Chitosan-functionalized nanostructured lipid carriers containing chloroaluminum phthalocyanine for photodynamic therapy of skin cancer

Eur J Pharm Biopharm. 2022 Oct:179:221-231. doi: 10.1016/j.ejpb.2022.09.009. Epub 2022 Sep 16.

Abstract

The objective of this study was to obtain optimized nanostructured lipid carriers (NLC) functionalized with chitosan containing chloroaluminum phthalocyanine (ClAlPc) as a photosensitizer. Initially, the optimization of the preparation method of the NLC was performed, where the influence of different surfactants such as PVA and Tween 80, as well as different solid lipids such as stearic acid and Glycerol Monostearate (GM) was evaluated. The formulation containing GM and PVA (NLC10) was considered promising. Following, by the adsorption method (NLC10q), the formulation was functionalized with chitosan and characterized. NLC10 and NLC10q presented sizes of 131.5 and 231.5 nm, and ZP of -24.30 and + 19.96 mV, respectively. The encapsulation efficiency of NLC10q was 96 %, higher than NLC10 (79 %). The formulations were able to promote significant cutaneous retention of ClAlPc, after 2 h and 4 h of the study, and showed to be non-toxic to fibroblasts (biocompatible). PDT in BF16-F10 melanoma resulted in reduced cell viability to 70 % and 50 % for NLC10 and NLCq, respectively. In view of the results obtained, NLC showed to be promising in the treatment of skin cancer through PDT. NLC10q showed higher encapsulation efficiency and stability than NLC10, but, contrary to what was expected, it presented lower photodynamic efficiency.

Keywords: Chitosan; Chloroaluminum phthalocyanine; Nanostructured lipid carriers; Photodynamic therapy; Skin cancer.

MeSH terms

  • Chitosan*
  • Drug Carriers
  • Glycerol
  • Humans
  • Indoles
  • Nanostructures*
  • Organometallic Compounds
  • Particle Size
  • Photochemotherapy* / methods
  • Photosensitizing Agents
  • Polysorbates
  • Skin Neoplasms* / drug therapy
  • Surface-Active Agents

Substances

  • Drug Carriers
  • Indoles
  • Organometallic Compounds
  • Photosensitizing Agents
  • Polysorbates
  • Surface-Active Agents
  • chloroaluminum phthalocyanine
  • aluminum phthalocyanine disulfonate
  • Chitosan
  • Glycerol