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

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 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.

scholarly journals Utilization of Poloxamer as Well as Combinations with Other Polymers as Base in Ophthalmic in Situ Gel Dosage Form

2020 ◽  
Vol 10 (01) ◽  
pp. 101-105
Author(s):  
Insan Sunan Kurniawansyah ◽  
Taofik Rusdiana ◽  
Iyan Sopyan ◽  
Anas Subarnas ◽  
Habibah A. Wahab
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Rabbit Eye ◽  
Release Drug

The aim of this review was to find out which formulation were good for making in-situ gels using a combination of poloxamer and other bases. Formulation was characterized for appearance and homogeneity, pH and gelation studies, viscosity measurements, in vitro drug release, drug content, and stability studies. In vivo rabbit, eye irritation tests were conducted to evaluate the irritation of the in-situ gel delivery system; in addition, osmolality testing, sterility test, and isotonicity evaluation were also carried out. The results have shown that in-situ gel solution can increase residence time and also maintain the mechanism of drug release.

Formulation of sustained-release microspheres of cefixime with enhanced oral bioavailability and antibacterial potential

2019 ◽  
Vol 10 (12) ◽  
pp. 769-782
Author(s):  
Karan Razdan ◽  
Nikhil S Sahajpal ◽  
Kuldeep Singh ◽  
Harmanpreet Singh ◽  
Harjeet Singh ◽  
...  
Keyword(s):  
Sustained Release ◽  
Entrapment Efficiency ◽  
Salmonella Typhi ◽  
In Vivo Studies ◽  
In Vitro Drug Release ◽  
Dosing Frequency ◽  
Twofold Decrease ◽  
Antibacterial Potential

Aim: The present work focused on the development of sustained-release microsphere formulation of cefixime to provide reduction in dosing frequency, improved antibacterial activity and patient compliance. Methodology & results: Microspheres were prepared by modified emulsion solvent evaporation method and evaluated by in vitro and in vivo studies. Optimized formulation (FK-07) was found to have entrapment efficiency of 81.12 ± 0.93% and particle size of 166.82 ± 0.86 μm. FK-07 sustained release up to 24 h as demonstrated by in vitro drug release and in vivo pharmacokinetic study in rats. FK-07 showed approximately twofold increase in bioavailability and twofold decrease in MIC90 value against Escherichia coli, Klebsiella pneumoniae and Salmonella typhi in comparison to marketed formulation. Conclusion: Sustaining the release of cefixime using microspheres enhanced its bioavailability, antibacterial efficacy and will help in reducing its dosing frequency.

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 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 In Vitro Evaluation of Poly(lactide-co-glycolide) In Situ Forming Gels for Bedaquiline Fumarate Salt and Pharmacokinetics Following Subcutaneous Injection in Rats

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1231
Author(s):  
Sandy Van Hemelryck ◽  
Rani Wens ◽  
Hannelore van Poppel ◽  
Milou Luijks ◽  
Koosha Shahidi ◽  
...  
Keyword(s):  
Drug Release ◽  
Point Of View ◽  
Solvent Ratio ◽  
Sustained Drug Release ◽  
Polyethylene Glycol 400 ◽  
In Situ Forming ◽  
Fumarate Salt

This study evaluated in vitro and in vivo drug release of bedaquiline from in situ forming gels (ISGs) containing 200 mg eq./g bedaquiline fumarate salt prepared with four different grades of poly(d,l-lactide) (PDLLA) or poly(d,l-lactide-co-glycolide) (PLGA) with a lactide/glycolide ratio of 50/50 or 75/25 and acid (A) or ester (E) end-capping in N-methyl-2-pyrrolidone at a polymer/solvent ratio of 20/80% (w/w). Mean in vitro drug release in 0.05 M phosphate buffer pH 7.4 with 1% (w/v) sodium lauryl sulphate was 37.3, 47.1, 53.3, and 62.3% within 28 days for ISGs containing PLGA5050A, PDLLA, PLGA7525A, and PLGA7525E, respectively. The data suggested that drug release was primarily controlled by precipitated drug redissolving, rather than polymer erosion. In vivo pharmacokinetic profiles after subcutaneous injections in rats were comparable for all ISGs (mean half-lives (t1/2) ranged from 1411 to 1695 h) and indicated a sustained drug release when compared to a solution of bedaquiline fumarate salt in polyethylene glycol 400/water 50/50% (v/v) (mean t1/2 of 895 h). In conclusion, PLGA or PDLLA-based ISGs have shown potential for parenteral sustained delivery of bedaquiline, suggesting further preclinical and clinical studies. From a formulation point of view, this case example highlights the importance of the interplay between drug solubility in biological media and dissolution of drug precipitates, which, in addition to the incorporation of diffusion controlling polymers, governs the release of the active drug.

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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