Formulation and Evaluation of Fish Oil-based Rizatriptan Microemulsion for Intranasal Migraine Treatment

2015 ◽  
Vol 8 (3) ◽  
pp. 2972-2978
Author(s):  
Kanchan P Upadhye ◽  
Divya Senpal ◽  
Minakshee Nimbalwar ◽  
Gouri Dixit
Keyword(s):  
Fish Oil ◽  
Nasal Cavity ◽  
Residence Time ◽  
Stability Study ◽  
Migraine Treatment ◽  
Existence Region ◽  
Microemulsion Based Gel ◽  
Micro Emulsion ◽  
Pseudoternary Phase Diagram

In the present study microemulsion based intranasal gel of rizatriptan using fish oil was prepared for treatment and management of migraine to sustain the drug release and improve the drug residence time in nasal cavity. Fish oil is reported to have antimigraine activity hence it has been used in the present formulation along with cremophore EL as surfactant and Transcutol P as co-surfactant. The pseudoternary phase diagram plotted with these components shown the microemulsion existence region in ratio of (1:9-9:1) surfactant and co-surfactant. The optimized micro-emulsion contained fish oil (45.29%), cremophore E/transcutol P (2:1) and was characterized for pH (6.3±0.02), viscosity (114 ± 3.00cp), % transmittance (99.5 ± 1.01), refractive index (1.335±0.01),). The prepared microemulsion gels were optimized and characterized for in-vitro studies, pH, drug content, rheological studies and stability study. The release of rizatriptan from micro-emulsion gel prepared from carbopol 934 (98.01%) was found to be higher and prolonged than plain gel. Thus, microemulsion based gel was able to prolong drug releaseand improve drug residence time in the nasal cavity. 

Development of Nasal Mucoadhesive Microspheres of Granisetron: A Potential Drug

Drug Research ◽  
2020 ◽  
Vol 70 (08) ◽  
pp. 367
Author(s):  
Jaideo Pandey ◽  
Ravi Shankar ◽  
Manish Kumar ◽  
Kuldeep Shukla ◽  
Beena Kumari
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Stability Study ◽  
Nasal Delivery ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Model Study ◽  
Maximum Stability ◽  
Pass Metabolism

Abstract Background Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. Objectives In this research mucoadhesive microspheres were developed in order to carry out the absorption of drug through nasal mucosa with the aim to improve therapeutic efficacy, avoid hepatic first pass metabolism and increase residence time. Material and Methods Mucoadhesive microspheres of Granisetron using chitosan as polymer were prepared by emulsification cross-linking method to increase the residence time on the mucosa. The surface of prepared microspheres was characterized by SEM (Scanning electron microscopy) and evaluated for particle size, encapsulation efficiency, production yield, swelling ability, in-vitro mucoadhesion, in-vitro drug release and stability study. Result Among all the formulations F6 with drug/polymer ratio of 1:3 displayed the best result. On drug release kinetic model study, all the formulations follow Zero order. Stability studies revealed that the microspheres kept at 25±2°C and 60±5% RH showed the maximum stability. Conclusion After all the evaluation parameters and result obtained it can be said that these results confirmed the suitability of Granisetron mucoadhesive chitosan microspheres for nasal delivery system.

scholarly journals FORMULATION OF MICROEMULSION BASED GEL OF SALBUTAMOL SULPHATE AND IT’S IN VITRO STUDIES

2020 ◽  
pp. 102-107
Author(s):  
LARAIB JAMIL ◽  
SYED UMER JAN ◽  
RAHMAM GUL
Keyword(s):  
Drug Release ◽  
In Vitro Study ◽  
Cellulose Membrane ◽  
Sustained Action ◽  
Microemulsion Based Gel ◽  
Micro Emulsion ◽  
Gel Preparation ◽  
Franz Diffusion Cells ◽  
Microemulsion Gel

