scholarly journals Formulation and Evaluation of Microemulsion Based in Situ Gel of Acyclovir for Vaginal Delivery

2020 ◽  
Vol 11 (4) ◽  
pp. 6336-6346
Author(s):  
Sanjeevani Shekhar Deshkar ◽  
Rutuja Prakash Bokare ◽  
Suhas Ashok Todmal
Keyword(s):  
Drug Release ◽  
Vaginal Delivery ◽  
Release Kinetics ◽  
Stability Study ◽  
Vaginal Tissue ◽  
Polyethylene Glycol 400 ◽  
In Situ Gel ◽  
Gelling Temperature

The purpose of the present study was to formulate and evaluate microemulsion based in situ gel of Acyclovir (ACV) for the vaginal delivery. The solubility of ACV in oils and surfactants and co-surfactant was evaluated to identify the components of the microemulsion. Microemulsion region was determined by using the pseudo-ternary phase diagrams for different formulations. Microemulsion formulation was prepared using Labrafil M1994C as oil phase, Cremophor RH40 as surfactant and Polyethylene glycol 400 and Transcutol P as co-surfactant and water. Microemulsion formulations were evaluated for pH, viscosity, conductivity and stability study. In situ gel of ACV, microemulsion was prepared using thermosensitive polymer, poloxamer.In situ gelwas characterized for viscosity, gelling temperature, the effect of dilution on gelling temperature, gelling ability, and in vitro drug release and release kinetics. The globule size of developed microemulsion was less than 100 nm with PDI in the range 0.307 to 0.641. The optimized microemulsion based in situ gel demonstrated shear thinning behaviour, the gelation temperature with and without dilution was in the range of 30-35ºC, and the drug release was sustained over eight hours. Mucoadhesive properties of microemulsion based in situ gel formulations were determined with a texture analyzer using a goat vaginal tissue, and the results indicated that the presence of microemulsion increased the mucoadhesion significantly. Microemulsion based in situ gel was successfully developed for vaginal delivery of Acyclovir.

Design, Development and Evaluation of Dexamethasone Sodium Phosphate Niosomal in-situ Gel for Visual Medication Conveyance

2018 ◽  
Vol 11 (5) ◽  
pp. 4274-4279
Author(s):  
Vipul P Patel ◽  
V. V Pande ◽  
Khedkar P. V.
Keyword(s):  
Drug Release ◽  
Sodium Phosphate ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Injection Technique ◽  
Eye Drops ◽  
In Situ Gel ◽  
Dexamethasone Sodium Phosphate

The main purpose of this study was to beat issues related with lachrymal seepage by eye drops, obscured vision with semi solid formulation, distinctive framework was joined together as niosomes and in-situ gel by fusing niosomes in-situ gel formulation, so it is anything but difficult to controlled and hold at the site for drag out timeframe. The Dexamethasone sodium phosphate, a glucocorticosteroid anti-inflammatory drug utilized as a part of treatment of eye hypersensitive condition, keratitis, after eye surgery, post cataract treatment. Niosomes containing Dexamethasone sodium phosphate definitions were prepared by solvent injection technique using cholesterol alongside different surfactants proportions. Prepared Niosomal preparations were fused in-situ gel formulation plan by scattering the Niosomes in solution of carbomer 974 P (0.2-0.6% w/v) and Hydroxypropyl-methylcellulose (HPMC) K4M (0.5-0.8% w/v). Prepared formulations were assessed for their vesicle measure, entanglement proficiency, in-vitro sedate discharge, thickness, in-vitro gelation study and so on. From the results it can be concluded that by utilizing cholesterol: Tween-80 (1:2) proportion, particle size of Niosomes was B4 was 368.7 nm with 93.15% drug entrapment efficiency. In-vitro drug release kinetics from Niosomal in-situ gel definition demonstrates that 98.42% drug release in 6 hrs with the utilization of 0.8% w/v of HPMC K4M and 0.6% w/v of Carbomer 974 P. In conclusion, the Niosomal in-situ gel is a practical contrasting option to routine eye drops due to excellence of its capacity to improve bioavailability through its more drawn out residence time and capacity to sustain the drug release.  

scholarly journals DESIGN AND EVALUATION OF MODIFIED CHITOSAN BASED IN SITU GEL FOR OCULAR DRUG DELIVERY

2017 ◽  
Vol 9 (10) ◽  
pp. 87 ◽  
Author(s):  
Anuja T. Kadam ◽  
Rahul L. Jadhav ◽  
Pradnya B. Salunke ◽  
Satwashila S, Kadam
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Phase Change Temperature ◽  
Modified Chitosan ◽  
Drug Content ◽  
Change Temperature

