Optimization of protoporphyrin IX skin delivery for topical photodynamic therapy: Nanodispersions of liquid-crystalline phase as nanocarriers

Author(s)

Rossetti, Fabia Cristina ^[1] ; Depieri, Livia Vieira ^[1] ; Praca, Fabiola Garcia ^[1] ; Del Ciampo, Jose Orestes ^[1] ; Fantini, Marcia C. A. ^[2] ; Riemma Pierre, Maria Bernadete ^[3] ; Tedesco, Antonio Claudio ^[4] ; Lopes Badra Bentley, Maria Vitoria ^[1]

Affiliation

^[1] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, Ave Cafe S-N, BR-14040160 Ribeirao Preto, SP - Brazil

^[2] Univ Sao Paulo, Inst Fis, BR-05508 Sao Paulo, SP - Brazil

^[3] Univ Fed Rio de Janeiro, Fac Farm, Ave Carlos Chaos Filho 373, BR-21941902 Rio De Janeiro, RJ - Brazil

^[4] Univ Sao Paulo, Fac Filosofia Ciencias & Letras Ribeirao Preto, BR-05508 Sao Paulo, SP - Brazil

• Document type: Journal article
• Source: European Journal of Pharmaceutical Sciences; v. 83, p. 99-108, FEB 15 2016.
• Web of Science Citations: 14

Abstract

Nanodispersions of liquid-crystalline phases (NLPs) composed of monoolein and oleic acid were chosen as nanocarriers to improve the topical retention of the photosensitizer protoporphyrin IX (PpIX) and thereby optimize photodynamic therapy (PDT) using this photosensitizer. The nanodispersions were characterized by polarized light microscopy, small-angle X-ray diffraction and dynamic light scattering. The stability and encapsulation efficiency (EE%) of the nanodispersions were also evaluated. In vitro and in vivo skin penetration studies were performed to determine the potential of the nanodispersions for cutaneous application. In addition, skin penetration and skin irritancy (in an animal model) after in vivo application were visualized by fluorescence light microscopy. The nanodispersion obtained was characterized as a monodisperse system (similar to 150.0 nm) of hexagonal liquid-crystalline phase, which provided a high encapsulation efficiency of PpIX (similar to 88%) that remained stable over 90 days of investigation. Skin penetration studies demonstrated that the nanodispersion enhanced PpIX skin uptake 11.8-and 3.3-fold (in vitro) and 23.6-and 20.8-fold (in vivo) compared to the PpIX skin uptake of control formulations, respectively. In addition, the hexagonal phase nanodispersion did not cause skin irritation after application for two consecutive days. Overall, the results show that the nanocarrier developed is suitable for use in topical PDT with PpIX. (C) 2015 Published by Elsevier B.V. (AU)

• FAPESP's process: 06/03929-7 - Liquid crystal nanodispersions as delivery systems for photosensitizers in the photodynamic therapy of skin cancer: in vitro and in vivo cutaneous permeation and retention tests
• Grantee: Fábia Cristina Rossetti
• Support Opportunities: Scholarships in Brazil - Doctorate