Abstract
Angiogenesis is the formation of new blood vessels from preexisting vasculature. Uncontrolled angiogenesis is associated with progression of several ocular pathologies, such as diabetic retinopathy and macular degeneration. Thus, the inhibition of this process consists in an interesting therapeutic target. Corosolic acid (CA) is a natural derivative of ursolic acid, found in many medicinal herbs and exhibits numerous biological properties, including the antiangiogenic activity. The present study reports the production of CA-loaded poly d,l-lactidecoglycolide acid (PLGA) devices by melt technique. HPLC-UV method was developed and validated to evaluate the uniformity and the release profile of the developed systems. The devices were also characterized by Fourier transform infrared spectroscopy, thermal analysis, and scanning electron morphology. It was studied the antiangiogenic activity of the CA-polymer system, using an in vivo model, the chorioallantoic membrane assay (CAM). CA was dispersed uniformly in the polymer matrix and no chemical interaction between the components of the formulation was verified. The implants presented a sustained release of the drug, which was confirmed by the morphological study and demonstrated an antiangiogenic activity. Therefore, the developed delivery system is a promising therapeutic tool for the treatment of ocular diseases associated with neovascularization or others related to the angiogenic process.
Highlights
Angiogenesis or neovascularization is a natural process responsible for the formation of new blood vessels from preexisting vasculature (Elshabrawy et al, 2015)
We focus on one of the triterpenes, corosolic acid (CA; C30H48O4; molar mass 472.71 g.mol-1)
Corosolic acid (CA)-loaded PLGA polymeric devices were successfully fabricated by the hot melt method and the drug showed to be dispersed uniformly in the matrix
Summary
Angiogenesis or neovascularization is a natural process responsible for the formation of new blood vessels from preexisting vasculature (Elshabrawy et al, 2015). The neovascularization is controlled by several molecules that stimulate (pro-angiogenic) and inhibit (antiangiogenic) the formation of new blood vessels (Gacche, Meshram, 2014). In pathological circumstances, the balance between these factors is lost by some chemical, mechanical, Among the factors involved in angiogenesis, vascular endothelial growth factor (VEGF) is one of the most important pro-angiogenic factors, due to its vascular endothelium specificity and its ability to induce vasodilation via NO endothelial production. VEGF is excessively produced, resulting in dysregulated angiogenesis that plays an important role in the progression of several pathologies, such as proliferative diseases of retina, chronic inflammation, rheumatoid arthritis, psoriasis, endometriosis, tumor growth and metastasis
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