Development of nanoemulsion of antiviral drug for brain targeting in the treatment of neuro-AIDS

Abstract

Abstract Background Delivery of drugs via the nasal route directly to the brain utilizing the olfactory pathway is purportedly known to be a more efficient method to deliver neuro-therapeutics to the brain by circumventing the BBB, thereby increasing the bioavailability of these drugs in the brain. The main objective of the project work is to improve the bioavailability of the antiretroviral drug and to minimize the side effects of this therapy which are observed at the higher side in the chronic HIV treatment. The advantage of nasal drug delivery is its noninvasiveness and self-administration. Nanoformulation provides fast onset of action and helps to achieve site-specific delivery. In the current work, nanoemulsion formulation was developed with a ternary phase system. In vitro characterization of nanoemulsion was performed. Result Optimized batch B2 had a zeta potential of − 18.7 mV showing a stable emulsion system and a particle size of 156.2 nmin desirable size range. Batch B2 has the least variation in globule size with PDI 0.463. Results from ex vivo studies revealed that developed nanoemulsion (B2) possessed a higher rate of drug release compared to other formulations. Conclusion Phase diagrams indicated more width of the nanoemulsion region with an increase in surfactant ratio. Stable nanoemulsion was prepared with a combination of surfactant and co-surfactants. Nanoemulsions could prove one of the best alternatives for brain delivery of potent medications. Graphical Abstract

Keywords

• Antiretroviral therapy
• Nanoemulsion
• Nose-to-brain delivery
• Ex vivo diffusion study
• Cytotoxicity study