|Potentials of proniosomes for improving the oral bioavailability of poorly water-soluble drugs|
|Song, Shuangshuang1; Tian, Baocheng1; Chen, Fen1; Zhang, Wenji1; Pan, Yusheng1; Zhang, Qiang2; Yang, Xinggang1; Pan, Weisan1|
|关键词||Oral bioavailability poorly water-soluble drugs proniosomes reconstituted/proniosome-derived niosomes vinpocetine|
|刊名||DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY|
|WOS标题词||Science & Technology|
|类目[WOS]||Chemistry, Medicinal ; Pharmacology & Pharmacy|
|研究领域[WOS]||Pharmacology & Pharmacy|
|关键词[WOS]||TRANSDERMAL DELIVERY ; DISSOLUTION RATE ; SALT FORMATION ; IN-VITRO ; SOLUBILITY ; 5-FLUOROURACIL ; NANOCRYSTALS ; DISPERSION ; CARRIERS ; SYSTEM|
Objective: 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.
Methods: 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, in vitro drug dissolution and release, integrity and stability at different GI tract pH conditions, in situ singlepass intestinal perfusion and in vivo bioavailability.
Results: 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. In vitro dissolution and release study, proniosomes did enhance the dissolution and release rate compared to vinpocetine suspension in phosphate buffer solution (pH 7.2). Proniosomederived niosomes could keep their integrity and stability at different GI tract pH conditions. The in situ single-pass intestinal perfusion indicated that encapsulation of vinpocetine into niosomes could largely improved the absorption of vinpocetine. The AUC(0-infinity) 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.
Conclusion: This study suggested the potential of proniosomes as stable precursors for the immediate preparation of niosome carrier systems.
|资助机构||National Basic Research Program of China for 973 Program|
|作者单位||1.Shenyang Pharmaceut Univ, Sch Pharm, Dept Pharmaceut, Shenyang 110016, Peoples R China|
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100871, Peoples R China
|Song, Shuangshuang,Tian, Baocheng,Chen, Fen,et al. Potentials of proniosomes for improving the oral bioavailability of poorly water-soluble drugs[J]. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,2015,41(1):51-62.|
|APA||Song, Shuangshuang.,Tian, Baocheng.,Chen, Fen.,Zhang, Wenji.,Pan, Yusheng.,...&Pan, Weisan.(2015).Potentials of proniosomes for improving the oral bioavailability of poorly water-soluble drugs.DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,41(1),51-62.|
|MLA||Song, Shuangshuang,et al."Potentials of proniosomes for improving the oral bioavailability of poorly water-soluble drugs".DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY 41.1(2015):51-62.|