Evaluation of an intestinal pressure-controlled colon delivery capsules prepared by a dipping method

Jeong, Young‐Il; Ohno, Tomoya; Hu, Zhaopeng; Yoshikawa, Yukako; Shibata, Nobuhito; Nagata, Shunji; Takada, Kanji

doi:10.1016/s0168-3659(01)00211-5

Cited by 53 publications

(15 citation statements)

References 11 publications

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“…They can be categorized as: (a) Prodrug approach (Riley & Turnberg, 1990;McLeod et al, 1994); (b) Pressure-based systems (Muraoka et al, 1998;Jeong et al, 2001); (c) The temporal control of delivery (Steed et al, 1997;Del Curto et al, 2009); (d) pH-based systems (Klein et al, 2005;Basak & Adhikari, 2009;Sareen et al, 2014), and (e) Enzyme-based systems (Xi et al, 2005;Varshosaz et al, 2006;Kshirsagar et al, 2011;Ramasamy et al, 2013;Rai et al, 2014). Polysaccharides which undergo hydrolysis of their glycosidic bonds by the microflora of the colon appear to be the most promising because of their attractive properties, such as wide availability, low cost of production, low toxicity and biodegradability (Chourasia & Jain, 2004).…”

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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“…17 HMPCP has been reported in many researches for use as various forms of drug carriers (such as microcapsules, 17 nanoparticles, 18 tablets 19 and enteric drugs. 20,21 To our knowledge, electrospinning of HPMCP fiber mat for drug delivery system has not yet been reported. Erythromycin is an antibiotic drug used to treat certain infections caused by bacteria.…”

Section: Introductionmentioning

confidence: 99%

Electrospun hydroxypropyl methyl cellulose phthalate (HPMCP)/erythromycin fibers for targeted release in intestine

Wang

Huang

2007

J of Applied Polymer Sci

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Ultrafine fiber mats of hydroxypropyl methyl cellulose phthalate (HPMCP) were successfully electrospun and explored as drug delivery vehicles using erythromycin as a model drug. The morphology of the electrospun fiber and the drug release process in the artificial gastric juice and in the artificial intestinal juice were investigated. With the same drug-to-matrix ratio (HPMCP/erythromycin ¼ 9/1), all the fibers were electrospun into a tape-like or ribbon shape and the average fiber diameter (AFD) was increased with the HPMCP concentration. Because of the pH-sensitive property of HPMCP, erythromycin was released from the erythromycin-containing electrospun HPMCP fiber mats by a slowly diffusion process in the artificial gastric juice, while it was released in nearly first-order kinetics in the artificial intestinal juice because of the first-order kinetics dissolution of the HPMCP fibers in the artificial intestinal juice. And the rate of erythromycin released in the artificial intestinal juice was about more than 2.5 times faster than that in the artificial gastric juice. The diameter of the fibers plays an important role on the rate and the total amount of the drug released both in stomach and in intestine, the rate and the total amount of the drug released decreasing with increasing AFD.

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“…The thickness of the ethylcellulose membrane is the most important factor for the disintegration of the formulation. 44,45 The system also appeared to depend on capsule size and density. Because of reabsorption of water from the colon, the viscosity of luminal content is higher in the colon than in the small intestine.…”

Section: Newly Developed Approaches For Cdds a Pressure Controlled Dmentioning

confidence: 99%

Colon Targeted Drug Delivery Systems: A Review on Primary and Novel Approaches

Philip

Philip²

2010

OMJ

309

182

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The colon is a site where both local and systemic delivery of drugs can take place. Local delivery allows topical treatment of inflammatory bowel disease. However, treatment can be made effective if the drugs can be targeted directly into the colon, thereby reducing the systemic side effects. This review, mainly compares the primary approaches for CDDS (Colon Specific Drug Delivery) namely prodrugs, pH and time dependent systems, and microbially triggered systems, which achieved limited success and had limitations as compared with newer CDDS namely pressure controlled colonic delivery capsules, CODESTM, and osmotic controlled drug delivery which are unique in terms of achieving in vivo site specificity, and feasibility of manufacturing process.

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Evaluation of an intestinal pressure-controlled colon delivery capsules prepared by a dipping method

Cited by 53 publications

References 11 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

Electrospun hydroxypropyl methyl cellulose phthalate (HPMCP)/erythromycin fibers for targeted release in intestine

Colon Targeted Drug Delivery Systems: A Review on Primary and Novel Approaches

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