Development of Sustained Release Lipid-Based Matrix Microparticles for Vaginal Delivery using Twin-Screw Hot Melt Extrusion

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.

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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.

Authors: V. Mohylyuk, T. Hutton, S. Dadou, S. Li, D.S. Jones, G.P. Andrews.