Optimization of nanostructured lipid carriers for Zidovudine delivery using a microwave-assisted production method

• Type: Article in International Scientific Journal
• Date: 2018

Authors

Cavalcanti, SMT (Author) Other; Nunes, C (Author) Other; Costa Lima, SAC (Author) Other; Soares Sobrinho, JL (Author) Other; Salette Reis (Author) FFUP

Journal

Title: European Journal of Pharmaceutical Sciences

Vol. 122

Pages: 22-30

ISSN: 0928-0987

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 4 Citations

Scopus - 8 Citations

Other information

Authenticus ID: P-00P-DBE

DOI: 10.1016/j.ejps.2018.06.017

Abstract (EN): An adapted methodology for obtaining lipid nanoparticles that only uses the microwave reactor in the synthesis process was developed. The method has the following features: one-pot, one-step, fast, practical, economical, safe, readiness of scaling-up, lack of organic solvents and production of nanoparticles with low polydispersity index (PDI) (below 0.3). This new method was applied for the development of nanostructured lipid carriers (NLC) loaded with a hydrophilic drug, the antiretroviral agent zidovudine (AZT). The aim of the present work was to develop, evaluate and compare optimized NLC formulations produced by two different methods - hot ultrasonication and microwave-assisted method. The development and optimization of the NLC formulations were supported by a Quality by Design (QbD) approach. All formulations were physicochemically characterized by the same parameters. The optimized formulations presented a suitable profile for oral administration (particle size between 100 and 300 nm, PDI < 0.3 and negative zeta potential>-20 mV). Furthermore, the morphologies assessed by TEM showed spherical shape and confirmed the results obtained by DLS. Both AZT loaded formulations were physically stable for at least 45 days and non-toxic on Jurkat T cells. Drug release studies showed a controlled release of AZT under gastric and plasma-simulated conditions.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9