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通过β-环糊精-低聚丙交酯衍生物的无聚合物静电纺丝制备恩诺沙星药物制剂。

Enrofloxacin Pharmaceutical Formulations through the Polymer-Free Electrospinning of β-Cyclodextrin-oligolactide Derivatives.

作者信息

Blaj Diana-Andreea, Peptu Cătălina Anișoara, Danu Maricel, Harabagiu Valeria, Peptu Cristian, Bujor Alexandra, Ochiuz Lăcrămioara, Tuchiluș Cristina Gabriela

机构信息

"Petru Poni" Institute of Macromolecular Chemistry, 700487 Iasi, Romania.

Faculty of Chemical Engineering and Protection of the Environment, "Gheorghe Asachi" Technical University of Iasi, 700050 Iasi, Romania.

出版信息

Pharmaceutics. 2024 Jul 5;16(7):903. doi: 10.3390/pharmaceutics16070903.

DOI:10.3390/pharmaceutics16070903
PMID:39065598
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11279624/
Abstract

Enrofloxacin (ENR), a member of the fluoroquinolone class of antibiotics, is widely used in veterinary medicine to treat bacterial infections. Like many antibiotics, ENR has limited water solubility and low bioavailability. To address these challenges, drug formulations using solid dispersions, nanosuspensions, surfactants, cocrystal/salt formation, and inclusion complexes with cyclodextrins may be employed. The approach described herein proposes the development of ENR formulations by co-electrospinning ENR with custom-prepared cyclodextrin-oligolactide (CDLA) derivatives. This method benefits from the high solubility of these derivatives, enabling polymer-free electrospinning. The electrospinning parameters were optimized to incorporate significant amounts of ENR into the CDLA nanofibrous webs, reaching up to 15.6% by weight. The obtained formulations were characterized by FTIR and NMR spectroscopy methods and evaluated for their antibacterial activity against , , and . This study indicates that the presence of CDLA derivative does not inhibit the antibacterial activity of ENR, recommending these formulations for further development.

摘要

恩诺沙星(ENR)是氟喹诺酮类抗生素的一种,在兽医学中广泛用于治疗细菌感染。与许多抗生素一样,ENR的水溶性有限且生物利用度低。为应对这些挑战,可采用使用固体分散体、纳米混悬液、表面活性剂、共晶/盐形成以及与环糊精形成包合物的药物制剂。本文所述方法提出通过将ENR与定制制备的环糊精-低聚丙交酯(CDLA)衍生物共电纺来开发ENR制剂。该方法得益于这些衍生物的高溶解度,能够进行无聚合物电纺。对电纺参数进行了优化,以将大量的ENR掺入CDLA纳米纤维网中,重量含量高达15.6%。通过傅里叶变换红外光谱(FTIR)和核磁共振光谱(NMR)方法对所得制剂进行了表征,并评估了它们对[具体菌种1]、[具体菌种2]和[具体菌种3]的抗菌活性。这项研究表明,CDLA衍生物的存在不会抑制ENR的抗菌活性,建议对这些制剂进行进一步开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/3f6a0b45ee25/pharmaceutics-16-00903-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/06be0fe56d3c/pharmaceutics-16-00903-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/b431a7e5ef92/pharmaceutics-16-00903-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/a106560d016a/pharmaceutics-16-00903-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/c270ca6f206e/pharmaceutics-16-00903-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/fb532bd58e5e/pharmaceutics-16-00903-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/41e0a0a64b1f/pharmaceutics-16-00903-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/66799c23df35/pharmaceutics-16-00903-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/9af80f5e95d6/pharmaceutics-16-00903-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/beafc0e62206/pharmaceutics-16-00903-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/6563291674f1/pharmaceutics-16-00903-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/3f6a0b45ee25/pharmaceutics-16-00903-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/06be0fe56d3c/pharmaceutics-16-00903-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/b431a7e5ef92/pharmaceutics-16-00903-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/a106560d016a/pharmaceutics-16-00903-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/c270ca6f206e/pharmaceutics-16-00903-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/fb532bd58e5e/pharmaceutics-16-00903-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/41e0a0a64b1f/pharmaceutics-16-00903-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/66799c23df35/pharmaceutics-16-00903-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/9af80f5e95d6/pharmaceutics-16-00903-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/beafc0e62206/pharmaceutics-16-00903-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/6563291674f1/pharmaceutics-16-00903-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31da/11279624/3f6a0b45ee25/pharmaceutics-16-00903-g009.jpg

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