Design of quetiapine fumarate loaded polyethylene glycol decorated graphene oxide nanosheets: Invitro-exvivo characterization

Gaurav S Patil; Sopan N Nangare; Dilip A Patil; Dinesh D Borhade; Ganesh B Patil

doi:10.1016/j.pharma.2024.04.009

Design of quetiapine fumarate loaded polyethylene glycol decorated graphene oxide nanosheets: Invitro-exvivo characterization

Ann Pharm Fr. 2024 Apr 27:S0003-4509(24)00066-X. doi: 10.1016/j.pharma.2024.04.009. Online ahead of print.

Authors

Gaurav S Patil¹, Sopan N Nangare¹, Dilip A Patil², Dinesh D Borhade¹, Ganesh B Patil³

Affiliations

¹ Department of Pharmaceutics, H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur, 425405 Dhule (MS), India.
² Department of Pharmaceutical Chemistry, H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur, 425405 Dhule (MS), India.
³ Department of Pharmaceutics, H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur, 425405 Dhule (MS), India. Electronic address: ganu16@gmail.com.

PMID: 38685472
DOI: 10.1016/j.pharma.2024.04.009

Abstract

Quetiapine Fumarate (QF) is an atypical antipsychotic with poor oral bioavailability (9%) due to its low permeability and pH-dependent solubility. Therefore, this study aims to design QF-loaded polyethylene glycol (PEG) functionalized graphene oxide nanosheets (GON) for nasal delivery of QF. In brief, GO was synthesized using a modified Hummers process, followed by ultra-sonication to produce GON. Subsequently, PEG-functionalized GON was prepared using carbodiimide chemistry (PEG-GON). QF was then decorated onto the cage of PEG-GON using the π-π stacking phenomenon (QF@PEG-GON). The QF@PEG-GON nanocomposite underwent several spectral characterizations, in vitro drug release, mucoadhesion study, ex vivo diffusion study, etc. The surface morphology of QF@PEG-GON nanocomposite validates the cracked nature of the nanocomposite, whereas the diffractograms and thermogram of nanocomposite confirm the conversion of QF into an amorphous form with uniform distribution in PEG-GON. Moreover, an ex vivo study of PEG-GON demonstrates superior mucoadhesion capacity due to its surface functional groups and hydrophilicity. The percent drug loading content and percent entrapment efficiency of the nanocomposite were found to be 9.2±0.62% and 92.3±1.02%, respectively. The developed nanocomposite exhibited 43.82±1.65% drug release within 24h, with the Korsemeyer-Peppas model providing the best-fit release kinetics (R²: 0.8614). Here, the interlayer spacing of PEG-GON prevented prompt diffusion of the buffer, leading to a delayed release pattern. In conclusion, the anticipated QF@PEG-GON nanocomposite shows promise as a nanocarrier platform for nasal delivery of QF.

Keywords: Fumarate de quétiapine; Graphene oxide nanosheet; Mucoadhesion; Mucoadhésion; Nanofeuillet d’oxyde de graphène; Polyethylene glycol; Polyéthylène glycol; Quetiapine fumarate; Schizophrenia; Schizophrénie.