Formulation and Evaluation of Colon Targeted Drug Delivery of Mesalamine

2017 ◽  
Vol 9 (1) ◽  
Author(s):  
Gadhave M. V. ◽  
Shevante Trupti B. ◽  
Takale Avinash A. ◽  
Jadhav S. L. ◽  
Gaikwad D. D.
Keyword(s):  
Drug Delivery ◽  
Targeted Drug Delivery ◽  
Gastrointestinal Transit ◽  
Drug Dissolution ◽  
Colonic Delivery ◽  
Arrival Times ◽  
Gastrointestinal Transit Time ◽  
Chitosan Concentration ◽  
The Core ◽  
Core Tablet

In this study, we report pectin–Chitosan compression coated core tablets of Mesalamine for colonic delivery. Each 150 mg core tablet contained Mesalamine and was compression coated using 100% pectin 1:1, 10 pectin:1 Chitosan, or 10 pectin :2 Chitosan, at coat weights as 400mg. Drug dissolution or system erosion or degradation studies were carried out in pH 1.2, 6.8,7.4 phosphate buffers using a pectinolytic enzyme. The system was designed based on the gastrointestinal transit time concept, under the assumption of colon arrival times of 6 h. It was found that pectin alone was not sufficient to protect the core tablets and Chitosan addition was required to control the solubility of pectin. The optimum Chitosan concentration was 1 and such system would protect the cores up to 6 h and after that under the influence of pectinase the system would degrade faster and delivering 5-ASA to the colon. The pectin– Chitosan (10:1) envelope was found to be a promising drug delivery system for those drugs to be delivered to the colon.

Recent Advances in Colon Drug Delivery Technology.

2021 ◽  
Vol 11 ◽  
Author(s):  
Rakesh Pahwa ◽  
Ridhi Bajaj ◽  
Pankaj Bhateja ◽  
Mona Piplani
Keyword(s):  
Drug Delivery ◽  
Targeted Drug Delivery ◽  
Drug Delivery Systems ◽  
Release Kinetics ◽  
Delivery Systems ◽  
Structure Property ◽  
Colonic Delivery ◽  
Colon Drug Delivery ◽  
Targeted Drug ◽  
Delivery Technology

: Colon targeted drug delivery technology; an approach of immense potential has acquired tremendous significance for managing a number of ailments particularly of colon and for delivering therapeutic proteins and peptides systemically. The major hurdles for delivering drug in colonic region include absorption and degradation pathways in the upper gastrointestinal tract (GIT). To achieve a triumphant colonic delivery, therapeutic agent must be sheltered from getting absorbed in the preliminary region of GIT, in addition, ensure its release in proximal colon in a controlled way. The principle approaches for instance prodrug approach, pH sensitivity, time-dependency (lag time), degradation by microbes etc. have been effectively applied for obtaining colon targeted drug delivery. These approaches have accomplished immense relevance. Therefore, incessant attempts have been mainly focused on the design of colon targeted drug delivery systems having enhanced site specificity along with study of its versatile drug release kinetics to achieve diverse therapeutic requirements. The current manuscript illustrates significance of different colon drug delivery systems and general considerations for designing colon targeting systems including primary as well as novel approaches. Recent investigational studies carried out by scientific communities worldwide for the designing and preparation of various colon targeted formulations along with their significant insights have been described. Recent patents, structure property relationship and dissolution aspects pertaining to the colon specific drug delivery have also been depicted.

scholarly journals Primary and Novel Approaches in Colon Targeted Drug Delivery System: A Review

2015 ◽  
Vol 3 (02) ◽  
pp. 37-57
Author(s):  
Komal . ◽  
Ujjwal Nautiyal ◽  
Ramandeep , Anita Devi Singh ◽  
Anita Devi
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Targeted Drug Delivery ◽  
Targeted Delivery ◽  
Local Treatment ◽  
Systemic Delivery ◽  
Colonic Delivery ◽  
Targeted Drug ◽  
Targeted Drug Delivery System

Targeted drug delivery into the colon is highly desirable for local treatment of a variety of bowel diseases such as ulcerative colitis, Crohn’s disease, amoeabiasis , colonic cancer, local treatment of colonic pathologies, and systemic delivery of protein and peptide drugs. Colonic delivery refers to targeted delivery of drugs into the lower GI tract, which occurs primarily in the large intestine (i.e. colon). The colon specific drug delivery system (CDDS) should be capable of protecting the drug en route to the colon i.e. drug release and absorption should not occur in the stomach as well as the small intestine, and neither the bioactive agent should be degraded in either of the dissolution sites but only released and absorbed once the system reaches the colon. Different approaches are designed based on prodrug formulation, pHsensitivity, time-dependency (lag time), microbial degradation and osmotic pressure etc to formulate the different dosage forms like tablets, capsules, multiparticulates, microspheres, liposomes for colon targeting. The efficiency of drug delivery system is evaluated using different in vitro and in vivo release studies. This review article discusses, in brief, introduction to targeted drug delivery system, anatomy and physiology of the colon and approaches utilized in the colon targeted drug delivery system.

