scholarly journals FORMULATION AND EVALUATION OF ITRACONAZOLE NIOSOMAL GEL

2018 ◽  
Vol 6 (5) ◽  
pp. 76-80
Author(s):  
Ashish Kumar ◽  
J.S Dua
Keyword(s):  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Systemic Fungal Infection ◽  
Drug Content ◽  
Carbopol 940 ◽  
Niosomal Gel ◽  
Span 60 ◽  
Anti Fungal

The preparation of niosomes. The main objective of the study was to enhance the antifungal activity of the formulation.  Itraconazole is a broad spectrum Imidazole derivative useful in the treatment of superfacial and systemic fungal infection. Various surfactants used were span 40 and span 60. Niosomes were prepared by using Rotary Vaccum evaporation method. Niosomes were prepared using different ratio of drug: surfactant: cholesterol (1:1:1, 1:2:1, 1:3:1).Evaluation of the Niosomal gel was done by determination of drug content 52.81-56.12, Entrapment Efficiency 42.20-45.20,Niosomal gel was prepared using Carbopol 940 (1.5%), Glycerol (10%), Triethanolamine (q.s.) and distilled water up to 15ml. Viscosity was determined by Brookfield programmable ultra-viscometer and the ranges 8173 centipoise. The drug content of the Itraconazole niosomal gel was determined at 262 nm against blank by using UV/visible spectrophotometer and found to be 56.12%. The percentage of drug entrapment in niosomal gel was calculated to be 45.20% .The in-vitro drug release study was carried out using phosphate buffer saline pH 7.4 and was found to be 41.18 ± 1.53% for 12 hours. It can be concluded that the gel formulation containing niosomes loaded with Itraconazole showed prolonged action than formulation containing Itraconazole in non-niosomal form and it can be developed successfully to improve the anti-fungal activity.

scholarly journals FORMULATION AND EVALUATION OF KETOCONAZOLE NIOSOMAL GEL

2018 ◽  
Vol 6 (5) ◽  
pp. 71-75
Author(s):  
Paninder Kaur ◽  
J.S Dua ◽  
D.N Prasad
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Drug Content ◽  
Novel Drug Delivery System ◽  
Niosomal Gel ◽  
Span 60 ◽  
Novel Drug ◽  
Rotary Vacuum

ABSTRACT   In recent years, treatment of infectious disease through Novel Drug delivery system (NDDS) has undergone a revolutionary shift. Niosomes are a Novel Drug Delivery system which has potential application to treat infectious disease topically. Niosomes are non-ionic surfactant vesicles, in which medication is encapsulated in a vesicle for controlled drug release. Ketoconazole niosomes were prepared by using Cholesterol, Span 60/ Span 40 as surfactants, chloroform, and diethyl ether using rotary vacuum evaporator method. Formulation was then evaluated for particle size, drug content, entrapment efficiency, and in-vitro drug release studies. The Entrapment efficiency and drug content were calculated at 225nm using UV spectrophotometer. The drug content was found to be 70.37% for Span 40 and 72.81% for Span 60.The percentage of drug entrapment in niosomes was 60.3 % for Span 40 and 62.21 % for Span 60. FT-IR studies for niosomes containing Span 40 shows -CH stretching (Aliphatic) at 2891 cm-1and2925 cm-1 for niosomes containing Span 60. Ketoconazole niosomal gel was prepared using Carbopol 940, glycerol, Triethanolamine and distilled water. Evaluation of niosomal gel was determined by Physical appearance, pH, viscosity, drug content, entrapment efficiency and In-vitro diffusion studies.The percentage of the drug release from the niosomal gel was found to be 40.78 % for Span 40 and 33.75% for Span 60 . This delivery system is cost effective and simple to prepare as only the prepared gel of niosomes was introduced in Rotary vacuum evaporator for solvent evaporation.    

scholarly journals Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin

1970 ◽  
Vol 1 (3) ◽  
pp. 43-49 ◽  
Author(s):  
Jovita Kanoujia ◽  
Kanchan Sonker ◽  
Manisha Pandey ◽  
Koshy M Kymonil ◽  
Shubhini A Saraf
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Carbopol 940 ◽  
In Situ Gelling ◽  
Gel Transition

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49

scholarly journals ENHANCEMENT OF DISSOLUTION CHARACTERISTICS OF CLOPIDOGREL BISULPHATE BY PRONIOSOMES

2019 ◽  
pp. 77-85 ◽  
Author(s):  
EMAN A. MAZYED ◽  
SHERIN ZAKARIA
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
International Normalized Ratio ◽  
Angle Of Repose ◽  
Morphological Examination ◽  
Span 60

