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Nanostructured Lipid Carriers (NLCs) of Lumefantrine with Enhanced Permeation

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Abstract

Purpose

Lumefantrine (LF) is an antimalarial agent with low water solubility and inconsistent oral bioavailability (4–11%), which limits its therapeutic potential. Hence, this research aimed to design nanostructured lipid carriers (NLCs) for LF to improve its oral administration.

Methods

LF-NLCs were formulated using the hot emulsification-probe sonication method. Solubility and molecular interactions studies were performed for the selection of appropriate formulation excipients. Various critical formulation and process variables were optimized during this process. The optimized LF-NLC was then evaluated for various physicochemical properties. Ex vivo gut permeation was done to analyze LF-NLC permeation across the gut, and in vitro drug release was performed to understand its release behavior.

Results

Particle size, polydispersity index (PDI), zeta potential, and % encapsulation efficiency of the optimized formulation were found to be 78.85 ± 2.55 nm, 0.255 ± 0.03, -8.25 ± 2.29 mV, and 74.32 ± 1.63%, respectively. Transmission electron microscopy revealed the particulate nature and spherical shape of LF-NLCs. The loss of sharp endothermic peak in DSC and reduced crystallinity in XRD indicated the amorphization of encapsulated drug. The in vitro drug release study showed sustained release of LF from NLC. Ex vivo gut permeation exhibited an almost 3.5-fold increase in permeation of NLCs over plain drug suspension.

Conclusion

According to the above findings, NLC could be a promising approach for the oral delivery of LF and drugs with similar properties.

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Acknowledgements

The authors express their sincere gratitude towards the All India Council for Technical Education (AICTE-NAFETIC) to offer research facilities. Authors are also thankful to Gattefosse, India, Mohini Organics Pvt. Ltd. India, Abitec Corporation, India, and BASF, India, for providing gift samples of various excipients.

Funding

This research is financially supported by the University Grants Commission of India.

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Authors and Affiliations

  1. Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur - 425405, Maharashtra, India

    Ganesh Shevalkar

  2. Department of Pharmaceutical Sciences and Technology, Elite Status and Center of Excellence- Govt. of Maharashtra, Institute of Chemical Technology, University under Section 3 of UGC Act – 1956, TEQIP Phase III Funded, Matunga (E), Mumbai - 400019, India

    Manoj Pawar & Pradeep Vavia

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  1. Ganesh Shevalkar
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Correspondence to Pradeep Vavia.

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Shevalkar, G., Pawar, M. & Vavia, P. Nanostructured Lipid Carriers (NLCs) of Lumefantrine with Enhanced Permeation. J Pharm Innov 17, 1221–1234 (2022). https://doi.org/10.1007/s12247-021-09590-1

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