Yutong Wang1, Changyuan Wang2, Jing Zhao3, Yanfang Ding4, Lei Li5. 1. School of Pharmacy, Dalian Medical University, No. 9 West Section Lvshun South Road, Dalian 116044, PR China. Electronic address: wyutong0703@163.com. 2. School of Pharmacy, Dalian Medical University, No. 9 West Section Lvshun South Road, Dalian 116044, PR China. Electronic address: 835553485@qq.com. 3. School of Pharmacy, Dalian Medical University, No. 9 West Section Lvshun South Road, Dalian 116044, PR China. Electronic address: 790713952@qq.com. 4. School of Pharmacy, Dalian Medical University, No. 9 West Section Lvshun South Road, Dalian 116044, PR China. 5. School of Pharmacy, Dalian Medical University, No. 9 West Section Lvshun South Road, Dalian 116044, PR China. Electronic address: lilei0304@dmu.edu.cn.
Abstract
BACKGROUND: 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.
BACKGROUND: 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.
Authors: María L Del Prado-Audelo; Isaac H Caballero-Florán; Jorge A Meza-Toledo; Néstor Mendoza-Muñoz; Maykel González-Torres; Benjamín Florán; Hernán Cortés; Gerardo Leyva-Gómez Journal: Biomolecules Date: 2019-02-08
Authors: Helmy Yusuf; Erlyn K D D Novitasari; Ni L W Purnami; Adhe W Mahbub; Retno Sari; Dwi Setyawan Journal: Adv Pharmacol Pharm Sci Date: 2022-03-07