DEVELOPMENT, EVALUATION AND TARGETING OF STAVUDINE LOADED SERUM ALBUMIN POLYMER BASED NANOCARRIERS TO HIV RESERVOIRS

Abstract

Objective: Stavudine is an antiretroviral drug that is part of the nucleoside reverse transcriptase inhibitor (NRTIs) family, which is used to delay the progression of HIV infection. The present investigation involves the development and evaluates stavudine loaded nanocarriers using natural polymer bovine serum albumin (BSA).

Methods: The desolvation technique was used to prepare nanoparticles and coated with 1% v/v polysorbate 80 to improve the targeting of drugs to the organs (HIV reservoirs). Biodistribution studies were also investigated for the best formulation to determine the targeting efficiency of nanocarriers loaded stavudine and compared with pure compound.

Results: The formulated nanocarriers have shown mean particle size below 300 nm, zeta potential in the range of -16.5 Mv, encapsulation efficiency in the range of 50.10 to 73.7%, drug loading in the range of 14.73 to73.84%. Cumulative % drug release was in the range of 24.72 to 71.20% and release kinetics studies showed that the mechanism of drug release was controlled simultaneously by diffusion and erosion of the matrix type formulations. The stability studies over a period of three months confirmed the stability of BSA nanoparticles. Biodistribution studies demonstrated that nanoparticles coated with 1% v/v polysorbate 80 were able to reach the HIV reservoirs in an amount higher than that of uncoated stavudine nanoparticles or pure drug itself.

Conclusion: The method adopted is simple and the biodistribution studies demonstrated that nanoparticles coated with 1% polysorbate 80 were able to reach the selected organs in an amount higher than that of uncoated stavudine nanoparticles or pure drug itself.