Development and In Vivo Evaluation of Mesalazine Colon Targeted Tablets

2019 ◽  
Vol 12 (3) ◽  
pp. 4552-4558
Author(s):  
Rawoof MD ◽  
Rajnarayana K ◽  
Ajitha M
Keyword(s):  
Drug Release ◽  
Wet Granulation ◽  
Time Intervals ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Ph Dependent ◽  
Rapid Hydrolysis

The main objective of the present study was to develop colon-targeted tablets of mesalazine by wet granulation method using 33 Response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16 % of mesalazine after 24 h, whereas marketed product drug release was 92.02 ± 2.15 after  24 h. From in vivo bioavailability studies, after oral administration of colon targeted tablet containing 400 mg mesalazine, the Cmax, Tmax, and AUC0–∞ of optimized formulation and marketed product was found to be 683.21 ± 0.03 ng/mL, 6.01 ± 0.04 h, 4150.12 ± 5.12 ng*h/mL and 445.34 ± 3.22 ng/mL, 4.00 ± 0.01 h, 3457.18 ± 5.32 ng*h/mL respectively. Cmax, Tmax and AUC values of optimized formulation were found to be significantly higher than of marketed product. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of mesalazine for the treatment of disease at colon region.

scholarly journals Design and Evaluation of Colon Targeted Dosage Form Containing Mesalazine Using pH Dependent Polymers

2017 ◽  
Vol 9 (06) ◽  
Author(s):  
MD. Rawoof ◽  
K. Rajnarayana ◽  
M. Ajitha
Keyword(s):  
Wet Granulation ◽  
Systemic Delivery ◽  
In Vitro Drug Release ◽  
Colonic Drug Delivery ◽  
Release Studies ◽  
Therapeutic Peptides ◽  
Ph Dependent ◽  
Irritable Bowel ◽  
Rapid Hydrolysis

Colonic drug delivery has gained importance not just for the delivery of the drugs for the treatment of local diseases associated with the colon like Crohn’s disease, ulcerative colitis and irritable bowel syndrome but also for the potential it holds for the systemic delivery of proteins and therapeutic peptides. The aim of the study was to develop colon targeted tablets of Mesalazine by wet granulation method using 33 response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16% of Mesalazine after 24 h. The results of the study showed that formulation F26 is the best formulation based on the evaluation parameters which provides targeting of Mesalazine for local action in the colon owing to its minimal release of the drug in the first 4 h. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of Mesalazine for the treatment of disease at colon region.

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

Synthesis and characterization of Chitosan-Catechol conjugates: Development and in vitro, in silico and in vivo evaluation of mucoadhesive pellets of lafutidine

2021 ◽  
pp. 088391152199784
Author(s):  
Loveleen Kaur ◽  
Ajay Kumar Thakur ◽  
Pradeep Kumar ◽  
Inderbir Singh
Keyword(s):  
Drug Release ◽  
In Silico ◽  
Ex Vivo ◽  
Strong Interactions ◽  
Dissolution Time ◽  
Sem Images ◽  
In Vivo Evaluation ◽  
Release Studies

Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t50%, t90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.

Formulation and in vitro evaluation of upconversion nanoparticle-loaded liposomes for brain cancer

2020 ◽  
Vol 11 (9) ◽  
pp. 557-571 ◽  
Author(s):  
Narendra ◽  
Abhishesh Kumar Mehata ◽  
Matte Kasi Viswanadh ◽  
Roshan Sonkar ◽  
Datta Maroti Pawde ◽  
...  
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Glioma Cells ◽  
C6 Glioma Cells ◽  
Upconversion Nanoparticles ◽  
Clinical Validation ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release

Aim: This work focused on the development of transferrin-conjugated theranostic liposomes consisting of docetaxel (DXL) and upconversion nanoparticles for the diagnosis and treatment of gliomas. Materials & methods: Upconversion nanoparticles and docetaxel-loaded theranostic liposomes were prepared by a solvent injection method. Formulations were analyzed for physicochemical properties, encapsulation efficiency, drug release, elemental analysis, cytotoxicity and fluorescence. Results: The particle size was around 200 nm with spherical morphology and an encapsulation efficiency of up to 75.93%, was achieved for liposomes with an in vitro drug release of 71.10%. The IC50 values demonstrated enhanced cytotoxicity on C6 glioma cells with targeted liposomes in comparison with nontargeted liposomes. Conclusion: Prepared theranostic liposomes may be promising for clinical validation after an in vitro and in vivo evaluation on cell lines and animals, respectively.

