RETRACTED: Thymoquinone-Loaded Soy-Phospholipid-Based Phytosomes Exhibit Anticancer Potential against Human Lung Cancer Cells (Retracted Article)

被引:53
作者
Alhakamy, Nabil A. [1 ,2 ,3 ]
Badr-Eldin, Shaimaa M. [1 ,4 ]
Fahmy, Usama A. [1 ]
Alruwaili, Nabil K. [5 ]
Awan, Zuhier A. [6 ]
Caruso, Giuseppe [7 ]
Alfaleh, Mohamed A. [8 ]
Alaofi, Ahmed L. [9 ]
Arif, Faris O. [10 ]
Ahmed, Osama A. A. [1 ,2 ]
Alghaith, Adel F. [9 ]
机构
[1] King Abdulaziz Univ, Fac Pharm, Dept Pharmaceut, Jeddah 21589, Saudi Arabia
[2] King Abdulaziz Univ, Fac Pharm, Adv Drug Delivery Res Grp, Jeddah 21589, Saudi Arabia
[3] King Abdulaziz Univ, Ctr Excellence Drug Res & Pharmaceut Ind, Jeddah 21589, Saudi Arabia
[4] Cairo Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo 11562, Egypt
[5] Jouf Univ, Coll Pharm, Dept Pharmaceut, Sakaka 2014, Al Jouf, Saudi Arabia
[6] King Abdulaziz Univ, Fac Med, Dept Clin Biochem, Jeddah 21589, Saudi Arabia
[7] Oasi Res Inst IRCCS, Via Conte Ruggero 73, I-94018 Troina, EN, Italy
[8] King Abdulaziz Univ, Fac Pharm, Dept Nat Prod & Alternat Med, Jeddah 21589, Saudi Arabia
[9] King Saud Univ, Coll Pharm, Dept Pharmaceut, POB 2457, Riyadh 11451, Saudi Arabia
[10] King Abdulaziz Univ Hosp, Gen Surg KAUH, Jeddah 21589, Saudi Arabia
关键词
thymoquinone; Box-Behnken design; biphasic release; cytotoxicity; cell cycle arrest; apoptotic potential; ROS generation; BREAST-CANCER; CYCLE ARREST; APOPTOSIS; DRUG; DELIVERY; COMPLEX; BIOAVAILABILITY; POLYMERIZATION;
D O I
10.3390/pharmaceutics12080761
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Thymoquinone (TQ), a natural polyphenol, has been associated with various pharmacological responses; however, low bioavailability of TQ limits its clinical application. Thus, a novel phytosomal delivery system of TQ-Phospholipon(R)90H complex (TQ-phytosome) was developed by refluxing combined with anti-solvent precipitation. This TQ delivery system was optimized by a three-factor, three-level Box-Behnken design. The optimized TQ-phytosome size was (45.59 +/- 1.82 nm) and the vesicle size was confirmed by transmission electron microscopy. The in vitro release pattern of the formulation indicated a biphasic release pattern, where an initial burst release was observed within 2 h, followed by a prolonged release. A remarkable increase in dose-dependent cytotoxicity was evident from the significant decrease in IC(50)value of TQ-phytosomes (4.31 +/- 2.21 mu M) against the A549 cell line. The differential effect of TQ-phytosomes in cell cycle analysis was observed, where cancer cells were accumulated on G2-M and pre-G1 phases. Furthermore, increased apoptotic induction and cell necrosis of TQ-phytosomes were revealed with the annexin V staining technique via activation of caspase-3. In reactive oxygen species (ROS) analysis, TQ-phytosomes acted to significantly increase ROS generation in A549 cells. In conclusion, the sustained release profile with significantly-improved anticancer potential could be obtained with TQ by this phytosomal nanocarrier platform.
引用
收藏
页码:1 / 17
页数:17
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