Gold-Polypyrrole-Loaded Eosin in Photo-Mediated Treatment of Hidradenitis Suppurativa: In Vivo Trans-Epidermal Permeation Study and Clinical Case Report.

This study reports a new protocol for the management of Hidradenitis Suppurativa (HS), depending on the synergistic photodynamic and photothermal effect of eosin yellow-gold-polypyrrole hybrid nanoparticles (E-G-Ppy NPs). E-G-Ppy NPs and gold-polypyrrole NPs (G-Ppy NPs) were synthesized, characterized, and formulated in topical hydrogels. Then, in vivo trans-epidermal permeation study, under both dark and white light-irradiation conditions, was done on albino mice. The E-G-Ppy hydrogel was then applied on a twenty-four years old female with recurrent axillary HS lesions pretreated with fractional CO2 laser. Thereafter, the treated lesions were irradiated sequentially, using an IPL system, in the visible (~550 nm) and NIR band (630-1100 nm) to activate the synthesized nanoparticles. Results showed that, upon application to mice skin, E-G-Ppy exhibited good tolerance and safety under dark conditions and induced degenerative changes into dermal layers after white-light activation, reflecting deep penetration. Photo-activation of E-G-Ppy hydrogel to a severe Hidradenitis Suppurativa case showed an improvement of 80% of the lesions according to average HS-LASI scores after 4 sessions with no recurrence during a follow-up period of six months. In summary, the dual photodynamic/photothermal activation of E-G-Ppy NPs can represent a promising modality for management of HS. Further expanded clinical studies may be needed.

(Rose Bengal)/(Eosin Yellow)-Gold-Polypyrrole Hybrids: A Design for Dual Photo-Active Nano-System with Ultra-High Loading Capacity.

PURPOSE: Enhancement of the photodynamic/photothermal efficiency of two water-soluble dyes, rose bengal (RB) and eosin yellow (EY), via conjugation to a polymeric nano-system gold-polypyrrole nanoparticle (AuPpy NPs). METHODOLOGY: A multi-step synthesis method and an in situ one-pot synthesis method were used. Loading percentage, particle size, zeta potential, morphology, UV-Vis-NIR spectrophotometry and in vitro photothermal activity were measured. Then, both hybrid nanocomposites were examined for their cytotoxicity and photocytotoxicity on HepG2 cell line as a model for cancer cells. RESULTS: Dyes loaded in the traditional multi-step method did not exceed 9% w/w, while in the one-pot synthesis method they reached ~67% w/w and ~75% w/w for EY-AuPpy NPs and RB-AuPpy NPs, respectively. UV-Vis-NIR spectrophotometry showed that both nano-systems exhibited intense absorption in the NIR region. The mean size of the nanoparticles was ~31.5 nm (RB-AuPpy NPs) and ~33.6 nm (EY-AuPpy NPs) with zeta potential values of -26.5 mV and -33 mV, respectively. TEM imaging revealed the morphology of both hybrids, showing ultra-nano spherical-shaped gold cores in the case of RB-AuPpy NPs, and different shapes of larger gold cores in the case of EY-AuPpy NPs, both embedded in the polymer film. Conjugation to AuPpy was found to significantly reduce the dark cytotoxicity of both RB and EY, preserving the photocytotoxicity of EY and enhancing the photocytotoxicity of RB. CONCLUSION: Gold-polypyrrole nanoparticles represent an effective delivery system to improve the photodynamic and photothermal properties of RB and EY. The in situ one-pot synthesis method provided a means to greatly increase the loading capacity of AuPpy NPs. While both hybrid nanocomposites exhibited greatly diminished dark cytotoxicity, RB-AuPpy NPs showed significantly enhanced photocytotoxicity compared to the free dyes. This pattern enables the safe use of both dyes in high concentrations with sustained action, reducing dose frequency and side effects.

One-Step Synthesis of Polypyrrole-Coated Gold Nanoparticles for Use as a Photothermally Active Nano-System.

OBJECTIVE: This paper introduces a simple one-step and ultra-fast method for synthesis of highly photothermally active polypyrrole-coated gold nanoparticles. The synthesis process is so simple that the reaction is very fast without the need for any additives or complicated steps. METHODOLOGY: Polypyrrole-coated gold nanoparticles (AuPpy NPs) were synthesized by reacting chloroauric acid (HAuCl4) with pyrrole (monomer) in aqueous medium at room temperature. These nanoparticles were characterized by UV-visible-NIR spectrometry, transmission electron microscopy (TEM), AC conductivity, zeta sizer and were evaluated for dark cytotoxicity and photocytotoxicity using human hepatocellular carcinoma (HepG2) cell line as a model for cancer cells. RESULTS: The synthesized AuPpy NPs showed a peak characteristic for gold nanoparticles (530-600 nm, molar ratio dependent) and a wide absorption band along the visible-NIR region with intensity about triple or even quadruple that of polypyrrole synthesized by the conventional FeCl3 method at the same concentration and under the same conditions. TEM imaging showed that the synthesized AuPpy NPs were composed of spherical or semi-spherical gold core(s) of about 4-10 nm coated with distinct layer(s) of polypyrrole seen either loosely or in clusters. Mean sizes of the synthesized nanoparticles range between ~25 and 220 nm (molar ratio dependent). Zeta potentials of the AuPpy NPs preparations indicate their good colloidal stability. AC conductivity values of AuPpy NPs highly surpass that of Ppy prepared by the conventional FeCl3 method. AuPpy NPs were non-toxic even at high concentrations (up to 1000 µM pyrrole monomer equivalent) under dark conditions. Unlikely, light activated the photothermal activity of AuPpy NPs in a dose-dependent manner. CONCLUSION: This method simply and successfully synthesized AuPpy NPs nanoparticles that represent a safe alternative photothermally active multifunctional tool instead of highly toxic and non-biodegradable gold nanorods.

One-step synthesis of phyto-polymer coated gold nanospheres as a delivery system to enhance resveratrol cytotoxicity.

This study introduces a simple method for one-step synthesis of highly stable nontoxic polymer-coated gold nanospheres for use in drug delivery, focuses on the ability of chloroauric acid (HAu Cl4 ) to induce polyphenols polymerization, puts up an easy procedure for loading hydrophobic drugs onto gold nanoparticles with ultra-high loading efficiency and studies the cytotoxicity of free and gold nanoparticles-loaded resveratrol. Gold nanospheres were synthesized simply by direct reaction between resveratrol itself and HAu Cl4 in aqueous medium. Synthesized gold nanospheres exhibited high stability in both aqueous and ethanolic solutions. UV-visible spectrum showed that the synthesized gold nanospheres have maximum absorption at 532 nm. TEM imaging, mass and FT-IR spectrometry revealed the presence of a distinct polymeric shell around each nanoparticle. Resveratrol, as a chemopreventive agent, was loaded onto the synthesized gold nanospheres with an ultra-high loading capacity (11.6% w/w). Free resveratrol, free gold nanospheres, and resveratrol-loaded gold nanospheres were examined for cytotoxicity on HepG2 cell line where cytotoxicity of loaded resveratrol was dramatically enhanced to reach about nine folds as that of free resveratrol at the same concentration.