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 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. 

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 IN-SITU GEL CONTAINING LINEZOLID IN THE TREATMENT OF PERIODONTITIS

2021 ◽  
pp. 79-86
Author(s):  
INAYATHULLA . ◽  
PRAKASH GOUDANAVAR ◽  
MOHAMMAD ALI ◽  
SHAHID UD DIN WANI ◽  
NAGARAJA SREEHARSHA
Keyword(s):  
Drug Release ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
In Situ Gel ◽  
Diffusion Controlled ◽  
Gelling Time ◽  
Carbopol 934P

Objective: The intent to prepare and evaluate Linezolid in-situ gel in the treatment of periodontitis. Methods: pH-sensitive in-situ gel was formed by the cold method using a varying concentration of the drug, carbopol 934P and hydroxypropyl methylcellulose (HPMC) and carbopol 934P and sodium carboxy methylcellulose (CMC) (1:1,1:1.5,1:2,1:2.5). An optimized batch was selected based on gelling time and gelling capacity. The prepared in-situ gels were evaluated for appearance, pH, gelling capacity, viscosity, in vitro release studies, rheological studies, and finally, was subjected to drug content estimation and antibacterial activity test. Results: FTIR study shows drug and physical mixture were compatible with each other. The rheology of formulated in-situ gel exhibited a pseudoplastic flow pattern. this may be because when polymer concentration was increased the prepared formulations become more viscous and in turn delayed the drug release and from the prepared formulation, LF4 and SF4 have polymer concentrations i. e, 0.9% carbopol and sodium CMC showed drug release up to 12 h. Conclusion: When carbopol is appropriately mixed with other suitable polymers it forms an in-situ gel-forming system that was substantiated by the property to transform into stiff gels when the pH is increased. The in-situ gel was prepared using a combination of carbopol-HPMC and carbopol-Na CMC The formulations LF1 to SF4 showed high linearity (R2 = 0.490-0.682), indicating that the drug was released from the prepared in-situ gel by the diffusion-controlled mechanism. Thus, the formulation of batches LF4 and SF4 containing carbopol: HPMC and carbopol: NaCMC in 1:2 ratios were considered as optimum formulation based on optimum viscosity, gelling capacity and to extend the in vitro drug release.

scholarly journals IN VITRO DRUG RELEASE STUDY OF CHLORAMPHENICOL IN SITU GEL WITH BASES MIXTURE OF POLOXAMER 407 AND HPMC BY OPTIMIZATION WITH FACTORIAL DESIGN

2021 ◽  
pp. 116-123
Author(s):  
INSAN SUNAN KURNIAWANSYAH ◽  
TAOFIK RUSDIANA ◽  
HURIYATUS TSANIYAH ◽  
HANDRIAN RAMOKO ◽  
HABIBAH A. WAHAB ◽  
...  
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
In Situ Gel ◽  
Vitro Assay ◽  
Cumulative Amount

Objective: The objective of this study was to find the best base mixture composition (poloxamer 407 and HPMC) of chloramphenicol in situ gel formula based on in vitro property (Cumulative amount of drug release). Methods: The in vitro diffusion of chloramphenicol in situ gel study was carried out using franz diffusion cells to know the effect of the Critical Process Parameters (CPPs) as independent variables (poloxamer 407 and hydroxypropyl methylcellulose (HPMC)) on the Critical Quality Attribute (CQA) as dependent variable (cumulative amount of drug release) with 22 factorial design. Results: 22 factorial design of chloramphenicol in situ gel yielded 4 variations of poloxamer 407 and HPMC bases component in %w/v as follows, F1 (5:0.45), F2 (10:0.45) F3 (5:1) and F4 (10:1). The amount of drug release results from in vitro dissolution assay were 30.60% (F1), 45.64% (F2), 58.30% (F3), and 22.50%) (F4). Conclusion: Formula 3 (F3) was considered as the best formula component in terms of in vitro assay of chloramphenicol in situ gel with a desirability value of 0.58.

Sustained ophthalmic delivery of pH triggered Cromolyn sodium in situ gel

2021 ◽  
pp. 6211-6215
Author(s):  
S. Subramanian ◽  
B. Prasanth
Keyword(s):  
Drug Release ◽  
Cromolyn Sodium ◽  
Fickian Diffusion ◽  
Molar Ratio ◽  
Eye Drops ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
In Situ Gelling

The research study intends to formulate pH triggered in situ gel of Cromolyn sodium composed of Polyacrylic acid (carbopol 934) polymer in combination with Hydroxypropyl Methylcellulose (HPMC K4M) polymer at 1:1, 1.5:1, 2:1 molar ratio by utilizing pH trigger method. Formulations were evaluated for pH, viscosity, gelling capacity, drug content and in vitro drug release. Results of Carbopol 934 and HPMC K4M based in situ gelling systems at 1:1, 1.5:1, 2:1 shown that the formulations were fluid state at room temperature in a formulated pH (pH 4.5) and went through fast progress into the viscous gel phase at the pH of the tear fluid 7.4. The viscosity of formulated pH triggered in situ gel at 2:1 molar ratio shown excellent result compares to 1:1, 1.5:1 molar ratio. The in vitro drug release of the developed in situ gelling formulations at 1:1, 1.5:1, 2:1 molar ratios increases the contact time and showed a non – fickian diffusion type of release behavior with 94.45%, 83.26%, 70.48% respectively over 8 hours periods compared with that of marketed formulation that shows 99.4% over 4 hours. Thus, the developed system at 2:1 molar ratio acts as a viable alternative to conventional eye drops and also prevent the rapid drainage.

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.

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.

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.

scholarly journals Formulation and investigation of crushed puffed rice-chitosan-HPMC based polymeric blends as carrier for sustained stomach specific drug delivery of piroxicam using 3(2) Taguchi mathematical design studies

2018 ◽  
Vol 6 (11) ◽  
pp. 61-80 ◽  
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Pharmaceutical Journal ◽  
Weight Variation ◽  
Zero Order Release ◽  
Puffed Rice

In the present experimental investigation an attempt has been made to assess the utility of Crushed Puffed Rice (CPR)-High Molecular Weight Chitosan (HMWCH)-Hydroxypropyl Methylcellulose K15M (HPMC K15M) as a polymeric carrier for the sustained stomach delivery of Piroxicam (PRX). A total of nine formulations were prepared by using 3 (2) Taguchi factorial design, physically blending drug and polymer(s) followed by encapsulation into hard gelatin capsules size 1. The prepared capsules were evaluated for various performance such as weight variation, drug contents, in vitro buoyancy and drug release in 0.1 M HCl. The effect of drug loading on in vitro performance of the formulations was also determined. Crushed puffed rice (CPR) remained buoyant for up to average time span of 06 hr as an unwetted irregular mass in 0.1 M HCl. However, when combined with HMWCH or HPMC K15M or HPMC K15M + HMWCH a low -density cylindrical raft type hydrogel was formed which remained buoyant for up to 12 hr and released up to 99% drug in a sustained manner from 8 to 12 hr following zero order release kinetics. It was also observed that drug release from drug + CPR matrices followed Fickian mechanism. Combination of CPR + HMWCH or HMWCH + HPMC K15M also follows Fickian mechanism. Obtained data from the research work suggests that CPR in combination with HMWCH or HPMC K15M or HPMC has sufficient potential to be used as a carrier for stomach specific delivery of gastric irritant drug like PRX.Soni et al., International Current Pharmaceutical Journal, April 2018, 6(11): 61-80http://www.icpjonline.com/documents/Vol6Issue11/01.pdf

Sign in / Sign up

Export Citation Format

Share Document