Brucea javanica-Derived Natural Lipid Droplets: Selective Oral Lymph Targeting and Endocytic Transport Mechanisms

Guo, Xiaofeng; Zeng, Shuni; Chen, Qiwei; Lin, Wen; Ma, Yan

doi:10.3390/pharmaceutics18020260

Open AccessArticle

Brucea javanica-Derived Natural Lipid Droplets: Selective Oral Lymph Targeting and Endocytic Transport Mechanisms

by

Xiaofeng Guo

^†

,

Shuni Zeng

^†,

Qiwei Chen

,

Wen Lin

and

Yan Ma

^*

School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, No. 232, Waihuan East Road, Guangzhou 510006, China

^*

Author to whom correspondence should be addressed.

^†

These authors contributed equally to this work.

Pharmaceutics 2026, 18(2), 260; https://doi.org/10.3390/pharmaceutics18020260

Submission received: 5 January 2026 / Revised: 5 February 2026 / Accepted: 16 February 2026 / Published: 20 February 2026

(This article belongs to the Special Issue A Commemorative Issue in Honor of Professor Gregory Gregoriadis: Liposomes for the Delivery of Drugs and Vaccines)

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Abstract

Background: Brucea javanica oil (BJO) suffers from poor oral bioavailability due to oxidative degradation and hepatic first-pass effect. Methods: Here, we report a one-step, solvent-free isolation of endogenous Brucea javanica lipid droplets (BJLDs) that function as a “drug-in-carrier” delivery platform. Results: BJLDs exhibited a uniform size distribution and superior oxidative stability. In vitro digestion showed 80% long-chain fatty acids released within 4 h following first-order kinetics. Caco-2 transport studies revealed caveolin-dependent endocytosis as the dominant uptake route and a 2.3-fold increase in rhodamine 123 accumulation versus free drug, indicating potent P-gp inhibition. A cycloheximide-blocked rat model quantified the intestinal lymphatic transport rate at 89.73%. Plasma t_1/2 and MRT of linoleic acid were 8.44 ± 3.16 h and 11.45 ± 2.72 h, respectively. LC-MS/MS confirmed retention of brusatol and bruceine inside BJLDs. Conclusions: This study provides direct evidence that micron-sized lipid droplets derived from plants can achieve >80% lymphatic targeting after oral administration, offering a green and scalable alternative to conventional BJO formulations.

Keywords: Brucea javanica; lipid droplets; lymphatic transport; P-gp inhibition; drug-in-carrier

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MDPI and ACS Style

Guo, X.; Zeng, S.; Chen, Q.; Lin, W.; Ma, Y. Brucea javanica-Derived Natural Lipid Droplets: Selective Oral Lymph Targeting and Endocytic Transport Mechanisms. Pharmaceutics 2026, 18, 260. https://doi.org/10.3390/pharmaceutics18020260

AMA Style

Guo X, Zeng S, Chen Q, Lin W, Ma Y. Brucea javanica-Derived Natural Lipid Droplets: Selective Oral Lymph Targeting and Endocytic Transport Mechanisms. Pharmaceutics. 2026; 18(2):260. https://doi.org/10.3390/pharmaceutics18020260

Chicago/Turabian Style

Guo, Xiaofeng, Shuni Zeng, Qiwei Chen, Wen Lin, and Yan Ma. 2026. "Brucea javanica-Derived Natural Lipid Droplets: Selective Oral Lymph Targeting and Endocytic Transport Mechanisms" Pharmaceutics 18, no. 2: 260. https://doi.org/10.3390/pharmaceutics18020260

APA Style

Guo, X., Zeng, S., Chen, Q., Lin, W., & Ma, Y. (2026). Brucea javanica-Derived Natural Lipid Droplets: Selective Oral Lymph Targeting and Endocytic Transport Mechanisms. Pharmaceutics, 18(2), 260. https://doi.org/10.3390/pharmaceutics18020260

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Brucea javanica-Derived Natural Lipid Droplets: Selective Oral Lymph Targeting and Endocytic Transport Mechanisms

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