Vilazodone Hydrochloride Multi-Dose Nasal Spray Solution for the Treatment of Depression: Design, Optimization, and Evaluation

2021 ◽  
Vol 16 ◽  
Author(s):  
Praful Giradkar ◽  
Deepa H. Patel
Keyword(s):  
Nasal Spray ◽  
Benzalkonium Chloride ◽  
Research Work ◽  
Tween 80 ◽  
Oral Route ◽  
Sodium Carboxymethylcellulose ◽  
Intranasal Route ◽  
Spray Solution ◽  
Treatment Of Depression ◽  
The Brain

Introduction: The aim of present research work was to prepare, optimized, and evaluate the multi-dose nasal spray solution for delivery of vilazodone hydrochloride to the brain by the intranasal route in order to overcome the drawback associated with the oral route for the treatment of depression. Background: Depression is a mental disorder associated with abnormalities in neuronal transport in the brain primarily serotonin, norepinephrine, and dopamine that adversely affects a person's lifestyle, sleep pattern, work, eating habits, and general health. Vilazodone hydrochloride acts by enhancing the serotonergic activity in the brain by inhibiting serotonin (5-HT) reuptake. Materials/ Methods: The excipients used to formulate vilazodone hydrochloride multi-dose nasal spray solution were sulphobutylether-β-cyclodextrin sodium (solubilizer), sodium carboxymethylcellulose (viscosity builder), tween 80 (surface tension modifier), glycerol (humectant), benzalkonium chloride (preservative), and purified water (vehicle). The simple conventional mixing technique was used for the preparation of the multi-dose nasal spray solution. The solution was prepared in two parts, in the first part sulphobutylether-β-cyclodextrin sodium and drug substance dissolved in purified water under stirring followed by the addition of glycerol and benzalkonium chloride solution. In the second part, tween 80 dissolved in warm water followed by the addition of sodium carboxymethylcellulose under stirring, finally both parts mixed and the required volume was adjusted with purified water. The central composite design was used for the optimization of the formulation. The solution was evaluated for physicochemical properties, selective toxicity, and experimental kinetics. Results: The prepared vilazodone hydrochloride multi-dose nasal spray solution was shown viscosity (40.5 ± 1.65 mPa.s), droplet size distribution (span) (1.88 ± 0.55 µm), spray area (288 ± 1.25 mm2), ovality (1.10 ± 1.35), dripping speed (0.25 cm /30 sec), visual appearance (clear free from particulate matter), pH (6.35 ± 0.10), shot weight (100.6 ± 0.32 mg), density (1.03 ± 0.20 g/ml), % drug content (101.8 ± 0.15 %), displacement value for in-vitro mucoadhesion (3.47 ± 0.25 cm), average flux (Jss) for permeability (241.06 ± 1.45 μg/cm2/hrs), permeability coefficient (48.21 ±1.46 cm/hrs), enhancement ratio (1.73), local toxicity study shows no epithelium cell damage, isotonicity (386.58 mOsmol / kg). Plasma Cmax (24.56 ±3.98 ng/ml), Tmax (1.0 hrs), and AUC 0-12 (82.68 ±10.22 ng.h/ml). Brian tissue Cmax (22.95 ±4.22), Tmax (1.0 hrs) and AUC 0-12 (77.82 ±6.25 ng.h/ml). Nasal bioavailability (251.74 ±45.12% ) and, drug targeting index 1.54 Conclusion: The present research work results showed that the prepared multi-dose nasal spray solution of vilazodone hydrochloride was suitable for the delivery of the drug to the brain by the intranasal route and might be beneficial to overcome drawbacks associated with the oral route of administration for the treatment of depression.

scholarly journals A study of rivastigmine liposomes for delivery into the brain through intranasal route

2008 ◽  
Vol 58 (3) ◽  
pp. 287-297 ◽  
Author(s):  
Karthik Arumugam ◽  
Ganesa Subramanian ◽  
Surulivel Mallayasamy ◽  
Ranjith Averineni ◽  
Meka Reddy ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Oral Route ◽  
Free Drug ◽  
Intranasal Route ◽  
Lipid Layer ◽  
New Approach ◽  
Model Drug ◽  
Per Oral ◽  
The Brain

A study of rivastigmine liposomes for delivery into the brain through intranasal routeThe present study is mainly aimed at delivering a drug into the brainviathe intranasal route using a liposomal formulation. For this purpose, rivastigmine, which is used in the management of Alzheimer's disease, was selected as a model drug. Conventional liposomes were formulated by the lipid layer hydration method using cholesterol and soya lecithin as lipid components. The concentration of rivastigmine in brain and plasma after intranasal liposomes, free drug and per oral administration was studied in rat models. A significantly higher level of drug was found in the brain with intranasal liposomes of rivastigmine compared to the intranasal free drug and the oral route. Intranasal liposomes had a longer half-life in the brain than intranasally or orally administered free drug. Delivering rivastigmine liposomes through the intranasal route for the treatment of Alzheimer's disease might be a new approach to the management of this condition.

