Enhanced Intestinal Permeability of Cefixime by Self-Emulsifying Drug Delivery System: In-Vitro and Ex-Vivo Characterization

Abstract

Background: Cefixime (CFX) belongs to a group of third-generation cephalosporin antibiotics with low water solubility and low intestinal permeability, which ultimately leads to significantly low bioavailability. Aim: This study aimed to increase solubility, improve drug release, and intestinal permeability of CFX by loading into SEDDS. Methods: Suitable excipients were selected based on drug solubility, percent transmittance, and emulsification efficiency. Pseudo-ternary phase diagram was fabricated for the identification of effective self-emulsification region. The best probably optimized formulations were further assessed for encumbered drug contents, emulsification time, cloud point measurement, robustness to dilution, mean droplet size, zeta potential, polydispersity index (PDI), and thermodynamic and chemical stability. Moreover, in vitro drug release studies and ex vivo permeation studies were carried out and apparent drug permeability Papp of different formulations was compared with the marketed brands of CFX. Results: Amongst the four tested SEDDS formulations, F-2 formulation exhibited the highest drug loading of 96.32%, emulsification time of 40.37 ± 3 s, mean droplet size of 19.01 ± 1.12 nm, and demonstrated improved long-term thermodynamic and chemical stability when stored at 4 °C. Release studies revealed a drug release of 97.32 ± 4.82% within 60 min in simulated gastric fluid. Similarly, 97.12 ± 5.02% release of CFX was observed in simulated intestinal fluid within 120 min; however, 85.13 ± 3.23% release of CFX was observed from the marketed product. Ex vivo permeation studies displayed a 2.7-fold increase apparent permeability compared to the marketed product in 5 h. Conclusion: Owing to the significantly improved drug solubility, in vitro release and better antibacterial activity, it can be assumed that CFX-loaded SEDDS might lead to an increased bioavailability and antibacterial activity, possibly leading to improved therapeutic effectiveness.

Self-Emulsifying Drug Delivery System for Enhanced Oral Delivery of Tenofovir: Formulation, Physicochemical Characterization, and Bioavailability Assessment

“…Incorporating TNF into SEDDS is an important factor for improving the penetration rate because it improves absorption by keeping the drug solubilized at absorption sites. Additionally, the nanosized droplets of SEDDS offer more interfacial surface area for drug release and a faster penetration process. , Therefore, the TNF-SEDDS F6 formulation has been shown to have much more drug penetration than the commercial tablet and API.…”

“…Additionally, the nanosized droplets of SEDDS offer more interfacial surface area for drug release and a faster penetration process. 28 , 29 Therefore, the TNF-SEDDS F6 formulation has been shown to have much more drug penetration than the commercial tablet and API.…”

Optimization of Potential Nanoemulgels for Boosting Transdermal Glimepiride Delivery and Upgrading Its Anti-Diabetic Activity

“…In contrast, the impact of increasing tween 80 concentration on the DE% values of tested NEs was positively observed; increasing surfactant concentration increased the DE% values ( Figure 2 F). The instant NE formation due to the decreased droplet size could facilitate the enhancement of the rate and extent of drug dissolution, ensuring the ability of NEs to readily retain GM in solubilized form and positively influencing the GM bioavailability in vivo afterwards [ 45 ].…”

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences

“…Delivery systems are also prepared to enhance the solubility and permeability of various compounds as it is presented in the literature [ 109 , 110 , 111 ]. The higher solubility of CBD and CBDA led to more efficient absorption and permeability across the gastrointestinal tract.…”