IMPACT OF LIGAND CONJUGATION OF PHYSICOCHEMICAL ATTRIBUTES OF POLYMERIC NANOPARTICLES OF ATYPICAL ANTIPSYCHOTIC DRUG FOR NOSE-TO-BRAIN DELIVERY

TEJA KUMAR PONDURI; CHAKRAVARTHI GUNTUPALLI; BALAMURUGAN JEGANATHAN; NARENDER MALOTHU

doi:10.22159/ijap.2024v16i6.52003

Authors

TEJA KUMAR PONDURI KL College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh, India https://orcid.org/0000-0001-6547-4870
CHAKRAVARTHI GUNTUPALLI KL College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh, India
BALAMURUGAN JEGANATHAN Formulation Development, Zhejiang Heze Pharmaceutical Technology Co., Ltd., 101, No. 1 Street, Qiantang New District, Hangzhou, Zhejiang. PR China https://orcid.org/0009-0006-9826-2536
NARENDER MALOTHU KL College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh, India

DOI:

https://doi.org/10.22159/ijap.2024v16i6.52003

Keywords:

Ziprasidone, Ligand conjugated nanoparticles, Transferrin, Chitosan, Click reaction, Nose to cerebrum

Abstract

Objective: To formulate and characterize the ligand-conjugated chitosan nanoparticles of Ziprasidone Hydrochloride (ZH) and compare with its plain chitosan nanoparticles.

Methods: Transferrin (Tf) conjugated Chitosan Nanoparticles (CH-NP) containing ZH were prepared by ionotropic gelation method by using modified chitosan and Tf. Physicochemical attributes of nanoparticles which can potentially impact the nose-to-brain delivery were evaluated.

Results: The Tf-CH-NP has demonstrated 207.1 nm mean particle size, 87.6% entrapment efficiency with a release of 89.34% at 24 h and has shown about 2.22 times more release than drug suspension and about 4.5% more than plain CH-NP. The similar trend was observed in Ex vivo nasal permeation study. Its acceptability was shown in histomorphology study, where a minimal inflammation seen, that might be due to the pH of the formulation. There is deeper penetration with Tf-CH-NP, which is more promising for penetration into brain.

Conclusion: The formulated Tf-CH-NP has a greater potential due to ligand conjugation to reach the brain and, facilitate targeted delivery and enables better treatment of schizophrenia at minimal doses.

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