Solid lipid nanoparticles and nanosuspension formulation of Saquinavir: preparation, characterization, pharmacokinetics and biodistribution studies

Abstract

Solid lipid nanoparticles (SLNs) and nanosuspensions (NSs) have shown great promise for improving bioavailability of poorly water-soluble drugs. This study was aimed to develop SLNs and NS of Saquinavir (SQ) for improvement in bioavailability. These formulations were characterized and their pharmacokinetics and biodistribution in mice were evaluated. Saquinavir-loaded SLNs (SQSLNs) showed particle size 215 ± 9 nm and entrapment efficiency 79.24 ± 1.53%, while solid-state studies (differential scanning calorimetry and X-ray diffraction) indicated entrapment of the drug in SLNs. Saquinavir NS (SNS) showed particle size 344 ± 16 nm with fourfold increase in saturation solubility and its solid-state studies showed reduction in crystallinity. Pharmacokinetics and biodistribution studies of orally administered SQSLN and SNS in mice exhibited higher plasma level concentration compared to saquinavir microsuspension (SMS). The relative bioavailabilities for SNS and SQSLN were 37.39% and 66.53%, respectively, compared to 18.87% bioavailability obtained after administration of SMS, indicating suitability of nanoparticulate formulations for improving bioavailability.

Preparation and Characterization of Naringenin Gold Nano Suspension for Breast Cancer

“…The sample was analyzed using UV spectrophotometer at λmax324 nm of naringenin. Total drug content (TDC) were calculated as below Total Drug Content= (Total volume of nano suspension//Volume of aliquot) * Amount of drug in aliquot*100 18 .…”

Enhancement of saquinavir absorption and accumulation through the formation of solid drug nanoparticles

“…For example, there is a 20-fold increase in SQV plasma concentrations; upon co-administration with RTV a potent P-gp Inhibitor; hence its use in boosting the drug [ 33 ]. Several attempts have therefore been made to improve its absorption through design of formulations that can increase its bioavailability, including SDNs [ 34 – 38 ]. Nanotechnology has been demonstrated to enhance delivery and bioavailability of SQV through increased solubility, improved transport and evasion of the P-gp-mediated drug efflux [ 38 – 40 ].…”

Nanocrystals for the parenteral delivery of poorly water-soluble drugs

“…Alternatively, the drug is fitted in cyclodextrins, which have a hydrophobic interior and a hydrophilic exterior, and made soluble in water [5]. Another way of enhancing the solubility of poorly soluble drugs is to produce nanoparticulate formulations, such as liposomes [6], micelles [7], nanoemulsion [8], solid lipid nanoparticles [9], and polymeric nanoparticles [10]. However, relatively low drug loading efficiency, concerns for the safety of excipients, and complicated manufacturing process are noted as potential disadvantages of these strategies.…”