Abstract
Polyelectrolyte polymers have been widely used in the pharmaceutical field as excipients to facilitate various drug delivery systems. Polyelectrolytes have been used to modulate the electrostatic environment and enhance favorable interactions between the drug and the polymer in amorphous solid dispersions (ASDs) prepared mainly by hot-melt extrusion. Polyelectrolytes have been used alone, or in combination with nonionic polymers as interpolyelectrolyte complexes, or after the addition of small molecular additives. They were found to enhance physical stability by favoring stabilizing intermolecular interactions, as well as to exert an antiplasticizing effect. Moreover, they not only enhance drug dissolution, but they have also been used for maintaining supersaturation, especially in the case of weakly basic drugs that tend to precipitate in the intestine. Additional uses include controlled and/or targeted drug release with enhanced physical stability and ease of preparation via novel continuous processes. Polyelectrolyte matrices, used along with scalable manufacturing methods in accordance with green chemistry principles, emerge as an attractive viable alternative for the preparation of ASDs with improved physical stability and biopharmaceutic performance.
Highlights
Over the past decades, novel drug delivery systems have been a key area of research into overcoming the limitations resulting from the development of poorly water-soluble drugs
The amorphous solid dispersion (ASD) method, where the drug is stabilized in the amorphous phase as it is incorporated into a polymeric matrix, is considered to be among the most desirable systems because of its high potential for solubility and bioavailability enhancement [3,7,8,9]
The use of interpolyelectrolyte complexes (IPECs), obtained as precipitates upon mixing polyelectrolytes with an opposite charge in aqueous media, has been reported as an effective approach to broaden the applicable polymers in oral drug delivery systems, and they could possibly be used as matrices in ASDs [109,110,111], Table 3
Summary
Novel drug delivery systems have been a key area of research into overcoming the limitations resulting from the development of poorly water-soluble drugs. Various formulation approaches have been utilized to overcome poor biopharmaceutical drug performance, such as the creation of prodrugs, cyclodextrin (CD) complexation, various nanotechnology techniques (nanocrystals, nanoemulsions, solid lipid particles etc.), liposomes, polymorphs, hydrates, cocrystals, and others [3,4,5,6] Among these strategies, the amorphous solid dispersion (ASD) method, where the drug is stabilized in the amorphous phase as it is incorporated into a polymeric matrix, is considered to be among the most desirable systems because of its high potential for solubility and bioavailability enhancement [3,7,8,9]. The uses for polyelectrolytes and polyelectrolyte complexes (PECs) are a field of increasing interest for ASD pharmaceutical applications, as they can promote strong intermolecular interactions of an electrostatic nature within the system They present high biocompatibility and lower toxicity compared to other polymeric carriers, and they have been reported to facilitate the release and dissolution of the drug [17,18]. This review thoroughly presents the applicability of the HME technique in the continuous, efficient, economical, and scalable formulation of ASDs, while modified polyelectrolyte matrices, and recently reported interpolyelectrolyte complexes as potential carriers for ASD formation, are extensively discussed
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