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

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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.