Development of a rectal nicotine delivery system for the treatment of ulcerative colitis

Dash, Alekha K.; Gong, Zheng; Miller, Donald W.; Huai‐Yan, Han; Laforêt, J.P

doi:10.1016/s0378-5173(99)00221-5

Cited by 30 publications

(21 citation statements)

References 23 publications

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“…13 GMO also possesses bioadhesive properties that can be used to enhance the therapeutic efficacy of the dosage forms by increasing the contact time at the site of action. [14][15][16] The self-emulsifying property of GMO can further enhance the solubility of this highly hydrophobic compound in this formulation.…”

Section: Introductionmentioning

confidence: 99%

A mucoadhesive in situ gel delivery system for paclitaxel

Jauhari

Dash

2006

AAPS PharmSciTech

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MUC1 gene encodes a transmembrane mucin glycoprotein that is overexpressed in human breast cancer and colon cancer. The objective of this study was to develop an in situ gel delivery system containing paclitaxel (PTX) and mucoadhesives for sustained and targeted delivery of anticancer drugs. The delivery system consisted of chitosan and glyceryl monooleate (GMO) in 0.33M citric acid containing PTX. The in vitro release of PTX from the gel was performed in presence and absence of Tween 80 at drug loads of 0.18%, 0.30%, and 0.54% (wt/wt), in Sorensen's phosphate buffer (pH 7.4) at 37°C. Different mucin-producing cell lines (Calu-39Caco-2) were selected for PTX transport studies. Transport of PTX from solution and gel delivery system was performed in side by side diffusion chambers from apical to basal (A-B) and basal to apical (B-A) directions. In vitro release studies revealed that within 4 hours, only 7.61% ± 0.19%, 12.0% ± 0.98%, 31.7% ± 0.40% of PTX were released from 0.18%, 0.30%, and 0.54% drugloaded gel formulation, respectively, in absence of Tween 80. However, in presence of surfactant (0.05% wt/vol) in the dissolution medium, percentages of PTX released were 28.1% ± 4.35%, 44.2% ± 6.35%, and 97.1% ± 1.22%, respectively. Paclitaxel has shown a polarized transport in all the cell monolayers with B-A transport 2 to 4 times higher than in the A-B direction. The highest mucin-producing cell line (Calu-3) has shown the lowest percentage of PTX transport from gels as compared with Caco-2 cells. Transport of PTX from mucoadhesive gels was shown to be influenced by the mucin-producing capability of cell.

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Section: Introductionmentioning

confidence: 99%

A mucoadhesive in situ gel delivery system for paclitaxel

Jauhari

Dash

2006

AAPS PharmSciTech

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“…Its 124 major functions are absorption at interface or on solids, promotion 125 of wetting phenomena, co-crystallization, complex formation 126 (with proteins or starch components) and self-association. 127 In the pharmaceutical area, glycerol monooleate was first used 128 as an emulsifier and an absorption enhancer in combination with 129 bile salts (Dash et al, 1999;Ganem-Quintanar et al, 2000;Herai 130 et al, 2007). As an absorption enhancer, glycerol monooleate 131 probably acts by causing a temporary and reversible disruption of (Chernik, 1999;Larsson et al, 2006;Larsson, 144 2009).…”

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confidence: 99%

Glycerol monooleate liquid crystalline phases used in drug delivery systems

Milak

Zimmer

2015

International Journal of Pharmaceutics

163

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“…However, the dose of nicotine to obtain adequate effectiveness for ulcerative colitis is complicated, because of the large first pass effect in the liver and the severe gastric and systemic adverse effects. In this aspect, some other formulas of nicotine such as sublingual nicotine tablets (Molander and Lunell, 2001), oral formulations of nicotine carbomers (Green et al, 1999), liquid enema (Zins et al, 1997), and rectal suppository formulations (Green et al, 1997;Dash et al, 1999) have been investigated. Considering the local delivery of nicotine such as enema to improve local bioavailability, it becomes more important to characterize the nicotine transport system across the epithelial cells in the large intestine and rectum itself.…”

mentioning

confidence: 99%

Transport Mechanisms of Nicotine across the Human Intestinal Epithelial Cell Line Caco-2

Fukada¹,

Saya²,

Inui³

2002

J Pharmacol Exp Ther

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Ulcerative colitis is a disease more commonly seen in nonsmokers. Because nicotine was postulated to be a beneficial component of tobacco smoke for ulcerative colitis, various formulations of nicotine have been developed to improve the local bioavailability within the gastrointestinal tissue. In the present study, to characterize the disposition of nicotine in the intestines, we investigated intestinal nicotine transport using Caco-2 cells. Nicotine was predominantly transported across Caco-2 cell monolayers in a unidirectional mode, corresponding to intestinal secretion, by pH-dependent specific transport systems. The specific uptake systems appear to be distinct from organic cation transporters and the transport system for tertiary amines, in terms of its substrate specificity and the pattern of the interaction. These transport systems could play a role in the intestinal accumulation of nicotine from plasma and could also be responsible for the topical delivery of nicotine for ulcerative colitis therapy. These findings could provide useful information for the design of effective nicotine delivery.

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Development of a rectal nicotine delivery system for the treatment of ulcerative colitis

Cited by 30 publications

References 23 publications

A mucoadhesive in situ gel delivery system for paclitaxel

A mucoadhesive in situ gel delivery system for paclitaxel

Glycerol monooleate liquid crystalline phases used in drug delivery systems

Transport Mechanisms of Nicotine across the Human Intestinal Epithelial Cell Line Caco-2

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