Preparation and characterization of micellar nanoparticles using crude saponins from five Congolese plant species

Abstract

Nanoparticles (NPs) have significantly advanced medical applications, including drug delivery, immunotherapy, vaccines, and diagnostics. This versatility is partly due to the potential of tailoring NPs from multiple sources. Notably, saponins, amphiphilic plant metabolites, have shown great promise in NP formulation. This study explored the development of micellar NPs using saponin crude fractions (SCFs) extracted from five Congolese plant species: Millettia laurentii, Penthaclethra eetveldeana, Schwenckia americana, Musa paradisiaca, and Musa sapientum. Plant materials were subjected to histological examination through optical microscopy, while phytochemical analyses by thin-layer chromatography confirmed the presence and predominance of saponins in the SCFs. We used a phthalocyanine-isoniazid hybrid (Pc-INH) as a hydrophobic probe to determine the critical micellar concentrations of SCFs and explore the feasibility of developing cost-effective saponin-based micelles (SBMs). Phytochemical screenings indicated saponins in the extracted SCF and other metabolites like flavonoids, phenolic acids, and anthocyanins. Dynamic light scattering and transmission electron microscopy analyses revealed the formation of nano-sized particles, particularly noting SBMs from P. eetveldeana with notable dimensions (157 ​nm, PDI of 0.27, and ZP of −4.01 ​mV) and spherical shape. The micelles from M. laurentii exhibited superior encapsulation efficiency for Pc-INH (55%) compared to control micelles formulated from pure saponin (33%). In vitro tests showed that M. paradisiaca SBMs have the best safety profile for red blood cells, with a 10% hemolysis rate compared to a 150% rate for bulk SCFs. However, there is a significant difference between SCFs and SBMs (p ​< ​0.0001). The release profiles of M. paradisiaca SBMs show a pH-dependent relationship, suggesting potential for stimuli-responsive drug delivery. This work lays the foundation for leveraging plant-derived crude saponins in nanotechnology, emphazising their encapsulation efficiency, controlled release potential, and biocompatibility, paving the way for the cost-effective production of high-value biomedical NPs.

Keywords

Saponins / Nanoparticles / Micelles / Secondary metabolites / Hemolysis / Drug delivery

CRediT authorship contribution statement

Pathy B. Lokole: Writing - original draft, Software, Methodology, Investigation, Formal analysis, Data curation. Nadège K. Ngombe: Writing - review & editing, Visualization, Validation. Dave I. Motomba: Writing - review & editing, Visualization, Validation, Investigation, Data curation. Justin B. Safari: Writing - review & editing, Software, Methodology, Formal analysis, Data curation. Michel K. Mpuza: Writing - review & editing, Visualization, Validation, Methodology, Formal analysis, Data curation. Rui W.M. Krause: Writing - review & editing, Visualization, Validation, Supervision, Resources, Investigation, Formal analysis. Paulin K. Mutwale: Writing - review & editing, Visualization, Validation, Supervision, Methodology, Investigation, Formal analysis. Christian I. Nkanga: Writing - review & editing, Visualization, Validation, Supervision, Resources, Project administration, Methodology, Funding acquisition, Formal analysis, Conceptualization.

Ethics approval

The ethical committee of the School of Public Health of the University of Kinshasa (Kinshasa, DR Congo) examined and approved the use of blood samples for the in vitro experiments in this study (Approval No.: ESP/CE/27B/2024).

Data availability

Not applicable.

Funding

This document was produced with the financial assistance of the European Union (Grant No. DCI-PANAF/2020/420-028) through the African Research Initiative for Scientific Excellence (ARISE) pilot program. ARISE is implemented by the African Academy of Sciences with support from the European Commission and the African Union Commission. The contents of this document are the sole responsibility of the authors. They can, under no circumstances, be regarded as reflecting the position of the European Union, the African Academy of Sciences, and the African Union Commission.

Declaration of competing interest

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Acknowledgments

We sincerely acknowledge the Laboratoire d'Analyses et de Recherches en Alimentation et Nutrition (LARAN) of the University of Kinshasa, Mr Néhémie E. Bala and Messie M. Muipata for their technical support. We also thank the Rhodes University Electron Microscopy Unit (EMU), particularly Mr. M. Randal, for training and guidance with TEM sample preparation and data collection. Further, we also thank the Rhodes University Biopharmaceutics Research Group (RUBRG) for DLS analysis and data collection.

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