Search

Excipient interaction has become essential knowledge for rational formulation design of nanoparticles. Nanostructured lipid carriers (NLCs) include at least three types of excipient, which enhance excipient interaction possibilities and relevance. The present article introduces an alternative approach for evaluating a great number of excipients with few samples, using NLC as a model delivery system. This approach is based on two sequential experiments using Hall-2 experimental design and analysis of excipient interactions in respect to their physicochemical properties by multilevel statistics. NLCs were prepared using a hot emulsification-ultrasonication method with lidocaine and nine excipients (solid lipids, oils and surfactants). The evaluated parameters were z-average size (DLS), dispersity (DLS), zeta potential (electrophoretic mobility) and entrapment efficiency (HPLC). Cetyl palmitate, beeswax, castor oil, capric/caprylic acid and polysorbate 80 all presented larger effects amongst the studied factors as well as a clear pattern of synergistic interactions. Following the verified trends, we produced an optimized NLC that exhibited all desirable physicochemical characteristics and a modified drug release profile. Our results demonstrate the methodology’s robustness, which can be applied to other nanoparticles and establish a cost-effective excipient evaluation.

A lidocaina (LDC) e um anestesico local que pode ser usado para dor pos-cirurgica ou relacionada ao câncer, por infusao intravenosa ou bolus. Uma alternativa para manter os niveis plasmaticos do farmaco sao os carreadores de liberacao sustentada, onde se destacam os carreadores lipidicos nanoestruturados (CLNs), por possuirem biocompatibilidade, baixa toxicidade, reprodutibilidade e alta eficiencia no transporte de drogas hidrofobicas. Este projeto teve como objetivo continuar o desenvolvimento de formulacoes com lipidios naturais altamente refinados iniciados em 2017, no primeiro ano de iniciacao cientifica, e realizar a caracterizacao fisico-quimica e cinetica (perfil de liberacao in vitro).

Lidocaine (LDC) is a local anesthetic that can be used for post-surgical or cancer related pain, via intravenous infusion or bolus. An alternative to maintain drug plasma levels are the sustained release carriers, whereas nanostructured lipid carriers (NLCs) stand out; they have biocompatibility, low toxicity, reproducibility and high efficiency in the transport of hydrophobic drugs.This work aims to study the solubility parameter of the LDC pre formulation in several ultra-purified lipids, compatible with the endovenous route, and to formulate NLCs based on these lipids for LDC encapsulation.