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左炔诺孕酮微针贴片的持续释放避孕：配方、优化和体内特征描述。

Levonorgestrel Microneedle Array Patch for Sustained Release Contraception: Formulation, Optimization and In Vivo Characterization.

机构信息

Nanomedicine Lab, Department of Biosciences and Bioengineering (BSBE), Indian Institute of Technology Bombay (IITB), Mumbai 400076, India.

Department of Pharmaceutics, Poona College of Pharmacy, Bharti Vidyapeeth Deemed University, Pune 411038, India.

出版信息

Molecules. 2022 Apr 6;27(7):2349. doi: 10.3390/molecules27072349.

DOI:10.3390/molecules27072349
PMID:35408746
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9000369/
Abstract

BACKGROUND

The goal of this work was to develop a levonorgestrel liposome-loaded microneedle array patch for contraception.

METHODS

Levonorgestrel-loaded liposome was formulated by a solvent injection technique, characterized, and studied.

RESULTS

The formulated liposomes were characterized for particle size (147 ± 8 nm), polydispersity index (0.207 ± 0.03), zeta potential (-23 ± 4.25 mV), drug loading (18 ± 3.22%) and entrapment efficiency (85 ± 4.34%). A cryo high-resolution transmission electron microscopy and cryo field emission gun scanning electron microscopy study showed spherical shaped particles with a smooth surface. The in vitro drug release and in vivo pharmacokinetic study showed sustained behaviour of Levonorgestrel for 28 days.

CONCLUSION

The levonorgestrel liposome-loaded microneedle array patch showed better contraception than the drug-loaded microneedle array patch.

摘要

背景

本研究旨在开发一种左炔诺孕酮脂质体负载的微针贴片用于避孕。

方法

采用溶剂注入技术制备左炔诺孕酮脂质体，并对其进行了表征和研究。

结果

所制备的脂质体的粒径（147±8nm）、多分散指数（0.207±0.03）、Zeta 电位（-23±4.25mV）、载药量（18±3.22%）和包封率（85±4.34%）。冷冻高分辨率透射电子显微镜和冷冻场发射枪扫描电子显微镜研究表明，这些粒子呈球形且表面光滑。体外药物释放和体内药代动力学研究表明，左炔诺孕酮的释放具有 28 天的持续行为。

结论

与载药微针贴片相比，左炔诺孕酮脂质体负载的微针贴片显示出更好的避孕效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/48316b8cb87d/molecules-27-02349-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/bec732757b7c/molecules-27-02349-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/2a7f48311e2f/molecules-27-02349-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/62fe3946c613/molecules-27-02349-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/b609cb1d5bc3/molecules-27-02349-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/48316b8cb87d/molecules-27-02349-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/bec732757b7c/molecules-27-02349-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/2a7f48311e2f/molecules-27-02349-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/62fe3946c613/molecules-27-02349-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/b609cb1d5bc3/molecules-27-02349-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7492/9000369/48316b8cb87d/molecules-27-02349-g005.jpg

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