scholarly journals Development and characterization of thermosensitive pluronic-based metronidazole in situ gelling formulations for vaginal application

2012 ◽  
Vol 62 (1) ◽  
pp. 59-70 ◽  
Author(s):  
El-Sayed Ibrahim ◽  
Sayed Ismail ◽  
Gihan Fetih ◽  
Omar Shaaban ◽  
Khaled Hassanein ◽  
...  
Keyword(s):  
Drug Release ◽  
Histopathological Examination ◽  
Vaginal Mucosa ◽  
Gelation Temperature ◽  
Acceptable Range ◽  
In Situ Gelling ◽  
Gel Formulations

Development and characterization of thermosensitive pluronic-based metronidazolein situgelling formulations for vaginal applicationThe purpose of this study was to develop pluronic-basedin situgelling formulations of metronidazole (MTZ) for treatment of bacterial vaginosis, aimed at prolonging the residence time, controlling drug release, enhancing efficacy, decreasing recurrence, and increasing patient compliance. Thein situgel formulations were prepared using different concentrations of pluronic F-127 (PF-127) alone and in combination with pluronic F-68 (PF-68). The prepared formulations were evaluated for their gelation temperature (Tgel),in vitrodrug release, rheological properties, mucoadhesion properties and tolerability by vaginal mucosa in tissue levels. TheTgeldecreased with increasing PF-127 concentration. TheTgelwas modulated by addition of PF-68 to be within the acceptable range of 25-37 °C. With increasing pluronic concentration, thein vitrodrug release decreased, viscosity and mucoadhesive force increased. Histopathological examination of rabbit vaginas from the control and treated groups revealed normal histology of the vagina and cervix. Based on thein vitroevaluation of prepared formulations, thein situgelling liquid formulated with PF-127/PF-68 (20/10 %,m/m) was selected for further clinical evaluation.

scholarly journals DEVELOPMENT AND EVALUATION OF AN IN SITU THERMOGELLING SYSTEM OF OFLOXACIN FOR CONTROLLED OCULAR DELIVERY

2019 ◽  
pp. 567-570 ◽  
Author(s):  
ANANTH PRABHU ◽  
MARINA KOLAND
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Poloxamer 407 ◽  
Temperature Sensitive ◽  
Gelation Temperature ◽  
Mucoadhesive Polymers ◽  
In Situ Gelling

Objective: The purpose of this study was to develop an in situ ocular gel of ofloxacin which aimed to prolong corneal residence time while controlling drug release. Method: In situ gelling solutions were prepared from Poloxamer 407, a temperature-sensitive gelling polymer and to which, mucoadhesive polymers such as hydroxypropyl methyl cellulose 15 cps and polyvinyl alcohol (PVA) were included to provide corneal adhesion. Drug incorporated gels were prepared and evaluated for their appearance, pH, gelation temperature, and in vitro drug release studies. Results: Incorporation of the drug into the formulation increased the gelation temperature while the addition of mucoadhesive polymers decreased the gelation temperature. Increasing the concentration of bio-adhesive polymers retarded the release of ofloxacin from the poloxamer solutions and drug release was sustained over a period of 9 h. PVA had no significant effect on the gelation temperature and could not sustain the drug release for a longer duration. The in vitro release profiles of the drug from all the formulations could be best expressed by Higuchi’s equation which indicated that gels followed matrix diffusion process and drug release from gel formulations followed first-order process. Conclusion: The results showed that the developed system would be promising in the treatment of ocular infections with the combined advantages of ease of administration, the accuracy of dosing, increased bioavailability, and prolonged retention time.

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.

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 Formulation and Evaluation of Meloxicam In-Situ Gel Designed for Sustained Drug Release to Reduce Dosing Frequency in the Management of Arthritis

2021 ◽  
Vol 69 (2) ◽  
Author(s):  
Meesala. Srinivasa Rao ◽  
M. S Chandra Goud ◽  
C. V. Reddy
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Dosing Frequency ◽  
Gel Formulations

