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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
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Self-Emulsifying Drug Delivery System for Enhanced Oral Delivery of Tenofovir: Formulation, Physicochemical
Nilesh Mahajan1, Md Ali Mujtaba2, Ritesh Fule3
1Department of Pharmaceutics, Dadasaheb Balpande College of Pharmacy, Besa, Nagpur, Maharashtra 440037, India.
ACS Omega
|February 26, 2024
Summary
This study developed a self-emulsifying drug delivery system (SEDDS) to improve tenofovir (TNF) oral bioavailability. The novel SEDDS formulation significantly enhanced drug absorption and stability, offering a promising alternative for antiretroviral therapy.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biopharmaceutics
Background:
- Tenofovir (TNF) is crucial in antiretroviral therapy but suffers from poor oral bioavailability and membrane permeability.
- Existing formulations limit the therapeutic efficacy of tenofovir.
- Novel drug delivery systems are needed to overcome these limitations.
Purpose of the Study:
- To develop and characterize a self-emulsifying drug delivery system (SEDDS) for tenofovir.
- To enhance the oral bioavailability and membrane permeability of tenofovir.
- To evaluate the physicochemical properties and pharmacokinetic profile of the developed SEDDS.
Main Methods:
- Formulation of SEDDS using eucalyptus oil, Kolliphor EL, Kollisolv MCT 70, and glycerol.
- Characterization of SEDDS including droplet size, zeta potential, and drug state (DSC, XRD, SEM).
- In vitro dissolution, drug permeability studies, and in vivo pharmacokinetic evaluation in rats.
Main Results:
- Optimized SEDDS (F6) exhibited a small droplet size (98.82 nm) and good stability (-13.03 mV zeta potential).
- SEDDS F6 demonstrated rapid in vitro drug release and enhanced drug permeability.
- Pharmacokinetic studies showed significantly higher Cmax and AUC0- in rats, with a 21.53-fold increase in relative bioavailability compared to marketed tablets.
Conclusions:
- The developed SEDDS formulation effectively enhances the physicochemical properties and oral absorption of tenofovir.
- SEDDS represents a promising strategy for improving the oral bioavailability of poorly water-soluble drugs like tenofovir.
- This approach holds potential for improving antiretroviral therapy outcomes.
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