Title:PEGylated Chitosan Biodegradable Nanoparticles Delivery of Salvia officinalis and Melissa officinalis for Enhanced Brain Targeting
Volume: 14
Issue: 1
Author(s): Sanjana Datta, Asmita Gajbhiye and Shailendra Patil*
Affiliation:
- SVN Institute of Pharmaceutical Sciences, Swami Vivekanad University, Sagar, Madhya Pradesh, 470228, India
Keywords:
PEGylation, chitosan, nanoparticles, natural extract, Alzheimer disease, brain targeting.
Abstract:
Background: Alzheimer's disease (AD) is a progressive neurodegenerative condition
characterized by the gradual decline of cognitive abilities, primarily caused by impairments in the
cholinergic system. AD is diagnosed based on the presence of specific pathological features, including
senile plaques, neurofibrillary tangles, and the loss of neurons and synapses. Despite ongoing
efforts, the etiology of AD remains unclear, and there is a significant lack of effective
treatments to meet the medical needs of affected individuals. The complex nature of AD, involving
multiple factors, presents challenges in the development of potential therapies. Numerous obstacles
hinder the achievement of optimal pharmacological concentration of promising molecules
for AD treatment. These obstacles include the presence of the blood-brain barrier (BBB), which
restricts the entry of therapeutic agents into the brain, as well as issues related to poor bioavailability
and unfavorable pharmacokinetic profiles. Unfortunately, many therapeutically promising
compounds have failed to overcome these hurdles and demonstrate efficacy in treating AD.
Methods: The PEGylated chitosan nanoconjugate was developed and evaluated for delivery of anti-Alzheimer natural extract of Salvia officinalis and Melissa officinalis to the brain. The nanoconjugates (S-PCN and M-PCN) were developed by ionic gelation technique.
Result: The nanoconjugates (S-PCN and M-PCN) were evaluated for various optical and in-vitro parameters. MTT assay on UCSD229i-SAD1-1 human astrocytoma cells indicated IC50 values of 0.42, 0.49, 0.67, and 0.75 μM for S-PCN, M-PCN formulations, and free Salvia officinalis and Melissa officinalis extracts, respectively. The In vitro assessments using cell lines have confirmed the improved uptake and distribution of nanoconjugates compared to free extracts. These findings were validated through confocal microscopy and apoptosis assays, revealing a substantial increase in the accumulation of nanoconjugates within the brain. The targeting potential OF M-PCN over S-PCN was found to be 2-fold significant.
Conclusion: Based on the findings, it can be inferred that biodegradable PEGylated chitosan nanoconjugates hold promise as effective nano-targeting agents for delivering anti-Alzheimer drugs to the brain. The incorporation of PEGylated chitosan nanoparticles in this approach demonstrates enhanced delivery capabilities, ultimately leading to improved therapeutic outcomes.