Meloxicam has short biological half-life and is rapidly eliminated, frequent oral administration is necessary to maintain its therapeutic concentration, but this can increase chances of missing dose. This makes Meloxicam a good applicant for oral sustained release formulation. The objective of study was to develop in-situ gel formulations of Meloxicam for sustained release to reduce the dosing frequency in the treatment of rheumatoid arthritis. Method of Ion sensitive in-situ gelation was used in this study. Meloxicam In-situ gel formulations were prepared by varying concentrations of sodium alginate as a bio-degradable gel forming polymer, CaCl2 as a cross-linking agent and Chitosan/ HPMCK4/HPMCK15/Guar gum/Gellan gum/ Xantha gum/pectin were used as drug release rate controlling polymers. The formulations F11-F18 were assessed for Physical appearance, pH, in-vitro drug release, viscosity, in-vitro gelling capacity and drug content. FTIR, DSC and in-vivo drug kinetics studies was conducted for Meloxicam, excipients used and optimized formulation. Formulations showed an optimum viscosity that will allow ease of administration and swallowing. All formulations are shown pH between4.7-4.9, floating lag time was 2-3sec and floated for >12 hrs. In vitro drug release studies reporting that commercially available product Meloxicam SR has showed 99.92% drug release in 8 hrs and out of eight formulations F11 showing in-vitro drug release of 99.52% over a 12hrs extended period. FTIR studies revealed no interaction between drug and excipients used. The results of In-vivo kinetic studies are approving the better performance of the optimized formulation in comparison to marketed formulation, The Cmax, Tmax, half-life AUC values are confirming the same thing. In conclusion, Formulation (F11) was selected as optimized formulations could be offered as shows optimum sustained drug release compared to commercial formulation. Hence Meloxicam containing Chitosan as drug release controll

In-Situ Gelling System based on Thiolated Gellan Gum as New Carrier for Nasal Administration of Dimenhydrinate

2009 ◽  
Vol 2 (2) ◽  
pp. 544-550
Author(s):  
Hitendra Mahajan ◽  
Hannan Shaikh ◽  
Surendra Gattani ◽  
Pankaj Nerkar
Keyword(s):  
Nasal Mucosa ◽  
Histopathological Examination ◽  
Polymer Concentration ◽  
Gellan Gum ◽  
Nasal Administration ◽  
In Vitro Permeation ◽  
Permeation Studies ◽  
In Situ Gelling

The purpose of the present study was to develop intranasal delivery system of dimenhydrinate using thiolated gellan gum and formulations were modulated so as to have gelation at physiological ion content after intranasal administration.  Gelation was determined by physical appearance.  The mucoadhesive force in terms of detachment stress, determined using sheep nasal mucosa, increased with increasing concentration of thiolated polymer. The results of in vitro drug permeation studies across sheep nasal mucosa indicate that effective permeation could be significantly increased by using in situ gelling formulation with thiolated polymer concentration.  Finally, histopathological examination did not detect any changes during in vitro permeation studies.  In conclusion the gel formulation of dimenhydrinate with in situ gelling and mucoadhesive properties with increased permeation rate is promising for prolonging nasal residence time and thereby nasal absorption.

In vitro and In vivo Characterization of Pectin Based In situ Gelling System of Famotidine

2013 ◽  
Vol 5 (4) ◽  
pp. 1885-1894
Author(s):  
Mohmadmoin K. Modasiya ◽  
A K Patel ◽  
V.M Patel ◽  
G.C Patel
Keyword(s):  
Drug Release ◽  
Calcium Chloride ◽  
Fickian Diffusion ◽  
Similarity Factor ◽  
Drug Content ◽  
Model Drug ◽  
In Situ Gelling

In this study famotidine was used as a model drug to formulate and evaluate pH-induced in situ gelling system for oral sustained release drug delivery in stomach which has shorter biological half-life. To study the effect of independent variables 32 full factorial design was employed, concentration of pectin as pH dependant polymer and concentration of calcium chloride on dependent variables like viscosity, drug content, 50% and 80% drug release and similarity factor. It was found that both the concentration of pectin and concentration of calcium chloride had significant effect on viscosity, drug content, 50% and 80% drug release and similarity factor of the system. In vitro drug release study showed that drug released from the in situ gel followed non-Fickian diffusion. Mathematical modeling was employed for quantitative evaluation of the effect of formulation variables. Rat pylorus legation model was used for in vivo study of the selected formulation. Results shows gel formation in gastric juice and reduction in ulcer index. There were few or no major changes in the formulation during three months stability testing. The in situ gelling systems are useful for delivery of famotidine.

