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Pharmaceutics 2014, 6(3), 494-511; doi:10.3390/pharmaceutics6030494

Bioadhesive Mini-Tablets for Vaginal Drug Delivery

1
SiteDel Research Group, School of Pharmacy, Faculty of Mathematics and Natural Sciences, University of Oslo, 0316 Oslo, Norway
2
Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø, 9037 Tromsø, Norway
Current affiliation: PharmaLuxLab Research Group, School of Pharmacy, Faculty of Mathematics and Natural Sciences, University of Oslo, 0316 Oslo, Norway.
*
Author to whom correspondence should be addressed.
Received: 4 July 2014 / Revised: 13 August 2014 / Accepted: 15 August 2014 / Published: 27 August 2014
(This article belongs to the Special Issue Dosage Forms and Delivery Systems for Vaginal Therapy)
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Abstract

Different non-ionic cellulose ethers (methyl cellulose, MC; hydroxyethyl cellulose, HEC; hydroxypropyl cellulose, HPC; hydroxypropylmethyl cellulose, HPMC) and microcrystalline cellulose (MCC) were investigated as matrix formers for preparation of mini-tablets targeting vaginal drug delivery. Hexyl aminolevulinat hydrochloridum (HAL) was used as a model drug. The mini-tablets were characterized with respect to their mechanical strength, bioadhesion towards cow vaginal tissue in two independent tests (rotating cylinder test, detachment test using texture analyzer), and dissolution rate in two media mimicking the pH levels of fertile, healthy and post-menopausal women (vaginal fluid simulant pH 4.5, phosphate buffer pH 6.8). Mini-tablets with a matrix of either HPMC or HPC were found to possess adequate mechanical strength, superior bioadhesive behavior towards vaginal tissue, and pH independent controlled release of the model drug, suggesting that both systems would be suited for the treatment of women regardless of age, i.e., respective of their vaginal pH levels. Bioadhesive mini-tablets offer a potential for improved residence time in the vaginal cavity targeting contact with mucosal tissue and prolonged release of the drug. View Full-Text
Keywords: bioadhesive polymers; vaginal application; multi-particulates; non-ionic cellulose ethers; hexyl aminolevulinat hydrochloridum bioadhesive polymers; vaginal application; multi-particulates; non-ionic cellulose ethers; hexyl aminolevulinat hydrochloridum
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Hiorth, M.; Nilsen, S.; Tho, I. Bioadhesive Mini-Tablets for Vaginal Drug Delivery. Pharmaceutics 2014, 6, 494-511.

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