title: Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats.
abstract: OBJECTIVE
  Insulin is a hormone used in the treatment of diabetes mellitus. Multiple injections of insulin every day may causes pain, allergic reactions at injection site, which lead to low patient compliance. The aim of this work was to develop and evaluate an efficient solid lipid nanoparticle (SLN) carrier for oral delivery of insulin.
  
  
  METHODS
  SLNs were prepared by double emulsion solvent evaporation (w/o/w) technique, employing glyceryltrimyristate (Dynasan 114) as lipid phase and soy lecithin and polyvinyl alcohol as primary and secondary emulsifier, respectively, and evaluated in vitro for particle size, polydispersity index (PDI) and drug entrapment.
  
  
  RESULTS
  Among the eight different developed formulae (F1-F8), F7 showed an average particle size (99 nm), PDI (0.021), high entrapment of drug (56.5%). The optimized formulation (F7) was further evaluated by FT-IR, DSC, XRD, in vitro release, permeation, stability, bioavailability and pharmacological studies. Insulin-loaded SLNs showed better protection from gastrointestinal environment as evident from the relative bioavailability, which was enhanced five times as compared to the insulin solution. A significant enhancement of relative bioavailability of insulin was observed, i.e. approximately five times of pure insulin solution when loaded in SLN (8.26% versus 1.7% only).
authors.affiliation: a Department of Pharmaceutics and.
authors.forename: Mohammad Javed
authors.initials: MJ
authors.lastname: Ansari
authors.affiliation: a Department of Pharmaceutics and.
authors.forename: Md Khalid
authors.initials: MK
authors.lastname: Anwer
authors.affiliation: a Department of Pharmaceutics and.
authors.forename: Shahid
authors.initials: S
authors.lastname: Jamil
authors.affiliation: a Department of Pharmaceutics and.
authors.forename: Ramadan
authors.initials: R
authors.lastname: Al-Shdefat
authors.affiliation: a Department of Pharmaceutics and.
authors.forename: Bahaa E
authors.initials: BE
authors.lastname: Ali
authors.affiliation: a Department of Pharmaceutics and.
authors.forename: Mohammad Muqtader
authors.initials: MM
authors.lastname: Ahmad
authors.affiliation: b Department of Pharmacology , College of Pharmacy, Prince Sattam Bin Abdulaziz University , Al-kharj , Kingdom of Saudi Arabia.
authors.forename: Mohammad Nazam
authors.initials: MN
authors.lastname: Ansari
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D003921:Diabetes Mellitus, Experimental / Q000378:metabolism*; D045703:Emulsifying Agents / Q000737:chemistry; D006801:Humans; D007328:Insulin / Q000008:administration & dosage* / Q000378:metabolism; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011142:Polyvinyl Alcohol / Q000737:chemistry; D051381:Rats
chemical_list: D045703:Emulsifying Agents; D007328:Insulin; D008055:Lipids; D011142:Polyvinyl Alcohol
keywords: Characterization; insulin; pharmacokinetic; solid lipid nanoparticles; stability