Development, optimization and evaluation of surfactant-based pulmonary nanolipid carrier system of paclitaxel for the management of drug resistance lung cancer using Box-Behnken design.

In the present study, nanostructured lipid carriers (NLCs) along with various surfactants loaded with paclitaxel (PTX) were prepared by an emulsification technique using a Box-Behnken design. The Box-Behnken design indicated that the most effective factors on the size and PDI were at high surfactant concentration (1.5%), low lipids ratio (6:4) and medium homogenization speed (6000 rpm).

Neuroprotective effect of hemeoxygenase-1/glycogen synthase kinase-3β modulators in 3-nitropropionic acid-induced neurotoxicity in rats.

The present study has been designed to explore the possible interaction between hemeoxygenase-1 (HO-1) and glycogen synthase kinase-3β (GSK-3β) pathway in 3-nitropropionic acid (3-NP)-induced neurotoxicity in rats. 3-NP produces neurotoxicity by inhibition of the mitochondrial complex II (enzyme succinate dehydrogenase) and by sensitizing the N-methyl-D-aspartate receptor. Recent studies have reported the therapeutic potential of HO-1/GSK-3β modulators in different neurodegenerative disorders.

Development and Characterization of Novel Medicated Nanofibers Against Periodontitis.

Periodontitis is an inflammatory disease of gums involving degeneration of periodontal ligaments, creation of periodontal pocket and resorption of alveolar bone, thus disrupting the support structure of teeth causing their loosening and finally removal. Since this disease is mainly confined to the periodontal pocket, so site specific drug delivery of an antibiotic is the best suitable option. This also eradicates the demerits of oral dosing like low drug concentration reaching the target site and the various systemic side effects.

Transmucosal delivery of linagliptin for the treatment of type- 2 diabetes mellitus by ultra-thin nanofibers.

The objective of the present research was to cultivate an oral formulation of an anti-diabetic drug using polymeric nanofiber. A biodegradable polymer i.e.

A review of emerging trends in the treatment of tuberculosis.

This review attempts to summarize the information available on emerging trends in the treatment of tuberculosis caused by the bacteria Mycobacterium tuberculosis. Nanostructured biomaterials, liposomes, microparticles and solid lipid nanoparticles have unique physicochemical properties such as particularly small and convenient size, sustained release, great surface area to mass ratio and high reactivity with structure. These properties can be useful in easing the administration of antimicrobial drugs, thereby reducing the number of limitations in long-established antimicrobial therapeutics.

Design, synthesis and evaluation of antimalarial potential of polyphosphazene linked combination therapy of primaquine and dihydroartemisinin.

Various polymer drug conjugates (13-16) such as primaquine and dihydroartemisinin conjugated 2-propoxy substituted polyphosphazenes (13), primaquine and dihydroartemisinin conjugated 4-acetamidophenoxy substituted polyphosphazenes (14), primaquine and dihydroartemisinin conjugated 4-formyl substituted polyphosphazenes (15) and primaquine and dihydroartemisinin conjugated 4-aminoethylbenzoate substituted polyphosphazenes (16) were synthesized using substituted polyphosphazenes as polymer and primaquine and dihydroartemisinin as combination antimalarial pharmacophores and formulated to nanoparticles to achieve novel controlled combined drug delivery approach for radical cure of malaria. The polymeric backbone was suitably substituted to impart different physicochemical properties. The polymer-drug conjugates were characterized by IR, (1)H NMR, (31)P NMR and their molecular weights were determined by Gel Permeation Chromatography.

Lipid polymer hybrid as emerging tool in nanocarriers for oral drug delivery.

The oral route for drug delivery is a widely accepted route. For that reason, many researchers are currently working to develop efficient oral drug delivery systems. Use of polymeric nanoparticles (NPs) and lipid carrier systems, including liposomes, solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLC), has limitations such as drug leakage and high water content of dispersions.

Potential role of nitric oxide synthase isoforms in pathophysiology of neuropathic pain.

Neuropathic pain triggers a cascade of events in the sensory neurons. It is the main complication of diabetes after cardiovascular disease. Nitric oxide (NO) produced from nitric oxide synthases (NOS) is an important signaling molecule which is crucial for many physiological processes such as synaptic plasticity, neuronal survival, vasodilation, vascular homeostasis, immune regulation.

Exploring versatile applications of cyclodextrins: an overview.

