Design of absorption enhancer containing self-nanoemulsifying drug delivery system (SNEDDS) for curcumin improved anti-cancer activity and oral bioavailability

被引:42
|
作者
Kanwal, Tasmina [1 ]
Saifullah, Salim [1 ]
Rehman, Jawad Ur [1 ]
Kawish, Muhammad [1 ]
Razzak, Anam [2 ]
Maharjan, Rukesh [1 ]
Imran, Muhammad [1 ]
Ali, Imdad [1 ]
Roome, Talat [2 ]
Simjee, Shabana Usman [1 ]
Shah, Muhammad Raza [1 ]
机构
[1] Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 74200, Pakistan
[2] Dow Univ Hlth Sci, Dow Int Med Coll, Dept Pathol, Dept Lab Anim Sci,Mol Pathol Sect,Dow Diagnost Re, Karachi 74200, Pakistan
关键词
Curcumin; SNEDDS; Absorption enhancer; Anticancer activity; Oral bioavailability; IN-VIVO EVALUATION; INTESTINAL-ABSORPTION; CROMOLYN SODIUM; FORMULATION; CANCER; PHARMACOKINETICS; MICROEMULSIONS; NANOMEDICINE; NARINGENIN; SEDDS;
D O I
10.1016/j.molliq.2020.114774
中图分类号
O64 [物理化学(理论化学)、化学物理学];
学科分类号
070304 ; 081704 ;
摘要
Curcumin is a versatile natural anticancer molecule with higher level of safety; however, its clinical applicability is hindered by its physico-chemical properties. This study was designed for developing absorption enhancer contaming self-nanocmulsifying drug delivery system (SNEDDS) for improving curcumin oral bioavailability and anticancer activity. Formulation components were identified based on solubility and emulsifying ability. Ternary phase diagram of selected components was constructed for optimizing concentrations of formulation constituent. Optimized formulations were characterized using FT1R, zetasizer and atomic force microscope and investigated for dilution and thermodynamic stability. Based on drug solubility and emulsification capability, Tween 80, PEG 200 and cinnamon oil were selected as surfactant, co-surfactant, and oil phase, respectively. The optimized formulation containing 30% each of selected surfactant and co-surfactant and 40% oil revealed homogeneously distributed nano -size droplets (10644 22.27 nm) with 26.2 243 mV surface negativity after drug loading. Developed SNEDDS was highly stable and did not alter the drug chemical nature. Inclusion of absorption enhancer in the SNEDDS increased curcumin anticancer activity and cellular uptake in colon cancer cells. Similarly, drug bioavailability improved significantly when delivered orally in developed SNEDDS. Efficient performance of novel SNEDDS for curcumin improved anticancer activity and bioavailability can be safely concluded from this study. (C) 2020 Elsevier B.V. All rights reserved.
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页数:10
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