Optimization of the supercritical fluidized bed process for sirolimus coating and drug release

Optimizing Paclitaxel Oral Absorption and Bioavailability: TPGS Co-Coating via Supercritical Anti-Solvent Fluidized Bed Technology

“…Screening experiments confirmed that operating at 45 °C and 80 bar represented the optimal conditions for the SAS-FB process within this study system. Consistent trends were observed for PTX coating efficiency compared to previous findings with sirolimus and three flavonoids [ 26 , 27 ]. These findings established that the optimal conditions for the SAS-FB process corresponded to the low-density region of SC-CO 2 at high temperature and low pressure, facilitating drug precipitation.…”

“…SEM images revealed that PTX particles in the SAS-FB sample were smaller and evenly dispersed on lactose surface, preventing crystal growth and aggregation. This result suggests that the SAS-FB process holds promise in resolving challenges posed by insoluble BCS class II and IV drugs, offering valuable support for handling such compounds [ 26 , 27 , 28 , 30 ]. Additionally, considering that excipients can exert their inhibitory effect on P-gp below the critical micelle concentration (CMC) [ 32 ], the SAS-FB and SAS-FB (TPGS) samples, which demonstrated high drug loading capacity and superior in vitro dissolution, were selected for further studies.…”

“…However, these particles tend to agglomerate due to their high surface energy, leading to poor flowability and difficulties in subsequent processing, limiting the application of SAS technology. To address this issue, SAS-precipitated drugs were combined with a coating process inside a dynamic fluidized bed (FB) to develop highly dispersed drug-loaded particles [ 26 , 27 , 28 ]. This approach, termed the supercritical anti-solvent fluidized bed (SAS-FB) procedure, achieves one-step simultaneous precipitation and coating, significantly enhancing drug dissolution and bioavailability.…”

“…Through SAS-FB, uniform curcumin precipitation onto lactose surfaces with coating efficiencies ranging from 71.0% to 93.3% and particle sizes between 0.41 and 12.08 μm can be achieved [ 29 ]. SAS-FB-processed Sirolimus demonstrated enhanced solubility and oral bioavailability [ 26 ], with additional improvements achieved by incorporating excipients into the SAS-FB process for co-precipitation with the drug [ 30 ]. In addition, flavonoids such as luteolin, naringenin, and dihydromyricetin achieved particle size reduction, solubility enhancement, and antioxidant activity increase through the SAS-FB process [ 27 ].…”

Tenoxicam (Mobiflex) Solubility in Carbon Dioxide under Supercritical Conditions

“…In pharmaceutical manufacturing of solid dosage oral formulations, the drug particles at micron or submicron sizes are favorable due to enhanced solubility of drugs at small size and the subsequent higher bioavailability of micron-sized drugs. Indeed, the SC technology can be utilized to prepare drug particles with engineered size and structure for advanced manufacturing. − However, understanding the process is of great importance for implementing this novel technology for solid dosage drug production at the industrial scale. The common parameter in all SC-based technologies applicable for pharmaceutical manufacturing that must be known for the desired micronization process is drug solubility versus temperature/pressure.…”