Development and evaluation of stavudine loaded injectable polymeric particulate systems

Area of Science:

• Pharmaceutics
• Biomaterials Science
• Drug Delivery Systems

Background:

• Human Immunodeficiency Virus (HIV) infection requires long-term management to delay Acquired Immunodeficiency Syndrome (AIDS) progression.
• Parenteral delivery systems aim to improve drug efficacy and patient compliance through sustained release.
• Biodegradable polymers offer a promising platform for developing advanced drug delivery depots.

Purpose of the Study:

• To formulate and characterize stavudine-loaded biodegradable microspheres for parenteral depot administration.
• To evaluate the influence of formulation variables on microsphere properties and drug release kinetics.
• To assess the potential of Poly (D, L Lactide-co-glycolide) microspheres for prolonged stavudine delivery.

Main Methods:

• Microspheres were prepared using the solvent evaporation technique with Poly (D, L Lactide-co-glycolide) (PLGA) grades (85:15 and 50:50).
• Various drug/polymer ratios and surfactant concentrations were investigated.
• Microsphere characterization included yield, entrapment efficiency, particle size, SEM, DSC, XRD, and in vitro release studies.

Main Results:

• Microspheres exhibited favorable surface topography and drug distribution.
• Maximum entrapment efficiency reached 68.0 ± 1.62% with particle diameters under 100µm.
• In vitro studies demonstrated 80-90% drug release over 6-8 weeks, following Higuchi kinetics and anomalous transport mechanisms.

Conclusions:

• Biodegradable PLGA microspheres are a feasible parenteral depot system for stavudine.
• The developed system offers prolonged drug release, potentially reducing HIV symptom severity and delaying AIDS progression.
• Further investigation into in vivo performance is warranted for clinical application.