Microbially triggered drug delivery to the colon

Sinha, Vivek Ranjan; Kumria, Rachna

doi:10.1016/s0928-0987(02)00221-x

Cited by 265 publications

(156 citation statements)

References 129 publications

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“…The colon is also a useful site for delivery of drugs where a delay in drug absorption is required from a therapeutic point of view, e.g. in case of nocturnal asthma, angina, rheumatoid arthritis, etc (Rubinstein, 1995;Vervoort et al, 1998;Sinha & Kumria, 2003;Ramasamy et al, 2013). Moreover, colonic delivery is beneficial for systemic absorption of some drugs, e.g.…”

Section: Introductionmentioning

confidence: 99%

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

et al. 2015

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The colon is a promising target for drug delivery owing to its long transit time of up to 78 h, which is likely to increase the time available for drug absorption. Progesterone has a short elimination half-life and undergoes extensive first-pass metabolism, which results in very low oral bioavailability ($25%). To overcome these shortcomings, we developed an oral multiparticulate system for the colonic delivery of progesterone. Zn-pectinate/chitosan microparticles were prepared by ionotropic gelation and characterized for their size, shape, weight, drug entrapment efficiency, mucoadhesion and swelling behavior. The effect of crosslinking pH, cross-linking time and chitosan concentration on progesterone release were also studied. Spherical microparticles having a diameter of 580-720 mm were obtained. Drug entrapment efficiency of $75-100% was obtained depending on the microparticle composition. Microparticle mucoadhesive properties were dependent on the pectin concentration, as well as the cross-linking pH. Progesterone release in simulated gastric fluids was minimal (3-9%), followed by burst release at pH 6.8 and a sustained phase at pH 7.4. The in vivo study revealed that the microparticles significantly increased progesterone residence time in the plasma and increased its relative bioavailability to $168%, compared to the drug alone. This study confirms the potential of Zn-pectinate/chitosan microparticles as a colon-specific drug delivery system able to enhance the oral bioavailability of progesterone or similar drugs.

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Section: Introductionmentioning

confidence: 99%

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

et al. 2015

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“…In these systems, the site of drug release is decided by the transit time of a formulation in the GI tract (Singh, 2007). The abundance of microflora in the colon area has also been used to achieve colon targeting (Sinha & Kumria, 2003). Hence, enzymatically controlled delivery systems are considered a convenient approach for site-specific drug delivery to the colon where no drug release can occur unless the system arrives to the colon.…”

Section: Introductionmentioning

confidence: 99%

Bumadizone calcium dihydrate microspheres compressed tablets for colon targeting: formulation, optimization andin vivoevaluation in rabbits

2014

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The objective of this study was the development of a colon-targeted microspheres which were compressed into tablets containing the non-steroidal anti-inflammatory bumadizone calcium dihydrate. A 3 2 full factorial design was adopted for the evaluation of the prepared microspheres. The effect of two independent variables namely polymer type (Eudragit RS100, ethyl cellulose and cellulose acetate butyrate), and drug: polymer ratio (1:1, 9:1 and 18:1) was studied on the entrapment efficiency and in vitro drug release for 12 h. Colon targeting aims to minimize the release of the drug off target area (pH 1.2 and 6.8) and to maximize the release of the drug in target area (pH 7.4). Candidate formulae were compressed into core tablets and colon targeting was achieved using the enzyme-dependent polymer (pectin) as coat in three different concentrations 50, 75 and 90%. Candidate formula F15 (microspheres prepared using BDZ:CAB in a ratio of 18:1 and compressed into tablets using 50% pectin and 50% Avicel in the coat) was able to adequately modulate drug release avoiding drug release in the gastric ambient, and reaching the colonic targeting where 99.7% release was achieved within 12 h following zero-order model. In vivo studies showed that F15 achieved significant decrease in myeloperoxidase activity and inflammation with delayed T max (4 h) and lower C max (2700 ng/ml) when compared to marketed product.

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“…The main function of this site of GIT is reabsorption of water from the chyme and act as a reservoir. [2] www.wjpps.com Microbially triggered drug release [5] The vast microflora fulfills its energy needs by fermenting the various types of substrates that have been left undigested in the small intestine i.e. truly the physiological roughage including di-,tri-polysaccharides, mucopolysaccharides, etc., reach the colon.…”

Section: Physiology Of Colonmentioning

confidence: 99%

Design and Development of Oral Dosage Form for Colon Specific Drug Release of Indomethacine

Parameshwar¹

2017

WJPPS

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Rheumatoid arthritis are severe in early morning hours, so an attempt has been made to overcome the problem by delaying drug release by colon targeting to maintain peak plasma concentrations in early morning hours. Indomethacin, a non-steroidal anti-inflammatory drug effectively used for treatment of inflammation and pain caused by Half enteric (10% CAP, 10% HPMCP, and 10% EUDRAGIT L-100) coated hydrogel plugs were selected for development of pulsincap in respect to its maximum swelling ratio shown in pH 6.8 compared to the full enteric coated hydrogel plugs. In-vitro release studies were

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Microbially triggered drug delivery to the colon

Cited by 265 publications

References 129 publications

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

Bumadizone calcium dihydrate microspheres compressed tablets for colon targeting: formulation, optimization andin vivoevaluation in rabbits

Design and Development of Oral Dosage Form for Colon Specific Drug Release of Indomethacine

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