Mucoadhesive therapeutic compositions: a patent review (2011-2014)

ABSTRACT

Introduction: With the introduction of mucoadhesion in 1980, pharmaceutical researchers have gained interest in mucoadhesive compositions. This interest has led to the development of mucoadhesive drug delivery systems aiming (I) to target a specific tissue, (II) to overcome barriers to absorption as well as (III) to control drug release of the therapeutic compositions.

Areas covered: In this review, the term mucoadhesion and a variety of targetable mucosa are described through review of the literature. Mucoadhesive drug delivery systems and mucoadhesive polymers, such as thiomers, which are reported within the patent literature or in related publications are described in detail, including their therapeutic uses.

Expert opinion: Mucoadhesion is associated with benefits such as controlled, sustained release, prolonged residence time at the site of action, the ability to target specific mucosae and ease of application which leads to higher rates of patient compliance. Although many research groups are investigating in this domain, not many drug delivery systems based on mucoadhesive polymers have got from bench to market. The most promising and advanced applications seen in patent literature within the last five years seems to be for oral application.

KEYWORDS:

• Mucoadhesion
• mucosa
• patents
• polymers
• thiomers

Article highlights

• Over recent decades mucoadhesion has attracted significant interest in pharmaceutical research.

• Mucoadhesive polymers have been investigated as promising drug delivery systems.

• Three generations of mucoadhesive polymers have been established in the pharmaceutical field.

• The pillars of mucoadhesion are stability, swelling behavior, the contact stage, and consolidation stage, as well as type of bond formation in relation to the characteristics of the target mucosa.

• A plethora of in vitro and in vivo studies has proven the potential of mucoadhesive drug delivery systems.

• Remarkable patents have been disclosed by the pharmaceutical market within the last 5 years.

This box summarizes key points contained in the article.

Financial and competing interests disclosure

The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.