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      Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs

      review-article
      1 , 2 , 1 , 3 , * , 3
      Journal of Drug Delivery
      Hindawi Publishing Corporation

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          Abstract

          Oral administration is the most commonly used and readily accepted form of drug delivery; however, it is find that many drugs are difficult to attain enough bioavailability when administered via this route. Polymeric micelles (PMs) can overcome some limitations of the oral delivery acting as carriers able to enhance drug absorption, by providing (1) protection of the loaded drug from the harsh environment of the GI tract, (2) release of the drug in a controlled manner at target sites, (3) prolongation of the residence time in the gut by mucoadhesion, and (4) inhibition of efflux pumps to improve the drug accumulation. To explain the mechanisms for enhancement of oral bioavailability, we discussed the special stability of PMs, the controlled release properties of pH-sensitive PMs, the prolongation of residence time with mucoadhesive PMs, and the P-gp inhibitors commonly used in PMs, respectively. The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.

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          Most cited references180

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          Mucus-penetrating nanoparticles for drug and gene delivery to mucosal tissues.

          Mucus is a viscoelastic and adhesive gel that protects the lung airways, gastrointestinal (GI) tract, vagina, eye and other mucosal surfaces. Most foreign particulates, including conventional particle-based drug delivery systems, are efficiently trapped in human mucus layers by steric obstruction and/or adhesion. Trapped particles are typically removed from the mucosal tissue within seconds to a few hours depending on anatomical location, thereby strongly limiting the duration of sustained drug delivery locally. A number of debilitating diseases could be treated more effectively and with fewer side effects if drugs and genes could be more efficiently delivered to the underlying mucosal tissues in a controlled manner. This review first describes the tenacious mucus barrier properties that have precluded the efficient penetration of therapeutic particles. It then reviews the design and development of new mucus-penetrating particles that may avoid rapid mucus clearance mechanisms, and thereby provide targeted or sustained drug delivery for localized therapies in mucosal tissues.
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            Oral drug delivery with polymeric nanoparticles: the gastrointestinal mucus barriers.

            Oral delivery is the most common method for drug administration. However, poor solubility, stability, and bioavailability of many drugs make achieving therapeutic levels via the gastrointestinal (GI) tract challenging. Drug delivery must overcome numerous hurdles, including the acidic gastric environment and the continuous secretion of mucus that protects the GI tract. Nanoparticle drug carriers that can shield drugs from degradation and deliver them to intended sites within the GI tract may enable more efficient and sustained drug delivery. However, the rapid secretion and shedding of GI tract mucus can significantly limit the effectiveness of nanoparticle drug delivery systems. Many types of nanoparticles are efficiently trapped in and rapidly removed by mucus, making controlled release in the GI tract difficult. This review addresses the protective barrier properties of mucus secretions, how mucus affects the fate of orally administered nanoparticles, and recent developments in nanoparticles engineered to penetrate the mucus barrier. Copyright © 2011 Elsevier B.V. All rights reserved.
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              Drug-like properties and the causes of poor solubility and poor permeability

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                Author and article information

                Journal
                J Drug Deliv
                J Drug Deliv
                JDD
                Journal of Drug Delivery
                Hindawi Publishing Corporation
                2090-3014
                2090-3022
                2013
                27 June 2013
                : 2013
                : 340315
                Affiliations
                1School of Pharmaceutical Science, Shandong University, Jinan 250012, China
                2Department of Pharmacy, Shandong Provincial Qian Foshan Hospital, Jinan 250014, China
                3Institute of Biopharmaceuticals of Shandong Province, Jinan 250101, China
                Author notes
                *Peixue Ling: lpx@ 123456sdfmg.com

                Academic Editor: Juan M. Irache

                Author information
                http://orcid.org/0000-0003-1548-7299
                Article
                10.1155/2013/340315
                3712247
                23936656
                50541ad2-2589-4c64-9f83-3214799de4b2
                Copyright © 2013 Wei Xu et al.

                This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                : 28 March 2013
                : 4 June 2013
                : 11 June 2013
                Categories
                Review Article

                Pharmaceutical chemistry
                Pharmaceutical chemistry

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