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.

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 In Situ Gelling Ophthalmic Drug Delivery System for the Optimization of Diagnostic and Preoperative Mydriasis: In Vitro Drug Release, Cytotoxicity and Mydriasis Pharmacodynamics

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 360
Author(s):  
Pierre-Louis Destruel ◽  
Ni Zeng ◽  
Françoise Brignole-Baudouin ◽  
Sophie Douat ◽  
Johanne Seguin ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Delivery Systems ◽  
Eye Drops ◽  
Active Ingredients ◽  
In Vitro Drug Release ◽  
In Situ Gelling

Mydriasis is required prior to many eye examinations and ophthalmic surgeries. Nowadays, phenylephrine hydrochloride (PHE) and tropicamide (TPC) are extensively used to induce mydriasis. Several pharmaceutic dosage forms of these two active ingredients have been described. However, no optimal therapeutic strategy has reached the market. The present work focuses on the formulation and evaluation of a mucoadhesive ion-activated in situ gelling delivery system based on gellan gum and hydroxyethylcellulose (HEC) for the delivery of phenylephrine and tropicamide. First, in vitro drug release was studied to assess appropriate sustained drug delivery on the ocular surface region. Drug release mechanisms were explored and explained using mathematical modeling. Then, in situ gelling delivery systems were visualized using scanning electron microscopy illustrating the drug release phenomena involved. Afterward, cytotoxicity of the developed formulations was studied and compared with those of commercially available eye drops. Human epithelial corneal cells were used. Finally, mydriasis intensity and kinetic was investigated in vivo. Mydriasis pharmacodynamics was studied by non-invasive optical imaging on vigilant rabbits, allowing eye blinking and nasolacrimal drainage to occur physiologically. In situ gelling delivery systems mydriasis profiles exhibited a significant increase of intensity and duration compared with those of conventional eye drops. Efficient mydriasis was achieved following the administration of a single drop of in situ gel reducing the required amount of administered active ingredients by four- to eight-fold compared with classic eye drop regimen.

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 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 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 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.

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 Evaluation of in situ gel forming system loaded with etoricoxib and herbal adjuvant nanoparticles against human colon cancer cell lines (HT-29)

2020 ◽  
Vol 9 (1) ◽  
pp. 789-795
Keyword(s):  
Drug Release ◽  
Human Colon ◽  
Human Colon Cancer ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Tamarind Seed ◽  
Ht 29

The aim of the research work was to fabricate the nanosuspension of etoricoxib with polyherbal components (extract of ginger root and basil leaf) to enhance the solubility of API; furthermorein situ gel forming system for stomach specific drug delivery was prepared utilizing formulated nanosuspension as base. The objective of the present research is to enhance the solubility of poorly aqueous soluble drug by fabricating nanoparticles and improve their residence time within stomach by formulating in situ gel forming system. Tamarind seed polysaccharide as polymer, etoricoxib as drug, ethanolic extract of ginger (GE) and basil (BE), was used for preparation of nanoparticles.Solvent antisolvent precipitation method was used to prepare nanoparticles. The fabricated nanoparticles were evaluated for various parameters such as physical appearance, Scanning electron microscope, drug content, in-vitro drug release. For preparation of in-situ gel containing nanoparticles, tamarind seed polysaccharides, calcium carbonate and sodium alginate were used. The prepared formulations were evaluated for different characterization parameters such as,- pH, viscosity, floating behaviour, drug content, in-vitro drug release and in-vitro cytotoxic study. The in-situ gel containing nanoparticles were successfully prepared and evaluated. Firstly, the nanoparticles were evaluated for physical appearance, Scanning electron microscope, drug content, in-vitro drug release and found that the formulations were clear as well as homogenous, size of nanoparticles was evaluated in the range of 498nm to 587nm, the drug content of etoricoxib was found in the range of 71.38±0.01 (F5) to 79.45±0.01 (F6), the drug content of GE was found in the range of 69.25±0.05 (F4) to 74.25±0.02 (F1) and the drug content of BE was 69.48±0.09 (F1) to 75.59±0.08 (F6). The drug release was taken up to 12 h and found to be 99%. In-situ gel containing nanoparticles were also evaluated for different parameters such as pH, viscosity, floating behaviour, drug content, and in-vitro drug release. The pH of the prepared formulation was found to be in the range of 7.1±0.04 to 7.5±0.02. The viscosity of the prepared formulation was found in the range of 11.25±0.023 to 12.78 ±0.025. The lag time was found in the range of 11 to 20 sec and floating time was upto 24 h. The drug release was taken up to 8 h and found to be 99±0.2%. It can be concluded that etoricoxib with phytoconstituents (GE and BE) improved its potential to control the growth of human colon cancer cell line (HT-29) in in-vitro conditions. It was concluded from the findings that the in-situ gel containing nanoparticles of etoricoxib from solvent antisolvent method was successfully prepared and found that it has improved the solubility of the poorly soluble drug etoricoxib and dissolution rates.

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.

scholarly journals FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF CIPROFLOXACIN

2019 ◽  
Vol 11 (1) ◽  
pp. 198
Author(s):  
Shailaja Pashikanti ◽  
Jyothsna B.
Keyword(s):  
Calcium Carbonate ◽  
Drug Release ◽  
Sodium Alginate ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Degradable Polymer ◽  
Gel Formulations

Objective: The objective of the study was to develop floating in situ gel formulations of Ciprofloxacin that has a narrow absorption window and mainly absorbed in the proximal areas of GIT. These formulations increases the targeted action on bacteria for a longer time that can be used in the treatment of Helicobacter pylori (H. pylori) infections and urinary tract infections.Methods: In situ gel formulations were prepared by varying concentrations of sodium alginate as in situ gel forming bio-degradable polymer and calcium carbonate as a cross-linking agent. The formulations were evaluated for Physical appearance, pH, in vitro drug release, viscosity, in vitro floating behaviour, in vitro gelling capacity and drug content. FTIR was conducted for Ciprofloxacin, excipients used and optimized formulation.Results: All the formulations showed an optimum viscosity that will allow ease of administration and swallowing. Floating lag time of all formulations was between 32-70 seconds and floated for>12 h. The in vitro gelling capacity increased with increasing the polymer and gelling agent concentrations. Increase in polymer concentration decreased the rate and extent of the drug release. Among all the formulations, F4 containing 4% w/v of sodium alginate and 4% w/v of calcium carbonate showed sustained in vitro drug release (95.6%) over an extended period of 12 h. FTIR studies revealed no interaction between drug and excipients used. Drug release from the formulations followed First order kinetics with Fickian diffusion.Conclusion: Ciprofloxacin was successfully formulated as a pH-triggered floating in situ gelling system using sodium alginate.

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