Objective: The present investigation aims to formulate and evaluate proniosomes of clopidogrel bisulphate for improving its dissolution characteristics. Methods: The slurry method was used for the preparation of proniosomes of clopidogrel using cholesterol, sorbitan monostearate (Span 60) and maltodextrin as a carrier. Clopidogrel proniosomes were evaluated for their entrapment efficiency and in vitro drug release. The best formula (F1) that achieved maximum drug release was further evaluated by measurement of the angle of repose, morphological examination, determination of vesicle size, determination of zeta potential, Fourier transform infrared spectroscopy and differential thermal analysis. The in vivo behavior of the selected proniosomal formula (F1) was studied by measuring the antiplatelet activity in adult male mice. Results: The entrapment efficiency of clopidogrel proniosomes was in the range of 83.04±1.99 to 90.14±0.30. % drug released from proniosomal formulations was in the range of 79.73±0.35 to 97.70±1.10 % within 4 h. Clopidogrel proniosomes significantly enhanced the in vitro release of clopidogrel compared with the plain drug that achieved 61.77±2.22 % drug release. F1 significantly (p ≤ 0.001) increased the bleeding time and bleeding volume and significantly (p ≤ 0.05) prolonged prothrombin time and decreased prothrombin activity and increased the international normalized ratio (INR) compared to plain clopidogrel. Conclusion: The present investigation introduced proniosomes as a promising carrier for clopidogrel that could enhance its dissolution and pharmacological effect.

scholarly journals Formulation and evaluation of nanoparticulate ofloxacin ophthalmic gel using ionic gelation method

2019 ◽  
Vol 1 (2) ◽  
pp. 73-78
Author(s):  
B Syed Salman ◽  
Mohd Abdul Hannan Baig
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Entrapment Efficiency ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
In Vitro Drug Release ◽  
Entire Study ◽  
Drug Content ◽  
Higuchi Model

Oflaxacin is an ophthalmic and topical anti-bacterial agent used in the management of Allergic conjunctivitis, Trachoma, Blepharitis. The basic idea behind the development of such a system is to maintain a sustained drug release from the dosage form. Oflaxacin is suitable candidate for formulation into sustained dosage form in order to prolong the release of drug. The drug-excipient compatibility studies were carried out by using FTIR technique. Based on the results, excipients were found to be compatible with ofloxacin. In preformulation study, estimation of Ofloxacin was carried out by systronics UV spectrophotometer at λmax 284nm using distilled water, which had a good reproducibility and this method was used in entire study. Formulation was prepared by using ionic gelation method .The response drug content, entrapment efficiency, diffusion, spreadability, In vitro drug release was evaluated Drug content ranging from to 82.6 % to 91.24% entrapment efficiency values are ranged from 91.25% to 94.02% and in -vitro drug release studies are also studied. The In-vitro drug release study of Ofloxacin was carried out by using In-vitro diffusion apparatus.100ml of using tear fluid was taken in a beaker. The solution was stirred with 100rpm by maintaining the temperature of 37˚c ± 5˚c. The drug release data were explored for this type of release mechanism followed. The best fit with the highest determination R2 coefficients was shown by both the models (zero and peppas) followed by Higuchi model which indicate the drug release via diffusion mechanism. However as indicated by the values of R both of the models (zero and peppas) followed by Higuchi model were found to be efficient in describing the release of Ofloxacin.

scholarly journals DEVELOPMENT AND PHYSICAL CHARACTERIZATION OF A PERIODONTAL BIOADHESIVE GEL OF GATIFLOXACIN

2017 ◽  
Vol 9 (3) ◽  
pp. 31
Author(s):  
Hanan Jalal Kassab ◽  
Lena Murad Thomas ◽  
Saba Abdulhadi Jabir
Keyword(s):  
Drug Release ◽  
Ph Value ◽  
Hydrophilic Polymers ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Carbopol 940 ◽  
Evaluation Parameters

