGylated Liposomes for Synergistic Anticancer Action Against Triple Negative Breast cancer.

Triple negative breast cancer (TNBC) exhibits higher susceptibility towards oxaliplatin (OXA) due to a faulty DNA damage repair system. However, the unfavorable physicochemical properties and risk of toxicities limit the clinical utility of OXA. Therefore, to impart kinetic inertness, site-specific delivery, and multidrug action, an octahedral Pt(IV) prodrug was developed by using chlorambucil (CBL) as a choice of ligand.

Enhancing oral bioavailability of dasatinib via supersaturable SNEDDS: Investigation of precipitation inhibition and IVIVC through in-vitro lipolysis-permeation model.

Dasatinib (DASA), a potent second-generation multitarget kinase inhibitor marketed as Sprycel® (Tablet), is limited by poor oral bioavailability (14-24 %) and dose-related gastrointestinal side effects. A supersaturable self-nanoemulsifying drug delivery system (su-SNEDDS) designed to enhance DASA's solubility, sustain supersaturation, and improve oral bioavailability. The su-SNEDDS formulation comprises DASA, an oil, surfactant, co-surfactant, and polyvinylpyrrolidone (PVP) K30 as a precipitation inhibitor (PI).

Addressing overlooked design considerations for nanoemulsions.

Despite progress in genetic and molecular research, which has opened up a myriad of targeted therapeutic possibilities, the compromised solubility and absorption profile of therapeutic entities restrict their passage across lipid barriers compromising efficacy. Consequently, nanoemulsions accrued significance as futuristic, safe, and effective lipid-based drug delivery systems due to their inherent array of physicochemical properties and provide exquisite bioavailability, reduced toxicity, and improved solubility of hydrophobic entities based on size and surface area. However, a pronounced gap exists in understanding and addressing challenges that arise during design and development of nanoemulsions.

Launching triple-hit chemo attack on TNBC through nanoparticle-mediated codelivery of cisplatin-chlorambucil conjugate and venetoclax.

The BRCA1 dysfunction and HR deficiency in TNBC are responsible for high effectiveness of DNA-damaging agents in TNBC treatment. Preclinical and clinical studies confirmed the effectiveness of cisplatin in TNBC treatment. Nevertheless, the clinical utility of cisplatin is inadequate due to severe systemic side effects and resistance development.

Investigation of Mirabegron-loaded Nanostructured Lipid Carriers for Improved Bioabsorption: Formulation, Statistical Optimization, and In-Vivo Evaluation.

Overactive bladder (OAB) is a usual medical syndrome that affects the bladder, and Mirabegron (MBG) is preferred medicine for its control. Currently, available marketed formulations (MYRBETRIQ® granules and MYRBETRIQ® ER tablets) suffer from low bioavailability (29-35%) hampering their therapeutic effectiveness and compromising patient compliance. By creating MBG nanostructured lipid carriers (MBG-NLCs) for improved systemic availability and drug release, specifically in oral administration of OAB treatment, this study aimed to address these issues.

Gemini surfactants as next-generation drug carriers in cancer management.

Introduction: Gemini surfactants (GS) are an elite class of amphiphilic molecules that have shown up as a potential candidate in the field of drug delivery because of their exceptional physicochemical properties. They comprise two hydrophilic headgroups connected by an adaptable spacer and hydrophobic tails that has shown promising results in delivering different therapeutic agents to cancer cells at preclinical level. However further studies are in demand to unlock the full potential of GS in this field.

A novel strategy to elicit enduring anti-morphine immunity and relief from addiction by targeting Acr1 protein nano vaccine through TLR-2 to dendritic cells.

Morphine addiction poses a significant challenge to global healthcare. Current opioid substitution therapies, such as buprenorphine, naloxone and methadone are effective but often lead to dependence. Thus, exploring alternative treatments for opioid addiction is crucial.