Context: Ever since the discovery of cyclodextrins, a family of cyclic oligosaccharides based on α (1 → 4) linkage among glucopyranose subunits, these versatile supramolecular hosts have received tremendous attention for scientific explorations. Due to their property of forming host-guest type inclusion complex, cyclodextrins and their synthetic derivatives exhibit wide range of utilities in different areas viz. pharmaceuticals, drug delivery systems, cosmetics, food and nutrition, textile and chemical industry etc.

Surface modified nanoparticulate carrier constructs for oral mucosal vaccine delivery.

Mucosal administration of vaccines is one of the most popular approaches to induce desired immunity against various types of antigen and microbial in central as well as peripheral blood and in most external mucosal surfaces. The oral route is a preferred choice over parenteral route for this purpose mainly due to an ease of administration and therefore, for the possibility of covering large population for mass immunization. Different strategies of mucosal vaccination aimed to prevent colony formation and infection by pathogens and block its development.

Mechanisms involved in attenuated cardio-protective role of ischemic preconditioning in metabolic disorders.

Myocardial infarction is a pathological state which occurs due to severe abrogation of the blood supply (ischemia) to a part of heart, which can cause myocardial damage. The short intermittent cycles of sub-lethal ischemia and reperfusion has shown to improve the tolerance of the myocardium against subsequent prolonged ischemia/reperfusion (I/R)-induced injury, which is known as ischemic preconditioning (IPC). Although, IPC-induced cardioprotection is well demonstrated in various species, including human beings, accumulated evidence clearly suggests critical abrogation of the beneficial effects of IPC in diabetes mellitus, hyperlipidemia and hyperhomocysteinemia.

Recent advances in polymeric electrospun nanofibers for drug delivery.

Electrospinning is a simple unit operation process by which polymeric nanofibers with diameters ranging from a few nanometers to hundreds of micrometers can be fabricated using an electrostatically operated jet of polymer solution or polymer melt. Nanofibers because of their interesting features, such as surface-to-volume ratio, high surface area, microporosity, and nonwoven structure, provide numerous opportunities to design novel carrier systems for large commodities of therapeutics. Physicochemical properties of nanofibers depend on several process and formulation parameters, such as applied voltage, flow rate, polymer selection, and concentration of polymer used.

Animal models of inflammatory bowel disease: a review.

Inflammatory bowel disease (IBD) represents a group of idiopathic chronic inflammatory intestinal conditions associated with various areas of the GI tract, including two types of inflammatory conditions, i.e., ulcerative colitis (UC) and Crohn's disease (CD).

Development and characterization of nanoemulsion as carrier for the enhancement of bioavailability of artemether.

The present study aimed to develop a kinetically stable nanoemulsion of artemether with improved solubility, stability and oral bioavailability. Nanoemulsion was prepared by ultrasonication technique using internal oil phase (consisted of the drug dissolved in coconut oil and span 80) and external phase (comprising tween 80 and ethanol dissolved in water). The formulations were optimized using various parameters like percentage transmittance, refractive index, drug content, viscosity, zeta potential and release rate.

Development, characterization and nasal delivery of rosmarinic acid-loaded solid lipid nanoparticles for the effective management of Huntington's disease.

Objective: The objective of the present study was to investigate the potential use of solid lipid nanoparticles (SLNs) as a drug delivery system to enhance the brain-targeting efficiency of rosmarinic acid (RA) following intranasal (i.n.) administration.

Role of neurosteroids in experimental 3-nitropropionic acid induced neurotoxicity in rats.

Huntington's disease is an autosomal dominant, progressive, and fatal neurodegenerative disease characterized by motor and non-motor symptoms. Systemic administration of 3-nitropropionic acid, a complex II inhibitor of the electron transport chain induces selective striatal lesions in rodents. Neurosteroids are synthesized in central nervous system, able to modulate GABAA receptor function and has been reported to have neuroprotective action.

Concepts and Strategies for the Site Specific Delivery of Nanocarrier Based Delivery Systems for Treating Hepatocellular Carcinoma.

Hepatocellular carcinoma (HCC) is most common lethal malignancy worldwide. About 80% of liver cancer cases are attributed to the combined effects of Hepatitis B and C virus infections. The factors affecting development of HCC include cirrhosis and histological markers of increased liver cell proliferation, environmental, dietary and lifestyle of the person.

