Antipsychotic Potential and Safety Profile of TPGS-Based Mucoadhesive Aripiprazole Nanoemulsion: Development and Optimization for Nose-To-Brain Delivery.

Delivering therapeutics to the brain using conventional dosage forms is always a challenge, thus the present study was aimed to formulate mucoadhesive nanoemulsion (MNE) of aripiprazole (ARP) for intranasal delivery to transport the drug directly to the brain. Therefore, a TPGS based ARP-MNE was formulated and optimized using the Box-Behnken statistical design. The improved in vitro release profile of the formulation was in agreement to enhanced ex vivo permeation through sheep mucous membranes with a maximum rate of permeation co-efficient (62.

Effect-directed profiling of Ficus religiosa leaf extracts for multipotent compounds via 12 effect-directed assays.

The interest in the therapeutic values of natural compounds from plants is growing worldwide because the development of modern synthetic drugs has not lived up to expectations. The tree Ficus religiosa native to India, China and Southeast Asia is traditionally used for curing almost 50 ailments, although the majority of the individual active compounds are not known. Hence, a hyphenated high-performance thin-layer chromatography (HPTLC) method was newly developed.

Diversified Synthetic Pathway of 1, 4-Dihydropyridines: A Class of Pharmacologically Important Molecules.

The current review discusses the different synthetic pathways for one of the most important and interesting heterocyclic ring systems, 1,4-dihydropyridine. This cyclic system depicts diverse pharmacological action on several receptors, channels, and enzymes. Dihydropyridine moiety plays an important role in several calcium-channel blockers.

Preparation, characterization, and optimization of asenapine maleate mucoadhesive nanoemulsion using Box-Behnken design: In vitro and in vivo studies for brain targeting.

The tight junctions between capillary endothelial cells of the blood-brain barrier (BBB) restricts the entry of therapeutics into the brain. Potential of the intranasal delivery tool has been explored in administering the therapeutics directly to the brain, thus bypassing BBB. The objective of this study was to develop and optimize an intranasal mucoadhesive nanoemulsion (MNE) of asenapine maleate (ASP) in order to enhance the nasomucosal adhesion and direct brain targetability for improved efficacy and safety.

Screening of nanoemulsion components for asenapine maleate using validated RP-HPLC method.

A novel, simple reversed-phase high-performance liquid chromatographic (RP-HPLC) analytical method was developed and validated for the quantitative determination of asenapine from various nanoemulsion components during pre-formulation screening. The developed method was validated according to ICH Q2 (R1) guidelines. The developed and validated method was precisely and accurately quantified asenapine in various oils, surfactants and co-surfactants.

Beneficial effects of Stevioside on AGEs, blood glucose, lipid profile and renal status in streptozotocin-induced diabetic rats.

The advanced glycated end products (AGEs) are formed in the diabetic patients; it is a major cause of macrovascular and microvascular complications in diabetes. Clinically there is no treatment available for the AGEs. Stveoside (Stv), a sweetener has potent anti-diabetic and anti-oxidant activity.

Formulation and evaluation of letrozole-loaded spray dried liposomes with PEs for topical application.

Letrozole (LET), an aromatase inhibitor widely used as a first-line drug for the estrogen-dependent breast cancer treatment in postmenopausal women. In this study, an attempt has been made to develop LET topical drug delivery which would be a more efficient system to treat elevated blood levels of estrogen found in breast cancer patients. The technique involves, encapsulation of the LET in phospholipids using spray dryer.

Nanostructured lipid carriers engineered for intranasal delivery of teriflunomide in multiple sclerosis: optimization and in vivo studies.

Background: Multiple sclerosis (MS) is one of the most severe autoimmune disorder of the central nervous system (CNS).

Objective: The present research work was aimed to formulate and investigate teriflunomide (TFM)-loaded intranasal (i.n.

Formulation and ex vivo-in vivo evaluation of pH-triggered brimonidine tartrate in situ gel for the glaucoma treatment using application of 3 factorial design.

Context: Short residence time, poor bioavailability and poor permeability are the major problems for conventional eye drops treatment.

Objective: The aim of this article is to develop, optimize and ex vivo-in vivo investigation of brimonidine tartrate in situ gel as compared to marketed eye drops for the treatment of glaucoma.

Materials And Methods: The effect of independent variables, namely concentrations of polymers, on various dependent variables like viscosity at physiological pH and in vitro drug release were studied by using 3 factorial design.

Mechanistic investigation of biopharmaceutic and pharmacokinetic characteristics of surface engineering of satranidazole nanocrystals.

The designing of surface engineered nanocrystals for improved stability and bioavailability is a multivariate process depending on several critical formulation and process variables. The present investigation deals with formulation of stable nanocrystals of poorly soluble satranidazole (SAT) for improving dissolution rate and pharmacokinetic profiling. SAT has low polar surface area, high dose and dosing frequency.

Transcutaneous delivery of leflunomide nanoemulgel: Mechanistic investigation into physicomechanical characteristics, in vitro anti-psoriatic and anti-melanoma activity.

