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. 2024 Dec 23;33(1):9.
doi: 10.1007/s40199-024-00544-9.

In-vivo and in-vitro assessment of curcumin loaded bile salt stabilized nanovesicles for oral delivery

Fahima M Hashem  1 , Dalia Elkhateeb  2 , Marwa M Ali  2 , Rania S Abdel-Rashid  3   4
Affiliations

In-vivo and in-vitro assessment of curcumin loaded bile salt stabilized nanovesicles for oral delivery

Fahima M Hashem et al. Daru. .

Abstract

Background: Bile salts enriched nanovesicles (bilosomes) have been attention worthy in the past few years due to their distinctive effect on the enhancement of drug delivery through various physiological administration routes. Oral delivery of multifunctioning phytochemical curcumin has faced a lot of difficulties due to its scarce solubility and poor oral bioavailability.

Objective: The current investigation aimed to develop curcumin loaded bilosomes for improvement of oral curcumin bioavailability with maximum efficiency and safety.

Methods: The effect of formulation variables (type of span, SDC % to total lipid content Span/Cholesterol molar ratio) on physicochemical characterization and in vitro drug release in simulated intestinal fluid was investigated. Furthermore, in-vivo protective effect of bilosomes on hepatic and renal functions was also studied.

Results: and conclusion. The results revealed that the best curcumin loaded bilosomal formulation showed spherical nanovesicular morphology with particle size 145.1 ± 19.42 nm with highly reasonable %EE (93%), Zeta potential (≥ -30mv), prominent controlled in-vitro release reaching 55.18 ± 1.10 after 96 h. The formulation also showed good storage stability with negligible differences in physical features and content. The IC50 values of bilosomal, niosomal, and free curcumin were 216.50, 211.44, and 121.63 mmol/ml, respectively revealing that the unencapsulated curcumin displayed high toxicity on Caco2 cell line (nearly 2 folds). Additionally, the prepared bilosomes showed significant in-vivo hepatic and renal protection in liver cirrhosis induced rats with conservation to all liver and renal markers and histopathological morphology. The study assumes the effectiveness and safety of oral delivery of curcumin loaded bile salts stabilized nanovesicles and its powerful commandment for further investigations.

Keywords: Bilosomes; Curcumin; Cytotoxicity; Drug delivery; Nanovesicles.

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Conflict of interest statement

Declarations. Ethics approval and consent to participate: All the animals were kept and used for the experiment in accordance with the Animal research ethical Committee, Faculty of Pharmacy, Helwan University (code 18A2021). Consent for publication: All authors have read and agreed to the published version of the manuscript. Moreover, they agree to be accountable for all aspects of the work. Competing interests: Authors have no conflict of interests in the current study.

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