Abstract
Famotidine as H2 receptor has antagonistic effects on gastric secretion. Unfortunately, its hydrophobic nature contributes to its variable and poor oral bioavailability. In the current study efforts are being made to fabricate famotidine loaded solid lipid nanoparticles with narrow size distribution. Prepared nanoformulations were pharmaceutically evaluated to confirm the desired boosted oral bioavailability. Famotidine loaded nanoformulation (FFSe-4) showed particle size 111.9±1.3 nm, polydispersity index 0.464±0.03, zeta potential −33.46±2 mV, entrapment efficiency 84±2.7%, and drug loading capacity 2.709±0.13%. Drug-excipients compatibility was confirmed by Fourier transformed infrared spectroscopy. Scanning electron microscopy confirmed spherical shaped, nanosized particles. Differential scanning calorimetry and powder X-ray diffractometry confirmed the change in crystalline nature. Prepared nanoformulation was more stable at refrigerated temperature. In vitro study showed that drug release time is proportional to drug pay load and followed zero order kinetics. Release exponent (n>0.5) confirmed non-Fickian-diffusion mechanism for drug release. In vivo pharmacokinetic studies showed 2.06-fold increase in oral bioavailability of famotidine dispersed in solid lipid nanoparticles compared to commercial product. These results authenticate solid lipid nanoparticles as drug delivery system and propose prolonged release with improved oral bioavailability for famotidine.
Highlights
40% of commercialized active pharmaceutical ingredients (APIs) are poorly water soluble, due to which sufficient amount of drug absorption from the gastrointestinal tract (GIT) is being a challenge for the researchers [1]
Specified amount of stearic acid was dissolved in chloroform which was emulsified with aqueous phase having surfactant (Tween-80) and cosurfactant (PVP) under magnetic stirring (1000 rpm) to form microemulsion
Unloaded Solid lipid nanoparticles (SLNs) were fabricated on the basis of three variable factors, that is, surfactant concentration, cosurfactant concentration, and magnetic stirring time
Summary
40% of commercialized active pharmaceutical ingredients (APIs) are poorly water soluble, due to which sufficient amount of drug absorption from the gastrointestinal tract (GIT) is being a challenge for the researchers [1]. Certain disadvantages were associated with them such as drug expulsion upon storage, limited stability, low drug loading, and polymers cytotoxicity [3]. This leads to the rise of fabricating solid lipid based nanodrug delivery system termed as solid lipid nanoparticle. Solid lipid nanoparticles (SLNs) were developed in the end of the 20th century [4]. It potentially gathers pluses of the old systems but avoids some of their major documented shortcomings [5].
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