title: A novel oral delivery system consisting in "drug-in cyclodextrin-in nanostructured lipid carriers" for poorly water-soluble drug: vinpocetine.
abstract: The purpose of this study was to develop a new delivery system based on drug cyclodextrin (CD) complexation and loading into nanostructured lipid carriers (NLC) to improve the oral bioavailability of vinpocetine (VP). Three different CDs and three different methods to obtain solid vinpocetine-cyclodextrin-tartaric acid complexes (VP-CD-TA) were contrasted. The co-evaporation vinpocetine-β-cyclodextrin-tartaric acid loaded NLC (VP-β-CD-TA COE-loaded NLC) was obtained by emulsification ultrasonic dispersion method. VP-β-CD-TA COE-loaded NLC was suitably characterized for particle size, polydispersity index, zeta potential, entrapment efficiency and the morphology. The crystallization of drug in VP-CD-TA and NLC was investigated by differential scanning calorimetry (DSC). The in vitro release study was carried out at pH 1.2, pH 6.8 and pH 7.4 medium. New Zealand rabbits were applied to investigate the pharmacokinetic behavior in vivo. The VP-β-CD-TA COE-loaded NLC presented a superior physicochemical property and selected to further study. In the in vitro release study, VP-β-CD-TA COE-loaded NLC exhibited a higher dissolution rate in the pH 6.8 and pH 7.4 medium than VP suspension and VP-NLC. The relative bioavailability of VP-β-CD-TA COE-loaded NLC was 592% compared with VP suspension and 92% higher than VP-NLC. In conclusion, the new formulation significantly improved bioavailability of VP for oral delivery, demonstrated a perspective way for oral delivery of poorly water-soluble drugs.
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 10016, China.
authors: Congcong
authors: C
authors: Lin
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 10016, China.
authors: Fen
authors: F
authors: Chen
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 10016, China.
authors: Tiantian
authors: T
authors: Ye
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 10016, China.
authors: Lina
authors: L
authors: Zhang
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 10016, China.
authors: Wenji
authors: W
authors: Zhang
authors: School of Biomedical & Chemical Engineering, Liaoning Institute of Science and Technology, 176 Xianghuai Road, Benxi 117004, China.
authors: Dandan
authors: D
authors: Liu
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 10016, China.
authors: Wei
authors: W
authors: Xiong
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 10016, China.
authors: Xinggang
authors: X
authors: Yang
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 10016, China. Electronic address: pwslsm@163.com.
authors: Weisan
authors: W
authors: Pan
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D006863:Hydrogen-Ion Concentration; D008055:Lipids / Q000737:chemistry*; D008297:Male; D049329:Nanostructures; D036103:Nanotechnology; D011817:Rabbits; D012995:Solubility; D013644:Tartrates / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D014748:Vinca Alkaloids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D014867:Water / Q000737:chemistry*; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D008055:Lipids; D013644:Tartrates; D014748:Vinca Alkaloids; D047392:beta-Cyclodextrins; D014867:Water; C013983:vinpocetine; C029768:tartaric acid
keywords: Cyclodextrins; Nanostructured lipid carriers (NLC); Oral bioavailability; Poorly water-soluble drugs; Vinpocetine