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Published on: August 15, 2016
Ondansetron/Cyclodextrin inclusion complex nanofibrous webs for potential orally fast-disintegrating antiemetic drug
Emmy Hsiung1, Asli Celebioglu1, Mehmet Emin Kilic2
1Fiber Science Program, Department of Human Centered Design, College of Human Ecology, Cornell University, Ithaca, NY 14853, USA.
Abstract:
Ondansetron (ODS) is an effective antiemetic drug which suffers from limited solubility and bioavailability during oral administration due to first-pass metabolism. However, these limitations can be mitigated through inclusion complexation with cyclodextrins (CDs). In this study, we have reported the electrospinning of polymer-free, free-standing ODS/CD nanofibrous webs (NW), a promising approach for developing a fast-disintegrating delivery system of an antiemetic drug molecule. Highly water soluble hydroxypropyl-beta-cyclodextrins (HPβCD) were used as both complexation agent and electrospinning matrix. The computational study revealed that the 1/2 (drug/CD) stoichiometry was more favorable compared to 1/1. The ODS/HPβCD NW was obtained with higher loading efficiency (∼96 %) compared to the control sample of ODS/polyvinyl alcohol (PVA) NW (∼80 %). The amorphous distribution of ODS raised by complexation and the highly water-soluble nature of HPβCD resulted into faster and better release profile and quite faster disintegration property (∼2 s) in artificial saliva than polymeric ODS/PVA NW. Here, ODS/HPβCD NW was generated in the absence of a toxic solvent or chemical to enable the drug loading in an amorphous state. From all reasons above, ODS/HPβCD NW might be a promising alternative to the polymeric based systems for the purpose of fast-disintegrating oral drug delivery.
Insights
This study developed polymer-free nanofibrous webs of ondansetron (ODS) and hydroxypropyl-beta-cyclodextrins (HPβCD) for enhanced oral drug delivery. The ODS/HPβCD webs offer rapid disintegration and improved drug release, presenting a promising alternative to traditional polymeric systems.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Drug Delivery Systems
Background:
- Ondansetron (ODS) exhibits poor oral bioavailability due to low solubility and first-pass metabolism.
- Cyclodextrins (CDs) can improve drug solubility and bioavailability through inclusion complexation.
- Polymeric systems often face limitations in drug delivery applications.
Purpose of the Study:
- To develop polymer-free, free-standing ondansetron/cyclodextrin nanofibrous webs (NW) for fast-disintegrating oral delivery.
- To investigate the use of hydroxypropyl-beta-cyclodextrins (HPβCD) as both a complexation agent and electrospinning matrix.
- To evaluate the drug loading, release profile, and disintegration properties of the ODS/HPβCD NW.
Main Methods:
- Electrospinning of polymer-free ODS/HPβCD nanofibrous webs.
- Computational study to determine optimal drug/CD stoichiometry (1/2 favored).
- Characterization of loading efficiency, drug distribution, release profile, and disintegration time.
Main Results:
- ODS/HPβCD NW achieved high loading efficiency (~96%) compared to ODS/PVA NW (~80%).
- Complexation resulted in amorphous distribution of ODS, enhancing solubility and release.
- ODS/HPβCD NW exhibited rapid disintegration (~2 seconds) in artificial saliva.
Conclusions:
- Polymer-free ODS/HPβCD NW represent a promising fast-disintegrating oral drug delivery system.
- This approach mitigates ODS solubility and bioavailability issues without toxic solvents.
- ODS/HPβCD NW offer a viable alternative to polymeric systems for enhanced antiemetic drug delivery.
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