Development and in vitro characterization of docetaxel-loaded ligand appended solid fat nanoemulsions for potential use in breast cancer therapy.

Context: Breast cancer accounts for 23% of all newly occurring cancers in women worldwide and represents 13.7% of all cancer deaths. Available chemotherapeutic agents are limited largely due to the low accumulation of chemotherapeutics at the tumors relative to their accumulation at normal (healthy) organs due to developed multidrug resistance (MDR) which translates into increased toxicities.

Pharmacosomes: an emerging novel vesicular drug delivery system for poorly soluble synthetic and herbal drugs.

In the arena of solubility enhancement, several problems are encountered. A novel approach based on lipid drug delivery system has evolved, pharmacosomes. Pharmacosomes are colloidal, nanometric size micelles, vesicles or may be in the form of hexagonal assembly of colloidal drug dispersions attached covalently to the phospholipid.

Mechanism of hyperhomocysteinemia-induced vascular endothelium dysfunction - possible dysregulation of phosphatidylinositol-3-kinase and its downstream phosphoinositide dependent kinase and protein kinase B.

Imbalance of l-arginine/endothelial nitric oxide synthatase (eNOS) activity is the hallmark of vascular endothelium dysfunction. Hyperhomocysteinemia (Hhy) has been identified as a potential risk factor for vascular endothelium dysfunction that leads to cardiovascular disorders. Phosphatidylinositol-3 kinase (PI3K) is a ubiquitous enzyme involved in plethora of cell signaling including the endothelial cells and it has been reported that signaling through this enzyme and its downstream pathway viz phosphoinositide-dependent kinase (PDK)/protein kinase B (Akt) and eNOS is impaired in diseased conditions.

Possible beneficial effect of peroxisome proliferator-activated receptor (PPAR)--α and γ agonist against a rat model of oral dyskinesia.

Tardive dyskinesia is a type of hyperkinetic movement disorder which consists of abnormal involuntary movements, characterized by orofacial movements. Previous studies suggest that oxidative stress and neuro-inflammation play important role in the pathogenesis of TD. Recently, PPAR-α and PPAR-ϒ have been reported as neuroprotective agent in various animal models.

Therapeutic potential of GABA(B) receptor ligands in drug addiction, anxiety, depression and other CNS disorders.

Glutamate and γ-aminobutyric acid (GABA) are the major excitatory and inhibitory neurotransmitter systems, respectively in the central nervous system (CNS). Dysregulation, in any of these or both, has been implicated in various CNS disorders. GABA acts via ionotropic (GABA(A) and GABA(C) receptor) and metabotropic (GABA(B)) receptor.

Phosphodiesterases: Regulators of cyclic nucleotide signals and novel molecular target for movement disorders.

Movement disorders rank among the most common neurological disorders. During the last two decades substantial progress has been made in understanding of the pathological basis of these disorders. Although, several mechanisms have been proposed, downregulation of cyclic nucleotide mediated signaling cascade has consistently been shown to contribute to the striatal dysfunctioning as seen in movement disorders.

Formulation and evaluation of mucoadhesive buccal films impregnated with carvedilol nanosuspension: a potential approach for delivery of drugs having high first-pass metabolism.

Context: Mucoadhesive buccal films containing three layers (mucoadhesive layer, nanosuspension containing layer and backing membrane) were incorporated with carvedilol nanosuspension.

Objective: Formulation and evaluation of nanosuspension incorporated mucoadhesive buccal films of carvedilol for bioavailability enhancement by avoiding first-pass metabolism.

Methods: Carvedilol-loaded nanosuspension was prepared by a precipitation-ultrasonication method with varying concentrations of the polymer.

Gemcitabine-loaded PLGA-PEG immunonanoparticles for targeted chemotherapy of pancreatic cancer.

The aim of the present study was the direct covalent coupling of the epidermal growth factor receptor (EGFR)-specific monoclonal antibody (mAb) to the surface of poly(lactide)-co-glycolide (PLGA)-polyethylene glycol (PEG) nanoparticles in order to achieve a cell type-specific drug carrier system against pancreatic cancer. The PLGA-PEG-NH diblock copolymer was synthesized by coupling reaction via amide linkage between PEG-diamine and activated PLGA. PLGA and PLGA-PEG-NH nanoparticles loaded with gemcitabine were prepared using the double-emulsion solvent evaporation method.