Monoolein-based nanoparticles containing indinavir: a taste-masked drug delivery system

Abstract

Objective

This study developed a novel child-friendly drug delivery system for pediatric HIV treatment: a liquid, taste-masked, and solvent-free monoolein-based nanoparticles formulation containing indinavir (0.1%).

Significance

Adherence to antiretroviral therapy by pediatric patients is difficult because of the lack of dosage forms adequate for children.

Methods

Monoolein-based nanoparticles were developed. The particle size, zeta potential, pH, drug content, small angle X-ray scattering, stability, in vitro drug release profile, biocompatibility, toxicity, and taste-masking properties were evaluated.

Results

Monoolein-based formulations containing indinavir had nanosized particles with 155 ± 7 nm, unimodal particle size distribution, and polydispersity index of 0.16 ± 0.03. The zeta potential was negative (−31.3 ± 0.3 mV) and pH was neutral (7.78 ± 0.01). A 96% drug incorporation efficiency was achieved, and the indinavir concentration remained constant for 30 days. Polarized light microscopy revealed isotropic characteristics. Transmission electron microscopy images showed spherical shaped morphology. Small-angle X-ray scattering displayed a form factor broad peak. Indinavir had a sustained release from the nanoparticles. The system was nonirritant and was able to mask drug bitter taste.

Conclusions

Monoolein-based nanoparticles represent a suitable therapeutic strategy for antiretroviral treatment with the potential to reduce the frequency of drug administration and promote pediatric adherence.

Keywords:

• Antiretroviral therapy
• pediatric
• indinavir
• solvent-free
• nanoparticles

Acknowledgments

The authors thank the fellowships, grants, and financial support provided by Fundação de Apoio à Pesquisa do Estado do Rio Grande do Sul (FAPERGS) - grant number 12/1285-0 and Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) - grant number 477196/2013-6. This study was financed in part by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - Brasil (CAPES) - Finance Code 001. The authors also thank Dr. Sílvia S. Guterres and Dr. Adriana R. Pohlmann for making available the Perkin Elmer HPLC and Malvern Mastersizer equipment. The authors are grateful to the Brazilian Synchrotron Light Laboratory (LNLS/CNPEM) for providing access to the D11A-SAXS1 beamline, to Lafepe (Brazil) for donating indinavir and for Centro de Microscopia e Microanálise (CMM-UFRGS).

Disclosure statement

No potential conflict of interest was reported by the author(s).