Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Abstract

Solid dispersion is the preferred technology to prepare efficacious forms of BCS class-II/IV APIs. To prepare solid dispersions, there exist a wide variety of polymeric carriers with interesting physicochemical and thermochemical characteristics available at the disposal of a formulation scientist. Since the advent of the solid dispersion technology in the early 1960s, there have been more than 5000 scientific papers published in the subject area. This review discusses the polymeric carrier properties of most extensively used polymers PVP, Copovidone, PEG, HPMC, HPMCAS, and Soluplus® in the solid dispersion technology. The literature trends about preparation techniques, dissolution, and stability improvement are analyzed from the Scopus® database to enable a formulator to make an informed choice of polymeric carrier. The stability and extent of dissolution improvement are largely dependent upon the type of polymeric carrier employed to formulate solid dispersions. With the increasing acceptance of transfer dissolution setup in the research community, it is required to evaluate the crystallization/precipitation inhibition potential of polymers under dynamic pH shift conditions. Further, there is a need to develop a regulatory framework which provides definition and complete classification along with necessarily recommended studies to characterize and evaluate solid dispersions.

Salts of purine alkaloids caffeine and theobromine with 2,6-dihydroxybenzoic acid as coformer: structural, theoretical, thermal and spectroscopic studies

“…The search for the appropriate form of a drug is often difficult and time-consuming because, on the one hand, its pharmacological action must be maintained or improved and, on the other hand, its physicochemical properties, which have a direct impact on its activity, should be improved (Kumar & Nanda, 2018;Yadav et al, 2009). Many methods are known to improve the physicochemical properties of an API, such as particle size reduction (Fang et al, 2020), synthesis of solid dispersion (Nair et al, 2020;Sareen et al, 2012), nanoparticles (Kumar et al, 2020), self-emulsifying drug delivery (SEEDS) (Pehlivanov, 2020), nanosuspension (Stefan et al, 2020) or advanced lipid technologies (ALT) (Lopez-Toledano et al, 2019). Another method is to introduce guest molecules into the crystal structure of an API, which is still a very popular method (Dai et al, 2018).…”

New Insights on Solvent Implications in the Design of Materials Based on Cellulose Derivatives Using Experimental and Theoretical Approaches

“…For example, a modeling technique of three-dimensional solubility was developed by Hansen [41,54], which considered that the total solubility parameter of a polymer represents a point located in three-dimensional space. This point is the center of a sphere, so-called Hansen solubility sphere, with radius R 0 , named the interaction radius of that polymer defined by Equation (21).…”

“…Nowadays, cellulose derivatives gained substantial consideration, due to their specific properties, e.g., biodegradability, biocompatibility, nontoxicity, solubility in water, etc., having large applicability in the chemical industries, biomedical, pharmaceutical, cosmetics, water desalination [1,2,21,22], as an effect of special viscometric behavior in solution. Particular properties of these derivatives can be optimized by utilization of polymer blends principle, which permits attaining of new models of materials, with a wide range of qualities [23].…”

“…Besides, the use of water as a solvent for HPMC and PVP can influence their flow behavior, and hence, the finite product performance [27]. Taking into account all the above, in the present study, (hydroxypropyl)methyl cellulose and poly(vinylpyrrolidone) were selected due to their excellent physical properties, including their solubility in water, absence of toxicity, high hydrophilicity, flexibility, film-forming, and outstanding chemical and thermal stabilities [1][2][3]15,18,21,23,28]. Based on such versatile properties, an extensive attention was accorded to the use of both polymers as multifunctional materials for a variety of applications.…”

Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual Behavior Studies in Male Rats

“…In order to molecularly dissolve the drug, a large quantity of the hydrophilic polymer is used, which in turn increases the physical instability of the dispersions due to phase separation. The mechanisms involved in the improved solubility and dissolution include the detachment of drug molecules as the hydrophilic carrier dissolves, subsequently forming a supersaturated solution of the drug [ 18 , 19 , 20 , 21 , 22 ]. A study on SDs using a ibuprofen model drug revealed that polymers under the trade names “poloxamer 407” and “poloxamer 188” could increase the solubility and reduce the crystal growth of the drug with their coexistence in the polymeric dispersion, which could have been due to the disruption of the ibuprofen and formation of hydrogen bonds between the drug and polymer [ 23 ].…”