scholarly journals Polysaccharide-Based Nanoparticles for Colon-Targeted Drug Delivery Systems

2021 ◽  
Vol 2 (3) ◽  
pp. 626-647
Author(s):  
Yubia De Anda-Flores ◽  
Elizabeth Carvajal-Millan ◽  
Alma Campa-Mada ◽  
Jaime Lizardi-Mendoza ◽  
Agustin Rascon-Chu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Targeted Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Gi Tract ◽  
Colonic Delivery ◽  
Drug Degradation ◽  
Non Invasive ◽  
Targeted Drug ◽  
Targeted Drug Delivery Systems

Polysaccharide biomaterials have gained significant importance in the manufacture of nanoparticles used in colon-targeted drug delivery systems. These systems are a form of non-invasive oral therapy used in the treatment of various diseases. To achieve successful colonic delivery, the chemical, enzymatic and mucoadhesive barriers within the gastrointestinal (GI) tract must be analyzed. This will allow for the nanomaterials to cross these barriers and reach the colon. This review provides information on the development of nanoparticles made from various polysaccharides, which can overcome multiple barriers along the GI tract and affect encapsulation efficiency, drug protection, and release mechanisms upon arrival in the colon. Also, there is information disclosed about the size of the nanoparticles that are usually involved in the mechanisms of diffusion through the barriers in the GI tract, which may influence early drug degradation and release in the digestive tract.

scholarly journals A two pulse drug delivery system for amoxicillin: An attempt to counter the scourge of bacterial resistance against antibiotics

2011 ◽  
Vol 61 (3) ◽  
pp. 313-322 ◽  
Author(s):  
Habban Akhter ◽  
Nitin Saigal ◽  
Sanjula Baboota ◽  
Shah Faisal ◽  
Javed Ali
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Microcrystalline Cellulose ◽  
Bacterial Resistance ◽  
Lag Time ◽  
Pore Former ◽  
The Core ◽  
Core Tablet

A two pulse drug delivery system for amoxicillin: An attempt to counter the scourge of bacterial resistance against antibiotics Bearing in mind the present scenario of the increasing biological tolerance of bacteria against antibiotics, a time controlled two pulse dosage form of amoxicillin was developed. The compression coating inlay tablet approach was used to deliver the drug in two pulses to different parts of the GIT after a well defined lag time between the two releases. This was made possible by formulating a core containing one of the two drug fractions (intended to be delivered as the second pulse), which was spray coated with a suspension of ethyl cellulose and a hydrophilic but water insoluble agent as a pore former (microcrystalline cellulose). Coating of up to 5 % (m/m) was applied over the core tablet, giving a corresponding lag of 3, 5, 7 and 12 h. Increasing the level of coating led to retardation of the water uptake capacity of the core, leading to prolongation of the lag time. Microcrystalline cellulose was used as a hydrophilic but water insoluble porosity modifier in the barrier layer, varying the concentration of which had a significant effect on shortening or prolongation of the lag time. This coated system was further partially compression coated with the remaining drug fraction (to be released as the first immediate release pulse) with a disintegrant, giving a final tablet. The core tablet and the final two pulse inlay tablet were further investigated for their in vitro performance.

scholarly journals Tailoring of drug delivery of 5-fluorouracil to the colon via a mixed film coated unit system

2011 ◽  
Vol 61 (3) ◽  
pp. 343-351 ◽  
Author(s):  
Ruchita Kumar ◽  
Vivek Sinha
Keyword(s):  
Drug Delivery ◽  
Release Kinetics ◽  
Kinetic Studies ◽  
Colonic Transit ◽  
Colonic Delivery ◽  
The Core ◽  
Unit System ◽  
Eudragit S100 ◽  
Mixed Film

Tailoring of drug delivery of 5-fluorouracil to the colon via a mixed film coated unit system The study was carried out to establish the effectiveness of a mixed film composed of ethylcellulose/Eudragit S100 for colonic delivery of 5-flourouracil (5-FU). Tablets cores containing 5-FU were prepared by direct compression method by coating at different levels (2-9 %, m/m) with a non-aqueous solution containing ethylcellulose/Eudragit S100. Coated tablets were studied for the in vitro release of 5-FU and the samples were analyzed spectrophotometrically at 266 nm. Drug release from coated systems depended on the thickness of the mixed film and the composition of the core. Channel formation was initiated in the coat by dissolution of the Eudragit S100 fraction at higher pH in the colonic region. The release was found to be higher in tablets containing Avicel as filler owing to its wicking action compared to that from lactose containing cores. Furthermore, batches containing superdisintegrant (1 %, m/m Cross-PVP) along with Avicel in the core released approximately 81.1 % drug during the colonic transit time. Kinetic studies indicated that all the formulations followed first-order release kinetics. The developed delivery system will expectedly deliver the drug to the colon.

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