Optimised formulation and characterisation of liposomes for enhanced stability and antiproliferative efficacy of Orthosiphon aristatus var. aristatus extract in lung cancer treatment

Hussein M., Baharetha and Amin Malik Shah Abdul, Majid and Mansoureh V., Nazari and Nozlena Abdul, Samad and Majed Ahmed, Al-Mansoub and Mohamad Taleb, Agha and Saad S., Dahham (2025) Optimised formulation and characterisation of liposomes for enhanced stability and antiproliferative efficacy of Orthosiphon aristatus var. aristatus extract in lung cancer treatment. Natural Product Research. pp. 1-10. ISSN 1478-6427

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Abstract

In this study, characterization and antiproliferative potencies of the standardized 50% ethanol extract of Orthosiphon aristatus var. aristatus leaves were assessed for human lung cancer in vitro. A liposomal drug delivery system was developed to improve the bioavailability and efficacy. Three formulations were developed based on the extract-to-phospholipid ratio, phospholipid, and cholesterol content. NP2, a formulation consisting of a 1:1 extract to phosphatidylcholine ratio with 20% cholesterol, showed optimum stability and efficacy. Liposomes were characterized qualitatively and quantitatively using light, TEM, SEM microscopy, zeta sizer, and zeta potential. NP2 showed significantly better release properties of the bioactive compounds and a good stability profile than the extract. The extract and the liposomes inhibited the proliferation of human lung adenocarcinoma (A549) and human normal endothelial cells (EA.hy926). All in all, the results of this study indicate that the extract has potent anti-lung cancer activity and the NP2 liposome formulation improves its efficacy.

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