Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology
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.
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or continue reading here: Nair, A.R., Lakshman, Y.D., Anand, V.S.K. et al. Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology. AAPS PharmSciTech 21, 309 (2020). https://doi.org/10.1208/s12249-020-01849-z
This article gives a great overview and covers the following topics:
- CLASSIFICATION OF POLYMERIC CARRIERS
- SELECTION CRITERIA FOR POLYMERIC CARRIERS
- VINYL PYRROLIDONE DERIVATIVES
- POLY VINYL PYRROLIDONE (PVP)
- COPOVIDONE
- POLY ETHYLENE GLYCOL (PEG)
- CELLULOSE DERIVATIVES
- HYDROXY PROPYL METHYL CELLULOSE (HPMC)
- HYDROXY PROPYL METHYL CELLULOSE ACETATE SUCCINATE (HPMCAS)
- SOLUPLUS®
- MANUFACTURING ISSUES OF POLYMERS IN SOLID DISPERSION TECHNOLOGY
Some interesting “outtakes” from this publication
Table I Various Types of Solid Dispersions and Their Relative Potential for Stability and Solubility Improvement
Table II Physicochemical Properties of Polymers Commonly Used in the Preparation of Solid Dispersions
| Polymer | Type | Physical form | Molecular weight (g/Mol) | Water solubility | Hygroscopicity | Glass transition/Melting temperature (°C) | Degradation temperature (°C) | Solubility parameter (Mpa1/2) |
|---|---|---|---|---|---|---|---|---|
| Poly-Vinyl-Pyrrolidone (PVP) | PVP K-12 | Amorphous | 5000 | Water soluble | High | 120a | 196 | 21.74 |
| Poly-Vinyl-Pyrrolidone (PVP) | PVP K-15 | Amorphous | 9700 | Water soluble | High | 130a | 215 | 21.63 |
| Poly-Vinyl-Pyrrolidone (PVP) | PVP K-30 | Amorphous | 66,800 | Water soluble | High | 163a | 171 | 21.69 |
| Poly-Vinyl-Pyrrolidone (PVP) | PVP K-60 | Amorphous | 396,000 | Water soluble | High | 170a | NA | 21.7 |
| Poly-Vinyl-Pyrrolidone (PVP) | PVP K-90 | Amorphous | 1,570,000 | Water soluble | High | 174a | 194 | 21.73 |
| Poly-Vinyl-Pyrrolidone (PVP) | PVP K-120 | Amorphous | 3,470,000 | Water soluble | High | 174a | 194 | 21.7 |
| Copovidone | Copovidone | Amorphous | 45,000–70,000 | Amphiphilic | Moderate | 100–105 | 230 | 21.2 |
| Poly ethylene glycol (PEG) | PEG 400 | Crystalline | 400 | Intermediate | High | NA | NA | 18.9 |
| Poly ethylene glycol (PEG) | PEG 600 | Crystalline | 600 | Intermediate | High | NA | 160 | 23.7 |
| Poly ethylene glycol (PEG) | PEG 800 | Crystalline | 800 | Intermediate | High | NA | 160 | 23.7 |
| Poly ethylene glycol (PEG) | PEG 1000 | Crystalline | 1000 | Intermediate | Moderate | 37–40 | 160 | 23.7 |
| Poly ethylene glycol (PEG) | PEG 1500 | Crystalline | 1500 | Intermediate | Moderate | 44–48 | 160 | 23.7 |
| Poly ethylene glycol (PEG) | PEG 2000 | Crystalline | 2000 | Intermediate | Moderate | 45–50 | 160 | 17.6 |
| Poly ethylene glycol (PEG) | PEG 3000 | Crystalline | 3000 | Intermediate | Moderate | 48–54 | NA | NA |
| Poly ethylene glycol (PEG) | PEG 4000 | Crystalline | 4000 | Intermediate | Moderate | 50–58 | NA | NA |
| Poly ethylene glycol (PEG) | PEG 6000 | Crystalline | 6000 | Intermediate | Moderate | 55–63 | NA | NA |
| Poly ethylene glycol (PEG) | PEG 8000 | Crystalline | 8000 | Intermediate | Moderate | 60–63 | NA | 19.8 |
| Poly ethylene glycol (PEG) | PEG 10000 | Crystalline | 10,000 | Intermediate | Moderate | 62–65 | NA | 16.6 |
| Poly ethylene glycol (PEG) | PEG 20000 | Crystalline | 20,000 | Intermediate | Moderate | 60–63 | NA | NA |
| Hydroxypropyl methylcellulose (HPMC) | HPMC-E | Amorphous | 85,000–150,000 | Water soluble | High | 141c | NA | 29.95b |
| Hydroxypropyl methylcellulose (HPMC) | HPMC-F | Amorphous | 85,000–150,000 | Water soluble | High | 160c | 240 | 29.05b |
| Hydroxypropyl methylcellulose (HPMC) | HPMC-K | Amorphous | 85,000–150,000 | Water soluble | High | 172c | 260 | 30.57b |
| Hydroxypropyl methylcellulose acetate succinate (HPMCAS) | HPMCAS L | Amorphous | 50,000 | Water soluble above pH 5.0 | High | 119 | 204 | 29.1 |
| Hydroxypropyl methylcellulose acetate succinate (HPMCAS) | HPMCAS M | Amorphous | 50,000 | Water soluble above pH 5.0 | High | 120 | 190 | 29.1 |
| Hydroxypropyl methylcellulose acetate succinate (HPMCAS) | HPMCAS H | Amorphous | 50,000 | Water soluble above pH 5.0 | High | 122 | NA | 29.1 |
| Soluplus® | Soluplus® | Amorphous | 118,000 | Amphiphilic | Moderate | 70 | 250 | 19.4 |