Objective: The aim of this study was to develop a bioadhesive gel of gatifloxacin for the treatment of periodontal diseases.Methods: Periodontal gels of gatifloxacin were prepared using different hydrophilic polymers such as carbopol 940 (CP 940), carboxymethyl cellulose (CMC) and hydroxypropylmethyl cellulose (HPMC) in varied concentrations, either alone or as a combination. The prepared gels were evaluated for their physical appearance, pH, drug content, viscosity, bioadhesiveness and in vitro drug release profile. The influence of the type and the concentration of polymer on the drug release as well as on viscosity and mucoadhesiveness of prepared gels were investigated.Results: The prepared gels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and pH value. Using different polymer types at different concentrations, as well as different polymer combinations, play a significant role in the variation of overall characteristics of formulations. Increasing the concentration of polymer increased the viscosity as well as mucoadhesion, and reduced drug release rate. Formulation F 11 (1 % CP 940 and 5 % CMC) was selected as the formula of choice based on the data of various evaluation parameters such as pH, drug content, viscosity, spreadability and bioadhesion as well as its ability to show a prolonged drug release pattern.Conclusion: The obtained results show that a bioadhesive periodontal gel of gatifloxacin can be prepared using hydrophilic polymers, and by using a combination of polymers the viscosity, mucoadhesiveness, spreadability and release behavior can be optimized.

scholarly journals INFLUENCE OF BIOENHANCERS ON THE RELEASE PATTERN OF NIOSOMES CONTAINING METHOTREXATE

2012 ◽  
Vol 02 (02) ◽  
pp. 36-40
Author(s):  
Narayana Charyulu R. ◽  
Gandhi Kinjal B. ◽  
Jobin Jose ◽  
Sneh Priya ◽  
Shastry C. S.
Keyword(s):  
Thin Film ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Pattern ◽  
Sustain Release ◽  
Pure Drug ◽  
Span 60 ◽  
Dicetyl Phosphate

AbstractThe aim of present study was to prepare sustained release formulations of niosomes of methotrexate (MTX) alone (N1 to N10) and along withbioenhancers (NB1 to NB9) by thin film hydration technique using span 60 as surfactant,cholesterol as membrane stabilizing agent, curcumin and piperine as bioenhancers and dicetyl phosphate (DCP) as charge inducing agent. All the formulations of niosomeswere characterized on the basis of physical appearance and entrapment efficiency. The invitro releasestudies of optimized formulation of niosomes of MTX alone and along with bioenhancers were performed and compared with pure drug released. The entrapment efficiency of MTX in optimized formulation of niosomes containing MTX along with bioenhancers was found to 56.9% and entrapment efficiency of bioenhancerscurcumin and piperinewas found to be 40.30% and 69.1%respectively. In vitro drug release of optimized formulationsof niosomes of MTX without and with bioenhancers (F3) was found to be 98.89% and 60.97% at the end of 12 h respectively. Results concluded that Niosomes of MTX containing bioenhancers followed sustain release pattern.

scholarly journals MUCOADHESIVE POLYMERIC FILMS OF ACYCLOVIR PRONIOSOMES FOR BUCCAL ADMINISTRATION

2021 ◽  
pp. 135-143
Author(s):  
DEEKSHA U. SUVARNA ◽  
MARINA KOLAND ◽  
ANANTH PRABHU ◽  
SINDHOOR S. M.
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Polymeric Films ◽  
Prolonged Release ◽  
Mucosal Permeability ◽  
In Vitro Drug Release ◽  
Ex Vivo Permeation ◽  
Span 60

Objective: The aim of the present work was to formulate and evaluate proniosomes of the poorly soluble drug, acyclovir incorporated in mucoadhesive polymeric films for improved buccal mucosal permeability of the drug while achieving prolonged release. Methods: Acyclovir was formulated as proniosomes using Span 60 and cholesterol. The prepared proniosomes were loaded into mucoadhesive polymeric films prepared with varying quantities of carbopol 934P and HPMC K15M. The proniosome incorporated films were evaluated for physicomechanical characters, mucoadhesion, swelling index, drug content, in vitro drug release and ex vivo permeation through porcine buccal mucosa. Results: Hydration of the proniosomes produced spherical vesicles or niosomes, which was confirmed by Scanning Electron Microscopy. The optimized formulation selected on the basis of vesicle size, entrapment efficiency PDI, Zetz potential and in vitro drug release was selected for incorporation into mucoadhesive polymeric films. All the films showed excellent physicomechanical characters. Formulations with higher proportions of carbopol produced slower in vitro drug release. The kinetics of release of drug from all the formulations appeared to be zero-order based on their regression coefficient values. Comparative evaluation of ex vivo permeation from niosomal and non-niosomal films indicated that the former demonstrated improved mucosal permeation and drug release was also sustained for the 8 h period. Conclusion: Mucoadhesive films impregnated with acyclovir loaded proniosomes could be a potential approach for buccal delivery of acyclovir for improving its absorption and bioavailability. 