Objective: The aim of this study was to develop a microemulsion based gel system considering transdermal delivery of Salbutamol with a purpose to increase the solubility and membrane drug deliverance. Methods: Oleic acid was favored for oil phase owing to the proficiency of solubility in this study. Despite surfactant and co-surfactant was determined by virtue of their solubilizing strength wherewith they developed MEs. Accomplishing Franz diffusion cells equipped with cellulose membrane for in vitro study. The Polymer carbopol 934 were used for based gel preparation to enhance the viscosity of microemulsion for transdermal utilization. The advanced micro emulsion-based gel, which was assessed for pH, centrifugation, spreadability conductivity, drug content, viscosity, SEM, XRD and stability studies. Results: The process of drug escape from microemulsion gel-based was noticed to pursue Korsmeyer-peppas model kinetics. The designed, microemulsion gel-based displayed acceptable stability layer than 3 mo. Drug release microemulsion within 24 h was observed 74%. Conclusion: The results illustrate that deliberated effort to establish microemulsion based gel (F3) was likely to produce sustained action of drug release (78.3%) and be permitted auspicious vehicle for transdermal distribution of Salbutamol.

scholarly journals Design and Evaluation of Flurbiprofen Micro-Emulsion Based Gel

2020 ◽  
Vol 11 (4) ◽  
pp. 7293-7300
Author(s):  
Manish Wani ◽  
Akshay Baheti ◽  
Satish Polshettiwar ◽  
Tanaji Nandgude ◽  
Aarti Shastri ◽  
...  
Keyword(s):  
Animal Studies ◽  
Chemical Properties ◽  
Tween 80 ◽  
Skin Penetration ◽  
Oral Route ◽  
Physico Chemical ◽  
Study Results ◽  
Microemulsion Based Gel ◽  
Micro Emulsion

Flurbiprofen via oral route has many side effects. Many inflammatory infections occur locally and close to the body's surface, so topical application of flurbiprofen is advantageous. Still, intact skin acts as a barrier and hampers skin penetration of the drug. Present objective of this work was to reduce the adverse effect of flurbiprofen and increase its bioavailability by formulating Flurbiprofen microemulsion based gel, evaluating it for its Physico-chemical properties and then finally conducting its in-vitro and animal studies to determine its efficiency. Arachis oil was selected as an oil phase as flurbiprofen showed maximum solubility in it. Microemulsion formulations (A1 to A9) were prepared by varying the qty of tween 80 (as a surfactant) and propylene glycol (as co-surfactant). Microemulsions which were found to give satisfactory results w.r.t microemulsion formation (F1 to F5) were converted to microemulsion gel using Carbopol 934 as gel base. The ability of different microemulsions to penetrate flurbiprofen through the skin was in-vitro evaluated. All the formulations were evaluated for their quantity of drug present in the formulation, pH, Viscosity, Spreadability, in vitro diffusion study. Formula F4, which showed good Physico-chemical properties, was subjected to anti-inflammatory study. Results showed that pH, spreadability, viscosity and amount of active ingredient present in formulations were in an acceptable limit. The standard calibration curve for flurbiprofen depicts the linear association between concentration and absorbance. The formulation F4 has the highest % release, 90.54% also showed a higher % inhibition of paw oedema after 4 hrs than marketed formulation.

Development and Characterization Colchicine-Loaded PEGylated Gelatin Nanoparticles for Targeted Delivery to Tumor

2013 ◽  
Vol 6 (2) ◽  
pp. 2058-2063
Author(s):  
G D Chandrethiya ◽  
P K Shelat ◽  
M N Zaveri
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
High Performance ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Spherical Particles ◽  
Precipitation Method ◽  
Antitumoral Activity ◽  
Gelatin Nanoparticles

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin.  Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized.  Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation.  Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay.  The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.  

