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

• Published in: Journal of drug delivery science and technology Vol. 41; pp. 344 - 350
• Main Authors: Shringirishi, Madhuri, Mahor, Alok, Gupta, Rishikesh, Prajapati, Sunil Kumar, Bansal, Kuldeep, Kesharwani, Prashant
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.10.2017
• Subjects: Anti-hypertensive; Diphenyl carbonate; Nanosponges; Nifedipine; β-Cyclodextrin; β-Cyclodextrin; Nanosponges; Anti-hypertensive; Diphenyl carbonate; Nifedipine
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2017.08.005

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, diphenyl 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. FTIR 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 (Cmax 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. [Display omitted]