Unveiling the potential of ursolic acid modified hyaluronate nanoparticles for combination drug therapy in triple negative breast cancer.

Triple negative breast cancer (TNBC) represents the most aggressive and heterogenous disease, and combination therapy holds promising potential. Here, an enzyme-responsive polymeric prodrug with self-assembly properties was synthesized for targeted co-delivery of paclitaxel (PTX) and ursolic acid (UA). Hyaluronic acid (HA) was conjugated with UA, yielding an amphiphilic prodrug with 13.

Gemcitabine-Phospholipid Complex Loaded Lipid Nanoparticles for Improving Drug Loading, Stability, and Efficacy against Pancreatic Cancer.

This study aims to encapsulate gemcitabine (GEM) using a phospholipid complex (PLC) in lipid nanoparticles (NPs) to achieve several desirable outcomes, including high drug loading, uniform particle size, improved therapeutic efficacy, and reduced toxicities. The successful preparation of GEM-loaded lipid NPs (GEM-NPs) was accomplished using the emulsification-solidification method, following optimization through Box-Behnken design. The size of the GEM-NP was 138.

Unlocking apoptosis in triple negative breast cancer: Harnessing "glutamine trap" to amplify the efficacy of lapatinib-loaded mixed micelles.

Certain aggressive cancers, such as triple-negative breast cancer (TNBC), heavily bank on glutamine for their proliferation and survival. In this context, TNBC functions as a "glutamine trap," extracting circulating glutamine at a rate surpassing that of any other organ. Moreover, the overexpression of Alanine, Serine, Cysteine Transporter 2 (ASCT2), a key player in glutamine uptake, further underscores the significance of targeted therapy to enhance TNBC treatment.

Oral delivery of aescin-loaded gelatin nanoparticles ameliorates carbon tetrachloride-induced hepatotoxicity in Wistar rats.

Aim: The liver plays a crucial role in biotransformation but it is susceptible to chemical-induced damage, known as hepatotoxicity. Traditional therapies for protecting the liver face significant challenges, including poor bioavailability, off-target effects, adverse reactions, drug breakdown, and inadequate uptake. These issues emphasize the need for precise, targeted therapeutic approaches against hepatotoxicity.

Enhancing anti-cancer potential by delivering synergistic drug combinations via phenylboronic acid modified PLGA nanoparticles through ferroptosis-based therapy.

In this study, we investigated the potential of the sorafenib (SOR) and simvastatin (SIM) combination to induce ferroptosis-mediated cancer therapy. To enhance targeted drug delivery, we encapsulated the SOR + SIM combination within 4-carboxy phenylboronic acid (CPBA) modified PLGA nanoparticles (CPBA-PLGA(SOR + SIM)-NPs). The developed CPBA-PLGA(SOR + SIM)-NPs exhibited a spherical shape with a size of 213.

Genipin-crosslinked albumin nanoparticles containing neratinib and silibinin: A dual-death therapy for triple negative breast cancer.

Triple negative breast cancer (TNBC) cells resist chemotherapy by hijacking apoptosis. Alternative cell death forms like ferroptosis offer new treatment options. A combined therapy using neratinib (NTB; ferroptosis inducer) and silibinin (SLB; apoptosis inducer) via albumin-based nanocarriers (N-S Alb NPs) was explored to target TNBC.

Enzyme targeted delivery of sivelestat loaded nanomicelle inhibits arthritic severity in experimental arthritis.

Aims: Rheumatoid arthritis (RA) is chronic inflammatory disorder mainly affects the lining of articular cartilage of synovial joints characterized by severe inflammation and joint damage. The expression of proteolytic enzymes like MMP-2 and Neutrophil Elastase (NE) worsens the RA condition. To address this concern, we have synthesized dual enzyme targeted chlorotoxin conjugated nanomicelles loaded with sivelestat as broad spectrum treatment for RA.

Synergistic anticancer therapy via ferroptosis using modified bovine serum albumin nanoparticles loaded with sorafenib and simvastatin.

