In this study, we prepared atorvastatin calcium (AVST) loaded chitosan nanoparticles to improve the oral bioavailability of the drug. Nanoparticles were prepared by solvent evaporation technique and evaluated for its particle size, entrapment efficiency, zeta potential, in vitro release and surface morphology by scanning electron microscopy (SEM). In addition, the pharmacokinetics of AVST from the optimized formulation (FT5) was compared with marketed immediate release formulation (Atorva ® ) in rabbits. Particle size of prepared nanoparticles was ranged between 179.3 ± 7.12 to 256.8 ± 8.24 nm with a low polydispersity index (PI) value. Zeta potential study showed that the particles are stable with positive values between 13.03 ± 0.32 to 46.90 ± 0.49 mV. FT-IR studies confirmed the absence of incompatibility of AVST with excipient used in the formulations. In vitro release study showed that the drug release was sustained for 48 h. Results of pharmacokinetics study showed significant changes in the pharmacokinetic parameter (2.2 fold increase in AUC) of the optimized formulation as compared to marketed formulation (Atorva ® ). Thus, the developed nanoparticles evidenced the improvement of oral bioavailability of AVST in rabbit model. Uniterms:Atorvastatin calcium/oral bioavailability/experimental study. Atorvastatin calcium/in vitro release. Atorvastatin calcium/pharmacokinetics. Nanoparticles/drugs bioavailability.No presente estudo, preparamos nanopartículas de quitosana com atorvastatina cálcica (AVST) para melhorar a biodisponibilidade oral do fármaco. As nanopartículas foram preparadas pela técnica de evaporação de solvente, avaliando-se a granulometria, a eficiência de encapsulamento, o potencial zeta, a liberação in vitro e a morfologia da superfície, por meio da microscopia eletrônica de varredura (MEV). Além disso, a farmacocinética da formulação otimizada de AVST (FT5) foi comparada com a formulação comercial, de liberação imediata, comercializada (Atorva®), em coelhos. O tamanho das das nanopartículas variou na faixa de 179,3 a 256,8 ± 7,12 ± 8,24 nm, com baixo índice polidispersibilidade (PI). O estudo do potencial Zeta mostrou que as partículas são estáveis, com valores positivos entre 13,03 ± 0,32 a 46,90 ± 0,49 mV. Os estudos de FT-IR confirmaram a ausência de incompatibilidade de AVST com o excipiente utilizado nas formulações. O estudo de liberação in vitro mostrou que liberação sustentada do fármaco por 48 horas. Os resultados do estudo farmacocinético mostraram alterações significativas nos parâmetros (aumento de 2,2 vezes na ASC) da formulação otimizada em relação à comercializada (Atorva® ). Assim, o desenvolvimento de nanopartículas evidenciou a melhora da biodisponibilidade oral de AVST em coelhos.Uniterms: Atorvastatina cálcica/biodisponibilidade oral/estudo experimental. Atorvastatina cálcica/ liberação in vitro. Atorvastatina cálcica/farmacocinética. Nanopartículas/biodisponibilidade de fármacos.
In the last 30 years, particle size reduction technologies turned from an exploratory approach into a mature commercial drug delivery platform. Nanonization technologies have gained a special importance due to a steadily increasing number of development compounds showing poor aqueous solubility. Many drug delivery companies and academic research groups have contributed to the currently existing large variety of different technologies to produce drug nanoparticles. These particles consist of pure active pharmaceutical ingredient (API) and are often stabilized with surfactants and/or polymeric stabilizers adsorbed onto their surface. The mean particle size ranges normally from 1 nm up to 1000 nm.Here we review formulation aspects, characteristics and application of nanoparticle as drug delivery system
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