Related Experiment Video
Updated: Jul 19, 2025
07:32
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
11.4K
Intramuscularly Administered PLGA Microparticles for Sustained Release of Rivastigmine: In Vitro, In Vivo and
Javier Avendaño-Godoy1, Arnoldo Miranda2, Sigrid Mennickent1
1Departamento de Farmacia, Facultad de Farmacia, Universidad de Concepción, Concepción, Chile.
Journal of Pharmaceutical Sciences
|August 18, 2023
Summary
This study developed polylactic-co-glycolic acid (PLGA) microparticles for sustained intramuscular delivery of rivastigmine, an Alzheimer's dementia drug. The formulation demonstrated stability and effective sustained release in vivo, offering a promising alternative to oral therapy.
Area of Science:
- Biomaterials Science
- Pharmaceutical Sciences
- Neuroscience
Background:
- Rivastigmine, an acetylcholinesterase (AchE) and butyrylcholinesterase (BchE) inhibitor, treats Alzheimer's dementia but suffers from poor oral tolerability due to first-pass metabolism and gastrointestinal side effects.
- Intramuscular (IM) sustained-release formulations offer a potential solution to overcome the limitations of oral rivastigmine therapy.
Purpose of the Study:
- To develop polylactic-co-glycolic acid (PLGA) microparticles for sustained rivastigmine release via IM administration.
- To evaluate the stability, in vitro release, and in vivo pharmacokinetics of the rivastigmine-loaded PLGA microparticles.
Main Methods:
- Rivastigmine-loaded PLGA microparticles were fabricated using the solvent evaporation emulsion method.
- Formulation parameters were optimized to achieve desired encapsulation efficiency and drug loading.
- Characterization included particle size, surface morphology (SEM), drug-polymer interaction (FT-IR), stability studies under various storage conditions, in vitro drug release, and in vivo pharmacokinetic analysis in rats following IM administration.
Main Results:
- Optimized PLGA microparticles achieved an encapsulation efficiency of 54.8% and a rivastigmine load of 3.3%.
- Microparticles exhibited a spherical shape (56.1 μm) with no chemical interaction between rivastigmine and PLGA, maintaining stability for at least 6 months under refrigerated and accelerated conditions.
- In vitro and in vivo studies confirmed sustained release of rivastigmine, and IM administration showed no significant tissue damage in rats.
Conclusions:
- PLGA microparticles provide a stable and effective system for sustained intramuscular delivery of rivastigmine.
- This novel formulation demonstrates potential to improve Alzheimer's dementia treatment by enhancing tolerability and efficacy compared to oral rivastigmine.
- Further studies with multiple doses are recommended to fully assess tolerability in chronic treatment scenarios.
