Berberine encapsulated phenylboronic acid-conjugated pullulan nanoparticles: Synthesis, characterization and anticancer activity validated in A431 skin cancer cells and 3D spheroids.

Polysaccharide-based drug delivery systems are in high demand due to their biocompatibility, non-toxicity, and low-cost. In this study, sialic acid receptor targeted 4-carboxy phenylboronic acid modified pullulan-stearic acid conjugate (4-cPBA-PUL-SA) was synthesized and characterized for the delivery of Berberine (BBR). BBR-loaded 4-cPBA-PUL-SA nanoparticles (BPPNPs) were monodispersed (PDI: 0.

Synthesis, characterization, and application of honey stabilized inulin nanoparticles as colon targeting drug delivery carrier.

Inulin (INU) is a versatile natural polysaccharide primarily derived from chicory roots. INU possesses the unique quality of evading digestion or fermentation in the early stages of the human digestive tract, instead reaching the lower colon directly. Exploiting on this distinctive attribute, INU finds application in the creation of targeted carrier systems for delivering drugs tailored to colon-related diseases.

Design of manganese-based nanomaterials for pharmaceutical and biomedical applications.

In the past few years, manganese-based nanostructures have been extensively investigated in the biomedical field particularly to design highly biocompatible theranostics, which can not only act as efficient diagnostic imaging contrast agents but also deliver the drugs to the target sites. The nanoscale size, large surface area-to-volume ratio, availability of cheap precursors, flexibility to synthesize nanostructures with reproducible properties and high yield, and easy scale up are the major reasons for the attraction towards manganese nanostructures. Along with these properties, the nontoxic nature, pH-sensitive degradation, and easy surface functionalization are additional benefits for the use of manganese nanostructures in biomedical and pharmaceutical sciences.

Development of thiolated xanthan gum-stearylamine conjugate based mucoadhesive system for the delivery of biochanin-A to melanoma cells.

Recently, instead of creating new active compounds, scientists have been working to increase the bioavailability and residence time of existing drugs by modifying the characteristics of the delivery systems. In the present study, a novel mucoadhesive bioconjugate (SN-XG-SH) was synthesized by functionalizing a polysaccharide xanthan gum (XG) with cysteamine hydrochloride (CYS) and a lipid stearylamine (SN). FTIR, CHNS and H NMR studies confirmed the successful synthesis of SN-XG-SH.

Nintedanib solid lipid nanoparticles improve oral bioavailability and ameliorate pulmonary fibrosis in vitro and in vivo models.

Nintedanib (NIN) and pirfenidone are the only approved drugs for the treatment of Idiopathic Pulmonary Fibrosis (IPF). However, NIN and pirfenidone have low oral bioavailability and limited therapeutic potential, requiring higher dosages to increase their efficacy, which causes significant liver and gastrointestinal toxicities. In this study, we aimed to develop nintedanib-loaded solid lipid nanoparticles (NIN-SLN) to improve the oral bioavailability and therapeutic potential against TGF-β-induced differentiation in IPF fibroblasts and bleomycin (BLM)-induced lung fibrosis in rat models.

Exploration of sialic acid receptors as a potential target for cancer treatment: A comprehensive review.

The potential to target anticancer drugs directly to cancer cells is the most difficult challenge in the current scenario. Progressive works are being done on multifarious receptors and are on the horizon, expected to facilitate tailored treatment for cancer. Among several receptors, one is the sialic acid (SA) receptor by which cancer cells can be targeted directly as hyper sialylation is one of the most distinguishing characteristics of cancer cells.

Folate Functionalized and Evodiamine-Loaded Pluronic Nanomicelles for Augmented Cervical Cancer Cell Killing.

Evodiamine (Evo) is a natural, biologically active plant alkaloid with wide range of pharmacological activities. In the present study Evo-loaded folate-conjugated Pluronic F108 nano-micelles (ENM) is synthesized to enhance the therapeutic efficacy of Evo against cervical cancer. ENM are synthesized, physicochemically characterized and in vitro anticancer activity is performed.

Amoxapine-Loaded Solid Lipid Nanoparticles with Superior Preclinical Pharmacokinetics for Better Brain Delivery: LC-MS/MS and GC-MS Analysis.

