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Triptorelin nanoparticle-loaded microneedles for use in assisted reproductive technology
Xiaoyan Lu1, Yiying Sun2, Meishan Han3
1School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, China.
Silk fibroin microneedles deliver triptorelin nanoparticles for improved bioavailability in assisted reproductive technology (ART). This innovation offers a less burdensome, self-administered alternative for women undergoing fertility treatments.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Reproductive Medicine
Background:
- Triptorelin is crucial for assisted reproductive technology (ART), but its low bioavailability and frequent injections negatively impact patient quality of life.
- Current delivery methods for triptorelin pose challenges for women undergoing fertility treatments, necessitating improved administration strategies.
Purpose of the Study:
- To develop silk fibroin (SF)-based microneedles (MNs) for transdermal delivery of triptorelin-loaded nanoparticles (NPs).
- To enhance triptorelin bioavailability, ensure controlled release, and facilitate safe, self-administered treatment for ART.
- To evaluate the therapeutic potential of these novel NPs-MNs in a preclinical model.
Main Methods:
- Triptorelin-loaded nanoparticles (NPs) were prepared using silk fibroin (SF) and shear force for controlled release and enzyme protection.
- Nanoparticles-encapsulated polymeric microneedles (NPs-MNs) were fabricated using a two-step pouring and centrifugation method.
- The mechanical properties and stratum corneum penetration capability of NPs-MNs were confirmed by increased β-sheet content.
Main Results:
- Transdermal release of triptorelin from NPs-MNs reached approximately 65%.
- Administration in rats demonstrated a prolonged drug half-life and increased relative bioavailability of triptorelin.
- Observed hormonal changes (luteinizing hormone, estradiol) suggest effective in vivo drug activity and downregulation.
Conclusions:
- Silk fibroin microneedles offer a promising platform for transdermal triptorelin delivery, significantly improving bioavailability.
- The developed triptorelin-loaded NPs-MNs provide a potential self-administration method, reducing the burden on patients undergoing ART.
- This innovative approach holds potential for improving the efficacy and patient experience in assisted reproductive technology regimens.
