Famotidine-loaded solid self-nanoemulsifying drug delivery system demonstrates exceptional efficiency in amelioration of peptic ulcer

[Display omitted] Famotidine (FMD) is a highly potent H2-receptor antagonist used in peptic ulcer treatment. However, the drug possesses poor aqueous solubility and permeability. FMD-loaded solid self-nanoemulsifying drug delivery system (FMD-S-SNEDDS) comprised of Labrafil® M 1944 CS, Tween® 20 and...

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Veröffentlicht in:International journal of pharmaceutics 2022-01, Vol.611, p.121303-121303, Article 121303
Hauptverfasser: El-Dakroury, Walaa A., Zewail, Moataz B., Elsabahy, Mahmoud, Shabana, Marwa E., Asaad, Gihan F.
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Sprache:eng
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Zusammenfassung:[Display omitted] Famotidine (FMD) is a highly potent H2-receptor antagonist used in peptic ulcer treatment. However, the drug possesses poor aqueous solubility and permeability. FMD-loaded solid self-nanoemulsifying drug delivery system (FMD-S-SNEDDS) comprised of Labrafil® M 1944 CS, Tween® 20 and PEG 400, adsorbed on Aerosil® 200, has been developed. FMD-S-SNEDDS has demonstrated acceptable micromeritic properties, and upon reconstitution in water, spherical nanosized particles were released, as demonstrated by dynamic light scattering studies and transmission electron microscopy imaging. High encapsulation efficiency of FMD in the developed SNEDDS has been attained, and the saturated solubility of the drug has increased by 20-fold when it was incorporated in the SNEDDS. Several in vitro characterizations have been carried out, including, Fourier transform-infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, and drug dissolution studies. In vivo, upon administration of the free drug suspension, marketed product (FAMOTIN®) and FMD-S-SNEDDS (40 mg/kg) in peptic ulcer rat models, FMD-S-SNEDDS and the marketed FMD demonstrated 12.5- and 4.7-fold reduction in ulcers number, and 28.7- and 7.2-fold reduction in ulcer severity, respectively, compared to the control untreated animals. FMD-S-SNEDDS showed a significant (p 
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2021.121303