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PubMed Journal Database | Molecular pharmaceutics RSS

01:25 EDT 25th March 2019 | BioPortfolio

The US National Library of Medicine and National Institutes of Health manage PubMed.gov which comprises of more than 29 million records, papers, reports for biomedical literature, including MEDLINE, life science and medical journals, articles, reviews, reports and  books.

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For example view all recent relevant publications on Epigenetics and associated publications and clincial trials.

Showing PubMed Articles 1–25 of 716 from Molecular pharmaceutics

Tailored nanocarriers for the pulmonary delivery of levofloxacin against Pseudomonas aeruginosa: a comparative study.

Cystic fibrosis (CF) patients are faced with chronic bacterial infections displaying persistent resistance if not eradicated during the first stage of the disease. Nanoantibiotics for pulmonary administration, such as liposomal ciprofloxacin or amikacin, have progressed through clinics thanks to their sustained release, prolonged lung residence time and low systemic absorption. In this work, we sought a nanoformulation of levofloxacin for the treatment of Pseudomonas aeruginosa. We prepared and compared PLA...

In vitro dissolution model can predict the in vivo taste masking performance of coated multiparticulates.

The majority of active pharmaceutical ingredients (APIs) are bitter. Therefore, compliance can be a problem where adequate taste masking has not been achieved; this is most problematic in paediatrics. Taste masking is thus a key stage during pharmaceutical development with an array of strategies available to the formulation scientist. Solid oral dosage forms can be taste-masked quite simply by polymer coating, which prevents drug release in the mouth, without unwantedly impairing drug release further down t...

Biodegradable and pH-Responsive Acetalated Dextran (Ac-Dex) Nanoparticles for NIR-Imaging and Controlled Delivery of a Platinum-based Prodrug into Cancer Cells.

Nanoparticles based on the biodegradable acetalated dextran polymer (Ac-Dex) were used for NIR-imaging and controlled delivery of a PtIV prodrug into cancer cells. The Ac-Dex NPs loaded with the hydrophobic PtIV prodrug 3 (PtIV/Ac‒Dex NPs) and with the novel hydrophobic NIR-fluorescent dye 9 (NIR-dye9/Ac-Dex NPs), as well as Ac-Dex NPs co-loaded with both compounds (co-loaded Ac-Dex NPs), were assembled using a single oil-in-water nanoemulsion method. Dynamic light scattering (DLS) measurements and scanni...

Correction to "Potential Eye Drop Based on a Calix4arene Nanoassembly for Curcumin Delivery: Enhanced Drug Solubility, Stability, and Anti-Inflammatory Effect.

Multifunctional nanosystem based on graphene oxide for synergesitic multistage tumor-targeting and combined chemo-photothermal therapy.

Locating nanomedicines at the active sites plays a pivotal role in nanoparticle-based cancer therapy field. Herein, a multifuntional nanotherapeutic is designed by using graphene oxide (GO) nanosheets with rich carboxyl groups as the supporter for hyaluronic acid (HA)-methotrexate (MTX) prodrug modification via adipic dihydrazide crosslinker, achieving synergistic tumor-targeting and combined chemo-photothermal therapy. As a tumor-targeting biomaterials, HA can increase affinity of the nanocarrier towards C...

Development of the Tc-Hydroxamamide Complex as a Probe Targeting Carbonic Anhydrase IX.

Carbonic anhydrase IX (CA-IX) is regarded as a favorable target for in vivo imaging because of its specific expression in hypoxic regions of tumors. Hypoxia assists tumor propagation and growth and is resistant to chemotherapy and radiotherapy. Here, we designed and synthesized [Tc]hydroxamamide ([Tc]Ham) and [Tc]methyl-substituted-hydroxamamide ([Tc]MHam) complexes including a bivalent CA-IX ligand, sulfonamide (SA), and ureidosulfonamide (UR). In a cell binding assay, [Tc]Ham complexes with bivalent SA ([...

A Site-Specific ImmunoPET Tracer to Image PD-L1.

The rapid ascension of immune checkpoint blockade treatments has placed an emphasis on the need for viable, robust, and noninvasive imaging methods for immune checkpoint proteins, which could be of diagnostic value. Immunoconjugate-based positron emission tomography (immuno-PET) allows for sensitive and quantitative imaging of target levels and has promising potential for the noninvasive evaluation of immune checkpoint proteins. However, the advancement of immuno-PET is currently limited by available imagin...

Development of 99mTc-Labeled Human Serum Albumin with Prolonged Circulation by Chelate-then-Click Approach: A Potential Blood Pool Imaging Agent.

Technetium-99m labeled human serum albumin (99mTc-HSA) has been utilized for blood pool imaging agent in the clinic for several decades. However, 99mTc-HSA has a short circulation time, which is a critical shortcoming for a blood pool imaging agent. Herein, we developed a novel 99mTc-labeled HSA with a long circulation time using click chemistry and a chelator, 2,2'-dipicolylamine (DPA), (99mTc-DPA-HSA). Specifically, we examined the feasibility of copper-free strain-promoted alkyne-azide cycloaddition (SPA...

