Development of Sustained Release Lipid-Based Matrix Microparticles for Vaginal Delivery using Twin-Screw Hot Melt Extrusion
![Illustration of cracks appeared after heating up and cooling down until room temperature.](https://www.pharmaexcipients.com/wp-content/uploads/2020/11/Development-of-Sustained-Release-Lipid-Based-Matrix-Microparticles-for-Vaginal-Delivery-using-Twin-Screw-Hot-Melt-Extrusion.png)
PURPOSE
- The development of sustained-release formulations for drugs administered via the vaginal route has the potential to increase treatment efficiency and patient compliance.
- One promising strategy to formulate such dosage forms is the incorporation of microparticles into a bio-adhesive gel.
OBJECTIVE
- To assess feasibility of formulating matrix microparticles using lipid-based carrier systems,
- namely, Syncrowax™ HGLC (hydrophobic insoluble lipid) or Gelucire® 50/13 (G-50/13; hydrophilic lipid),
- with Avicel® PH-101 (MCC) or hypromellose K100M used as diluents.
CONCLUSIONS
- The number of drug-loaded formulations was successfully reduced due to the screening of placebo formulations with WU/WL test.
- Insoluble matrix system based on the insoluble lipid Syncrowax™ HGLC (≥80 % w/w) and loaded with model drugs AZT or MTZ was successfully prepared using the twin-screw hot melt extrusion method and provided as sustained release.
- The addition of diluents as Avicel® PH-101 or hypromellose type K100M (at the 10% w/w level) can be used for the adjustment of drug release profile.
- The development of cracks in the Syncrowax™ HGLC lipid matrix during the cooling down stage could be accounted as an additional aspect of drug release facilitation.
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Authors: V. Mohylyuk, T. Hutton, S. Dadou, S. Li, D.S. Jones, G.P. Andrews.