Drug development and industrial pharmacy · 2013
Design of polymeric nanoparticles and its applications as drug delivery systems for acne treatment.
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Reis Catarina Pinto, Martinho Nuno, Rosado Catarina, Fernandes Ana S, Roberto Amílcar
Аннотация
OBJECTIVE: The aim of this study was to evaluate a formulation made of poly(lactide-co-glycolide) (PLGA) nanoparticles containing azelaic acid for potential acne treatment.
METHODS: Azelaic acid-loaded PLGA nanoparticles were prepared by spontaneous emulsification processes using poloxamer 188 as stabilizer. Several manufacturing parameters such as stirring rate, concentration of stabilizer and different recovery methods were investigated. Nanoparticles were evaluated in terms of size, zeta potential, encapsulation efficiency, release kinetics and permeation kinetics in vitro. Furthermore, in vitro toxicological studies were performed in Saccharomyces cerevisiae model.
RESULTS: The results showed that by adjusting some formulation conditions it was possible to obtain nanoparticles with high loading and a controlled drug release. Freeze-dried recovery altered the nanoparticles structure by enhancing porous structures and mannitol was required to control the mean particle size. The centrifugation recovery was found to be the best approach to nanoparticles recovery. Similar toxicity profiles were observed for both drug-free and azelaic acid-loaded nanoparticles, with concentration-dependent decreases in cell viability.
CONCLUSION: These results indicate a potential formulation for controlled release delivery of azelaic acid to the follicular unit.
METHODS: Azelaic acid-loaded PLGA nanoparticles were prepared by spontaneous emulsification processes using poloxamer 188 as stabilizer. Several manufacturing parameters such as stirring rate, concentration of stabilizer and different recovery methods were investigated. Nanoparticles were evaluated in terms of size, zeta potential, encapsulation efficiency, release kinetics and permeation kinetics in vitro. Furthermore, in vitro toxicological studies were performed in Saccharomyces cerevisiae model.
RESULTS: The results showed that by adjusting some formulation conditions it was possible to obtain nanoparticles with high loading and a controlled drug release. Freeze-dried recovery altered the nanoparticles structure by enhancing porous structures and mannitol was required to control the mean particle size. The centrifugation recovery was found to be the best approach to nanoparticles recovery. Similar toxicity profiles were observed for both drug-free and azelaic acid-loaded nanoparticles, with concentration-dependent decreases in cell viability.
CONCLUSION: These results indicate a potential formulation for controlled release delivery of azelaic acid to the follicular unit.
Предметные рубрики MeSH
Acne VulgarisCell SurvivalChemistry, PharmaceuticalDelayed-Action PreparationsDicarboxylic AcidsDrug CarriersDrug Delivery SystemsExcipientsFreeze DryingLactic AcidMannitolNanoparticlesParticle SizePoloxamerPolyglycolic AcidPolylactic Acid-Polyglycolic Acid CopolymerPolymersPorositySaccharomyces cerevisiaeToxicity Tests