Design and development of zolmitriptan niosomal in situ nasal gel for the treatment of migrain

2021 ◽  
Vol 12 (3) ◽  
pp. 1861-1869
Author(s):  
Anilkumar J. Shinde ◽  
Karan B. Swami ◽  
Firoj A. Tamboli ◽  
Harinath N. More
Keyword(s):  
Particle Size ◽  
Entrapment Efficiency ◽  
Migraine Treatment ◽  
Diffusion Study ◽  
In Situ Gel ◽  
Dsc Studies ◽  
In Vitro Diffusion ◽  
In Situ Nasal Gel

The objective of the present study was to development of Zolmitriptan (ZMT) niosomal in situ nasal gel formulation for migraine treatment. By intranasal route delivered drug to the central nervous system (CNS) through the olfactory lobes, which bypasses the first-pass metabolism and consequently enhances the bioavailability. Noisome of ZMT were prepared by using the lipid film hydration method. Optimized niosomal formulation was used to prepare in situ gel. The developed Noisomal formulations were characterized for vesicle size, shape, zeta potential, entrapment efficiency, drug content and in-vitro diffusion study, mucoadhesive strength, permeation study, FTIR, DSC and XRD studies. The FTIR and DSC studies predicted that there was no any interaction in drug and excipients. ZMT niosomes were showed particle size, Polydispersity index (PDI), Zeta potential, % entrapment efficiency and drug content, 149nm, 0.223, -28.9, 88.16±0.8 % and 96.23±1.2% respectively. In-vitro  diffusion study of niosomes shows 96.23±0.7% at 8h. The permeation rate of in situ niosomes gel and the pure drug was about 98.56% and 79.46%, respectively. XRD & DSC studies were showed that reduce crystalinity in the formulations. The SEM images of niosomes were found spherical in shape to some extent showing particle size distribution. Thus, it can be concluded that developed ZMT niosomal in situ gel formulation can be considered as a promising system for which may reduce dose requirement, improve patient acceptability and efficient targeting drug delivery to the brain through the olfactory lobe for migraine treatment.

scholarly journals FORMULATION AND DEVELOPMENT OF IN SITU FORMING GEL FOR THE TREATMENT OF ORAL THRUSH

2018 ◽  
Vol 11 (8) ◽  
pp. 342 ◽  
Author(s):  
Akshay Kumar S ◽  
Vishal Gupta N ◽  
Gowda Dv ◽  
Praveen Sivadasu
Keyword(s):  
Gelation Time ◽  
Adhesive Force ◽  
In Situ Gel ◽  
Dsc Studies ◽  
In Situ Forming ◽  
In Vitro Diffusion ◽  
In Situ Forming Gel ◽  
Oral Thrush

Objective: The objective of the present work was to develop an in situ gel composed of Pluronic F-127, Carbopol 934, and methylparaben and loaded with fluconazole using DoE software to sustain the delivery of drug in the buccal cavity.Methods: In situ gels were prepared by temperature-induced method, by employing DoE and characterized by Fourier transform infrared (FTIR), differential scanning calorimeter (DSC), and evaluated for gelation temperature, gelation time, adhesive force, and in vitro diffusion studies.Results: Both FTIR and DSC studies suggested that there were no chemical interactions present between both drug and polymers. The formulated gels S1, S3, and S9 showed gelation at a body temperature. The viscosity, gel strength, and mucoadhesive force for the formulated in situ gels were found to be within the ranges of 375–738 cps, 35–62 s, and 4650–5210.32 dynes/cm2, respectively. The in vitro diffusion studies indicated that optimized in situ gel S3 exhibited the improved ability to sustain the drug compared to other formulations.Conclusion: Thus, developed in situ gel system was determined to be effective in terms of eradication of oral thrush.

scholarly journals FORMULATION AND EVALUATION OF NIOSOMAL IN SITU GEL OF PREDNISOLONE SODIUM PHOSPHATE FOR OCULAR DRUG DELIVERY

2019 ◽  
pp. 97-116 ◽  
Author(s):  
PRAVEEN D. CHAUDHARI ◽  
UJWALA S. DESAI
Keyword(s):  
Drug Delivery ◽  
Sodium Phosphate ◽  
Entrapment Efficiency ◽  
Diffusion Study ◽  
In Situ Gel ◽  
Drug Diffusion ◽  
Sustained Action ◽  
Span 60

