Characterization and in vitro antitumor activity of polymeric nanoparticles loaded with Uncaria tomentosa extract

Abstract

Uncaria tomentosa (UT) extracts have been shown to have promising antitumor activity. We hypothesized that its incorporation into nanostructured systems could improve the anticancer properties. Here, poly-e-caprolactone (PCL) and poly-d,l-lactideco-glycolide (PLGA) were employed to generate nanoparticles loaded with UT extract in a single emulsion solvent evaporation method. The nanoparticles were characterized by particle size, zeta potential, morphology and entrapment efficiency along with stability and release profiles. The nanoparticles presented entrapment efficiencies above 60% and a mean diameter below 300nm. UT-PCL nanoparticles presented higher entrapment efficiency and mean particle size as well as a slow release rate. The UT-PLGA nanoparticles showed higher drug loading. Two prostate cancer cell-lines, LNCaP and DU145 that were derived from metastatic sites, served as model systems to assess cytotoxicity and anticancer activity. In vitro, both formulations reduced the viability of DU145 and LNCaP cells. Yet, the UT-PLGA nanoparticles showed higher cytotoxicity towards DU145 cells while the UTPCL against LNCaP cells. The results confirm that the incorporation of UT into nanoparticles could enhance its anti-cancer activities that can offer a viable alternative for the treatment of prostrate canner and highlights the potential of nanostructured systems to provide a promising methodology to enhance the activity of natural extracts.

Nano-Drug Delivery Systems Entrapping Natural Bioactive Compounds for Cancer: Recent Progress and Future Challenges

“…DC. (UT) extracts have been shown to have promising antitumor activity for the enhancement and delivery, in which PCL and PLGA were employed for the generation of NPs loaded with UT extract by a single emulsion solvent evaporation method ( 218 ).…”

Hybrid Nanoparticles of Proanthocyanidins from Uncaria tomentosa Leaves: QTOF-ESI MS Characterization, Antioxidant Activity and Immune Cellular Response

“…Five dissolution media reported in the literature were tested preliminarily for both PA-E nanoformulations and free PA-E, considering the solubility of PA-E on them, the chemical instability of PA-E biomolecules at acidic or basic pHs [48] and their similarity with physiological conditions. HCl 0.1% (pH 3.2) [49], acetic acid 0.1% (pH 5.0) [50], phosphate-buffered saline containing 10% of EtOH (pH 7.2) [51], phosphate-buffered saline composed of 20% of MeOH and 2.5% of Tween (pH 7.4) [52] and water (pH 7.3) [53] were screened. Effectively, under acidic conditions, PA-E was not detected, and an abnormal dissolution profile of PA-E was observed in phosphate-buffered saline composed of 20% of MeOH and 2.5% of Tween (pH 7.4).…”

Development of Polymer-Assisted Nanoparticles and Nanogels for Cancer Therapy: An Update

“…PLGA, a co-polymer made from poly lactic acid and poly glycolic acid was also used to produce NPs [126]. Afatinib or miR-loaded PLGA NPs were able to prevent the degradation of afatibin and miR, thereby resulting in the stable and potent delivery of these compounds in colon cancer [127]. UT-PLGA and UTPCL exhibited efficient delivery of drugs but UT-PLGA had a slightly better drug loading and could target prostate cancer cells effectively [127].…”

“…Afatinib or miR-loaded PLGA NPs were able to prevent the degradation of afatibin and miR, thereby resulting in the stable and potent delivery of these compounds in colon cancer [127]. UT-PLGA and UTPCL exhibited efficient delivery of drugs but UT-PLGA had a slightly better drug loading and could target prostate cancer cells effectively [127]. In addition to the PLGA NPs, Cur-PLGA NPs was able to stabilize curcumin in the presence of light and improve curcumin serum stability when compared to free curcumin [128].…”