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Advances in the Development of Amorphous Solid Dispersions: the Role of Polymeric Carriers
Advances in the Development of Amorphous Solid Dispersions: the Role of Polymeric Carriers
Amorphous solid dispersion (ASD) is one of the most effective approaches for delivering poorly soluble drugs. In ASDs, polymeric materials serve as the carriers in which the drugs are dispersed at the molecular level. To prepare the solid dispersions, there are many polymers with various physicochemical and thermochemical characteristics available for use in ASD formulations. Polymer selection is of great importance because it influences the stability, solubility and dissolution rates, manufacturing process, and bioavailability of the ASD. This review article provides a comprehensive overview of ASDs from the perspectives of physicochemical characteristics of polymers, formulation designs and preparation methods. Furthermore, considerations of safety and regulatory requirements along with the studies recommended for characterizing and evaluating polymeric carriers are briefly discussed.
Table 3. Physicochemical properties of different types and grades of polymers used in ASD [14,15,[21], [22], [23], [24]].
| Category | Chemical name | Polymer type | Molecular weight | Solubility | Hygroscopicity | Tg (or Tm°C) | Degradation temperature (°C) |
|---|---|---|---|---|---|---|---|
| Polyvinyllactam polymers | PVP | Kollidon® 12 PF | 2,000 – 3,000 | Water soluble | High | 72 | 196 |
| Kollidon® 17 PF | 7,000 – 11,000 | 140 | 217 | ||||
| Kollidon® 25 | 28000 – 34,000 | 153 | 166 | ||||
| Kollidon® 30 | 44,000 – 54,000 | 160 | 171 | ||||
| Kollidon® 90F | 1,000,000 – 1,500,000 | 177 | 194 | ||||
| PVP/VA | Kollidon® VA64 | MW 45,000 – 70,000 | Water soluble | High | 105 | 270 | |
| Soluplus® | Soluplus® | MW 90,000 – 140,000 | Water soluble | High | 72 | 278 | |
| Cellulosic polymers | HPMC | Pharmacoat® 606 | MW – 10,000 | Water soluble | High | 139 | 244 |
| Methocel™ K100LV | MW – 25,000 | 147, 168 | 259 | ||||
| Methocel™ K100M | MW – 150,000 | 96, 173 | 259 | ||||
| HPC | Klucel® LF | MW – 95,000 | Water soluble | High | 0[25] | 170 | |
| HPMCAS | Shin-etsu AQOAT® MF | MW – 18,000 (3cps) | Dissolves above pH 5.0 | Low | 122 | 204 | |
| HPMCP | HP-55 | MW – 45,600 (40cps) | Dissolves above pH 5.0 | Low | 147 | 194 | |
| HP-50 | MW – 37,900 (55cps) | 143 | 199 | ||||
| CAP | N/A | MW – 2534.12 | Dissolves at higher pH (more than 6) | Low | 175 | 200 | |
| Acrylate and methacrylate (co-)polymers | Eudragit®E PO | N/A | MW – 47,000 Da | Dissolves in gastric fluid below pH 5.0 | Low | 52 | 250 |
| Eudragit®L 100 | N/A | MW – 125,000 | Dissolves above pH 6.0 | Low | 195 | 176 | |
| Eudragit®S 100 | N/A | MW – 125,000 | Dissolves above pH 7.0 | Low | 173 | 173 | |
| Eudragit®L 100-55 | N/A | MW – 320,000 | Dissolves above pH 5.5 | Low | 111 | 176 | |
| Other polymers | PVAP | N/A | MW 47,000–60,700 | Dissolves above pH 5 | Low | 42.5 | 150 |
| PAA | N/A | MW 1,800–450,000 | Water soluble | Low | 126 | 200 | |
| PEG/PEO | N/A | MW 1,000–7,000,000 | Water soluble | Low | Tm=55-66 | >200 | |
| Poloxamer | N/A | MW 7,600–17,400 | Water soluble | Low | Tm=52-57 | >200 |
Download the full article as PDF here: Advances in the Development of Amorphous Solid Dispersions: the Role of Polymeric Carriers
or read it here
Jie Zhang, Minshan Guo, Minqian Luo, Ting Cai, Advances in the Development of Amorphous Solid Dispersions: the Role of Polymeric Carriers, Asian Journal of Pharmaceutical Sciences, 2023, 100834, ISSN 1818-0876,
https://doi.org/10.1016/j.ajps.2023.100834.
