Quantification and Brain Targeting of Eugenol-Loaded Surface Modified Nanoparticles Through Intranasal Route in the Treatment of Cerebral Ischemia

Niyaz Ahmad; Rizwan Ahmad; Md Aftab Alam; Farhan Jalees Ahmad

doi:10.1055/a-0596-7288

Drug Research, Table of Contents

Drug Res (Stuttg) 2018; 68(10): 584-595
DOI: 10.1055/a-0596-7288

Original Article

Quantification and Brain Targeting of Eugenol-Loaded Surface Modified Nanoparticles Through Intranasal Route in the Treatment of Cerebral Ischemia

Niyaz Ahmad

¹Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Kingdom of Saudi Arabia

,

Rizwan Ahmad

²Department of Natural Products and Alternative Medicine, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Kingdom of Saudi Arabia

,

Md Aftab Alam

³Department of Pharmaceutics, School of Medical and Allied Sciences, Galgotias University, Gautam Budh Nagar, Greater Noida, India

,

Farhan Jalees Ahmad

⁴Nanomedicine Lab, Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi, India

› Author Affiliations

Abstract

Objective To enhance brain bioavailability for intranasally administered Eugenol-encapsulated-chitosan-coated-PCL-Nanoparticles (CS-EUG-PCL-NPs).

Methods Chitosan-coated-PCL-Nanoparticles (CS-PCL-NPs) were developed through double emulsification-solvent evaporation technique and further characterized for particle size, zeta potential, size distribution, encapsulation efficiency as well as in vitro drug release. UPLC-PDA method was developed to evaluate brain-drug uptake for optimized CS-EUG-PCL-NPs and to determine it’s pharmacokinetic in rat’s brain as well as plasma.

Results Mean particles size (224.5±5.31), polydispersity index (PDI) i. e. (0.216±0.020) and entrapment efficiency (68.13±5.03) was determined for developed NPs. UPLC-PDA-eλ study showed a significantly high mucoadhesive potential of CS-EUG-PCL-NPs and least for conventional and homogenized nanoformulation; elution time for EUG and internal standard (IS) thymoquinone as 3.50 and 3.61 min were observed respectively. Furthermore, intra and inter-assay (%CV) of 0.25–1.57, %accuracy (97.11-99.00%) as well as a linear dynamic range (100.00 ng/mL–2500.0 ng/mL), was observed. Pharmacokinetic studies in Wistar rat brain and plasma exhibited a high AUC_0-24 alongwith an amplified C_max (p**<0.01) as compared to i. v. treated group.

Conclusions Intranasal administration of developed CS-coated-EUG-loaded-PCL-NPs enhanced the drug bioavailability in rat brain and thus preparation of Eugenol-NPs may help treat cerebral ischemia effectively. The toxicity studies performed at the end revealed safe nature of optimized nanoformulation.

Key words

Eugenol - UPLC-PDA-eλ - CS-PCL-NPs - Intranasal drug delivery - Brain bioavailability and Brain Pharmacokinetic

Full Text

References

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