Noninvasive and Quantitative Monitoring of the Distributions and Kinetics of MicroRNA-targeting Molecules In Vivo by Positron Emission Tomography.

MicroRNAs (miRNAs) are endogenous, small, non-coding ribonucleic acids (RNAs) that bind to the 3' untranslated regions of messenger RNAs (mRNAs) and induce translational repression or mRNA degradation. Although numerous studies have reported that miRNAs are of potential use for disease diagnostics and gene therapy, little is known about their fates in vivo. This study elucidated the whole-body distributions and kinetics of intravenously administered miRNA-targeting molecules in vivo by positron emission tom...

Cannabidiol enhances the passage of lipid nanocapsules across the blood-brain barrier both in vitro and in vivo.

Diseases affecting the central nervous system (CNS) should be regarded as a major health challenge due to the current lack of effective treatments given the hindrance to brain drug delivery imposed by the blood-brain barrier (BBB). Since efficient brain drug delivery should not solely rely on passive targeting, active targeting of nanomedicines into the CNS is being explored. The present study is devoted to the development of lipid nanocapsules (LNCs) decorated with non-psychotropic cannabinoids as pioneeri...

Glatiramer Acetate (Copaxone®) is a Promising Gene Delivery Vector.

Glatiramer acetate (GA), the active ingredient of Copaxone®, consists of random polypeptides used to treat multiple sclerosis (MS). GA was originally designed to emulate myelin basic protein (MBP) and contains the four amino acids: alanine, glutamic acid, tyrosine, and lysine. We found that GA can complex, condense, and transfect plasmid DNA. Mixing the positively-charged GA and the negatively-charged genetic material at the correct proportions produced small, stable, and highly positively-charged nanopart...

Targeted delivery of miRNA 155 to tumor associated macrophages for tumor immunotherapy.

Tumor associated macrophages (TAMs) are important components residing in the tumor microenvironment. They are immunosuppressive and promote tumor progression. Targeting TAMs and reprogramming their phenotype may be a promising strategy that can restore antitumor immune responses. In this study, we developed a microRNA delivery system based on lipid-coated calcium phosphonate nanoparticles (CaP/miR@pMNPs) containing conjugated mannose and sterically shielded with a pH-responsive material. The nanocarrier cou...

A novel oligo-guanidyl-PEG carrier forming rod-shaped polyplexes.

A novel unconventional supramolecular oligo-cationic structure (Agm6-M-PEG-OCH3) has been synthesized to yield high efficiency therapeutic oligonucleotide (ON) delivery. Agm6-M-PEG-OCH3 was obtained by a multi-step protocol that included the conjugation of agmatine (Agm) moieties to maltotriose (M), which was further derivatized with one poly(ethylene glycol) (PEG) chain. Gel electrophoresis analysis showed that the 19 base pairs dsDNA model ON completely associates with Agm6-M-PEG-OCH3 at 3 N/P molar ratio...

The topography of simulated intestinal equilibrium solubility.

Oral administration of a solid dosage form requires drug dissolution in the gastro-intestinal tract before absorption. Solubility is a key factor controlling dissolution and it is recognised that within the intestinal tract this is influenced by the luminal fluid pH, amphiphile content and composition. Various simulated intestinal fluid recipes have been introduced to mimic this behaviour and studied using a range of different experimental techniques. In this paper we have measured equilibrium solubility ut...

Transtympanic Delivery of Local Anesthetics for Pain in Acute Otitis Media.

Acute otitis media (AOM) commonly causes pain and distress in children. Existing analgesic ototopical drops have limited effectiveness due to the impermeable nature of the tympanic membrane. We developed a local drug delivery system to provide sustained pain relief in patients with AOM, achieved by applying a single dose of a hydrogel formulation onto the tympanic membrane. Successful drug delivery across intact tympanic membranes was demonstrated using the amino-amide anesthetic, bupivacaine, and a highly ...

Liposomes Enhance Dye Localization within the Mammary Ducts of Porcine Nipples.

Transductal and transepidermal diffusion are two distinct penetration routes of molecules administered via the nipple. To improve the therapeutic potential of this drug administration technique, drug penetration into the mammary ducts should be maximized, which may be accomplished through design optimization of drug delivery vehicles. In this study, we evaluated liposomes, ranging in size from 100 to 3,000 nm, to improve ductal penetration of model fluorescent dyes using fluorescence microscopy and image an...

Impact of Ferroquine on the Solubilization of Artefenomel (OZ439) during in Vitro Lipolysis in Milk and Implications for Oral Combination Therapy for Malaria.