scholarly journals Formulation and Evaluation of Controlled Release Maintenance Dose Loaded Niosomes of Anti-Hypertensive Drug

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Chandani Makvana ◽  
Satyajit Sahoo
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Zeta Potential ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Drug Carriers ◽  
Vesicle Size ◽  
Drug Content ◽  
Span 60

The present study was aimed to formulate, comparatively evaluate and optimize multiple lipid drug carriers of valsartan for oral controlled release to overcome the problems associated with the drug such as bioavailability, to reduce the dosage regimen, half life and to determine the appropriateness of niosomal formulation as a drug carrier. Ether injection method was chosen for the formulation of physically and chemically stable niosomes of valsartan. The formulation and process parameters were optimized by manufacturing placebo niosomes. Than drug loaded niosome was prepared by varying the concentration of span 60. The prepared nine formulations were evaluated for various parameters. Placebo niosomes were evaluated for appearance, odour, texture, creaming volume, pH and changes after 15 days. The medicated nine formulations were evaluated for organoleptic properties (appearance/color, odour), pH, total drug content, entrapment efficiency, mean particle size and polydispersibility index, zeta potential and In-vitro drug release. All formulations were off-white in color, odourless, and fluid in nature. It was stable and did not show sedimentation. The pH was found to be in the range of 4.6-5.4. Drug content was found in the range of 89.13 to 99.52. The Entrapment efficiency was found in range of 79.05 to 98.24. The mean vesicle size of drug loaded niosomes of the different batches ranged between 2.52-3.42μm. The polydispersvity index was in the range of 0.325 to 0.420 which indicates a narrow vesicle size distribution. The values of zeta potential were in the range of -20.29 mV to -30.55 mV which indicates that niosome had sufficient charge and mobility to inhibit aggregation of vesicles. All the nine formulations shows constant drug release in controlled manner up to 24 h. Formulation V7 was considered to be the best formulation as the % drug content (99.52 ± 0.97), % entrapment efficiency (98.24 ± 1.50) and % drug release at the end of 24th h (98.55) were high for V7. The optimized formulation V7 showed higher degree of correlation coefficient (r2) 0.9805 which indicates process of constant drug release from dosage form. The present study concludes that the prepared niosome is a convenient and efficiency carrier for the delivery of antihypertensive drug. Besides this, it provided controlled delivery of drug.

Elastic Bilayer Vesicles of Flurbiprofen for Transdermal Delivery: Development and In-Vitro Characterization

2020 ◽  
Vol 10 (1) ◽  
pp. 54-60
Author(s):  
Rashmi Sareen ◽  
Nitin Jain
Keyword(s):  
Transdermal Delivery ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Systemic Circulation ◽  
Molar Ratio ◽  
Vesicle Size ◽  
Cholesterol Ratio ◽  
Niosomal Gel ◽  
Span 60

Objective: The purpose of the present study was to develop a novel elastic bilayer vesicle entrapped with Flurbiprofen (FLB) for transdermal use to avoid adverse effect associated with oral administration of the drug. Encapsulation of drug in vesicle prolongs the existence of the drug in the systemic circulation and thus enhances penetration into the target site and reduces toxicity. Method: Niosomes were prepared using surfactants (span 40 and span 60) and cholesterol in the molar ratio of 1:1, 2:1, 3:1 and 3:2. Vesicles prepared by thin film hydration method were characterized for morphology, vesicle size and zeta potential, thermal analysis and Entrapment Efficiency (EE). Results: Results revealed that the EE and size of niosomes were influenced by surfactant type and cholesterol ratio. F8 (span 60: cholesterol in 3:2) exhibited the highest encapsulation of FLB (76.77 ± 0.55) with vesicle size of 154 ± 2.96 nm and Polydispersity Index (PDI) of 0.09. The optimized formulation F8 was selected for incorporation into the gel. Niosomal gel was evaluated for homogeneity, pH, spreadability and in-vitro drug release. Conclusion: All the parameters of niosomal gel were found to be satisfactory and in-vitro release study revealed prolonged and complete release of entrapped FLB (93.23±0.65%) in comparison to FLB hydrogel (42.65±0.29%). The results suggested that niosomes may serve as promising vehicles for the transdermal delivery of FLB.

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.

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