Objective: The main purpose of the study was to develop niosomal in situ gel of prednisolone sodium phosphate (PSP) with increased bioavailability (enhanced permeation) and sustained action (drug retention at the target site). Methods: Using different ratios of span 60 and cholesterol (chol), niosomes were prepared by thin film hydration method and optimized by evaluating different parameters like drug content, entrapment efficiency, particle size and in vitro drug diffusion study. The niosomal pellets were further incorporated in in situ gel, prepared by the cold method and further optimized by parameters like gelling parameters, mucoadhesive strength and in vitro, in vivo drug release study. Results: The optimized niosomal formulation containing span 60 and chol in equal proportion (1:1) showed better drug content (DC) i.e. 86.3±0.39% and entrapment efficiency (EE) i.e. 83.4±0.22 with vesicle size of 465±0.24 nm. The in vitro drug diffusion study indicated t90 value of 490 min thus proving sustained action of the formulation. The optimized in situ gel containing poloxamer 407 (P407) and poloxamer 188 (P188) in the ratio of 1:2.7 showed gelation temperature at 37 ⁰C (physiological temperature of the body) and t90 value of 10 h thus depicting sustained action. The increased area under curve (AUC) value by 1.75 folds proved increased bioavailability of the drug. Conclusion: Thus sustained drug delivery with increased bioavailability was designed for prednisolone sodium phosphate for the treatment of ocular inflammation.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF DICLOFENAC SODIUM LOADED EUDRAGIT RS100 POLYMERIC MICROSPONGE INCORPORATED INTO IN SITU GEL FOR OPHTHALMIC DRUG DELIVERY SYSTEM

2021 ◽  
pp. 63-69
Author(s):  
RAJASHRI B. AMBIKAR ◽  
ASHOK V. BHOSALE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Entrapment Efficiency ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content

Objective: Purpose of the study to design and formulate Diclofenac sodium (DIC) microsponges. Methods: With varied polymer: drug ratio DIC loaded microsponges were prepared with Eudragit RS100 polymer by quasi solvent diffusion method. Microsponges evaluated for particle size, entrapment efficiency, drug content, in vitro drug release, Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetry (DSC) and Scanning electron microscopy (SEM). DIC loaded microsponges incorporated into ocular in situ gel to attained controlled release by microsponge and improved residence time by gelling system. Ocular in situ gel evaluated for pH, drug content determination, gelling capacity, in vitro drug release and sterility study. Results: DSER4 microsponge formulation having polymer to drug ratio 1:7 showed satisfactory production yield (68.13%), entrapment efficiency (62.86%), drug content (80.73%), requisite particle size (less than 10 µm) (7.52 µm) and in vitro release 87.94% after 6 h. Selected DSER4 formulation was incorporate into in situ gel. Carbopol 940 forms stiff gel at higher pH so used as a gelling agent, whereas Hydroxypropyl Methylcellulose E4M was used as a viscosity-enhancing agent for the formulation of in situ gel in varied compositions. In situ gel formulation IG4 showed sustained release of 76.92% till the end of 8 h and satisfactory gelling capacity so IG4 further evaluated for sterility test. Rheological studies reveal the sol-gel transition of in situ gel occur at the physiological condition to form stiff gel. Conclusion: Prepared in situ gel formulations showed sustained drug release for a period of 8 h, which is satisfactory for management of ocular pain.

DEVELOPMENT AND EVALUATION OF NANOPARTICULATE BASED IN-SITU GELLING SYSTEM FOR NASAL DRUG DELIVERY OF AN ANTI-EPILEPTIC DRUG

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (09) ◽  
pp. 83-85
Author(s):  
A Ambavkar ◽  
◽  
N. Desai
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Poloxamer 407 ◽  
Nasal Drug Delivery ◽  
Anti Epileptic Drug ◽  
Nanolipid Carriers ◽  
In Situ Nasal Gel

The objective of the study was to develop and evaluate nanolipid carriers based in situ gel of Carbamazepine, for brain delivery through intranasal route. The non – invasive nasal route can provide rapid delivery of drugs directly to the central nervous system by bypassing the blood brain barrier. The nanolipid carriers of carbamazepine as in situ nasal gel can prolong the drug release for control of repetitive seizures and were prepared by Phase Inversion Temperature technique. The retention of the carriers in the nasal cavity was improved by using Poloxamer 407 as thermoresponsive and Carbopol 974P as mucoadhesive gelling polymers, respectively. The developed gel was evaluated for particle size, polydispersity index, zeta potential, morphology, entrapment efficiency, mucoadhesive and thermoresponsive behaviour, in vitro drug release, ex vivo permeation and nasociliotoxicity. The gel showed sustained release over prolonged periods and was found to be non-toxic to the sheep nasal mucosa.

