Nanotechnology for the treatment of deep endometriosis: uptake of lipid core nanoparticles by LDL receptors in endometriotic foci

Abstract

OBJECTIVE: Rapidly dividing cells in multiple types of cancer and inflammatory diseases undergo high low density lipoprotein (LDL) uptake for membrane synthesis, and coupling an LDL-like nanoemulsion, containing lipid nanoparticles (LDE) to a chemotherapeutic agent efficiently targets these cells without significant systemic effects. This was a prospective exploratory study that evaluated the uptake of a radioactively labeled LDE emulsion by receptors of endometriotic foci and the capacity of the LDE for cellular internalization. METHODS: The lipid profile of each patient was determined before surgery, and labeled LDE were injected into fourteen patients with intestinal or nonintestinal endometriosis. The radioactivity of each tissue sample (intestinal endometriosis, nonintestinal endometriosis, healthy peritoneum, or topical endometrium) was measured. RESULTS: The group with intestinal endometriosis presented higher levels of plasma LDL but lower LDE uptake by foci than the nonintestinal group, suggesting less cell division and more fibrosis. The uptake of LDE was highest in the topical endometrium, followed by the healthy peritoneum, and lowest in the endometriotic lesion. Since the endometriotic foci showed significant LDE uptake, there was likely increased consumption of LDL by these cells, similar to cells in cancers and inflammatory diseases. Plasma cholesterol levels had no influence on LDE uptake, which showed that the direct delivery of the nanoemulsion to target tissues was independent of serum lipoproteins. There were no significant differences in the parameters ( p >0.01) because of the small sample size, but the findings were similar to those of previous studies. CONCLUSION: Nanotechnology is a promising therapeutic option for surgery and hormonal blockage for deep endometriosis, with a lower complication rate and no systemic side effects.

Nanomedicines for Endometriosis: Lessons Learned from Cancer Research

“…quantified the uptake of lipid nanoparticles in endometriotic lesions of affected patients scheduled for surgical intervention. [ 47 ] One day before surgery, patients were intravenously administered 0.1 mL of solid cholesterol lipid core nanoparticles containing cholesterol [ 14 C]‐oleate. Following resection and biopsy, 14 C in endometrial, peritoneal, and endometriotic tissues were evaluated using liquid scintillation spectrometry.…”

Ox-LDL-mediated ILF3 overexpression in gastric cancer progression by activating the PI3K/AKT/mTOR signaling pathway

“…For example, a number of investigators have proposed the role of lipoproteins in the promotion of cancer progression [ 44 ]. And LDL is the largest cholesterol transporter of the body [ 45 ]. The LDL receptor on tumor cells is overexpressed to meet the high demand of cholesterol which is necessary for the rapid cell proliferation and de novo membrane synthesis.…”

The nano-revolution in the diagnosis and treatment of endometriosis

“…Bedin et al showed preliminary results in which they found a high uptake of labelled LDE by the topical endometrium, which can be used as a nanosystem. 104 Another mechanism of endometriosis that can be studied regard the autophagy process, in which Beclin-1 play an essential positive regulatory role. 105 Zhao et al devised a hyaluronic acid (HA) (PEI-SA/ DNA) as a tool for Beclin-1 gene delivery and consequent Beclin-1 upregulation within endometrial lesions.…”