Fabrication and characterization of nifedipine loaded β-cyclodextrin nanosponges: An in vitro and in vivo evaluation

被引:37
作者
Shringirishi, Madhuri [1 ]
Mahor, Alok [1 ]
Gupta, Rishikesh [1 ]
Prajapati, Sunil Kumar [1 ]
Bansal, Kuldeep [2 ]
Kesharwani, Prashant [3 ,4 ]
机构
[1] Bundelkhand Univ, Inst Pharm, Jhansi, Uttar Pradesh, India
[2] GLA Univ, Inst Pharmaceut Res, Mathura, Uttar Pradesh, India
[3] Int Med Univ, Dept Pharmaceut Technol, Kuala Lumpur 57000, Malaysia
[4] CSIR, Cent Drug Res Inst, Pharmaceut Div, Lucknow 226031, Uttar Pradesh, India
关键词
Nanosponges; beta-Cyclodextrin; Nifedifiine; Diphenyl carbonate; Anti-hypertensive; FORMULATION; AGENTS; DRUG;
D O I
10.1016/j.jddst.2017.08.005
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Cyclodextrin based nanosponges are gaining much consideration due to their aptitude to augment oral solubility of poorly water-soluble medications such as nifedipine. Here in the contemporary research, diphpyl carbonate was employed for crosslinking the cyclodextrin successfully. DLS studies confirmed particle size in the range of 400-500 nm with monodisperse size distribution. TEM measurement established spherical shape and size range of the nanosuspension. SEM photomicrograph confirmed porous structure of placebo nanosponges while drug loaded nanosponge formulation NS3 revealed solid surface. FUR studies established no drug-polymer interaction. DSC thermograms showed molecular level dispersion of drug in nanosponges. In vitro drug release exhibited a burst release for first fourth hour and delivered drug in sustained manner for subsequent 24 h. When encapsulated within nanosponges, oral bioavailability of nifedipine was enhanced in comparison to control formulation (C-max for test formulation was 0.2; 0.055 for control). The fabricated nanosponges displayed admirable stability under normal and stress conditions. %Drug entrapment encountered a slight decline (77.33 +/- 1.62% to 74.13 +/- 1.47%) during storage while %drug release from initial batch was almost identical when compared with stored nanosponges. (C) 2017 Elsevier B.V. All rights reserved.
引用
收藏
页码:344 / 350
页数:7
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