THERMOREVERSIBLE, MUCOADHESIVE IN SITU GELLING FORMULATIONS FOR NASAL DELIVERY OF PROPRANOLOL HYDROCHLORIDE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (09) ◽  
pp. 41-51
Author(s):  
R Bhat ◽  
◽  
Z. Abbas ◽  
N.G.N. Swamy
Keyword(s):  
Nasal Delivery ◽  
Propranolol Hydrochloride ◽  
Gelation Temperature ◽  
Enhanced Absorption ◽  
Diffusion Controlled ◽  
Thixotropic Behaviour ◽  
In Situ Gelling ◽  
Carbopol 934P

Mucoadhesive, thermoreversible propranolol hydrochloride formulations were made to overcome firstpass metabolism, to prolong the drug residence time in the nasal cavity and to improve the therapeutic efficacy. In situ gelling formulations were prepared by cold technique using Pluronic F-127, Pluronic F-68 / Polyvinyl Alcohol complex and Carbopol 934P as the mucoadhesive polymer. Formulations were so modulated as to have gelation temperature below 340C to ensure gelation at the physiological temperature after intranasal administration. Gelation was characterized by physical appearance as well as by rheological evaluation. The gelation temperature decreased with increase in Carbopol concentration, whereas mucoadhesive force increased. The formulations displayed a thixotropic behaviour. The pH of the nasal gels was found to be in the range of 5.3 to 5.6 very much ideal for nasal delivery. The results of in vitro drug diffusion studies across the sheep nasal mucosa indicated that the drug release increased with increase in Carbopol concentration. The release was found to be matrix diffusion controlled and occurred by Fickian mechanism. It could be concluded that, the mucoadhesive, in situ gelling formulations of propranolol hydrochloride proved to be physically stable, convenient, effective nasal delivery systems ensuring prolonged nasal residence and assuring enhanced absorption.

scholarly journals Formulation and Evaluation of Floating Oral In Situ Gelling System of Amoxicillin

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Dasharath M. Patel ◽  
Divyesh K. Patel ◽  
Chhagan N. Patel
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Lag Time ◽  
Solution Viscosity ◽  
High Dose ◽  
In Situ Gelling

Purpose. Effective Helicobacter pylori eradication requires delivery of the antibiotic locally in the stomach. High dose of amoxicillin (750 to 1000 mg) is difficult to incorporate in floating tablets but can easily be given in liquid dosage form. Keeping the above facts in mind, we made an attempt to develop a new floating in situ gelling system of amoxicillin with increased residence time using sodium alginate as gelling polymer to eradicate H. pylori. Methods. Floating in situ gelling formulations were prepared using sodium alginate, calcium chloride, sodium citrate, hydroxypropyl methyl cellulose K100, and sodium bicarbonate. The prepared formulations were evaluated for solution viscosity, floating lag time, total floating time, and in vitro drug release. The formulation was optimized using a 32 full factorial design. Dissolution data were fitted to various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. Results. All formulations (F1–F9) showed floating within 30 s and had total floating time of more than 24 h. All the formulations showed good pourability. It was observed that concentration of sodium alginate and HPMC K100 had significant influence on floating lag time, cumulative percentage drug release in 6 h and 10 h. The batch F8 was considered optimum since it showed more similarity in drug release () to the theoretical release profile. Conclusion. Floating in situ gelling system of amoxicillin can be formulated using sodium alginate as a gelling polymer to sustain the drug release for 10 to 12 h with zero-order release kinetics.

scholarly journals Formulation and Evaluation of Sustained Release Sumatriptan Mucoadhesive Intranasal in-Situ Gel

2019 ◽  
Vol 28 (2) ◽  
pp. 95-104
Author(s):  
Hussein K. Alkufi ◽  
Hanan J. Kassab
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Poloxamer 407 ◽  
Gelation Temperature ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Ex Vivo Permeation ◽  
Ex Vivo Permeation Study

     Objective: The purpose of this study to develop and optimize nasal mucoadhesive in situ gel IG of sumatriptan ST (serotonin agonist) to enhance nasal residence time for migraine management.      Method: Cold method was used to prepare ST nasal in-situ gel, using thermosensitive polymers (poloxamer 407  and/or poloxamer 188) with a mucoadhesive polymer (hyaluronic acid HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, mucoadhesive force determination, viscosity,  in-vitro drug release, and the selected formula was subjected to ex-vivo permeation study and histological evaluation of the sheep mucosal tissue after application.     Results: The results showed that the formula IG7 prepared from poloxamer 407(19%), poloxamer188 (4%) and HA (0.5%)   had an optimum gelation temperature (32.66±1.52°C), gel  strength (43.66± 1.52 sec),  mucoadhesive force (8067.93± 746.45dyne\cm2), in-vitro drug release (95.98%) over 6hr, ex-vivo permeation study release (89.6%)  during the 6 h. study with no  histological or pathological change in the nasal sheep tissue.     Conclusion: The ease of administration via a nasal drop of ST coupled with less frequent administration and prolong drug release, will enhance patient compliance.

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