Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Lumefantrine-neusilin® based amorphous multi-component solid dispersion: In vivo and in vitro characterization

Calister E Ugwu¹ , Bridget C Obitte², Edith O Diovu³, Mumuni A Momoh⁴, Ikechukwu V Onyishi¹, Godswill C Onunkwo¹

¹Department of Pharmaceutical Technology and Industrial Pharmacy,; ²Department of Science Laboratory Technology, Faculty of Physical Sciences,; ³Department of Pharmacognosy and Environmental Medicine,; ⁴Drug Delivery Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka 410001, Nigeria.

For correspondence:- Calister Ugwu Email: calister.ugwu@unn.edu.ng Tel:+234-8038933463

Received: 15 November 2024 Accepted: 8 December 2024 Published: 28 December 2024

Citation: Ugwu CE, Obitte BC, Diovu EO, Momoh MA, Onyishi IV, Onunkwo GC. Lumefantrine-neusilin® based amorphous multi-component solid dispersion: In vivo and in vitro characterization. Trop J Pharm Res 2024; 23(12):1973-1981 doi: 10.4314/tjpr.v23i12.2

© 2024 The authors.
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Abstract

Purpose: To develop Neusilin-based amorphous multi-component solid dispersions (NAM-SDs) to improve poor aqueous solubility, low bioavailability and absorption of lumefantrine and enhance the antiplasmodial activity. Methods: Solvent evaporation technique was adopted to produce second-generation SDs (N1 - N3); third-generation SDs (N4 - N6 and N10 - N12); and multi-component SDs, NAM-SDs, (N7 - N9 and N13 - N18). In vitro drug release, in vivo anti-plasmodial activity, differential scanning calorimetry (DSC), and wide-angle x-ray diffraction (WAXD) were carried out on the SDs. Results: The highest drug release (80 %) was observed in multi-component SDs (NAM-SDs, formulation N17 containing Kollidon® VA 64). A significant antiplasmodial activity (p < 0.05) was observed in mice that received NAM-SDs. The DSC and WAXD studies showed that the formulations solubilized and exhibited an amorphous state. Conclusion: Multi-component amorphous-based lumefantrine SDs (NAM-SDs) may serve as a potential alternative carrier system for oral lumefantrine delivery.

Keywords: Multi-component solid dispersion, Lumefantrine, Neusilin®, Kollidon® VA 64, Antiplasmodial