Novel Swellable/Expandable Gastroretentive Floating Films of Gliclazide Folded in Capsule Shell for the Effective Management of Diabetes Mellitus: Formulation Development, Optimization and In vitro Evaluation

2020 ◽  
Vol 15 ◽  
Author(s):  
Diksha Sharma ◽  
Deepak Sharma
Keyword(s):  
Diabetes Mellitus ◽  
Drug Absorption ◽  
Gastric Fluid ◽  
Stability Study ◽  
Gastric Retention ◽  
Effective Management ◽  
In Vitro Evaluation ◽  
Capsule Shell ◽  
Study Results

Background: Gliclazide (GLZ) belongs to the second-generation of sulphonylureas, is a drug of choice for the management of type II DM. It belongs to BCS Class II. The major site of drug absorption for GLZ is the stomach; it displayed variation in the drug absorption rate and bioavailability due to the shorter gastric retention time. Floating mechanism performance gets affected when the gastric fluid level not sufficiently higher, which ultimately obstructs the floating behavior, which is the major limitation of reported formulations. This limitation can get over by folded the film into the capsule shell that dissolved in gastric fluid and film swell/expands to dimensions higher than pylorus sphincter (12mm), thus prevents its evacuation. Objective: To explore the floating mechanism in the designing of films along with a tendency to expand by swelling and unfolding by utilizing a mixture of hydrophilic and hydrophobic polymer to achieve the controlled drug delivery and prolonged gastric retention of drug. Methods: The gastroretentive floating films were formulated by the solvent casting technique using 32 full factorial design and subjected to in vitro evaluation parameters, drug-excipient compatibility, X-ray diffraction and accelerated stability study. Results: The pre-formulation study established the purity and identification of drug. FTIR study confirmed no drug excipient interaction. F3, F6, and F9 were optimized based on in vitro floating characteristics, swelling/expanding ability, and unfolding time study. All developed formulations were unfolded within 14-22 min after capsule disintegration. The F3 was selected as final formulation as its ability to control the release of drug for 24 hrs followed by Zero-order kinetics having super case 2 transport. XRD confirmed the amorphousness of drug within formulation. The stability study results revealed that formulation was quite stable at extreme storage condition. Conclusion: The developed novel formulation has a good potential for the effective management and treatment of Diabetes Mellitus.

scholarly journals In Vitro Studies on Nasal Formulations of Nanostructured Lipid Carriers (NLC) and Solid Lipid Nanoparticles (SLN)

2021 ◽  
Vol 14 (8) ◽  
pp. 711
Author(s):  
Cláudia Pina Costa ◽  
Sandra Barreiro ◽  
João Nuno Moreira ◽  
Renata Silva ◽  
Hugo Almeida ◽  
...  
Keyword(s):  
Nasal Cavity ◽  
Solid Lipid Nanoparticles ◽  
Local Treatment ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
In Vitro Studies ◽  
Brain Diseases ◽  
In Vivo Studies ◽  
Solid Lipid

The nasal route has been used for many years for the local treatment of nasal diseases. More recently, this route has been gaining momentum, due to the possibility of targeting the central nervous system (CNS) from the nasal cavity, avoiding the blood−brain barrier (BBB). In this area, the use of lipid nanoparticles, such as nanostructured lipid carriers (NLC) and solid lipid nanoparticles (SLN), in nasal formulations has shown promising outcomes on a wide array of indications such as brain diseases, including epilepsy, multiple sclerosis, Alzheimer’s disease, Parkinson’s disease and gliomas. Herein, the state of the art of the most recent literature available on in vitro studies with nasal formulations of lipid nanoparticles is discussed. Specific in vitro cell culture models are needed to assess the cytotoxicity of nasal formulations and to explore the underlying mechanism(s) of drug transport and absorption across the nasal mucosa. In addition, different studies with 3D nasal casts are reported, showing their ability to predict the drug deposition in the nasal cavity and evaluating the factors that interfere in this process, such as nasal cavity area, type of administration device and angle of application, inspiratory flow, presence of mucoadhesive agents, among others. Notwithstanding, they do not preclude the use of confirmatory in vivo studies, a significant impact on the 3R (replacement, reduction and refinement) principle within the scope of animal experiments is expected. The use of 3D nasal casts to test nasal formulations of lipid nanoparticles is still totally unexplored, to the authors best knowledge, thus constituting a wide open field of research.

scholarly journals Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

2011 ◽  
Vol 61 (2) ◽  
pp. 217-226 ◽  
Author(s):  
Komuravelly Someshwar ◽  
Kalyani Chithaluru ◽  
Tadikonda Ramarao ◽  
K. Kumar
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Floating Tablets ◽  
Gastric Residence Time

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h.

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

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