Title:Drug Delivery through Co-amorphous Solid Dispersions: A Comprehensive and Updated Review on Physicochemical Characteristics and Biological Potential
Volume: 19
Issue: 4
Author(s): Shailender Mohan and Abdul Hafeez*
Affiliation:
- Faculty of Pharmacy, Integral University, Lucknow, 226026, India
Keywords:
Co-amorphous solid dispersion, biological potential, co-former, physical stability, solubility improvement, bioavailability enhancement.
Abstract: New chemical entities with low aqueous solubility and permeability encounter significant
challenges in formulation development. Low solubility is further accompanied by slow dissolution
and poor bioavailability, which in turn leads to unpredictability in terms of both bioavailability
and toxicity. Therefore, a significant amount of exertion is necessary to enhance solubility, dissolution,
and eventually bioavailability. Additionally, to enhance the solubility properties and amorphous
stability of BCS Class II medications and ultimately increase drug bioavailability, coamorphization
has emerged as a promising strategy. Co-amorphous solid dispersions (CASD) are
multi-component single-phase amorphous solid dispersions comprising two or more small molecules
(usually known as co-formers) that might be a combination of drug-drug or drug-excipients.
The selection of appropriate co-formers is critical, and the surface properties of co-amorphous formulations
must be carefully evaluated, as they influence physical and chemical stability in addition
to dissolution performance. Scaling up and processing co-amorphous formulations into the final
dosage forms presents challenges that need to be addressed. This review will largely concentrate on
the challenges, improvements, and innovations in physicochemical properties, biological characterization,
and advancements of co-amorphous systems. This review will also furnish a comprehensive
explanation of both established and emerging approaches utilized in the estimation of physicochemical
attributes and characterization of CASD (in vitro and in vivo). Regarding CASD’s potential to
improve patient outcomes and therapeutic efficacy, it has emerged as a viable approach for drug
candidates posing the problems of solubility and bioavailability. This approach has also increased
the physical stability of drugs.