Khan, Arshad Ali and Atiya, Akhtar and Akhtar, Safia and Yadav, Yogesh and Qureshi, Kamal A. and Jaremko, Mariusz and Mahmood, Syed (2022) Optimization of a cefuroxime axetil-loaded liquid self-nanoemulsifying drug delivery system: enhanced solubility, dissolution and caco-2 cell uptake. Pharmaceutics, 14 (4). DOI https://doi.org/10.3390/pharmaceutics14040772.
Full text not available from this repository.Abstract
Cefuroxime axetil (CA) is an oral cephalosporin which hydrolyzes rapidly to the active parent compound cefuroxime. CA is known to have incomplete oral bioavailability (30-50%) due to its poor solubility and enzymatic conversion to cefuroxime in the gut lumen. In order to overcome these drawbacks, a lipid-based self-nanoemulsifying drug delivery system (SNEDDS) has been developed and optimized. The SNEDDS formulations were prepared using the aqueous phase titration method. The greatest self-emulsifying area was found in the 2:1 Smix ratio. As a result, different SNEDDS formulations were carefully selected from this phase diagram based on their smaller droplet size < 100 nm, polydispersity index <= 0.5, dispersibility (Grade A), and transmittance (%) > 85%. Thermodynamic stability tests were carried out in order to rule out any metastable/unstable SNEDDS formulations. The droplet size, polydispersity index, zeta potential, and entrapment efficiency (% EE) of optimized CA-loaded SNEDDS (C-3) were 18.50 +/- 1.83 nm, 0.064 +/- 0.008, -22.12 +/- 1.20 mV, and 97.62 +/- 1.06%, respectively. In vitro release studies revealed that the SNEDDS formulation had increased CA solubility. CA-SNEDDS-C3 increased CA cellular uptake, possibly due to increased CA solubility and the inhibition of enzymatic conversion to cefuroxime. Finally, in terms of the improvement of oral bioavailability, CA-loaded-SNEDDS could be a viable alternative to commercially available CA formulations.
| Item Type: | Article |
|---|---|
| Funders: | Small Research Group Program, King Khalid University, Abha, Saudi Arabia [Grant No:RGP-1/37/43] |
| Uncontrolled Keywords: | Cefuroxime axetil; Pseudo-ternary phase diagrams; Self-nanoemulsifying drug delivery system; Caco-2 cells; cytotoxicity; cellular uptake |
| Subjects: | R Medicine > RM Therapeutics. Pharmacology R Medicine > RS Pharmacy and materia medica |
| Divisions: | Faculty of Pharmacy Faculty of Pharmacy > Department of Pharmaceutical Technology |
| Depositing User: | Ms. Juhaida Abd Rahim |
| Date Deposited: | 05 Oct 2023 01:27 |
| Last Modified: | 05 Oct 2023 01:27 |
| URI: | http://eprints.um.edu.my/id/eprint/42927 |
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