Objective: The object of the present study was to formulate and evaluate in-situ gel of modified chitosan by using temperature triggered method to improve bioavailability.Methods: Modified chitosan-based moxifloxacin HCl was prepared by cold method. polaxomer 407 adding in distilled water and this solution kept in the refrigerator. Modified chitosan and moxifloxacin HCl was dissolved separately in distilled water and added to the polymeric solution with continuous stirring until thoroughly mixed. Prepared formulation was evaluated for drug content, gelling capacity, rheological study, in vitro drug release behavior, measurement of phase change temperature, antibacterial study, release kinetics, statistical analysis.Results: The prepared formulations were evaluated for their, drug content, gelation temperature, in vitro drug release studies, rheological study and release kinetics. All batches of in situ formulations had satisfactory pH ranging from 6.2±0.2, drug content between 98.8±0.2 showing uniform distribution of drug. As the concentration of each polymeric component was increased, there was a decrease in phase change temperature. The in vitro drug release decreased with increase in polymeric concentrations. The antibacterial efficiency of the selected formulation against staphylococcus aureus confirmed that designed formulation has prolonged effect and retained its properties against bacterial infection.Conclusion: The prepared in situ gelling formulation had the appropriate combination of polaxomer 407 and modified chitosan were suitable satisfactorily sustained the drug release from moxifloxacin HCl in situ gel. The prepared formulation of moxifloxacin HCl appears to be promising drug delivery for bacterial infectious disease.

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 DEVELOPMENT AND CHARACTERIZATION OF IN SITU GEL OF XANTHAN GUM FOR OPHTHALMIC FORMULATION CONTAINING BRIMONIDINE TARTRATE

2018 ◽  
Vol 11 (7) ◽  
pp. 277 ◽  
Author(s):  
Vazir Ashfaq Ahmed ◽  
Divakar Goli
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Gelation Time ◽  
Gel Strength ◽  
Eye Drops ◽  
In Situ Gel ◽  
23 Factorial Design ◽  
Brimonidine Tartrate

Objective: The goal of this study was to develop and characterize an ion-activated in situ gel-forming brimonidine tartrate, solution eye drops containing xanthan gum as a mucoadhesive polymer.Method: Sol-gel formulation was prepared using gellan gum as an ion-activated gel-forming polymer, xanthan gum as mucoadhesive agent, and hydroxypropyl methyl cellulose (HPMC E50LV) as release retardant polymer. Phenylethyl alcohol is used as preservatives in borate buffer. The 23 factorial design was employed to optimize the formulation considering the concentration of gelrite, xanthan gum and HPMC as independent variables, gelation time, gel strength, and mucoadhesive force (N). Gelation time , gel strength, mucoadhesive force (N), viscosity (cP) and in vitro percentage drug release were chosen as dependent variables. The formulation was characteristics for pH, clarity, isotonicity, sterility, rheological behavior, and in vitro drug release, ocular irritation, and ocular visualization.Result: Based on desirability index of responses, the formulation containing a concentration of gelrite (0.4%), xanthan gum (0.21%), and HPMC (HPMC E50 (0.24%) was found to be the optimized formulation concentration developed by 23 factorial design. The solution eye drops resulted in an in situ phase change to gel-state when mixed with simulated tear fluid. The gel formation was also confirmed by viscoelastic measurements. Drug release from the gel followed non-fickian mechanism with 88% of drug released in 10 h, thus increased the residence time of the drug.Conclusion: An in situ gelling system is a valuable alternative to the conventional system with added benefits of sustained drug release which may ultimately result in improved patient compliance.

scholarly journals IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM

2018 ◽  
Vol 10 (5) ◽  
pp. 76
Author(s):  
Methaq Hamad Sabar ◽  
Iman Sabah Jaafar ◽  
Masar Basim Mohsin Mohamed
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
High Viscosity ◽  
In Situ Gel ◽  
Alginate Concentration

Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).Conclusion: This study showed the formulation of Na alginate with GG and CaCO3, led to gain floating in situ gel and a sustained release of keto. 

scholarly journals FORMULATION, OPTIMIZATION, AND EVALUATION OF IN-SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE FOR OPHTHALMIC DRUG DELIVERY

2019 ◽  
pp. 147-158
Author(s):  
Chitra Gupta ◽  
VIJAY JUYAL ◽  
Upendra Nagaich
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Influential Factors ◽  
Drug Formulation ◽  
In Situ Gel ◽  
Formulation Optimization ◽  
Ophthalmic Drug Delivery ◽  
Ophthalmic Drug

