Development and in vitro/in vivo evaluation of controlled release provesicles of a nateglinide–maltodextrin complex  

作　　者：Ranjan Ku.Sahoo Nikhil Biswas Arijit Guha Nityananda Sahoo Ketousetuo Kuotsu 

机构地区：[1]Department of Pharmaceutical Technology,Jadavpur University,Kolkata 700032,India

出　　处：《Acta Pharmaceutica Sinica B》2014年第5期408-416,共9页药学学报（英文版）

基　　金：This work was financially supported by the All India Council of Technical Education(AICTE)India(Grant No.KLECOP/QIP/2010).

摘　　要：The aim of this study was to characterize the provesicle formulation of nateglinide(NTG)to facilitate the development of a novel controlled release system of NTG with improved efficacy and oral bioavailability compared to the currently marketed NTG formulation(Glinate^(™)60).NTG provesicles were prepared by a slurry method using the non-ionic surfactant,Span 60(SP),and cholesterol(CH)as vesicle forming agents and maltodextrin as a coated carrier.Multilamellar niosomes with narrow size distribution were shown to be successfully prepared by means of dynamic laser scattering(DLS)and field emission scanning electron microscopy(FESEM).The absence of drug-excipient interactions was confirmed by Fourier transform infrared spectroscopy(FT-IR),differential scanning calorimetry(DSC)and X-ray diffraction(XRD)studies.In vitro release of NTG in different dissolution media was improved compared to pure drug.A goat intestinal permeation study revealed that the provesicular formulation(F4)with an SP:CH ratio of 5:5 gave higher cumulative amount of drug permeated at 48 h compared to Glinate^(™)60 and control.A pharmacodynamic study in streptozotocin-induced diabetic rats confirmed that formulation F4 significantly(P<0.05)reduced blood glucose levels in comparison to Glinate 60.Overall the results show that controlled release NTG provesicles offer a useful and promising oral delivery system for the treatment of type Ⅱ diabetes.

关 键 词：Provesicles NIOSOMES MALTODEXTRIN NATEGLINIDE In vitro release Goat intestinal permeation HYPOGLYCEMIC 

分 类 号：O72[理学—晶体学]