Supercritical fluid coating of API on excipient enhances drug release

Abstract

A process to coat particles of active pharmaceutical ingredient (API) onto microcrystalline cellulose (MCC) excipient shows promise as a new way to dosage forms showing enhanced drug release. The process consists of a fluidized bed operated at elevated pressure in which API particles are precipitated from a Supercritical Anti-Solvent process (SAS). MCC particles were used as an excipient in the fluidized bed and collect the SAS-generated API particles. Naringin was selected as the model API to coat onto MCC. A number of operational parameters of the process were investigated: fluidization velocity, coating pressure, temperature, concentration of drug solution, drug solution flow rate, drug mass, organic solvent, MCC mass and size and CO2-to-organic solution ratio. SEM and SPM analyses showed that the MCC particle surfaces were covered with near-spherical nanoparticles with a diameter of approximately 100– 200 nm, substantially smaller than the as-received API material. XRD showed that naringin changed from crystalline to amorphous during processing. The coated particles resulting from the SAS fluidized bed process have a higher loading of API, gave faster release rates and higher release ratios in comparison with those produced using a conventional fluidized bed coating process. The approach could be transferred to other industries where release is important such as agrochemical, cosmetic and food

Supercritical fluid coating of flavonoids on excipients enhances drug release and antioxidant activity

“…The drug particles precipitated from the SAS process are captured on the surface of the carrier instantly, without risks of agglomeration, and retain similar properties to the original nanoscale to microscale drug particles, thus increasing the solubility and flowability of the drug. Li et al (Li et al, 2017) coated amorphous naringin nanoparticles on microcrystalline cellulose (MCC) and showed complete dissolution within 1 min. Therefore, SAS-FB offers an effective alternative to improve the release and bioavailability of poorly soluble flavonoids and their antioxidant activity can be maintained in solid dosage forms.…”

Synthesis of Celecoxib-Eutectic Mixture Particles via Supercritical CO2 Process and Celecoxib Immediate Release Tablet Formulation by Quality by Design Approach

“…Figure 6 shows SAS, SCF assisted mixing and spray drying CEL EM under optical microscopy. Obtained SAS crystallization CEL-EM were like snow flakes; the cause of this flake shape is the rapid depressurization of CEL in SCF [ 21 ]. The same phenomenon happened to SCF assisted mixing where CEL was dissolved in SCF, but the formed particles were not uniform because the samples went from a completely amorphous state at low tempreture to a nearly amorphous state at ambient temprature; during that process, recrystalization occurred.…”

Microencapsulation and Nanoencapsulation Using Supercritical Fluid (SCF) Techniques

“…The supercritical CO 2 plays the role of a drying medium (for aqueous solutions) or an antisolvent (for organic solutions) to dry the fluidized particles in the bed. The coating of API and ingredients such as curcumin has been demonstrated using supercritical fluid coating processes [61,63,64,65]. This technique has promising development for the production of controlled multi-layered coatings on APIs to achieve formulations with desired sustained release or surface properties.…”