Evaluation of precorneal residence time of brimonidine tartrate nanoparticles loaded in situ gel using gamma scintigraphy

2020 ◽  
pp. 1-8
Author(s):  
Pankaj Kumar Sharma ◽  
Nidhi Sandal ◽  
Meenakshi Kanwar Chauhan
Keyword(s):  
Residence Time ◽  
Gamma Scintigraphy ◽  
In Situ Gel ◽  
Brimonidine Tartrate

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 Physiologically active hydrogel (in situ gel) of sparfloxacin and its evaluation for ocular retention using gamma scintigraphy

2015 ◽  
Vol 7 (3) ◽  
pp. 195 ◽  
Author(s):  
Aqil Malik ◽  
RK Khar ◽  
Asgar Ali ◽  
Aseem Bhatnagar ◽  
Gaurav Mittal ◽  
...  
Keyword(s):  
Gamma Scintigraphy ◽  
In Situ Gel ◽  
Ocular Retention

scholarly journals Floating Oral In-Situ Gel: A Review

2019 ◽  
Vol 9 (2) ◽  
pp. 442-448 ◽  
Author(s):  
Rabiah Bashir ◽  
Asmat Majeed ◽  
Tabasum Ali ◽  
Saeema Farooq ◽  
Nisar Ahmad Khan
Keyword(s):  
Drug Delivery ◽  
Residence Time ◽  
Immediate Release ◽  
Oral Route ◽  
Local Effect ◽  
In Situ Gel ◽  
Gastric Residence Time ◽  
Gastric Contents ◽  
Absorption Window

The drugs having a narrow absorption window in the gastrointestinal tract (GIT) when administered by oral route are often limited by poor bioavailability due to incomplete drug release and short residence time at the site of absorption. Novel drug delivery systems in the form of gastroretentive systems such as floating systems, mucoadhesive, high-density, expandable have been developed as they provide controlled delivery of drugs with prolonged gastric residence time. Liquid orals are more prone to low bioavailability because they are eliminated quickly from the stomach since they are subjected to faster transit from the stomach/ duodenum. The problems of immediate release and short gastrointestinal residence of liquids are eliminated by formulating as oral in situ gels as they provide the best means to overcome these problems The in situ gel dosage form is a liquid before administration and after it comes in contact with gastric contents due to one or more mechanisms gets converted to gel which floats on gastric contents. This achieves increased residence as well as sustained release. This approach is useful for systemic as well as local effect of drugs administered. This review gives a brief idea about floating oral in-situ gel formation and research done by various scientists on a number of drugs and polymers. Keywords: Floating drug delivery, gastric retention time, In-situ gel.

scholarly journals Design and Optimization of Thermo-reversible Nasal in situ Gel of Atomoxetine Hydrochloride Using Taguchi Orthogonal Array Design

2019 ◽  
Vol 18 (2) ◽  
pp. 183-193 ◽  
Author(s):  
PK Lakshmi ◽  
K Harini
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Poloxamer 407 ◽  
Release Mechanism ◽  
Gelation Temperature ◽  
In Situ Gel ◽  
Design And Optimization ◽  
Mucoadhesive Polymers ◽  
Carbopol 934P

The present investigation was aimed to develop a thermo-reversible nasal in situ gel of atomoxetine hydrochloride (AH) with reduced nasal muco-ciliary clearance in order to improve residence time and targeting the brain through nasal mucosa for the treatment of attention-deficit hyperactivity disorder (ADHD). In situ gel formulations were prepared using different concentrations of the thermo-gelling poloxamer 407 and mucoadhesive polymers. Temperature-triggered ionic gelation is the mechanism involved. Taguchi L9 OA experimental design was employed for the optimization of the effect of independent variables (Poloxamer 407 and Carbopol 934P) on the response (gelation temperature). In situ gel formulation F4 having 20% poloxamer 407 and 0.3% carbopol 934P and formulation F6 having 20% poloxamer 407 and 0.2% HPMC K100 were optimized based on evaluation parameters. The gelation temperature of F4 and F6 was found to be 37°C ± 0.4 and 37°C ± 0.2, drug content 98.34 and 98.33% and drug release was 83.18, 82.4% in 4 hrs with a flux of 436.9 and 428.1 μg.cm2/hr, respectively. The release pattern of drug followed first-order kinetics with Higuchi release mechanism. The value of ‘n’ from Korsemeyer equation indicated the anomalous diffusional drug release. This study concluded that in situ gel enhanced the nasal residence time and thus may improve the bioavailability of the drug through nasal route by avoiding first pass metabolism Dhaka Univ. J. Pharm. Sci. 18(2): 183-193, 2019 (December)

