Zinc phthalocyanine tetrasulfonate-loaded polyelectrolytic PLGA nanoparticles for photodynamic therapy applications.

BACKGROUND: Photodynamic Therapy (PDT) is a modality for the treatment of neoplastic tissues, which is based on the administration of a phototherapeutic agent and light irradiation at an appropriate wavelength, aiming to locate and destroy the target cell with the formation of reactive oxygen species. Nanoencapsulation technology presents itself as a tool for incorporation of bioactive substances aiming to improve their solubility in physiological environment, obtain a longer circulation time in the organism, administration of lower dosages and the minimization of side effects. The present work aimed at the development of poly (lactic acid-glycolic acid) (PLGA) nanoparticles coated with polyelectrolyte film layers for encapsulating zinc phthalocyanine tetrasulfonated (ZnPcSO4) as a bioactive substance model. METHODS: PLGA nanoparticles were produced by the double emulsion/solvent evaporation technique and polyelectrolytic coating was performed using polyalkylamine hydrochloride (PAH) as a weak polycation and poly (4-styrene sulfonate) (PSS) as a strong polyanion by layer-by-layer self-assembly technique (known as layer-by-layer-LbL). The nanoparticulate system was studied by scanning electron microscopy, steady-state, and their biological activity was evaluated using in vitro cancer cell lines by classical MTT assay. RESULTS: The polyelectrolytic PLGA nanoparticles had an average diameter of 384.7 ± 138.6 nm, restricted distribution size with a polydispersity index. The obvious change in zeta potential indicates successful alternation in polycation (PAH) and polyanion (PSS) deposition directly in PLGA nanoparticles. Scanning electron microscopy (SEM) analysis showed that the formed system had morphology spherical, typical of these release systems. The loading efficiency was 82.1 % ± 1.2 %. The polyelectrolytic nanoparticles loaded with phthalocyanine maintained their photophysical behavior after encapsulation. Cell viability was determined, obtaining 90 % cell death. CONCLUSIONS: Therefore, the presented work depicts ZnPcSO4-loaded polyelectrolytic PLGA nanoparticles as a promise drug delivery system for phototherapeutic agent, which are thus expected to have superior therapeutic efficiency than free drug.

Synthesis, photophysical and photobiological characterization of BSA nanoparticles loaded with chloroaluminium phthalocyanine by one-step desolvation technique for photodynamic therapy action.

This work describes the preparation of bovine serum albumin (BSA) nanoparticles by one-step desolvation method using acetone/ethanol as precipitating agent, glutaraldehyde as crosslinking agent, sodium azide as a preservative and water as reaction media for chloroaluminium phthalocyanine (ClAlPc) incorporation for photodynamic therapy action. The characterization of the nanoparticulate system was carried out using steady-state technique, scanning electron microscopy study and their biological activity was evaluated using in vitro macrophages cell lines by classical MTT assay. All the spectroscopy measurements demonstrated good photophysical properties and the in vitro cytotoxicity study showed that the system is not cytotoxic in the darkness, but it exhibits a substantial phototoxicity at 0.90 mol.L-1 of photosensitizer concentration and 10.0 J cm-2 of light. These conditions are sufficient to kill about 90% of the cells. The results allowed us to conclude that ClAlPc-loaded in BSA nanoparticles might have potential application on drug delivery system for PDT protocols.

Gelatin nanoparticles loaded methylene blue as a candidate for photodynamic antimicrobial chemotherapy applications in Candida albicans growth.

Gelatin nanoparticles (GN) with an intrinsic antimicrobial activity maybe a good choice to improve the effectiveness of photodynamic antimicrobial chemotherapy (PACT). The aim of this study was to development gelatin nanoparticles loaded methylene blue (GN-MB) and investigate the effect of GN-MB in the Candida albicans growth by PACT protocols. The GN and GN-MB were prepared by two-step desolvation. The nanoparticulate systems were studied by scanning electron microscopy and steady-state techniques, the in vitro drug release was investigated, and we studied the effect of PACT on C. albicans growth. Satisfactory yields and encapsulation efficiency of GN-MB were obtained (yield = 76.0% ± 2.1 and EE = 84.0% ± 1.3). All the spectroscopic results presented here showed excellent photophysical parameters of the studied drug. Entrapment of MB in GN significantly prolongs it's in vitro release. The results of PACT experiments clearly demonstrated that the photosensitivity of C. albicans was higher when GN-MB was used. Gelatin nanoparticles loaded methylene blue-mediated photodynamic antimicrobial chemotherapy may be used against Candida albicans growth.