Studies Based on Preparation, Physical Characteristics, and Cellular Pharmacological Activities of Thin PLGA Film Loaded with Geniposide

Haiyan Zhang,Xin Wang,Ya He,Guangming Luo,Ming Yang,Hao Liu,Nan Huang,Tingting Lei

doi:10.1155/2014/352423

Abstract

In this primary study, thin polylactic-co-glycolic acid (PLGA) film loaded with geniposide was first prepared and demonstrated on both physical and pharmacological aspects for its potential application on drug-eluting vascular stents. Physical parameters of geniposide-loaded thin film, such as crystal structure, molecular spectral characteristics, and release behavior in the whole process were detected. From X-Ray diffraction, the characteristic peak of crystal geniposide disappeared on geniposide-loaded PLGA film (GLPF) after it formed, which meant there was no agglomeration phenomenon, as geniposide was distributed in the form of single molecule. According to scanning electron microscopy (SEM) figure, the GLPF was more flat and uniform with better compactness. It inferred that release behavior of geniposide at the early stage (0~15 d) was in the form of free diffusion. Carrier PLGA began to degrade 15 days later, so the residual geniposide was also dissolved. Cellular pharmacological effects of geniposide on endothelial cells (ECs) and smooth muscle cells (SMCs) were also demonstrated on GLPF. 5% and 10% (w/w) geniposide-loaded PLGA (60 : 40) membrane indicated its significant effect on ECs promotion and SMCs inhibition. All provided feasible evidences for the development of new geniposide-coating vascular stent using PLGA as carrier.

Highlights

In recent years, since vascular stent is successfully applied in clinical surgery, practitioners have to consider more complication problems caused by it such as endothelial damage, thrombosis, and vascular restenosis
The results of different geniposide-loaded doses (10%, 15%, and 20%, w/w) showed that only 10% geniposide content resulted in no precipitation during membrane formation with good compatibility
The results suggested that geniposide loading improved the thermal stability of polylactic-co-glycolic acid (PLGA) membrane

Summary

Introduction

Since vascular stent is successfully applied in clinical surgery, practitioners have to consider more complication problems caused by it such as endothelial damage, thrombosis, and vascular restenosis. As the vascular endothelial injury may happen during the inserting, moving, or even supporting processes of stent, injury would promote vascular inflammation and inspire platelet aggregation. Both smooth muscle cell proliferation (VSMC) induced by series of inflammation response and thrombosis induced by platelet aggregation development would result into intimal hyperplasia . Both of intimal hyperplasia and thrombosis would lead to restenosis. Drugcoating vascular stent (DES) gradually became a very ideal design for efficient prevention for neointimal proliferation and vascular restenosis [4,5,6]

Methods

Results

Conclusion