Berberine liposomes encapsulate berberine, a plant-derived alkaloid, within lipid bilayers, improving its solubility and bioavailability. This encapsulation is particularly advantageous for increasing the therapeutic efficacy of berberine, which is otherwise limited by its poor water solubility and low oral bioavailability.
Berberine liposomes can be prepared using methods like ethanol-injection and thin-film hydration. These techniques help achieve a narrow size distribution and high entrapment efficiency, which are crucial for consistent therapeutic effects.
Berberine liposomes are used in various therapeutic areas including the treatment of hypercholesterolemia, inflammation, diabetes, and atherosclerosis. They have also been explored for their anti-leishmanial activity, showing promise in enhancing drug delivery to infected organs in visceral leishmaniasis.
Liposomal encapsulation of berberine significantly enhances its bioavailability by protecting it from rapid metabolic degradation and facilitating its absorption into the systemic circulation. This leads to higher and more sustained levels of the drug in the bloodstream.

Entrapment efficiency of the berberine-loaded liposomes generated by ethanol-injection and thin-film hydration methods
The study explores the development of liposomes as a delivery system for berberine (BBR), a poorly water-soluble alkaloid with therapeutic potential. Berberine's oral administration is limited by first-pass metabolism and poor absorption. To address this, BBR-loaded liposomes were fabricated using ethanol-injection and thin-film hydration methods. The liposomes exhibited sizes ranging from 50 nm to 449 nm with a polydispersity index (PDI) below 0.3, indicating uniformity. The entrapment efficiency (EE) varied from 56% to 92%, with higher EE generally observed in liposomes prepared by the thin-film hydration method.
Experimental data showed that BBR accumulated within the phospholipid bilayers of the liposomes, enhancing stability and providing controlled release. In vitro studies demonstrated extended release of BBR from both types of liposomes, which is crucial for improving its bioavailability. The findings highlight the potential of BBR-loaded liposomes to overcome the limitations of BBR's oral delivery, offering a promising strategy for its therapeutic use. The study concludes that both nanofabrication methods are effective for creating BBR-loaded liposomes with desirable size, uniformity, and drug release characteristics.
Duong, T. T., Isomäki, A., et al. Nanoformulation and evaluation of oral berberine-loaded liposomes. Molecules. 2021, 26(9): 2591. Under Open Access license CC BY 4.0, without modification.
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