Formulation, Characteristic Evaluation, Stress Test and Effectiveness Study of Matrix Metalloproteinase-1 (MMP-1) Expression of Glutathione Loaded Alginate Microspheres and Gel

Abstract

Background: The present study aimed to formulate and evaluate the stability, characteristics and effectiveness of glutathione-loaded alginate microspheres through increased lipophilicity using surfactant with a Hydrophylic-Lipophilic Balance (HLB) value equal to 7. The selection of glutathione as an antioxidant was based on its prominent role in maintaining intracellular redox balance. Alginate was used as the polymer, while calcium chloride constituted a cross-linking agent and Tween and Span were employed as surfactants. Methods: The study applied an ionotropic gelation-aerosolization method. Microspheres were characterized by their morphology, size, drug loading, entrapment efficiency and yield. Stress testing utilized a forced degradation method, while an effectiveness study of glutathione incorporated a Matrix Metalloproteinase I (MMP-1) parameter on mouse skin. Glutathione-microspheres, to which had been added surfactants with a HLB value equal to 7, were compared to those without surfactants. Results: Microspheres demonstrated both high yield and encapsulation efficiency. From the stability study conducted, it was evident that the glutathione-microspheres with additional surfactant were more stable than glutathione with surfactant, but without microspheres. Similarly, the glutathione-microspheres with additional surfactant were more stable than the glutathione without surfactant. The in vivo effectivity showed lipophilic glutathione microspheres were able to decrease MMP-1 expression in the dermis tissue of mice. Conclusion: The results of freeze-dried glutathione-loaded alginate microspheres with surfactant with a HLB value equal to 7 can be utilized as potential glutathione delivery systems.

Keywords: Alginate microspheres, Aerosolization, Glutathione, Surfactants, Mmp-1 expression