Affiliations 

  • 1 Department of Pharmaceutics, Delhi Pharmaceutical Science and Research University, New Delhi, India
  • 2 Department of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, India
  • 3 Central Council for Research in Unani Medicine (CCRUM), Ministry of AYUSH, Government of India, New Delhi, India
  • 4 Institute of Nuclear Medicine & Allied Sciences, DRDO, New Delhi, India
  • 5 Faculty of Pharmaceutical Sciences, UCSI University, Kuala Lumpur, Malaysia
  • 6 Department of Pharmacy, School of Healthcare and Allied Sciences, GD Goenka University, Gurugram, India
J Drug Target, 2024 Sep 04.
PMID: 39229894 DOI: 10.1080/1061186X.2024.2397800

Abstract

BACKGROUND: Intranasal drug delivery shows potential for brain access via olfactory and trigeminal routes.

PURPOSE: This work aimed to ensure brain availability of nalbuphine via the nasal route.

METHOD: Chitosan based nanoparticles loaded with nalbuphine were successfully prepared using ionic gelation method and characterised.

RESULT: SEM results revealed that the nanoparticles were spherical in shape, with an average size of 192.4 ± 11.6 nm. Zeta potential and entrapment efficiency was found 32.8 mV and 88.43 ± 7.75%, respectively. The X-ray diffractometry and DSC results unravel a profound understanding on the physical and thermal characteristics. The in-vitro release of nalbuphine from the nanoparticles was biphasic, with an initial burst release followed by a slow-release profile. In-vitro cell study on HEK-293 cells and microscopic images of brain tissue confirmed the safety profile of formulation. In-vivo efficacy studies on animal confirmed the effectiveness of developed intranasal formulation as compared to the standard therapy. The in-vivo pharmacokinetic studies showed that the prepared nanoparticles were able to efficiently deliver nalbuphine to the brain in comparison to the other body organs. Gamma scintigraphy images showed retention of the drug in the brain. Furthermore, the efficacy studies confirmed that the nanoparticles were found significantly more effective than the marketed formulation in pain management.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.