Cationic and anionic unloaded polymeric nanocapsules: Toxicological evaluation in rats shows low toxicity

Biomed Pharmacother. 2019 Aug:116:109014. doi: 10.1016/j.biopha.2019.109014. Epub 2019 May 27.

Abstract

The experimental design aiming at evaluating the performance of drugs nanoencapsulated involves inclusion of a formulation without drug (unloaded). This formulation has sometimes presented per se effect. In this sense, we sought to evaluate the toxicity of unloaded polymeric nanocapsules (NCs) with different surfaces (cationic and anionic) in male Wistar rats in male Wistar rats. The physicochemical characterization of NCs with different surfaces: polysorbate 80 (P80), polyethylene glycol (PEG), eudragit ®RS 100 (EUD) and chitosan (CS) was performed. Rats were treated with unloaded NCs (P80, PEG, EUD and CS surfaces) daily for 14 days per oral route. 24 h of last treatment, animals were euthanized and organs were removed and weighted. After, biochemical determinations were performed. In general, NCs-surfaces did not cause alterations in body weight, weight of organs and histopathological analysis. PEG-surface NCs did not generate hepatotoxicity. In investigation of lipid profile, the surface with P80 changed TC and HDL-C levels. Besides that, all NCs did not alter oxidative stress markers in organs studied (TBARS and Reactive Species) and CS-surface presented antioxidant activity in kidney. This study demonstrated that NCs-surfaces depending on their physicochemical characteristics had low or no toxicity.

Keywords: Lipid-core; Nanocapsules; Nanotoxicology; Surfaces.

MeSH terms

  • Alanine Transaminase / metabolism
  • Animals
  • Anions
  • Antioxidants / metabolism
  • Aspartate Aminotransferases / metabolism
  • Body Weight / drug effects
  • Cations
  • Cholesterol / metabolism
  • Creatinine / metabolism
  • Drinking Behavior / drug effects
  • Feeding Behavior / drug effects
  • Iron / metabolism
  • Male
  • Nanocapsules / chemistry
  • Nanocapsules / toxicity*
  • Organ Size / drug effects
  • Oxidation-Reduction
  • Polymers / toxicity*
  • Rats, Wistar
  • Reactive Oxygen Species / metabolism
  • Thiobarbituric Acid Reactive Substances / metabolism
  • Toxicity Tests*
  • Urea / metabolism

Substances

  • Anions
  • Antioxidants
  • Cations
  • Nanocapsules
  • Polymers
  • Reactive Oxygen Species
  • Thiobarbituric Acid Reactive Substances
  • Urea
  • Cholesterol
  • Creatinine
  • Iron
  • Aspartate Aminotransferases
  • Alanine Transaminase