Assessing Mucoadhesion in Polymer Gels: The Effect of Method Type and Instrument Variables.

Jéssica Bassi Da Silva,Adriano Reis,Michael Cook,Marcos Bruschi,Sabrina Ferreira

doi:10.3390/polym10030254

Jéssica Bassi Da Silva, Adriano Reis + Show 3 more

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https://doi.org/10.3390/polym10030254

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Abstract

The process of mucoadhesion has been widely studied using a wide variety of methods, which are influenced by instrumental variables and experiment design, making the comparison between the results of different studies difficult. The aim of this work was to standardize the conditions of the detachment test and the rheological methods of mucoadhesion assessment for semisolids, and introduce a texture profile analysis (TPA) method. A factorial design was developed to suggest standard conditions for performing the detachment force method. To evaluate the method, binary polymeric systems were prepared containing poloxamer 407 and Carbopol 971P®, Carbopol 974P®, or Noveon® Polycarbophil. The mucoadhesion of systems was evaluated, and the reproducibility of these measurements investigated. This detachment force method was demonstrated to be reproduceable, and gave different adhesion when mucin disk or ex vivo oral mucosa was used. The factorial design demonstrated that all evaluated parameters had an effect on measurements of mucoadhesive force, but the same was not observed for the work of adhesion. It was suggested that the work of adhesion is a more appropriate metric for evaluating mucoadhesion. Oscillatory rheology was more capable of investigating adhesive interactions than flow rheology. TPA method was demonstrated to be reproducible and can evaluate the adhesiveness interaction parameter. This investigation demonstrates the need for standardized methods to evaluate mucoadhesion and makes suggestions for a standard study design.

Highlights

Mucosal surfaces cover the nasal, ocular, buccal, rectal, vaginal, and gastrointestinal areas among other parts of the body
poloxamer 407 (P407) increases the viscosity of the system and the other decreases it (C971P, Carbopol 974P® (C974P), or PCB)
This study utilized the tensile strength method with porcine mucin disks and porcine oral mucosa, flow and oscillatory rheometry, as well as texture profile analysis, to evaluate the mucoadhesive performance of the three polymeric systems composed of poloxamer 407 and poly(acrylic acid) derivatives

Summary

Introduction

Mucosal surfaces cover the nasal, ocular, buccal, rectal, vaginal, and gastrointestinal areas among other parts of the body. Drugs may be administered to these sites for local effect, and their high permeability makes them attractive for systemic drug delivery. Mucoadhesive polymers are a group of materials employed in different pharmaceutical systems. They are defined as hydrophilic macromolecules, which contain numerous functional organic groups (i.e., carboxylic, hydroxyl, amide, and amine groups) able to establish interactions with mucosal membranes [6,7]. These polymers can be classified according to their interactions with the mucosa (covalent bonds or non-covalent intermolecular interactions). Non-covalent bonds believed to enhance mucoadhesion include hydrogen-bonding, hydrophobic interactions, and electrostatic interactions

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