Fabrication of acetazolamide loaded leciplex for intraocular delivery: Optimization by 3 full factorial design, in vitro, ex vivo and in vivo pharmacodynamics.

The complex structure of the eye poses challenges in delivering drugs effectively, which can be circumvented by employing nanotechnologies. The present study aimed to prepareacetazolamide-loadedleciplex (ACZ - LP) using a simple one-step fabrication approach followed byoptimization employing a 3 Full Factorial Design. The ACZ - LP demonstrated high entrapment efficiency (93.

"Fabrication of pellets via extrusion-spheronization for engineered delivery of Famotidine through specialized straws for Paediatrics".

Objective: A simple and efficient drug delivery device was designed, viz. specialized straw comprising of famotidine-loaded fast disintegrating pellets.

Significance: Pediatric dosage forms are designed and developed considering the palatability in children of all ages.

Potential biomaterials and experimental animal models for inventing new drug delivery approaches in the neurodegenerative disorder: Multiple sclerosis.

The tight junction of endothelial cells in the central nervous system (CNS) has an ideal characteristic, acting as a biological barrier that can securely regulate the movement of molecules in the brain. Tightly closed astrocyte cell junctions on blood capillaries are the blood-brain barrier (BBB). This biological barrier prohibits the entry of polar drugs, cells, and ions, which protect the brain from harmful toxins.

Nose-to-brain delivery of octreotide acetate in situ gel for pituitary adenoma: Pharmacological and in vitro cytotoxicity studies.

Octreotide acetate (OA), a potent octapeptide, is used in the treatment of pituitary adenoma. An approach has been made in the present research to formulate an OA-loaded intranasal in situ gel (OA-ISG) to target pituitary adenoma. To achieve the objective of the present work, OA-ISG was fabricated using cold method, and further optimization was done by 3 factorial design.

Nose-to-brain delivery of paliperidone palmitate poloxamer-guar gum nanogel: Formulation, optimization and pharmacological studies in rats.

Oral delivery of paliperidone palmitate (PPD), a potent antipsychotic agent, has been reported with a potential risk of very serious drug-induced adverse events such as tachycardia, hyperprolactinemia, sexual dysfunction, and neutropenia. Alternatively, the potential of nasal delivery has also been explored to treat CNS complications by delivering the medicines directly to the brain bypassing the blood-brain barrier. Hence, the objectives of current work were to formulate, design, optimize, and investigate the therapeutic potency of PPD-loaded intranasal in-situ gel (PPGISG) in the treatment of schizophrenia.

Nose-to-brain delivery of amisulpride-loaded lipid-based poloxamer-gellan gum nanoemulgel: In vitro and in vivo pharmacological studies.

Unfavorable side effects of available antipsychotics limit the use of conventional delivery systems, where limited exposure of the drugs to the systemic circulation could reduce the associated risks. The potential of intranasal delivery is gaining interest to treat brain disorders by delivering the drugs directly to the brain circumventing the tight junctions of the blood-brain barrier with limited systemic exposure of the entrapped therapeutic. Therefore, the present research was aimed to fabricate, optimize and investigate the therapeutic efficacy of amisulpride (AMS)-loaded intranasal in situ nanoemulgel (AMS-NG) in the treatment of schizophrenia.

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.

Nose-to-brain delivery of teriflunomide-loaded lipid-based carbopol-gellan gum nanogel for glioma: Pharmacological and in vitro cytotoxicity studies.

The research work was intended to formulate teriflunomide (TFM) loaded nano lipid-based (TNLC) carbopol-gellan gum in situ gel (TNLCGHG) and to investigate its therapeutic efficacy against glioma, a brain and spine tumor. Nanoformulation was developed using gellan gum and carbopol 974P as gelling and mucoadhesive agents, respectively, Glyceryl di-behenate and Glyceryl mono-linoleate blend as lipids, and Gelucire 44/14: water blend as surfactant system. Globule size, PDI, zeta potential, encapsulation efficiency, mucoadhesive strength, and nasal permeation were found to be 117.

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.

Efavirenz-loaded intranasal microemulsion for crossing blood-CNS interfaces in neuronal-AIDS: pharmacokinetic and safety evaluation.

Development of delivery tool for the existing antiretroviral drugs against the neuronal-AIDS in itself is a big challenge because of blood-brain-barrier (BBB). Aim of present research is to formulate efavirenz (EFV) based mucoadhesive microemulsion (EMME) and investigates its efficiency through intranasal delivery. The EFV microemulsion (EME) was formulated by aqueous titration method.

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.