A cost-effective method to prepare curcumin nanosuspensions with enhanced oral bioavailability

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• 作者：Yutong Wang ^{wyutong0703@163.com" class="auth_mail" title="E-mail the corresponding author} ; Changyuan Wang ^{835553485@qq.com" class="auth_mail" title="E-mail the corresponding author} ; Jing Zhao ^{790713952@qq.com" class="auth_mail" title="E-mail the corresponding author} ; Yanfang Ding ; Lei Li ; ^{lilei0304@dmu.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; ^{dingyanfang1201@163.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Curcumin ; Nanosuspension ; CO2 ; Bioavailability
• 刊名：Journal of Colloid and Interface Science
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：485
• 期：Complete
• 页码：91-98
• 全文大小：1880 K

文摘

Nanosuspension is one of the most promising strategies to improve the oral bioavailability of insoluble drugs. The existing techniques applied to produce nanosuspensions are classified as “bottom-up” or “top-down” methods, or a combination of both. Curcumin (CUR), a Biopharmaceutics Classification System (BCS) class IV substance, is a promising drug candidate in view of its good bioactivity, but its use is limited due to its poor solubility and permeability. In the present study, CUR nanosuspensions were developed to enhance CUR oral bioavailability using a cost-effective method different from conventional techniques.

Results

The physicochemical properties of CUR nanosuspensions were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The crystalline state of CUR in different nanosuspensions analyzed using differential scanning calorimeter (DSC) and X-ray diffraction analysis (PXRD) confirmed its amorphous state. In vitro dissolution degree of the prepared CUR nanosuspensions using TPGS or Brij78 as stabilizer was greatly increased. Pharmacokinetic studies demonstrated that the oral bioavailability of CUR was increased 3.18 and 3.7 times after administration of CUR/TPGS nanosuspensions or CUR/Brij78 nanosuspensions, when compared with the administration of CUR suspension.

Conclusions

CUR nanosuspensions produced by our cost-effective method could improve its oral bioavailability. In addition, the low-cost and time-saving method reported here is highly suitable for a fast and inexpensive preparation.