Ferroptosis is a non-apoptotic cell death pathway characterized by the accumulation of lipid-peroxy radicals within the affected cells. Here, we investigate the synergistic capacity of sorafenib (SOR) and simvastatin (SIM) to trigger ferroptosis for cancer therapy. For precise in-vivo delivery, SOR + SIM was ratiometrically loaded in bovine serum albumin nanoparticles (BSA-NPs) modified with 4-carboxy phenylboronic acid (CPBA).

Exploring Sorafenib and Simvastatin Combination for Ferroptosis-Induced Cancer Treatment: Cytotoxicity Screening, In Vivo Efficacy, and Safety Assessment.

Ferroptosis, a pathway dependent on oxygen and iron catalysts, holds promise as a therapeutic approach for cancer treatment due to its manageable regulation, direct control, and immunogenic properties. The sensitivity of cancer cells to ferroptosis induction varies based on their metabolic, genetic, and signalling pathways, prompting the use of combination therapy. In this study, we conducted a screening of drug combinations, including sorafenib (SOR) with simvastatin (SIM), phenethyl isothiocyanate, and trigonelline, in MDA-MB-231, A549, and HeLa cells to assess their cytotoxicity.

Enhancing oral bioavailability of insulin through bilosomes: Implication of charge and chain length on apical sodium-dependent bile acid transporter (ASBT) uptake.

This study investigates the impact of charge and chain length of bile salts in the bilosomes on the oral bioavailability of insulin (IN) by examining their uptake via the apical sodium-dependent bile acid transporter (ASBT). Deoxycholic acid bile salt was conjugated with different amino acids to create conjugates with varying charge and chain length, which were then embedded in liposomes. The resulting bilosomes had a particle size <400 nm, a PDI of 0.

Exploring the synergistic behavior of paclitaxel and vorinostat upon co-loading in albumin nanoparticles for breast cancer management.

Breast cancer is challenging to treat accompanied with poor clinical outcomes. Paclitaxel (PTX) is a first-line chemotherapeutic agent, but possesses limitations due to side effects, high dose, non-specific tissue distribution, and drug resistance. An epigenetic modulator, vorinostat (VOR) is known to enhance PTX efficacy and therefore to resolve the issues of conventional PTX formulations, we designed PTX- and VOR-bound albumin nanoparticles (PTX-VOR-BSA-NPs) using antisolvent precipitation technique where albumin is used as a carrier and a targeting agent.

α-Terpineol Mitigates Dextran Sulfate Sodium-Induced Colitis in Rats by Attenuating Inflammation and Apoptosis.

Ulcerative colitis (UC) is one of the major inflammatory disorders of the gastrointestinal tract. α-Terpineol (αTL) is naturally present in several plants, and it belongs to the monoterpenes category. αTL possesses various pharmacological properties such as antioxidant, antibacterial, antifungal, anticancer, and antiulcer activities.

Antibody-conjugated pH-sensitive liposomes for HER-2 positive breast cancer: development, characterization, and assessment.

The object of the current study was to develop and evaluate trastuzumab-conjugated Paclitaxel (PTX) and Elacridar (ELA)-loaded PEGylated pH-sensitive liposomes (TPPLs) for site-specific delivery of an anticancer drug. In this study, paclitaxel is used as an anticancer drug which promotes microtubules polymerization and arrest cell cycle progression at mitosis and subsequently leading to cell death. The single use of PTX causes multiple drug resistance (MDR) and results failure of the therapy.

Highly Biocompatible Smart Injectable Hydrogel for the Management of Rheumatoid Arthritis.

Rheumatoid arthritis (RA) is a chronic inflammatory disease that severely affects joints and restricts locomotion. Various treatment regimens are available for RA, providing short-term relief from pain, but long-term relief from the disease is still not available. Evidently, cytokines play a crucial role in the pathophysiology of the disease.