scholarly journals Micro spect in vivo bio-distribution study of azithromycin ophthalmic in situ gel

2020 ◽  
Vol 11 (3) ◽  
pp. 4546-4554
Author(s):  
Manish Wani ◽  
Swati Jagdale ◽  
Vishal Bhujbal ◽  
Akshay Baheti ◽  
Ashwin Kuchekar
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Polymer Concentration ◽  
Experimental Studies ◽  
Poloxamer 407 ◽  
Gelling Agent ◽  
In Situ Gel ◽  
Biodistribution Studies

Azithromycin (AZT) is a broad-spectrum antibiotic and is found in ocular tissues when administered systemically. AZT inhibits RNA-dependent protein synthesis and hence has effective bactericidal capability against Staphylococcus aureus, Pseudomonas aeruginosa, which are the primary causative organisms for bacterial infection. In situ ophthalmic gels are systems which undergo a sol-to-gel transformation when instilled in eyes. In situ gels overcome the shortcoming of ophthalmic drops as they get washed out and diluted due to tear fluid. The aim and objective of present study was to formulate in situ ophthalmic gelling systems of Azt and determine in vivo ocular residence time in rat eyes of Tc99 labelled Azt by Micro SPECT. The in situ gel was formulated using Poloxamer 407, which is a temperature-induced gelling agent and HPMC K4M, which is known to increases mucosal adhesivity and enhance viscosity to facilitate sustained release of drug. The formulations developed were evaluated for pH, clarity, viscosity, gelling capacity and % drug release. The selected formulation was subjected to isotonicity and In Vivo Bio-distribution studies. Experimental studies on compatibility showed no interaction between polymers and AZT. AZT was found soluble in PB6.8. All formulations were found clear immediately after preparation and after sterilization & pH after gelation was satisfactorily in the range of 6 to 7. Viscosity and Gelation capacity of in situ gel increased with increase in polymer concentration. Formulations F2 showed desired results w.r.t viscosity, gelation capacity, drug release. In Vivo Biodistribution studies of Tc99 labelled AZT by Micro SPECT showed there was a significant increase in ocular residence time of in situ gel when compared with Tc99 labelled marketed solutions.

scholarly journals The Advantages of In situ Gel from Every Different Formulation

2020 ◽  
Vol 11 (4) ◽  
pp. 7198-7206
Author(s):  
Iyan Sopyan ◽  
Wulan Intani ◽  
Insan Sunan K S ◽  
Cikra Ikhda N H S
Keyword(s):  
Phase Transition ◽  
Residence Time ◽  
Google Scholar ◽  
Good Effect ◽  
Gel Formation ◽  
In Situ Gel ◽  
Gelling Agents ◽  
Lengths Of Stay ◽  
Gel Formulations

The in situ gel system is one of the polymer-based solutions that show the sol phase transition to gel. In addition to being used to improve bioavailability, this gel is also used to make the drug increase the residence time in the area of ​​use, so that it can provide maximum effectiveness via enhancing of per cent permeation, The use of in situ gel, usually used in ocular administration of drugs, for the treatment of cancer, administration of drugs in the vaginal, rectal, topical, oral, and any route administration. There are many formulations of in situ gel formation that are used for medicinal preparations for many purposes, with different lengths of stay. Searching for articles is done online, browsing the PubMed and Google scholar site with the keyword "Formulation In situ Gel". The fourty articles used, there were 40 in situ gel formulations with gelling agents and also different uses. The purpose of this article review is to look at the superiority of in situ gel formulations and to compare various in situ gel formulations studied from 40 articles used, so that it can be seen which formulation is most often used and has a good effect on drugs preparations.