DEVELOPMENT AND INVESTIGATION OF TIMOLOL MALEATE AND TRAVOPROST COMBINATION NIOSOMAL IN SITU GELLING SYSTEM FOR THE TREATMENT OF GLAUCOMA

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (07) ◽  
pp. 33-35
Author(s):  
A Dubey ◽  
◽  
P Prabhu ◽  
N Nair ◽  
K Beladiya ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Timolol Maleate ◽  
In Situ Gel ◽  
Vesicle Size ◽  
Gelling Time ◽  
In Situ Gelling ◽  
Vitro Release

The aim of the present investigation was to develop a combination of timolol maleate and travoprost niosomal in situ gelling system for the treatment of glaucoma. Niosomes were prepared by thin film hydration technique using rotary flash evaporator. A 32 factorial design was utilized to study the effect of the molar ratio of Span 60 (X1) and cholesterol (X2) on vesicle size, drug entrapment efficiency and in vitro release study. On the basis of vesicle size, maximum entrapment efficiency and in vitro release of drug, best formulations were selected for the preparation of niosomal in situ gel (Drop). On the basis of gelling time and viscosity, optimized ratio of the polymers was selected for the desired preparation. Selected niosomal batches were dispersed in carbopol 940 and HPMC K4M polymer solution (combination IF6) to form in situ gel niosomal formulations (Drop). The gelling time of the niosomal in situ gel (NIF1) was found to be the best (+++) and the viscosity was found to be 1190 cP. Zeta potential, average size analysis, polydispersibility index value was found to be -45.1 mV, 256.5 nm, 0.228 respectively. In vitro drug release was found to be within the range of 50.23 ± 0.54 to 60.23 ± 0.33% over the period of 6 h. IOP lowering activity of best formulation (NIF1) showed more significant and sustained effect than the marketed eye drops. Best formulation (NIF1) was found to be stable, sterile, non irritant and isotonic. Hence niosomal in situ gelling combination system may have the potential of bringing better application than the conventional ocular therapy with improved ocular bioavailability and increased patient compliance.

scholarly journals Design of a Reversible Cholinesterase Inhibitor Mamentine HCL Nanogel: Formulation and In-vitro Evaluation

2021 ◽  
pp. 352-359
Author(s):  
Subhasri Mohapatra ◽  
Sourabh Jain ◽  
Karunakar Shukla
Keyword(s):  
Particle Size ◽  
Cholinesterase Inhibitor ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Storage Period ◽  
Spherical Particles ◽  
Average Particle ◽  
In Situ Gel

Memantine hydrochloride is a is a reversible cholinesterase inhibitor used in the treatment of Alzheimer’s disease, low-moderate affinity, uncompetitive n-methyl-d-aspartate (NMDA) receptor antagonist, with strong voltage dependency and rapid blocking/unblocking kinetics. The present study was explore the potential of thermosensitive nanogel of mamentine loaded nanoparticle. In situ gel choosing due to restrict unwanted exposure in blood and other healthy tissues, thus eliminate hemolytic side effects of the drug and offer easy administration in vivo. Nanoparticle prepared by ionic gelation method and further the dried nanoparticle incorporates with in situ gel.  The in situ gel prepared by cold method using the solutions of Poloxamer-188 and Carbopol-934. The Transmission electron microscopy showed the spherical particles  with  smooth surface which was in conformity  with the SEM and Zetasizer  data for particle size. The pH of the formulations was found to be satisfactory and was in the range of 6.8±0.039 -7.4±0.053 and also mucoadhesive strength was show in table. The mucoadhesive strength of all formulations was varies from 2398±0.0004 to 4945±0.0002 dynes/cm2. In-vitro diffusion study of the in situ gel (N1-N8) was performed using modified Franz diffusion cell with dialysis membrane in phosphate buffer pH 6.5 for a period of 24 hours. The in vitro release study were fitted into various kinetic models viz zero order, first order, higuchi model and korsmeyer peppas equation. Stability studies for optimized formulations were carried out at 4.0 ± 0.5°C and 37 ± 0.5ºC for a period of four weeks. There was no significant variation found in physical appearance, average particle size and % drug content of the in situ nanogel N2. No visible changes in the appearance of the gel formulation were observed at the end of the storage period.

scholarly journals Formulation and Characterization of Tranylcypromine loaded Polymeric Micellar In-Situ Nasal Gel for treatment of Depression

2020 ◽  
pp. 149-165
Keyword(s):  
Polymeric Micelles ◽  
Research Work ◽  
In Vitro Release ◽  
Polymeric Micelle ◽  
In Situ Gel ◽  
Treatment Of Depression ◽  
In Situ Nasal Gel

:Tranylcypromine is a drug used as antidepressant,anxiolytic, nonselective MAO A/B inhibitor. This drug is used to treat depression.The research was conducted to develop a polymeric micelle using a block copolymer, Pluronic F-68 and Gelucire 50/13 to improve the permeability of Tranylcypromine (TCP). A direct dissolution method was used to prepare polymeric micelles. The prepared micelles were characterised for particle size, % EE, zeta potential, in-vitro release. These micelles solution was used to prepare in situ gel by cold method in order to achieve controlled release. Central composite design was used for optimization of both polymeric micelles and insitu nasal gel.The main objective of this research work is to develop formulation acting centrally without undergoing first pass metabolism i.ie. directly nasal to brain delivery route.