Intranasal delivery of asenapine loaded nanostructured lipid carriers: formulation, characterization, pharmacokinetic and behavioural assessment

RSC Advances ◽  
2016 ◽  
Vol 6 (3) ◽  
pp. 2032-2045 ◽  
Author(s):  
Sanjay Kumar Singh ◽  
Parth Dadhania ◽  
Parameswara Rao Vuddanda ◽  
Achint Jain ◽  
Sitaram Velaga ◽  
...  
Keyword(s):  
Therapeutic Efficacy ◽  
Research Work ◽  
Nanostructured Lipid Carriers ◽  
Intranasal Delivery ◽  
Intranasal Route ◽  
Behavioural Assessment ◽  
The Brain

The aim of the present research work was to develop asenapine (ASM) loaded nanostructured lipid carriers (ANLC) for the delivery of drugs in the brain by an intranasal route to enhance therapeutic efficacy.

scholarly journals Thermogravimetric studies of a nasal preparation with an interleukin-1β (IL-1Ra) antagonist

2021 ◽  
Vol 14 (1) ◽  
pp. 56-63
Author(s):  
B. S. Burlaka
Keyword(s):  
Active Substance ◽  
Phosphate Buffer ◽  
Benzalkonium Chloride ◽  
Dosage Form ◽  
Interleukin 1 ◽  
Phosphate Buffer Solution ◽  
Tween 80 ◽  
Sodium Carboxymethylcellulose ◽  
Buffer Solution ◽  
Thermogravimetric Studies

Interleukin-1 receptor antagonist (IL-1Ra) is an active pharmaceutical ingredient obtained by the method of gene transformation of Escherichia coli, provides a neuroprotective effect, namely – inhibition of oxidative modification of proteins, normalization of functional activity of mitochondrial energy, mitochondrial energy. Early complex physical-chemical, microbiological, and biopharmaceutical studies have developed a new intranasal formulation, the formulation of which contains: IL-1Ra, sodium carboxymethyl cellulose, D-panthenol, benzalkonium chloride, trilon B, Tween-80, phosphate buffer solution. Given the peculiarities of the technological process, when creating a new gel dosage form, it is necessary to justify the temperature of the carrier base, the introduction of the active substance into the base, as well as to predict the possible chemical interaction of individual components in the dosage form. Therefore, the application of thermogravimetric analysis in pharmaceutical technology is relevant. The aim of the work is to conduct thermogravimetric studies of a new nasal form with an antagonist of interleukin-1β (IL-1Ra). Materials and methods. The objects of thermogravimetric studies were: semi-finished product-solution of the receptor antagonist of interleukin-1 (IL-1Ra). Excipients were: sodium carboxymethylcellulose, tween-80, D-panthenol, trilon B, benzalkonium chloride. To ensure the appropriate pH value used phosphate buffer solution (pH 6.0), according to the recipe to State Pharmacopoeia 2 ed. In addition to the individual components of the finished nasal gel, also prepared nasal gel without IL-1Ra, as well as gel with IL-1Ra. The thermographic analysis was performed on a derivatograph – Shimadzu DTG-60 (Japan) with a platinum-platinum-rhodium thermocouple when heating the samples in aluminum crucibles (from 15 °C to 250 °C). Al2O3 was used as a reference substance. The heating rate was 10 °C per minute. The weight of the test samples ranged from 19.22 mg to 52.91 mg. The derivatograph graphically recorded the obtained data in the form of curves T, DTA, TGA. The T curve on the derivatogram shows the change in temperature, and the TGA curve shows the change in mass of the sample during the study period. The DTA curve reflects the differentiation of thermal effects, contains information about endothermic and exothermic maxima, can be used for qualitative evaluation of the derivatogram. Results. The study consisted of two stages. At the first stage, we studied the derivatograms of experimental samples – individual ingredients of the finished nasal gel - active and excipients, namely: IL-1Ra, sodium carboxymethylcellulose, tween-80, D-panthenol, trilon B, benzalkonium chloride, phosphate buffer solution 6.0. In the second stage, samples of nasal gels were prepared: nasal gel with the required amount of excipients, in addition to the active substance – IL-1Ra, as well as a nasal gel containing IL-1Ra and the required amount of excipients. As a result, we obtained some parameters of thermogravimetric analysis in the form of a graphical image – derivatograms, which were then analyzed. Conclusions. Thermogravimetric studies of individual components of nasal gel with IL-1Ra, as well as nasal gels with active substance and without active substance, were found that the manufacturing process of gel with IL-1Ra should be carried out taking into account thermolabile compounds. First, you need to prepare the base without preservative and IL-1Ra. Then at a temperature not exceeding 40 °C dissolve the preservative, and then when cooled to 20 °C add IL-1Ra. It was found that the developed dosage form of the gel with IL-1Ra is a mixture of active and excipients, the ingredients of which do not interact with each other and can be combined in one dosage form.

