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Oral Bioactive Self-Nanoemulsifying Drug Delivery Systems of Remdesivir and Baricitinib: A Paradigmatic Case of Drug
Mohsin Kazi1, Yousef Alanazi1, Ashok Kumar2
1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Abstract:
Oral anticancer therapy mostly faces the challenges of low aqueous solubility, poor and irregular absorption from the gastrointestinal tract, food-influenced absorption, high first-pass metabolism, non-targeted delivery, and severe systemic and local adverse effects. Interest has been growing in bioactive self-nanoemulsifying drug delivery systems (bio-SNEDDSs) using lipid-based excipients within nanomedicine. This study aimed to develop novel bio-SNEDDS to deliver antiviral remdesivir and baricitinib for the treatment of breast and lung cancers. Pure natural oils used in bio-SNEDDS were analyzed using GC-MS to examine bioactive constituents. The initial evaluation of bio-SNEDDSs were performed based on self-emulsification assessment, particle size analysis, zeta potential, viscosity measurement, and transmission electron microscopy (TEM). The single and combined anticancer effects of remdesivir and baricitinib in different bio-SNEDDS formulations were investigated in MDA-MB-231 (breast cancer) and A549 (lung cancer) cell lines. The results from the GC-MS analysis of bioactive oils BSO and FSO showed pharmacologically active constituents, such as thymoquinone, isoborneol, paeonol and p-cymenene, and squalene, respectively. The representative F5 bio-SNEDDSs showed relatively uniform, nanosized (247 nm) droplet along with acceptable zeta potential values (+29 mV). The viscosity of the F5 bio-SNEDDS was recorded within 0.69 Cp. The TEM suggested uniform spherical droplets upon aqueous dispersions. Drug-free, remdesivir and baricitinib-loaded bio-SNEDDSs (combined) showed superior anticancer effects with IC50 value that ranged from 1.9-4.2 µg/mL (for breast cancer), 2.4-5.8 µg/mL (for lung cancer), and 3.05-5.44 µg/mL (human fibroblasts cell line). In conclusion, the representative F5 bio-SNEDDS could be a promising candidate for improving the anticancer effect of remdesivir and baricitinib along with their existing antiviral performance in combined dosage form.
Insights
Novel bioactive self-nanoemulsifying drug delivery systems (bio-SNEDDSs) enhance oral delivery of remdesivir and baricitinib for breast and lung cancers. These bio-SNEDDS formulations show promising combined anticancer effects, improving drug efficacy.
Area of Science:
- Nanomedicine
- Drug Delivery Systems
- Cancer Therapeutics
Background:
- Oral anticancer drugs often suffer from poor solubility, irregular absorption, and systemic toxicity.
- Bioactive self-nanoemulsifying drug delivery systems (bio-SNEDDSs) offer a promising approach to overcome these limitations using lipid-based excipients.
- Natural oils contain bioactive compounds with potential therapeutic benefits.
Purpose of the Study:
- To develop novel bio-SNEDDS for the oral delivery of remdesivir and baricitinib.
- To evaluate the anticancer efficacy of these bio-SNEDDS in breast and lung cancer cell lines.
- To characterize the physicochemical properties of the developed bio-SNEDDS.
Main Methods:
- Analysis of bioactive natural oils using Gas Chromatography-Mass Spectrometry (GC-MS).
- Formulation and characterization of bio-SNEDDSs, including self-emulsification, particle size, zeta potential, viscosity, and Transmission Electron Microscopy (TEM).
- In vitro evaluation of anticancer effects of remdesivir and baricitinib loaded bio-SNEDDSs in MDA-MB-231 (breast) and A549 (lung) cancer cell lines.
Main Results:
- GC-MS identified pharmacologically active constituents in the natural oils (e.g., thymoquinone, squalene).
- The F5 bio-SNEDDS formulation exhibited uniform nanosized droplets (247 nm), acceptable zeta potential (+29 mV), and low viscosity (0.69 cP).
- Combined remdesivir and baricitinib in bio-SNEDDS demonstrated superior anticancer activity with low IC50 values across cancer cell lines and human fibroblasts.
Conclusions:
- The developed bio-SNEDDS effectively delivered remdesivir and baricitinib.
- The F5 bio-SNEDDS formulation shows significant potential for enhancing combined anticancer therapy for breast and lung cancers.
- This nanomedicine approach may improve the therapeutic index of oral anticancer agents.
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