scholarly journals FORMULATION AND EVALUATION OF IN SITU MUCOADHESIVE THERMOREVERSIBLE NASAL GEL OF SERTRALINE HYDROCHLORIDE

2019 ◽  
pp. 195-202
Author(s):  
DIKSHA SHARMA ◽  
SHAWETA AGARAWAL
Keyword(s):  
Drug Release ◽  
Biological Membrane ◽  
Poloxamer 407 ◽  
Compatibility Study ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Sertraline Hydrochloride ◽  
In Situ Nasal Gel

Objective: The objective of the study was to aiming to formulate and evaluate temperature based in situ nasal gel of sertraline HCL. Materials and Methods: Preformulation studies of sertraline hydrochloride including tests for identification, solubility studies, Fourier-transformer infrared (FTIR) spectroscopy, melting point determination, and other studies were carried out and compared with the specification as per literature. The solubility of sertraline hydrochloride was determined in different solvents such as in distilled water, ethanol, acetone, isopropyl alcohol, and 2-propanol. Each value for solubility was determined in triplicate and average values were reported. The drug excipient compatibility study was determined by FTIR. Thermal analysis was performed using a differential scanning calorimetric equipped with a computerized data station. The UV spectrum of sertraline hydrochloride was obtained using UV JascV630. The in situ gel formulation was prepared by changing the concentration and using only one polymer (Carbopol 934) has been used at the same concentration. Mucoadhesive strength and in vitro permeation study were determined using gout nasal mucosal membrane, whereas in vitro drug release study was carried out using diffusion cell through egg membrane as a biological membrane. The stability studies were conducted according to ICH guidelines. Results: The FTIR studies of formulation show no interaction between drug and excipient. In situ gel was prepared using Carbopol 934 and Poloxamer 407 to improve its adhesion property. The optimized formulation (F6) was transparent and clear in appearance with 101.15% drug content. The sol-gel transformation of in situ gel was found at temperature 34.92°C with immediate gelation property. The in vitro drug release of optimized formulation was found 95.80% drug release in 8 h. Formulations F4 and F6 showed immediate gelation within 60 s and remained stable for an extended period. All the formulations were liquid at room temperature and underwent rapid gelation on contact with simulated nasal fluid. Conclusion: The results concluded that the formulations of in situ nasal gel showing to improve the bioavailability through its longer residence time and ability to sustain drug release.

scholarly journals Formulation and Evaluation of A Nanoparticle Laden in Situ Gel System for Enhancing the Ocular Delivery of Ciprofloxacin

2021 ◽  
Vol 70 (2) ◽  
Author(s):  
Sourav Datta ◽  
Ratul Bhowmik ◽  
Ranajit Nath ◽  
Rajarshi Chakraborty ◽  
Apala Chakraborty
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Average Particle ◽  
Eye Drops ◽  
Physiological Factors ◽  
In Situ Gel ◽  
Gel System

The human eye can be a tricky issue for topical administration of the drugs due to its unique anatomical arrangements of surface tissue and corneal impermeability. Topical instillation of drugs in the form of eye drops is the major and well-accepted route of administration for the treatment of varied eye disorders. Conventional ophthalmic drug delivery systems often lead to poor bioavailability and thus reduced therapeutic response. Several new preparations are developed to enhance the contact time of the medicament on the surface of the eye. Successful results have been obtained in the form of inserts and collagen shields. However, these preparations have also some disadvantages, such as poor patient compliance, particularly in the case of elderly patients. These problems could be solved by using nanoparticles laden in situ gel-forming systems that exhibit phase transition from solution to gel. These nanoparticle in situ gel systems may be formulated as eye drops suitable for administration through instillation into the eye, which upon exposure to the eye, stimulated by various ocular physiological factors, converts to the gel phase. The advantage of those formulations is that unlike inserts and films they do not require complicated equipment for manufacture and that they are scalable without any difficulty. The objective of the present study was to prepare a pH-dependent nanoparticle-laden in situ gel system for Ciprofloxacin, to prolong the release of the drug into the ocular compartment. No incompatibility was found between the drug and the excipients. Nanoparticles were developed using the nanoprecipitation technique. Eudragit RL 100 was used as the polymer. While the in situ gel solution was formulated using chitosan as polymer. The Ciprofloxacin nanoparticles were measured for particle size and the average particle size was ranged from 295.3-458.7 nm. Entrapment efficiency ranged from 13.83% to 6.29%. Nanoparticleladen in situ gels had the pH of the formulati

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