PLGA and Eudragit-based long-acting microspheres for Parkinson's disease management

Abstract

Oral medications available for Parkinson's disease require multiple administrations, which significantly affects the plasma concentration of the drug, and patients struggle to adhere to the treatment regimen due to the complexity of frequent dosing. Therefore, the idea of developing a long-acting biodegradable microsphere formulation was adopted. The biodegradable microspheres were prepared using a combination of PLGA_50:50 and Eudragit L-100. This combination incorporates the advantages of both PLGA_50:50 and Eudragit L-100 to achieve optimum drug release. The drug loaded was pramipexole. Since pramipexole is hydrophilic in nature, microspheres were fabricated using a double emulsion solvent evaporation process. The optimized microsphere formulation demonstrated an initial burst release of up to 24.18%, followed by a slow release of pramipexole for up to 18 days (93.78%) without the need to convert the drug into its salt form. The ex vivo drug release showed 78.96% release of pramipexole in 10 days. The optimized microspheres were further studied by DSC, FTIR, NMR, and SEM. The syringeability analysis of the microspheres, when suspended in sodium CMC solution, demonstrated an injectable force of 3.25 ± 0.24 N.