title: Nanostructured lipid carriers of pioglitazone for transdermal application: from experimental design to bioactivity detail.
abstract: Pioglitazone (PZ) an anti-hyperglycemic agent is used in the treatment of type 2 diabetes. The aim of this study was to design PZ-loaded nanostructured lipid carriers (NLC) to investigate the bioavailability improvement by transdermal delivery. PZ NLCs were prepared using high-pressure homogenization followed by ultrasonication. The NLCs were evaluated for particle size analysis, drug loading, ex vivo skin transport studies and in vivo bioactivity study. The prepared NLCs had a mean size of 166.05 nm and drug loading of 10.41% with flux value of 47.36 µg/cm(2)/h. The entrapment of PZ is >70% in the NLCs with enhancement ratio of 3.2 times. The in vivo pharmacokinetic study showed 2.17 times enhancement in bioavailability study and pharmacodynamics study showed that PZ NLC-based transdermal therapeutic system (PNLG-TTS) lowers blood sugar level in a sustained pattern for a prolonged period of time as compared to Piosys tablet (marketed). The shelf life of the optimized formulation was found to be 1.83 years. These results clearly provide a lead that above NLCs-based TTS is potential controlled release formulation for PZ and could be a promising drug delivery system for the treatment of diabetes.
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Hamdard University , New Delhi , India.
authors.forename: Sohrab
authors.initials: S
authors.lastname: Alam
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Hamdard University , New Delhi , India.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Aslam
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Hamdard University , New Delhi , India.
authors.forename: Anam
authors.initials: A
authors.lastname: Khan
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Hamdard University , New Delhi , India.
authors.forename: Syed Sarim
authors.initials: SS
authors.lastname: Imam
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Hamdard University , New Delhi , India.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Aqil
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Hamdard University , New Delhi , India.
authors.forename: Yasmin
authors.initials: Y
authors.lastname: Sultana
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Hamdard University , New Delhi , India.
authors.forename: Asgar
authors.initials: A
authors.lastname: Ali
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D001682:Biological Availability; D015415:Biomarkers / Q000378:metabolism; D001786:Blood Glucose / Q000187:drug effects* / Q000378:metabolism; D018360:Crystallography, X-Ray; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles; D036103:Nanotechnology; D010316:Particle Size; D000077205:Pioglitazone; D033362:Powder Diffraction; D011312:Pressure; D017208:Rats, Wistar; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013010:Sonication; D013678:Technology, Pharmaceutical / Q000379:methods; D045162:Thiazolidinediones / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D014465:Ultrasonics
chemical_list: D015415:Biomarkers; D001786:Blood Glucose; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D008055:Lipids; D045162:Thiazolidinediones; D000077205:Pioglitazone
keywords: Antidiabetic; experimental design; lipid carrier; pioglitazone