Objective: The present study emphasizes the synthesis, optimization, and evaluation of ocular in-situ gel for ophthalmic drug delivery against conjunctivitis. Methods: Pre-formulation studies on the drug and polymers were carried out, which included the study of various physicochemical properties of the drug and drug-polymer compatibility studies. The 12 different formulations were further pre-optimised by Taguchi method for determining the number of influential factors. Furthermore, the formulation optimization was done by using ‘Box–Behnken’ design (BBD) (Design expert 10 software) for assessing the effect of formulation variables on product characteristics viz. viscosity, gelation temperature (GT), and mean release time (MRT). About 13 suggested runs of the experiment were carried out and formulations were optimised. Finally, three batches of the optimised formulation were prepared and evaluated for in vitro drug release, isotonicity of formulation, anti-microbial potential, ocular irritancy, and accelerated stability testing. Results: Pre-formulation study confirmed the purity, solubility, and compatibility of drug measured by λmax, partition coefficient, stability study, and Fourier-transform infrared spectroscopy (FTIR) analysis. Taguchi screening method suggested about 12 different formulations and 3 most prominent influential factors including viscosity, GT, and drug release. 13 different formulations designed based on ‘BBD’ method were further optimised by considering the most influential factors suggested by Taguchi screening. The in vitro evaluation of the optimised formulation gave satisfactory results in terms of drug release, and anti-microbial activity. It was found to be isotonic with no ocular irritancy. Further, the preparation immediately transformed from sol to gel upon administration into cul-de-sac region of the eye due to multi-dimensional approaches utilised for in-situ gel formation namely temperature change Pluronic, ion sensitivity due to Gellan-gum, pH sensitivity because of Carbopol. Conclusion: The optimised in-situ gelling ocular drug formulation showed promising potency for ophthalmic drug delivery with no irritancy due to the multifactorial mechanism.

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

Fabrication and Characterization of Ocular Phase Transition Systems for Blepharitis: A Novel Approach

2020 ◽  
Vol 10 (1) ◽  
pp. 24-37
Author(s):  
Deepali Verma ◽  
Shreya Kaul ◽  
Neha Jain ◽  
Upendra Nagaich
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Eye Drops ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Erythromycin Estolate

Introduction: In the present research, erythromycin estolate loaded in-situ gel was formulated and evaluated for blepharitis in order to improve its therapeutic efficacy, precorneal residence time of the system and to enhance the ocular bioavailability. Material and Methods: The developed formulation was characterized by several parameters viz. FTIR, clarity, pH, gelation temperature, rheological studies, drug content, in vitro drug release studies, transcorneal permeation studies, bioadhesion studies, isotonicity and stability studies. Results: The optimized formulation exhibited non-fickian release diffusion with a sustained release of drug 82.76 ± 0.94% up to 8h and drug content 93.64%. Isotonicity revealed that the formulation was isotonic in nature and there was no shrinkage and busting of cells. Bioadhesion study was performed to check the adherence of the prepared in situ gel to the corneal surface for 4h. Ex vivo transcorneal permeation was observed to be significantly higher when compared with market eye drops. Histopathological studies were conducted to confirm the presence of normal ocular surface tissues by maintaining their morphological structures without causing damage to the tissues. The formulation was nonirritant as confirmed by the HET-CAM test. Stability studies and accelerated stability studies were conducted for 13 weeks and 26 weeks respectively and formulations were analyzed for the visual appearance, pH, viscosity, gelling capacity, drug content and in vitro drug release and results showed no change in the formulations. Conclusion: The formulation was therapeutically efficacious, sterile, stable and provided controlled release over a period of time. The developed system could be a viable alternative to conventional eye drops for treatment of various ocular diseases.

scholarly journals FORMULATION AND EVALUATION OF NOVEL IN SITU GEL OF LAFUTIDINE FOR GASTRO RETENTIVE DRUG DELIVERY

2018 ◽  
Vol 11 (8) ◽  
pp. 88
Author(s):  
Sindhoor S M ◽  
Sneh Priya ◽  
Amala Maxwell
Keyword(s):  
Drug Release ◽  
Imaging Study ◽  
Lag Time ◽  
In Vivo Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content

Objective: The aim of the present study was to formulate and evaluate the novel in situ gel of lafutidine for gastroretentive drug deliveryMethods: A gastroretentive in situ gel of lafutidine was formulated by pH-triggered ionic gelation method using different concentrations of gelling polymer such as sodium alginate, gellan gum, and xanthum gum. Prepared formulations were evaluated for viscosity, density, buoyancy lag time and buoyancy duration, and drug content. In vitro drug release studies of all formulations were also performed. In vivo fluorescence imaging study was conducted for optimized formulation and compared with control.Results: The concentration of gelling agents and release retardant polymers significantly affected viscosity, floating behavior, and in vitro drug release of the formulations. The pH and drug content were found in the range of 6.72–7.20 and 88.74–95.33%, respectively. Floating lag time was <2 min; duration of floating was more than 12 h. Minimum and maximum in vitro drug release were found to be for formulation F9 (51.74%) and F1 (82.76%), respectively, at the end of 12 h. The drug was released from the all the formulations in a sustained manner. In vivo studies confirmed the gastroretention of the formulation in mice stomach for 8 h. Stability studies indicated that the there was no significant change in the visual appearance, floating behavior, and drug content.Conclusion: The gastroretentive in situ gel system, prolonged the gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract.

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.

Sign in / Sign up

Export Citation Format

Share Document