Design, in vitro and in vivo Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets

1970 ◽  
Vol 9 (1) ◽  
pp. 3143-3149
Author(s):  
Sushma Appala ◽  
Ramesh Bomma ◽  
Kishan Veerabrahma
Keyword(s):  
Helicobacter Pylori ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Gastro Retentive

Objective of the investigation was to develop gastro retentive dosage form of gemifloxacin mesylate for local action in the stomach as it has antibacterial activity against Helicobacter pylori. Gemifloxacin mesylate is a synthetic broad-spectrum antibacterial agent for oral administration, having 7 hrs half-life and 71% oral bioavailability. In present study, gemifloxacin mesylate floating matrix tablets were prepared by direct compression method using polymers (HPMC K4M, HPMC K15M and polyox WSR 1105) and evaluated for various parameters like drug content, floating behavior (floating lag time and total floating time), in vitro drug release, swelling index, weight variation, friability, hardness and thickness. Sodium bicarbonate was incorporated as gas generating agent in all formulations. Drug-excipients compatibility was studied by Differential Scanning Calorimetry. Results have shown that the amount of polymer in the formulation affected the drug release. Optimized formulation (F8 containing polyox WSR1105 as release retarding agent) was selected based on in vitro drug release, floating lag time, floating time and other parameters. This formulation followed zero order kinetics and non-Fickian mechanism of drug release. In vivo radiographic study was conducted in healthy human volunteers using tablets containing BaSO4 as radio opaque agent. The average residence time was found to be 4.5± 0.86 h (n=3). This design of gastro retentive drug delivery system helps in increasing the local delivery of drug in patients with Helicobacter pylori infection

scholarly journals Steroid Eluting Esophageal-Targeted Drug Delivery Devices for Treatment of Eosinophilic Esophagitis

Polymers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 557
Author(s):  
Alka Prasher ◽  
Roopali Shrivastava ◽  
Denali Dahl ◽  
Preetika Sharma-Huynh ◽  
Panita Maturavongsadit ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Porcine Model ◽  
Pharmacokinetic Studies ◽  
Specific Drug ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
3D Printed

Eosinophilic esophagitis (EoE) is a chronic atopic disease that has become increasingly prevalent over the past 20 years. A first-line pharmacologic option is topical/swallowed corticosteroids, but these are adapted from asthma preparations such as fluticasone from an inhaler and yield suboptimal response rates. There are no FDA-approved medications for the treatment of EoE, and esophageal-specific drug formulations are lacking. We report the development of two novel esophageal-specific drug delivery platforms. The first is a fluticasone-eluting string that could be swallowed similar to the string test “entero-test” and used for overnight treatment, allowing for a rapid release along the entire length of esophagus. In vitro drug release studies showed a target release of 1 mg/day of fluticasone. In vivo pharmacokinetic studies were carried out after deploying the string in a porcine model, and our results showed a high local level of fluticasone in esophageal tissue persisting over 1 and 3 days, and a minimal systemic absorption in plasma. The second device is a fluticasone-eluting 3D printed ring for local and sustained release of fluticasone in the esophagus. We designed and fabricated biocompatible fluticasone-loaded rings using a top-down, Digital Light Processing (DLP) Gizmo 3D printer. We explored various strategies of drug loading into 3D printed rings, involving incorporation of drug during the print process (pre-loading) or after printing (post-loading). In vitro drug release studies of fluticasone-loaded rings (pre and post-loaded) showed that fluticasone elutes at a constant rate over a period of one month. Ex vivo pharmacokinetic studies in the porcine model also showed high tissue levels of fluticasone and both rings and strings were successfully deployed into the porcine esophagus in vivo. Given these preliminary proof-of-concept data, these devices now merit study in animal models of disease and ultimately subsequent translation to testing in humans.

scholarly journals Formulation, Characterisation and Evaluation of the Ethosuximide Oral Immediate Release Tablets

2020 ◽  
Vol 11 (2) ◽  
pp. 1807-1813
Author(s):  
Naga Sujan M ◽  
Kunal K Mehta ◽  
Amit B Patil ◽  
Anusha Vajhala
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Immediate Release ◽  
Rice Starch ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Release Studies

