Abstract
Poly(lactic-co-glycolic acid) (PLGA) nanoparticles were studied as drug delivery vehicles for calcitriol, the active form of vitamin D3. In vitro effects of calcitriol encapsulated in PLGA nanoparticles were evaluated with respect to free calcitriol on human pancreatic cell lines, S2-013 and hTERT-HPNE, and the lung cancer cell line A549. Encapsulated calcitriol retained its biological activity, reducing the cell growth. Cytotoxicity assays demonstrated that encapsulation of calcitriol enhanced its inhibitory effect on cell growth at a concentration of 2.4 μM for the S2-013 cells (91%) and for A549 cells (70%) comparared to the free calcitriol results. At this concentration the inhibitory effect on nontumor cells (hTERT-HPNE) decreased to 65%. This study highlights the ability of PLGA nanoparticles to deliver vitamin D3 into cancer cells, with major effects regarding cancer cell cycle arrest and major changes in the cell morphological features.
Highlights
Vitamin D3, a secosteroid hormone produced through sunlight exposure [1], can be found with different chemical structures: calciol or cholecalciferol, calcidiol and calcitriol
A Poly(lactic-co-glycolic acid) (PLGA) NP system was developed for calcitriol delivery
The in vitro cytotoxic studies proved that unloaded PLGA NPs are biocompatible and revealed the toxicity effect of calcitriol against human pancreatic and lung cells
Summary
Vitamin D3, a secosteroid hormone produced through sunlight exposure [1], can be found with different chemical structures: calciol or cholecalciferol, calcidiol and calcitriol. Cholecalciferol is inert and must be metabolized in the liver and the kidney through two hydroxylation processes in order to be converted into its active form, calcitriol [2]. Calcitriol acts like classical steroid hormones, binding to vitamin D receptor (VDR) and targeting gene expression via both genomic and nongenomic pathways [1]. Calcitriol is regarded as a cancer chemopreventive agent due to promising epidemiological, preclinical and clinical findings [4]. The protective role of vitamin D against cancer has been mainly attributed to its anti-inflammatory activity [5]
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