Exploring of Taguchi design in optimization of Brinzolamide and Timolol maleate ophthalmic In-situ gel used in treatment of Glaucoma

2019 ◽  
Vol 14 ◽  
Author(s):  
Purvi Shah ◽  
Vaishali Thakkar ◽  
Vishvas Anjana ◽  
Jenee Christiana ◽  
Roma Trivedi ◽  
...  
Keyword(s):  
Patient Compliance ◽  
Residence Time ◽  
Research Work ◽  
Methyl Cellulose ◽  
Taguchi Design ◽  
Fixed Dose ◽  
Timolol Maleate ◽  
In Situ Gel ◽  
Enhanced Solubility

Objective: The present research work focuses on experimental design assisted In-situ gel for fixed dose combination. Significance: Brinzolamide(BZ) BCS class II drug and timolol maleate(TM), a BCS class I drug is formulated for obtaining sustained effect, increased ocular bioavailability and reduction of dose leading to better patient compliance. Methods: The material attributes were gelrite, hydroxy propyl methyl cellulose K4M(HPMC K4M) and HP-β-CD and critical quality attribute identified were gel strength, mucoadhesive index and percent of drug release of both drugs. BZ and TM were successfully formulated in ion-triggered In-situ gelling system using Taguchi design with minimum trials. Results: The final optimized formula 0.5 %w/v gelrite, 0.5 %w/v HPMC K4M, 1:2.5 Ratio of drug to HP-β-CD as well as 150rpm stirring rate exhibited acceptable results with enhanced solubility of BZ. Pharmacodynamic study revealed decrease in intraocular pressure for In-situ gel (17.3) compared to conventional formulation. Moreover, delayed mean residence time and high AUC(61.237 and 4523.65) of In-situ gel indicates prolonged residence time with sustained release. Conclusion: In conclusion, an excellent ocular tolerance and longer action of gelrite and HPMC K4M. In-situ gel for BZ and TM can be explored as potential alternative to marketed formulation reducing frequency of administration and improving patient compliance in glaucoma.

HPLC–MS/MS studies of brimonidine in rabbit aqueous humor by microdialysis

Bioanalysis ◽  
2021 ◽  
Author(s):  
Zhan Tang ◽  
Xiumin Li ◽  
Hongyan Xu ◽  
Saizhen Chen ◽  
Binhui Wang ◽  
...  
Keyword(s):  
Pharmacokinetic Study ◽  
Mobile Phase ◽  
Internal Standard ◽  
In Situ Gel ◽  
Rabbit Eye ◽  
Relative Standard ◽  
Brimonidine Tartrate ◽  
Aqueous Formic Acid ◽  
Good Linear Correlation

Aim: The pharmacokinetic study of the brimonidine tartrate in situ gel in the anterior chamber of the rabbit eye was studied by microdialysis technique, and samples were analyzed by HPLC–MS/MS. Materials & methods: It was monitored in ESI mode at transition 291.9→212.0 and 296.0→216.0 for brimonidine and internal standard, respectively. Acetonitrile and 0.1% aqueous formic acid (50:50, v/v) were used as the mobile phase at 0.4 ml/min. Results & conclusion: It showed a good linear correlation between 5 and 5000 ng/ml in microdialysis solution, and the inter- and intra-day precision (relative standard deviation) was less than 4.0%. The pharmacokinetic study showed that the AUC(0-t) of in situ gel was 3.5-times than that of eyedrops, which significantly improve the bioavailability of brimonidine.

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