Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies

• Published in: Acta pharmaceutica Sinica. B Vol. 11; no. 8; pp. 2505 - 2536
• Main Authors: Bhujbal, Sonal V., Mitra, Biplob, Jain, Uday, Gong, Yuchuan, Agrawal, Anjali, Karki, Shyam, Taylor, Lynne S., Kumar, Sumit, (Tony) Zhou, Qi
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.08.2021; Elsevier
• Subjects: Amorphous solid dispersions; Co-precipitation; Downstream processing; Drug delivery; Manufacturing; Melting process; Review; Selection criteria; Solvent evaporation; Stability; SAS; CO2; SEDS; Drug delivery; Amorphous solid dispersions; PVP; FDM; Solvent evaporation; Tg; CSG; Soluplus; Manufacturing; SCFs; SLS; Co-precipitation; Selection criteria; HME; Stability; USC; Downstream processing; Melting process; Eudragit; HPMCP; PCA; PGSS; CAP; PLGA; scCO2; RESS; GAS; HPMCAS; HPC; PVPVA; EPAS; ASES; ASDs; HPMC; 3DP; Soluplus®, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; scCO2, supercritical CO2; PGSS, precipitation from gas-saturated solutions; 3DP, three-dimensional printing; PLGA, poly(lactic-co-glycolic acid; CSG, continuous-spray granulation; HPC, hydroxypropyl cellulose; Eudragit®, polymethacrylates derivatives; GAS, gas antisolvent; FDM, fused deposition modeling; PVP, polyvinylpyrrolidone; Tg, glass transition temperature; CAP, cellulose acetate phthalate; PCA, precipitation with compressed fluid antisolvent; SCFs, supercritical fluids; EPAS, evaporative aqueous solution precipitation; HME, hot-melt extrusion; PVPVA, polyvinylpyrrolidone/vinyl acetate; SAS, supercritical antisolvent; SLS, selective laser sintering; ASDs, amorphous solid dispersions; USC, ultrasound compaction; CO2, carbon dioxide; ASES, aerosol solvent extraction system; HPMC, hydroxypropyl methylcellulose; SEDS, solution-enhanced dispersion by SCF; HPMCAS, hydroxypropyl methylcellulose acetate succinate; HPMCP, hypromellose phthalate; RESS, rapid expansion of a supercritical solution
• ISSN: 2211-3835; 2211-3843
• DOI: 10.1016/j.apsb.2021.05.014

Amorphous solid dispersions (ASDs) are popular for enhancing the solubility and bioavailability of poorly water-soluble drugs. Various approaches have been employed to produce ASDs and novel techniques are emerging. This review provides an updated overview of manufacturing techniques for preparing ASDs. As physical stability is a critical quality attribute for ASD, the impact of formulation, equipment, and process variables, together with the downstream processing on physical stability of ASDs have been discussed. Selection strategies are proposed to identify suitable manufacturing methods, which may aid in the development of ASDs with satisfactory physical stability. The review provides an updated overview of amorphous solid dispersion (ASD) manufacturing techniques. The impact of manufacturing variables of each method and downstream processing on the critical physical stability of ASDs are discussed. [Display omitted]