A team of scientists from the Institute of Nano Science & Technology (INST) has developed nanorods from the nonsteroidal anti-inflammatory drug (NSAID) Aspirin, a popular medicine used for pain reduction, fever, or inflammation and found it to be an effective non–invasive small molecule-based nano-therapeutics against cataract. This will bring in a process of economical non-surgical prevention of cataract.
INST is an autonomous institute under the Department of Science & Technology, Government of India.
Cataract is a major type blindness that occurs when the structure of crystallin proteins that make up the lens in our eyes deteriorates, causing damaged or disorganised proteins to aggregate and forms a milky blue or brown layer, which subsequently affects lens transparency. Therefore, prevention of the formation of these aggregates as well as their destruction in the early stage of disease progression is very effective as a treatment strategy for cataracts.
With ageing or various other reasons such as like diabetes, past surgery and high blood pressure, the lens protein crystallin aggregates to form opaque structures in the eye lens, which impairs vision and cause cataract.
With so many cataract cases in India, it’ important to make cataract operations affordable and accessible. This becomes possible when the material used in the treatment process is cost-effective and less complicated for the common man.
The team of scientists published their research in the Journal of Materials Chemistry B. The research findings will help prevent cataracts in an economical and less complicated way.
The scientists have used the anti-aggregation ability of self-build aspirin nanorods as an effective non –invasive small molecule-based nanotherapeutics against cataract.
Aspirin nanorods obstruct the aggregation of crystallin protein and various peptides derived from its fragmentation, which play a critical role in cataract formation. They stop the protein/peptide aggregation through biomolecular interactions, which convert beta-turn like the structure of the crystallin peptides, responsible for amyloid formation into coils and helices, those fail to aggregate. These were found to stop cataract formation by inhibiting aggregation of crystallin, and crystallin derived peptide aggregates.
The targeted disaggregation of the accumulated alpha-crystallin protein and crystallin derived peptide aggregates in aged and cataractous human lenses are considered as a viable therapeutic strategy for the prevention of cataract formation. The aspirin nanorods are created using the process of molecular self-assembly, which is an economical and high–yield technique to generate the aspirin nanorods as compared to the high cost and laborious physical methods generally used for the synthesis of nanoparticles.
Computational studies based on molecular dynamics (MD) simulations were performed to identify the molecular mechanism of aspirin’s anti-aggregation behaviour and the nature of the protein (peptide)-inhibitor interactions between the synthetic peptides and aspirin.
The scientists observed that the peptide-aspirin (inhibitor) interactions eventually transformed peptides secondary structures from beta-turns, those are responsible for the formation of the amyloid, into various coils and helixes, preventing its aggregation. These simulations disclosed the secret behind aspirin’s ability to act as a potential inhibitor towards amyloid-like fibril formation by the model cataract peptides.
Many natural compounds have already been reported as potential aggregation inhibitors for crystallin aggregation. However, the utility of nonsteroidal anti-inflammatory drugs (NSAIDs) like aspirin in this direction will open a new paradigm.
Moreover, aspirin nanorods due to their nano-size will enhance the bioavailability, improve drug loading, lower toxicity, etc. Accordingly, the delivery of the aspirin nanorods as eye drops is going to serve as an effective and viable option to treat cataract non-invasively.
This easy to use and economical alternative nonsurgical treatment method will help patients in many developing countries in the world who cannot access expensive cataract treatments and surgeries.