Coencapsulation of gemcitabine and thymoquinone in citrem-phosphatidylcholine hexosome nanocarriers improves in vitro cellular uptake in breast cancer cells

Loo, Yan Shan and Zahid, N. Idayu and Madheswaran, Thiagarajan and Ikeno, Shinya and Nurdin, Armania and Azmi, Intan Diana Mat (2023) Coencapsulation of gemcitabine and thymoquinone in citrem-phosphatidylcholine hexosome nanocarriers improves in vitro cellular uptake in breast cancer cells. Molecular Pharmaceutics, 20 (9). pp. 4611-4628. ISSN 1543-8384, DOI https://doi.org/10.1021/acs.molpharmaceut.3c00333.

Full text not available from this repository.

Abstract

Lyotropicliquid crystalline nanoassemblies (LLCNs) areinternallyself-assembled (ISA)-somes formed by amphiphilic molecules in a mixturecomprising a lipid, stabilizer, and/or surfactant and aqueous media/dispersant.LLCNs are unique nanoassemblies with versatile applications in a widerange of biomedical functions. However, they comprise a nanosystemthat is yet to be fully explored for targeted systemic treatment ofbreast cancer. In this study, LLCNs proposed for gemcitabine and thymoquinone(Gem-TQ) co-delivery were prepared from soy phosphatidylcholine (SPC),phytantriol (PHYT), or glycerol monostearate (MYVR) in optimized ratioscontaining a component of citric and fatty acid ester-based emulsifier(Grinsted citrem) or a triblock copolymer, Pluronic F127 (F127). Hydrodynamicparticle sizes determined were below 400 nm (ranged between 96 and365 nm), and the series of nanoformulations displayed negative surfacecharge. Nonlamellar phases identified by small-angle X-ray scattering(SAXS) profiles comprise the hexagonal, cubic, and micellar phases.In addition, high entrapment efficiency that accounted for 98.3 & PLUSMN;0.1% of Gem and 99.5 & PLUSMN; 0.1% of TQ encapsulated was demonstratedby the coloaded nanocarrier system, SPC/citrem/Gem-TQ hexosomes. Lowcytotoxicity of SPC-citrem hexosomes was demonstrated in MCF10A cellsconsistent with hemo- and biocompatibility observed in zebrafish (Danio rerio) embryos for up to 96 h postfertilization (hpf).SPC/citrem/Gem-TQ hexosomes demonstrated IC50 of 24.7 & PLUSMN;4.2 & mu;M in MCF7 breast cancer cells following a 24 h treatmentperiod with the moderately synergistic interaction between Gem andTQ retained (CI = 0.84). Taken together, biocompatible SPC/citrem/Gem-TQhexosomes can be further developed as a multifunctional therapeuticnanodelivery approach, plausible for targeting breast cancer cellsby incorporation of targeting ligands.

Item Type: Article
Funders: Malaysia Toray Science Foundation (MTSF) Science and Technology Research Grant, Universiti Putra Malaysia [Grant No: 9734400]
Uncontrolled Keywords: Lyotropic liquidcrystalline nanoparticles; Soy phosphatidylcholine; Gemcitabine; Thymoquinone; Combination therapy
Subjects: R Medicine > RM Therapeutics. Pharmacology
R Medicine > RS Pharmacy and materia medica
Divisions: Faculty of Science > Department of Chemistry
Depositing User: Ms. Juhaida Abd Rahim
Date Deposited: 01 Nov 2025 12:27
Last Modified: 01 Nov 2025 12:27
URI: http://eprints.um.edu.my/id/eprint/48661

Actions (login required)

View Item View Item