The present study is a mechanistic validation of 'proof of concept' of effective topical delivery of leflunomide (LFD) nanoemulgel for localized efficient treatment of psoriatic lesions as well as melanoma affected skin regions. Hyperproliferation of keratinocytes in psoriasis and symbiotic relationship between keratinocytes and melanocytes, justifies the need of dual acting treatment. LFD is recently introduced significantly effective disease modifying anti-rheumatic drug and has been considered valuable for the treatment of psoriatic arthritis as well as melanoma.

Identification and Characterization of Hydrolytic Degradation Products of Cefditoren Pivoxil using LC and LC-MS/TOF.

The present research work was carried out to determine stability of cefditoren pivoxil, an orally absorbed prodrug that is rapidly hydrolysed by intestinal esterases to the active cephalosporin cefditoren. Cefditoren was subjected to stress conditions recommended by the International Conference on Harmonization of Technical Requirements for Registration of Pharmaceuticals for Human Use guideline Q1A (R2). Cefditoren pivoxil was susceptible for degradation under acidic, alkaline and neutral hydrolytic conditions while it was stable under photolytic and thermal stress conditions.

Lipid based nanoemulsifying resveratrol for improved physicochemical characteristics, in vitro cytotoxicity and in vivo antiangiogenic efficacy.

Resveratrol, a dietary non-flavonoid polyphenolic phytoalexin, has gained attention in cancer chemoprevention. However, poor aqueous solubility and cellular bioavailability has limited its therapeutic application. We formulated a lipid based delivery system of resveratrol with self nanoemulsifying ability.

Protective effect of hesperetin in rat model of partial sciatic nerve ligation induced painful neuropathic pain: an evidence of anti-inflammatory and anti-oxidative activity.

Behavioral, biochemical and gene expression changes were investigated in a rat model of partial sciatic nerve ligation (PSNL) after administration of hesperetin (20, 50mg/kg; p.o.), pregabalin (10mg/kg; p.

Multivariate analysis of physicochemical characteristics of lipid based nanoemulsifying cilostazol--quality by design.

Simultaneous analysis of the effect of multiple formulation ingredients on the critical physico-chemical properties of lipid based nanoemulsifying cilostazol was studied using integrated quality by design approach. Cilostazol is a poorly soluble drug belonging to class II of the biopharmaceutics classification system. To improve the solubility and in turn bioavailability of cilostazol, a lipid based nanoemulsifying cilostazol was developed.

1, 4-Dihydropyridines: a class of pharmacologically important molecules.

The 1, 4-dihydropyridines (DHPs), a class of drugs possess a wide variety of biological and pharmacological actions. It represents one of the most important groups of calcium-channel modulating agents and has experienced widespread use in the treatment of cardiovascular disease which includes antihypertensive, antianginal, vasodilator and cardiac depressants activities. It also shows antibacterial, anticancer, antileishmanial, anticoagulant, anticonvulsant, antitubercular, antioxidant, antiulcer, CFTR, antimalarials, neuroprotection properties, HIV-1 protease inhibitors, antifertility activities and many more.

Improvement of anti-inflammatory and anti-angiogenic activity of berberine by novel rapid dissolving nanoemulsifying technique.

Berberine, an isoquinoline alkaloid, has wide biological and pharmacological actions. Despite the promising pharmacological effects and safety of berberine, poor oral absorption due to its extremely low aqueous solubility results in poor oral systemic bioavailability. This limits its clinical usage.

Effect of newly synthesized 1,2,4-triazino[5,6-b]indole-3-thione derivatives on olfactory bulbectomy induced depression in rats.

Objective: To study the derivatives of 1,2,4-triazino[5,6-b]indole-3-thione for antidepressant activity in olfactory bulbectomized (OBX) rats. Out of various derivatives tested for acute tail suspension test, the two derivatives showing prominent action were selected for bilateral olfactory bulbectomy model of chronic depression in rats.

Methods: The sub acute effects of 14-day oral pretreatment of two derivatives labeled as 3a (70 mg/kg) and 3r (70 mg/kg), imipramine (20 mg/kg), fluoxetine (30 mg/kg) and moclobemide (15 mg/kg) were evaluated on bilateral bulbectomy induced rise in body weight, hyperphagia, hyperactivity, and on sexual dysfunction.

Ex vivo permeation characteristics of venlafaxine through sheep nasal mucosa.

Venlafaxine, a dual acting antidepressant is a new therapeutic option for chronic depression. Depression is a common mental disorder associated with the abnormalities in neuronal transport in the brain. Since the nose-to-brain pathway has been indicated for delivering drugs to the brain, we analyzed the transport of venlafaxine through sheep nasal mucosa.

Antiosteoporotic activity of phytoestrogen-rich fraction separated from ethanol extract of aerial parts of Cissus quadrangularis in ovariectomized rats.

Objective: Cissus quadrangularis L. (C. quadrangularis L.