Carvedilol-loaded propolis nanoparticles embedded in gel-casted film and 3D electrospun nanofiber film – an in vivo study to enhance the bioavailability via the intranasal route

Fifth Author's Department

Chemistry Department

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https://doi.org/10.1016/j.jddst.2025.107254

All Authors

Noha Khalil Mahdy Aliaa E.M.K. El-Mosallamy Ethar A. Mohamed Mahmoud Hassan Teaima Hassan Mohamed El-Said Azzazy Mohamed El-Nabarawi Sammar Fathy Elhabal

Document Type

Research Article

Publication Title

Journal of Drug Delivery Science and Technology

Publication Date

10-1-2025

doi

10.1016/j.jddst.2025.107254

Abstract

Hypertension, a prevalent cardiovascular ailment, necessitates effective management to avert critical complications. Carvedilol, a non-selective beta-blocker, is widely employed for hypertension yet hindered by poor solubility and restricted disintegration, which in turn results in suboptimal bioavailability. Thus, the work aimed to improve carvedilol bioavailability through the preparation of Propolis Nanoparticles (PNP) and then incorporate them into HPMC Gel-Casted film and Hydroxypropyl-beta-Cyclodextrin (HPbCD) electrospun nanofiber film. PNPs were derived from Bee Propolis, which is proven to show antihypertensive and cardioprotective activities. Bee Propolis revealed improved dissolution and bioavailability after precipitation as nanoparticles. Propolis nanoparticles were prepared using the nanoprecipitation method optimized Via Box-Behnken Design. The optimum carvedilol-loaded Propolis nanoparticles (CPNP) formula was subjected to physicochemical characterization, where the PNP was imaged using transmission electron microscopy, showing spherical nanoparticles with a diameter of 34.18 ± 7.29 nm. Carvedilol's amorphization inside the nanoparticles was presented by Thermogravimetric Analysis (TGA), confirming that it was entrapped in the PNP framework. Afterward, these nanoparticles were integrated into nasal inserts to bypass carvedilol's first-pass metabolism and utilize the nose-to-heart delivery pathways, resulting in higher bioavailability. Gel-Casted film and electrospun nanofiber film were the two nasal inserts prepared in this study, both incorporated with CPNP. The two nasal inserts demonstrated relative bioavailabilities of 235.79 % and 213.98 %, respectively, compared to the commercial oral carvedilol in an In Vivo pharmacokinetic study. This study demonstrates how propolis extract-based nanoparticles and nanofiber films increase bioavailability and may improve hypertension treatment using cost-effective materials and a scalable nanoprecipitation method.

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