The present study is aimed to formulate, characterization, and evaluate oral immediate-release tablets of Ethosuximide. It is employed as an anti-epileptic agent used in the treatment of epilepsy, in all the age groups who were≥ 1 year. The dosage form is formulated by directly compressing the blend and granulating the powder blend by wet granulation methods. The optimized formulation is achieved by the trial and error method by changing the concentration of lactose monohydrate and di-basic calcium phosphate dehydrate as diluents, sodium starch glycolate as Super-dis-integrant, rice Starch as an intra-granular binder, hydroxypropyl cellulose as binder talc as a lubricant. Evaluation parameters such as micrometric properties, disintegration time along with in-vitro drug release studies were performed for characterizing the dosage form. In-vitro drug release studies were carried out using 0.1 N HCl as dissolution media with 75 rpm and temperature of 370C ± 50C by employing USP apparatus II (Paddle type). Estimation of the % drug release of the tablet was carried out using the UV method. The prepared formulation and the marketed formulation were tested for the in-vitro drug release profile and the prepared formulation was compared with the marketed formulation. All the evaluated result was found to be within the specifications. Therefore, from the obtained evaluation results F6 trail was selected as the best formulation.

scholarly journals Formulation, Optimization and in vitro Characterization of Stavudine Gastro Retentive Floating Matrix Tablets

2016 ◽  
Vol 8 (03) ◽  
Author(s):  
Mahendar Rupavath ◽  
Kranthi G. ◽  
Chinna Palem ◽  
K. S. K. Patnaik
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
In Vitro Drug Release ◽  
Weight Variation

The aim of the present investigation was to develop floating matrix tablets of stavudine to achieve prolong gastric residence time, leading to an increase in drug bioavailability and patient compliance. Floating tablets were prepared by wet granulation technique, using hydroxypropyl methylcellulose (HPMC K15M) as synthetic, pullulan gum as natural rate controlling polymers and optimum amounts of sodium-bicarbonate and citric acid as gas generating agents in suitable ratios to generate optimum buoyancy. Developed formulations were evaluated for weight variation, thickness, hardness, friability, drug content, in vitro drug release, floating lag time and floating buoyancy. All the formulations exhibited acceptable physical properties and the best formulation (F3) was selected based on in vitro characteristics. Further, the optimized formulation was evaluated for in vivo radiographic studies by incorporating BaSO4 as radio opaque substance. All the formulations were studied for in vitro drug release characteristics for 16 h. Optimized formulation showed controlled and prolonged drug release profiles while floating over the dissolution medium. Diffusion followed by erosion drug release mechanism was observed for the formulation, indicating that water diffusion and polymer erosion played an essential role in drug release. In vivo radiographic studies revealed that the tablets remained in the stomach for 8 ± 0.5 h in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered and desirable for absorption window drugs.

scholarly journals FORMULATION AND EVALUATION OF PH-DEPENDENT COLON-TARGETED TABLETS OF RIFAXIMIN BY DESIGN OF EXPERIMENT

2019 ◽  
pp. 249-254
Author(s):  
RAWOOF MD ◽  
RAJNARAYANA K ◽  
AJITHA M
Keyword(s):  
Drug Release ◽  
Proximal Colon ◽  
Drug Dissolution ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Release Studies ◽  
Ph Dependent ◽  
The Fourier Transform ◽  
The Stability

Objective: The research is designed at formulating and evaluating pH-sensitive rifaximin colon-targeted tablets for targeted action in proximal colon. Method: The colon-targeted tablets are done by granulation of three levels of polymers such as Eudragit L30D, Carbopol 974P, and ethyl cellulose. The evaluation parameters such as swelling studies, drug dissolution, in vitro drug release studies, stability, and the Fourier transform infrared studies carried out for optimized formulations. Results: Physicochemical parameters of all the 27 formulations (RF1-RF27) evaluated and RF21 is chosen for further investigation based on weight variation, hardness, drug content, and swelling index. The in vitro drug release studies indicate that the optimized formulation RF21 released 98.75% drug within 24 h. The stability studies indicate that the formulation is stable. Conclusion: An effective and stable pH-dependent rifaximin colon-targeted tablet formulated for the targeted treatment of bowel syndrome.

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