Development, characterization and evaluation of antiretroviral drug – Didanosine loaded serum albumin nanocarriers for an antiretroviral therapy

Abstract

AimDidanosine, a nucleoside reverse transcriptase inhibitor, is used to treat HIV infection in patients with or without acquired immunodeficiency syndrome. The objective of this study is to prepare didanosine loaded bovine serum albumin nanoparticles by desolvation technique and coated with 1% polysorbate 80 to improve antiretroviral therapy. MethodBovine serum albumin nanoparticles containing didanosine were prepared by desolvation technique and cross linked with 8% v/v glutaraldehyde solution. Ethanol and mannitol were used as a desolvating agent and cryoprotectant respectively. The formulated nanoparticles were characterized, evaluated and were subjected to stability studies over a period of three months. Biodistribution studies were investigated for the best formulation (D1). ResultsNanoparticle size was averaged below 270 nm with 0.2 PDI and zeta potential was in the range of −23.0 to −36.6. Encapsulation efficiency ranges from 66 to 85.71% and % drug loading ranges from 9.48 to 28.34. Cumulative percent drug release was in range of 60–80% and release kinetics suggested that drug release was Fickian diffusion controlled. The stability studies over period of 3 months confirmed the stability of BSA nanoparticles. Biodistribution studies demonstrated that the drug level in macrophage organs can be enhanced by coating of nanoparticles with 1% polysorbate 80. ConclusionThe method adopted is simple and able to prepare stable, spherical shaped nanoparticles which exhibit slow and sustained release.