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Updated: Jan 4, 2026
Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
Preparation of an oil suspension containing ondansetron hydrochloride as a sustained release parenteral formulation
Thi-Thao-Linh Nguyen1, Van-An Duong1, Han-Joo Maeng1
1College of Pharmacy, Gachon University, 191 Hambakmoero, Yeonsu-gu, Incheon, 21936, South Korea.
Abstract:
Ondansetron hydrochloride (ODS) is a selective 5-hydroxytryptamine type 3 antagonist for nausea and emesis prevention in neoplastic patients. To reduce dosing frequency and side effects and improve patient compliance, a sustained release parenteral formulation of ODS was developed. Microparticles of methylcellulose (MC) and ODS were prepared using the spray-drying method and suspended in oils to form oil suspensions. The formulations were evaluated for residual moisture, drug content, size distribution, DSC, XRD, FTIR, SEM, drug release, and pharmacokinetic studies. The effects of polymers and oils on the drug release were evaluated. MC showed the most prominent sustained release effect among various polymers examined with the optimum MC/ODS ratio of 2:1 (w/w). The particle size of the produced microparticles was in the mean diameter of approximately 3 μm. Physicochemical characterization suggested that ODS existed in an amorphous matrix within the microparticles and interacted with MC via hydrogen bonds. Corn oil was selected as the appropriate oil for suspension due to the sustained release of ODS and the appropriate viscosity. The optimized sustained release formulation of ODS was the corn oil suspension of spray-dried microparticles containing MC and ODS (2:1, w/w). It showed an in vitro drug sustained release up to 120 h, while the oil suspension of ODS without any polymer released the drug within 2 h. Following subcutaneous administration in rats, the optimized formulation could prolong the drug release until 72 h with the enhanced bioavailability in comparison with the ODS solution. The oil suspension of spray-dried microparticles might be an efficient approach for prolongation of the drug effect in the management of nausea and emesis. Graphical abstract.
Insights
A novel sustained-release formulation using methylcellulose microparticles and corn oil effectively delivered ondansetron hydrochloride (ODS), prolonging drug effect for nausea and emesis management.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Ondansetron hydrochloride (ODS) is crucial for managing chemotherapy-induced nausea and emesis.
- Current formulations require frequent dosing, leading to compliance issues and side effects.
- Developing a sustained-release parenteral formulation can improve patient outcomes.
Purpose of the Study:
- To develop and characterize a sustained-release parenteral formulation of ODS.
- To evaluate the impact of methylcellulose (MC) and oils on ODS release kinetics.
- To assess the in vitro and in vivo performance of the optimized ODS formulation.
Main Methods:
- Spray-drying technique to prepare ODS-loaded MC microparticles.
- Formulation of microparticles into oil suspensions using various oils.
- Comprehensive physicochemical characterization (DSC, XRD, FTIR, SEM).
- In vitro drug release studies and in vivo pharmacokinetic evaluation in rats.
Main Results:
- Optimized MC/ODS ratio (2:1 w/w) in spray-dried microparticles yielded sustained release up to 120 hours in vitro.
- Corn oil suspension demonstrated optimal viscosity and sustained ODS release.
- Subcutaneous administration in rats showed prolonged drug release up to 72 hours and enhanced bioavailability compared to ODS solution.
Conclusions:
- Spray-dried methylcellulose microparticles suspended in corn oil represent an effective strategy for sustained parenteral delivery of ODS.
- This formulation significantly prolongs drug release and improves bioavailability, offering a promising approach for managing nausea and emesis.
- The developed formulation enhances patient compliance and potentially reduces side effects associated with frequent dosing.
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