The tricyclic antidepressant amoxapine (AMX) has been reported for a rapid onset of action compared to other cyclic antidepressants. It has very low solubility and bioavailability due to first-pass metabolism. Therefore, we planned to develop solid lipid nanoparticles (SLNs) of AMX using a single emulsification method to increase its solubility and bioavailability.

Dendrimer-Mediated Delivery of Anticancer Drugs for Colon Cancer Treatment.

The third most common cancer worldwide is colon cancer (CC). Every year, there more cases are reported, yet there are not enough effective treatments. This emphasizes the need for new drug delivery strategies to increase the success rate and reduce side effects.

A Clinical Insight on New Discovered Molecules and Repurposed Drugs for the Treatment of COVID-19.

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) began churning out incredulous terror in December 2019. Within several months from its first detection in Wuhan, SARS-CoV-2 spread to the rest of the world through droplet infection, making it a pandemic situation and a healthcare emergency across the globe. The available treatment of COVID-19 was only symptomatic as the disease was new and no approved drug or vaccine was available.

Advances in Xanthan Gum-Based Systems for the Delivery of Therapeutic Agents.

In the last three decades, polymers have contributed significantly to the improvement of drug delivery technologies by enabling the controlled and sustained release of therapeutic agents, versatility in designing different delivery systems, and feasibility of encapsulation of both hydrophobic and hydrophilic molecules. Both natural and synthetic polymers have been explored for the delivery of various therapeutic agents. However, due to the disadvantages of synthetic polymers, such as lack of intrinsic biocompatibility and bioactivity, hydrophobicity, and expensive and complex procedure of synthesis, there is a move toward the use of naturally occurring polymers.

Preparation and characterization of amoxapine- and naringin-loaded solid lipid nanoparticles: drug-release and molecular-docking studies.

Amoxapine (AMX) has been reported to be metabolized by CYP3A4 and CYP2D6. Naringin (NG) has been reported to inhibit CYP enzymes. Therefore, the current work was designed to develop AMX solid lipid nanoparticles (AMX-SLNs) and NG-SLNs for better therapeutic performance.

Ameliorating the antitumor activity of gemcitabine against breast tumor using αβ integrin-targeting lipid nanoparticles.

Objective: The main objective is to formulate solid lipid nanoparticles conjugated with cyclic RGDfk peptide encapsulated with gemcitabine hydrochloride drug for targeting breast cancer.

Significance: The hydrophilic nature of gemcitabine hampers passive transport by cell membrane permeation that may lead to drug resistance as it has to enter the cells nucleoside transporters. The art of encapsulating the drug in a nanovesicle and then anchoring it with a targeting ligand is one of the present areas of research in cancer chemotherapy.

Matrix metalloproteinase enzyme responsive delivery of 5-Fluorouracil using Collagen-I peptide functionalized Dendrimer-Gold nanocarrier.

Objective: The aim was to develop matrix metalloproteinase 1 (MMP1) responsive nanoparticle system for the delivery of 5-fluorouracil (5Fu) anticancer drug.

Significance: The MMP1 in the cancer microenvironment-induced drug release have the advantage of targeted drug release and reduce the distribution of drug to the healthy tissues.

Method: G5 poly(amidoamine) (PAMAM) dendrimer (G5)-coated gold nanoparticles (G5AuNP) were synthesized and loaded with 5Fu.

Improving Anticancer Activity of Chrysin using Tumor Microenvironment pH-Responsive and Self-Assembled Nanoparticles.

Chrysin is a natural bioactive compound with potential biological activities. However, unfavorable physicochemical properties of native chrysin make it difficult to achieve good therapeutic efficacies. In this study, poly(ethylene) glycol (PEG)-conjugated chrysin nanoparticles were prepared.

Self-assembled and pH-responsive polymeric nanomicelles impart effective delivery of paclitaxel to cancer cells.

Chemotherapy is an essential component of breast cancer therapy, but it is associated with serious side effects. Herein, a pluronic F68-based pH-responsive, and self-assembled nanomicelle system was designed to improve the delivery of paclitaxel (PTX) to breast cancer cells. Two pH-responsive pluronic F68-PTX conjugates succinoyl-linked conjugate (F68-SA-PTX) and -aconityl-linked conjugate (F68-CAA-PTX) were designed to respond the varying pH-environment in tumour tissue.

Genistein encapsulated inulin-stearic acid bioconjugate nanoparticles: Formulation development, characterization and anticancer activity.

