Feasibility of AquasolveTM HPMC-AS Lg via Hot-melt Extrusion: Effect of Pressurized CO2 on Physico-mechanical Properties

The objective of the current study was to investigate the processability of Aquasolve™ HPMC-AS LG via hot-melt extrusion, and to examine the effect of pressurized carbon dioxide (P-CO2) on the physico-mechanical properties of Efavirenz (EFA)-loaded extrudates (EXT). EFA is as a poorly water-soluble drug and HPMC-AS LG was chosen as a carrier for this study. To optimize the process parameters and formulations, various physical mixtures were prepared with the following composition: EFA (30-40-50% w/w) and HPMC-AS LG (70-60-50 % w/w) respectively. Physical mixtures were extruded through the co-rotating twin-screw extruder (16mm Prism Euro Lab, Thermo Fisher Scientific) utilizing a standard screw configuration. P-CO 2 was injected into eight zone of extruder using a high-pressure regulator connected to flexible stainless-steel hose with armor casing. The thermal characterization of extrudates was obtained by using differential scanning calorimetry (DSC) and thermal gravimetric analysis (TGA). A scanning electron microscopy (SEM) was conducted to study morphology and porosity of formulations. The macroscopic morphology changed to a foam-like structure, resulting in increased specific surface area, porosity and dissolution rate. Thus, HPMC-AS LG extrudates with P-CO2 injection exhibited relatively higher dissolution rate than extrudates without P-CO2. Additionally, HPMC-AS LG was able to physically and chemically stabilize the amorphous state of high-loading EFA in the extrudates. The milling efficiency was improved for extrudates with P-CO2 injection due to porous nature and morphology changes.

Name thesis:degree_name

M.S. in Pharmaceutical Science

Level thesis:degree_level

Thesis

Discipline thesis:degree_discipline

Pharmaceutics and Drug Delivery

Year dc:date.available

2018

Author dc:creator

• Almutairi, Mashan

Contributors dc:contributor

• Michael A. Repka
• S. Narasimha Murthy
• Samir A. Ross

• Pharmacy and Pharmaceutical Sciences

Repository record dc:identifier

https://egrove.olemiss.edu/etd/1338

OAI identifier oai:identifier

oai:egrove.olemiss.edu:etd-2337