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.

Factors Affecting the Synthesis of Bovine Serum Albumin Nanoparticles Using the Desolvation Method

“… 68 Based on the literature study ( Table 2 ), six studies discussed optimization by varying the ratio of drug: BSA. According to Abd Ellah et al 69 Jenita, Wilson, and Chocalingam, 70 Spada et al 71 Jenita, 72 and Syed and Sailaja 73 the particle size and polydispersity index value increase with the amount of BSA used. This is in accordance with previous studies also stating that the higher the concentration of BSA, the larger the particle size and the greater the polydispersity index.…”

“…This relationship can be explained through the classical nucleation theory. 65 On the other hand, several studies have reported that increasing BSA concentrations only had a slight influence on the size of BSA nanoparticles. 55 Radwan SES et al stated that an increase in BSA concentration from 2.5% to 10% resulted in a decrease in particle size from 260 nm to 100.5 nm.…”

“…As reported by Burns and Zydney, the surface charge had a strong influence on protein adsorption. 75 Based on the literature review in Table 2 , five studies conducted by Fatemeh et al 57 Bronze-Uhle et al 76 Hemlata, Gupta, and Tejavath, 77 Jenita et al 65 and Tarhini et al 4 discussed the influence of BSA solution pH on the physicochemical characterization of the formed nanoparticles.…”

“…BSA solution with a pH of 8 produced a small particle size because the aggregation between molecules was hindered by electrostatic repulsion. 65 …”

“…BSA solution with a pH of 8 produced a small particle size because the aggregation between molecules was hindered by electrostatic repulsion. 65 In a study by Bronze-Uhle et al where salicylic acid was used as the active ingredient, modifying the pH of the solution significantly affected the net charge on the protein surface. This is because proteins are made up of amino acids and hydrogen, which interact with ions in the solution.…”