Achieving controlled and site-specific delivery of hydrophobic drugs in the colon environment is a major challenge. The primary goal of this research was to synthesize inulin-stearic acid (INU-SA) conjugate and to evaluate its potential in the site-specific delivery of genistein (GEN) for the treatment of colon cancer. INU is a hydrophilic polysaccharide biological macromolecule was modified with hydrophobic SA to form amphiphilic conjugate (INU-SA) which can self-assemble into spherical nanoparticles with interesting drug release properties.

Inulin coated MnO nanocuboids coupled with RNA interference reverse intestinal tumorigenesis in Apc knockout murine colon cancer models.

This study reports the development and pre-clinical evaluation of biodrug using RNA interference and nanotechnology. The major challenges in achieving targeted gene silencing in vivo include the stability of RNA molecules, accumulation into pharmacological levels, and site-specific targeting of the tumor. We report the use of Inulin for coating the arginine stabilized manganese oxide nanocuboids (MNCs) for oral delivery of shRNA to the gut.

Biotinylated MnO nanocuboids for targeted delivery of gemcitabine hydrochloride to breast cancer and MRI applications.

Multifunctional nanocarriers have been found as potential candidate for the targeted drug delivery and imaging applications. Herein, we have developed a biocompatible and pH-responsive manganese oxide nanocuboid system, surface modified with poly (ethylene glycol) bis(amine) and functionalized with biotin (Biotin-PEG-MNCs), for an efficient and targeted delivery of an anticancer drug (gemcitabine, GEM) to the human breast cancer cells. GEM-loaded Biotin-PEG@MNCs showed high drug loading efficiency, controlled release of GEM and excellent storage stability in the physiological buffers and different temperature conditions.

Modulating the Delivery of 5-Fluorouracil to Human Colon Cancer Cells Using Multifunctional Arginine-Coated Manganese Oxide Nanocuboids with MRI Properties.

5-Fluorouracil (5-FU) is one of the most prescribed drugs and the major component of chemotherapy for the treatment of colorectal cancer. In this study, we have designed arginine-functionalized manganese oxide nanocuboids (Arg@MNCs) for the effective delivery of 5-FU to colon cancer cells. Arginine was used as multifunctional agent to provide stability to MNCs, achieve high drug loading, control the release of loaded drug, and improve delivery to cancer cells.

Morin hydrate loaded solid lipid nanoparticles: Characterization, stability, anticancer activity, and bioavailability.

Nanotechnology has come up as a protean field integrating concepts of alternate drug delivery systems using nanocarriers. The idea of encapsulating a drug molecule into a colloidal carrier like solid lipid nanoparticle has been a promising approach for development of nanomedicines. In this research work, a hydrophobic, natural, and an anticancer bioflavonoid, morin hydrate (MH) was encapsulated into solid lipid nanoparticles to overcome the issues of its poor aqueous solubility and low oral bioavailability.

Baicalin encapsulating lipid-surfactant conjugate based nanomicelles: Preparation, characterization and anticancer activity.

Lung cancer is one of the most common malignant tumors and emerged as one of the leading causes of cancer-related death worldwide. Surgical resection can be a curative treatment for early stage but the most of lung cancer patients are diagnosed at an advanced stage when the pulmonary tumor has been invaded beyond the respiratory system. Therefore, chemotherapy is suitable for curing metastasized tumor.

Inulin-pluronic-stearic acid based double folded nanomicelles for pH-responsive delivery of resveratrol.

Herein, we introduce a novel amphiphilic bioconjugate (INU-F68-SA), synthesized by functionalization of pluronic F68 with a polysaccharide inulin (INU) and a lipid stearic acid (SA). The synthesis of INU-F68-SA was confirmed by FTIR and H-NMR analysis. INU-F68-SA can self-assemble into nanomicelles and therefore, its application in delivering of hydrophobic resveratrol (RSV) was investigated.

Serotonin-Functionalized Vit-E Nanomicelles for Targeting of Irinotecan to Prostate Cancer Cells.

Receptor-mediated endocytosis is key in the success of targeted nanomedicines for the treatment of cancer. Various receptors have been explored for the active targeting of anticancer drugs to avoid the drawbacks of conventional anticancer drugs. This research work aimed to investigate the potential of serotonin (ST)-conjugated Vit-E nanomicelles for the targeted delivery of irinotecan hydrochloride (IRI) to human prostate cancer cells.