Milk is an attractive lipid-based formulation for the delivery of poorly water-soluble drugs to pediatric populations. We recently observed that solubilization of artefenomel (OZ439) during in vitro intestinal lipolysis was driven by digestion of triglycerides in full-cream bovine milk, reflecting the ability of milk to act as an enabling formulation in the clinic. However, when OZ439 was co-administered with a second antimalarial drug, ferroquine (FQ) the exposure of OZ439 was reduced. The current study th...

Peptide-free synthetic nicotine vaccine candidates with α-Galactosylceramide as adjuvant.

Peptides are generally needed as T-helper epitopes in nicotine vaccines to induce effective antibody responses, but the highly polymorphic property of MHC molecules may limit opportunities of B cell to receive CD4+ T-cell help. iNKT cells recognize lipid antigens presented by the nonpolymorphic CD1d molecule that is conserved in mammals to a great extent. iNKT cells also display some similar functions to conventional CD4+ T-helper cells, especially they license dendritic cells stimulate antibody isotype swi...

Combined application of MRI and the salivary tracer technique to determine the in vivo disintegration time of immediate release formulation administered to healthy, fasted subjects.

The process of disintegration is a crucial step in oral drug delivery with immediate release dosage forms. In this work, the salivary tracer technique was applied as a simple and inexpensive method for the investigation of the in vivo disintegration time of hard gelatin capsules filled with caffeine. The disintegration times observed with the salivary tracer technique were verified by magnet resonance imaging (MRI). After an overnight fast of at least 10 h and caffeine abstinence of minimum 72 h, convention...

Minocycline and silver dual-loaded polyphosphoester-based nanoparticles for treatment of resistant Pseudomonas aeruginosa.

Pseudomonas aeruginosa has been detected in the lungs of about 50% of patients with cystic fibrosis (CF) patients, including 20% of adult CF patients. The majority of these adult patients harbor multi-drug resistant (MDR) strains limiting the available treatment options. Silver has long been used as a broad-spectrum antimicrobial agent with a low incidence of resistance. Despite low toxicity, poor availability of silver cations mandates a high dosage to effectively eradicate infections. To address these sho...

Microstructure Formation for Improved Dissolution Performance of Lopinavir Amorphous Solid Dispersions.

Amorphous solid dispersions (ASDs), where the drug is dispersed in a polymer, have become increasingly prevalent as a formulation strategy for the oral delivery of poorly-soluble drugs due to their potential for substantial solubility enhancement. However, ASDs are susceptible to amorphous phase separation, which may promote crystallization and/or alter the release performance. Nevertheless, the mechanisms by which phase separation and subtle microstructural changes affect ASD release remain poorly understo...

Oral Delivery of Puerarin Nanocrystals to Improve Brain Accumulation and Anti-Parkinsonian Efficacy.

Puerarin (PU) has emerged as a promising herb-derived anti-Parkinsonism compound. However, the undesirable water solubility as well as unwanted bioavailability of PU limit its application. Therefore, this study aimed to develop and characterize PU nanocrystals (PU-NCs) with enhanced oral bioavailability and improved brain accumulation for the treatment of Parkinson's disease (PD). The fabricated PU-NCs were approximately spherical, with a mean size of 83.05 ± 1.96 nm, a PDI of 0.047 ± 0.009, a drug loadin...

Intracellular mechanism of rosuvastatin-induced decrease in mature hERG protein expression on membrane.

The hERG potassium channel (IKr) encoded by human ether-a-go-go-related gene plays an important role in cardiac repolarization. Decreased IKr may lead to long QT syndrome, which subsequently causes torsade de pointes and sudden cardiac death. Previous studies have shown that statins inhibit IKr and are more potent in inhibiting hERG currents when combined with other drugs. Since chemical structure of rosuvastatin is similar to that of several IKr blockers (ibutilide and E-4031), the present study aimed to r...

Cyclodextrin Polymer Preserves Sirolimus Activity and Local Persistence for Antifibrotic Delivery over the Time Course of Wound Healing.

Fibrosis and dysphagic stricture of the esophagus is a major unaddressed problem often accompanying endoscopic removal of esophageal cancers and precancerous lesions. While weekly injections of antiproliferative agents show potential for improved healing, repeated injections are unlikely clinically and may alternatively be replaced by creating an esophageal drug delivery system. Affinity-based polymers have previously shown success for continuous delivery of small molecules for weeks to months. Herein, we e...

Mechanism of supersaturation suppression in dissolution process of acidic drug salt.

Supersaturable active pharmaceutical ingredients (sAPI), such as salts, cocrystals, and amorphous solids, can form supersaturated solutions after dissolving in the gastrointestinal fluids. However, there are cases in which supersaturation is not observed in an in vitro non-sink dissolution test. The purpose of the present study was to investigate the mechanisms of supersaturation suppression in the dissolution process of acidic drug salts. Diclofenac sodium (DCF Na, pKa = 4.0) was employed as a model drug. ...


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