title: 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.
authors: Drug Delivery Laboratory, TIFAC Centre of Relevance and Excellence in NDDS, Department of Pharmacy, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda , Donors Plaza, Fatehgunj, Vadodara 390 002, India.
authors: Shamsunder S
authors: SS
authors: Dodiya
authors: Sandip S
authors: SS
authors: Chavhan
authors: Krutika K
authors: KK
authors: Sawant
authors: Aruna G
authors: AG
authors: Korde
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D015658:HIV Infections / Q000188:drug therapy; D017320:HIV Protease Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008055:Lipids / Q000737:chemistry*; D008297:Male; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D019258:Saquinavir / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D012995:Solubility; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D017320:HIV Protease Inhibitors; D008055:Lipids; D019258:Saquinavir