Colon Targeted Rifaximin Nanosuspension for the Treatment of Inflammatory Bowel Disease (IBD)

Author(s): Jatinder Kumar, AMJ Newton

Journal Name: Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Formerly Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents

Volume 15 , Issue 2 , 2016

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Graphical Abstract:


Background: Although, a number of formulations have been developed for the treatment of IBD yet the developed formulations are having side effects such as high dose, lack of solubility and permeability problems at the site of action. Very few formulations have been developed for the IBD treatment in the form of nanoparticles. Nanoparticles have shown their potential in the recent findings in the treatment of IBD at cellular level. This research work aims to develop nanosuspension of newly introduced drug Rifaximin currently available in the form of tablet for the treatment of IBD. Rifaximin in the form of tablet is given in high dose concentration so to avoid the large dose and to increase the permeability action of drug a nanosuspension is prepared using a well known polymer Eudragit S 100 which is itself a colon targeted polymer and simultaneously improves the site specific delivery of the drug.

Method: We thoroughly reviewed and tested the previous work for the development of nanoparticles in the laboratory for the treatment of IBD. A number of research as well as review articles were followed in order to get quality information. For this all the research as well as review work was collected from the quality journals. A simple yet a high result oriented technique nanoprecipitation was used for the development of nanoparticles.

Results: A total of 21 research and review papers were studied deeply. Before developing the final formula a number of trials were carried out and from the trials, the formulation which showed better release profile and presence of nanoparticles was then optimized and a total of five formulations were developed. In each of the five formulations the concentration of the polymer and external phase was varied along with the concentration change in P.F. 68 for getting a superior formulation in terms of release, size and entrapment. The least size nanosuspension was subjected to Transmission Electron Microscopy for confirmation of nanoparticles and to check the morphological characters of the prepared nanoparticles and size of the nanoparticles was in the range of 19nm to 25nm. The prepared formulation was subjected to stability studies and it was freeze dried.

Conclusion: The outcome of this research work confirms the formation of nanoparticles and release profile of the prepared nanosuspension proved its site specificity. The release graphs indicated the release of the drug in colon proving its potential in the treatment of IBD and entrapment study indicates the drug entrapment capacity for delivering the required concentration of drug at the site of action. Moreover, the nanoformulation reduces the dose and the side effects due to its specific targeting at the site of inflammation which makes it a better choice over the tablets.

Keywords: Eudragit S 100, pluronic F.68, release kinetics, transmission electron microscopy.

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Article Details

Year: 2016
Published on: 19 July, 2016
Page: [101 - 117]
Pages: 17
DOI: 10.2174/1871523015666160720103732
Price: $65

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