Solubility Enhancement of Poorly Water-Soluble Antifungal Drug Acyclovir by Nanocrystal Formulation Approach

2018 ◽  
Vol 11 (2) ◽  
pp. 4036-4042
Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H
Keyword(s):  
Chemical Interaction ◽  
Research Work ◽  
Antiviral Drug ◽  
In Vitro Release ◽  
Oral Route ◽  
Water Soluble ◽  
Precipitation Method ◽  
Dsc Studies ◽  
Ft Ir

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 

Stroke Lesion Segmentation and Analysis using Entropy/Otsu’s Function – A Study with Social Group Optimization

2019 ◽  
Vol 14 (4) ◽  
pp. 305-313 ◽  
Author(s):  
Suresh Chandra Satapathy ◽  
Steven Lawrence Fernandes ◽  
Hong Lin
Keyword(s):  
Social Group ◽  
Research Work ◽  
Lesion Segmentation ◽  
Permanent Disability ◽  
Brain Abnormality ◽  
Inspection Process ◽  
Stroke Lesion ◽  
Social Group Optimization ◽  
The Brain ◽  
Otsu’S Function

Background: Stroke is one of the major causes for the momentary/permanent disability in the human community. Usually, stroke will originate in the brain section because of the neurological deficit and this kind of brain abnormality can be predicted by scrutinizing the periphery of brain region. Magnetic Resonance Image (MRI) is the extensively considered imaging procedure to record the interior sections of the brain to support visual inspection process. Objective: In the proposed work, a semi-automated examination procedure is proposed to inspect the province and the severity of the stroke lesion using the MRI. associations while known disease-lncRNA associations are required only. Method: Recently discovered heuristic approach called the Social Group Optimization (SGO) algorithm is considered to pre-process the test image based on a chosen image multi-thresholding procedure. Later, a chosen segmentation procedure is considered in the post-processing section to mine the stroke lesion from the pre-processed image. Results: In this paper, the pre-processing work is executed with the well known thresholding approaches, such as Shannon’s entropy, Kapur’s entropy and Otsu’s function. Similarly, the postprocessing task is executed using most successful procedures, such as level set, active contour and watershed algorithm. Conclusion: The proposed procedure is experimentally inspected using the benchmark brain stroke database known as Ischemic Stroke Lesion Segmentation (ISLES 2015) challenge database. The results of this experimental work authenticates that, Shannon’s approach along with the LS segmentation offers superior average values compared with the other approaches considered in this research work.</P>

Comments on the special issue

2018 ◽  
Vol 31 (2) ◽  
pp. 183-212
Author(s):  
Paul McGhee
Keyword(s):  
Physical Health ◽  
Training Program ◽  
Research Work ◽  
Well Being ◽  
Special Issue ◽  
Sense Of Humor ◽  
Practical Applications ◽  
The Brain

Abstract This article includes comments on each contributing author’s article in this special issue of Humor. The articles represent an assessment of McGhee’s research, work on practical applications or influence in the following areas: 1) the development of children’s humor, 2) construction and validation of the Sense of Humor Scale (SHS), 3) usefulness of specific subscales of the SHS, including “playfulness” and “laughing at yourself,” 4) development and evaluation of the 7 Humor Habits Program—a training program for learning to use humor to cope with stress, 5) humor’s impact on physical health and emotional well being, 6) impact on the field of nursing, and 7) humor and the brain. McGhee provides here his response to each contributed article.

scholarly journals Brain Tumor Detection from MR Images using Image Process Techniques and Tools in Matlab Software

2021 ◽  
Vol 1 (4) ◽  
pp. 1-4
Author(s):  
Faisal Rehman ◽  
◽  
Syed Sheeraz Ali ◽  
Hamadullah Panhwar ◽  
Dr. Akhtar Hussain Phul ◽  
...  
Keyword(s):  
Brain Tumor ◽  
Image Quality ◽  
Research Work ◽  
Cost Effective ◽  
Image Process ◽  
Medical Sciences ◽  
Mr Images ◽  
Research Areas ◽  
Tumor Identification ◽  
The Brain

In the medical era the Brain tumor is one of the most important research areas in the field of medical sciences. Researcher are trying to find the reliable and cost effective medical equipment’s for the cancer and its type for the diagnosed, especially tumor has deferent kinds but the major two type are discussed in this research paper. Which are the benign and Pre-Malignant, this research work is proposed for these factors such as the accuracy of the MRI image for the tumor identification and actual placing were taken into consideration. In this study, an algorithm is proposed to detect the brain tumor from magnetic resonance image (MRI) data simple. As enhance the image quality for the easiness the tumor treatments and diagnosed for the patients. The proposed algorithm enhances the MR image quality and detects the Brain tumor which helps the Physician to diagnose the tumor easily. As well this algorithm automatically calculates the area of tumor, size and location of the tumor where it is present for diagnostic the Patient.

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