TY - JOUR
T1 - Improved antimicrobial activity and oral bioavailability of delafloxacin by self-nanoemulsifying drug delivery system (SNEDDS)
AU - Anwer, Md Khalid
AU - Iqbal, Muzaffar
AU - Aldawsari, Mohammed F.
AU - Alalaiwe, Ahmed
AU - Ahmed, Mohammed Muqtader
AU - Mohamed Muharram, Magdy
AU - Ezzeldin, Essam
AU - Mahmoud, Mohamed A.
AU - Imam, Faisal
AU - Ali, Raisuddin
N1 - Publisher Copyright:
© 2021 Elsevier B.V.
PY - 2021/8
Y1 - 2021/8
N2 - In the current study, a novel self-nanoemulsifying drug delivery system (SNEDDS) was developed in order to improve the oral bioavailability of delafloxacin (DLF). Various oils, surfactants and co-surfactants were screened by solubility studies. Based on solubilization, potential of DLF in various vehicles, Lauroglycol™-90 (oil), Tween® 80 (surfactant) and Transcutol®-HP (co-surfactant) were selected for the development of DLF loaded SNEDDS (DLF-SNEDDS). Four formulae of DLF loaded SNEDDS (DLF1-DLF4) were prepared and evaluated for their droplet size, polydispersity index (PDI), zeta potential (ZP), refractive index (RI), percent transmittance (%T), thermodynamic stability, emulsifying efficiency and in vitro release studies. Among developed DLF loaded SNEDDS (DLF1-DLF4), DLFI was found optimum with a droplet size (73.3 ± 6.5 nm) PDI (0.298) ZP (−22.3) RI (1.334 ± 0.05) and %T (99.2 ± 0.09). Optimized DLF loaded SNEDDS (DLF1) demonstrated a superior anti-microbial activity against tested gram positive and gram negative strains with no resistance. The pharmacokinetic studies showed that oral bioavailability of DLF was significantly improved (3- fold) by optimized DLF loaded SNEDDS (DLF1) in comparison to pure DLF suspension. Hence, the results of this work suggest that the developed SNEDDS could be a potential carrier in enhancing bioavailability and therapeutic efficacy of DLF.
AB - In the current study, a novel self-nanoemulsifying drug delivery system (SNEDDS) was developed in order to improve the oral bioavailability of delafloxacin (DLF). Various oils, surfactants and co-surfactants were screened by solubility studies. Based on solubilization, potential of DLF in various vehicles, Lauroglycol™-90 (oil), Tween® 80 (surfactant) and Transcutol®-HP (co-surfactant) were selected for the development of DLF loaded SNEDDS (DLF-SNEDDS). Four formulae of DLF loaded SNEDDS (DLF1-DLF4) were prepared and evaluated for their droplet size, polydispersity index (PDI), zeta potential (ZP), refractive index (RI), percent transmittance (%T), thermodynamic stability, emulsifying efficiency and in vitro release studies. Among developed DLF loaded SNEDDS (DLF1-DLF4), DLFI was found optimum with a droplet size (73.3 ± 6.5 nm) PDI (0.298) ZP (−22.3) RI (1.334 ± 0.05) and %T (99.2 ± 0.09). Optimized DLF loaded SNEDDS (DLF1) demonstrated a superior anti-microbial activity against tested gram positive and gram negative strains with no resistance. The pharmacokinetic studies showed that oral bioavailability of DLF was significantly improved (3- fold) by optimized DLF loaded SNEDDS (DLF1) in comparison to pure DLF suspension. Hence, the results of this work suggest that the developed SNEDDS could be a potential carrier in enhancing bioavailability and therapeutic efficacy of DLF.
KW - Anti-mircobial activity
KW - Bioavailability
KW - Delafloxacin
KW - SNEDDS
UR - http://www.scopus.com/inward/record.url?scp=85107031023&partnerID=8YFLogxK
U2 - 10.1016/j.jddst.2021.102572
DO - 10.1016/j.jddst.2021.102572
M3 - Article
AN - SCOPUS:85107031023
SN - 1773-2247
VL - 64
JO - Journal of Drug Delivery Science and Technology
JF - Journal of Drug Delivery Science and Technology
M1 - 102572
ER -