Potentials of proniosomes for improving the oral bioavailability of poorly water-soluble drugs. (January 2015)

• Record Type: Journal Article
• Authors: Song, Shuangshuang; Tian, Baocheng; Chen, Fen; Zhang, Wenji; Pan, Yusheng; Zhang, Qiang; Yang, Xinggang; Pan, Weisan
• Is Part Of: Drug development and industrial pharmacy. Volume 41:Number 1(2015:Jan.)
• Page Start: 51
• Page End: 62
• Publication Date: 2015-01
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmaceutical industry -- Periodicals; Drug Industry -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615.05
• DOI: 10.3109/03639045.2013.845841
• Languages: English
• ISSNs: 0363-9045

Abstract

<abstract> <title>Abstract</title> <p> <italic>Objective</italic>: The objectives of this study were, first, to develop a free-flowing and stable proniosome formulation for poorly water-soluble drugs such as vinpocetine; and second, to estimate its bioavailability as oral drug delivery system.</p> <p> <italic>Methods</italic>: The proniosomes consisting of span60, cholesterol, sorbitol and vinpocetine were prepared by a novel approach. After the proniosomes were contacted with water, the suspension of vinpocetine-loaded niosomes formed automatically. The proniosomes and reconstituted niosomes were evaluated for their physicochemical characteristics, <italic>in vitro</italic> drug dissolution and release, integrity and stability at different GI tract pH conditions, <italic>in situ</italic> single-pass intestinal perfusion and <italic>in vivo</italic> bioavailability.</p> <p> <italic>Results</italic>: The proniosome powder exhibited excellent flowability. The reconstituted niosomes with high drug entrapment efficiency (89.67 ± 3.28%) showed spherical morphology with smooth surface under transmission electron microscope (TEM). X-ray diffraction (XRD) indicated that the drug was in an amorphous or molecular state in proniosome powder. <italic>In vitro</italic> dissolution and release study, proniosomes did enhance the dissolution and release rate compared to vinpocetine suspension in phosphate buffer solution (pH 7.2). Proniosome-derived niosomes could keep their integrity and stability at different GI tract pH conditions. The <italic>in situ</italic> single-pass intestinal perfusion indicated that encapsulation of vinpocetine into niosomes could largely improved the absorption of vinpocetine. The AUC(0−∞) of F2 and F3 was about 4.0- and 4.9-fold higher than that of the vinpocetine suspension, respectively. The results demonstrated the proniosomes indeed remarkably enhanced the oral bioavailability of vinpocetine.</p> <p> <italic>Conclusion</italic>: This study suggested the potential of proniosomes as stable precursors for the immediate preparation of niosome carrier systems.</p> </abstract>