PMID- 29497294
OWN - NLM
STAT- MEDLINE
DCOM- 20180425
LR  - 20240313
IS  - 1178-2013 (Electronic)
IS  - 1176-9114 (Print)
IS  - 1176-9114 (Linking)
VI  - 13
DP  - 2018
TI  - Polymeric micelles for potentiated antiulcer and anticancer activities of 
      naringin.
PG  - 1009-1027
LID - 10.2147/IJN.S154325 [doi]
AB  - Naringin is one of the most interesting phytopharmaceuticals that has been widely 
      investigated for various biological actions. Yet, its low water solubility, 
      limited permeability, and suboptimal bioavailability limited its use. Therefore, 
      in this study, polymeric micelles of naringin based on pluronic F68 (PF68) were 
      developed, fully characterized, and optimized. The optimized formula was 
      investigated regarding in vitro release, storage stability, and in vitro 
      cytotoxicity vs different cell lines. Also, cytoprotection against 
      ethanol-induced ulcer in rats and antitumor activity against Ehrlich ascites 
      carcinoma in mice were investigated. Nanoscopic and nearly spherical 1:50 
      micelles with the mean diameter of 74.80+/-6.56 nm and narrow size distribution 
      were obtained. These micelles showed the highest entrapment efficiency (EE%; 
      96.14+/-2.29). The micelles exhibited prolonged release up to 48 vs 10 h for free 
      naringin. The stability of micelles was confirmed by insignificant changes in 
      drug entrapment, particle size, and retention (%) (91.99+/-3.24). At lower dose 
      than free naringin, effective cytoprotection of 1:50 micelles against 
      ethanol-induced ulcer in rat model has been indicated by significant reduction in 
      mucosal damage, gastric level of malondialdehyde, gastric expression of tumor 
      necrosis factor-alpha, caspase-3, nuclear factor kappa-light-chain-enhancer of 
      activated B cells, and interleukin-6 with the elevation of gastric reduced 
      glutathione and superoxide dismutase when compared with the positive control 
      group. As well, these micelles provoked pronounced antitumor activity assessed by 
      potentiated in vitro cytotoxicity particularly against colorectal carcinoma cells 
      and tumor growth inhibition when compared with free naringin. In conclusion, 1:50 
      naringin-PF68 micelles can be represented as a potential stable nanodrug delivery 
      system with prolonged release and enhanced antiulcer as well as antitumor 
      activities.
FAU - Mohamed, Elham Abdelmonem
AU  - Mohamed EA
AD  - Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 
      Egypt.
FAU - Abu Hashim, Irhan Ibrahim
AU  - Abu Hashim II
AD  - Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 
      Egypt.
FAU - Yusif, Rehab Mohammad
AU  - Yusif RM
AD  - Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 
      Egypt.
AD  - Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, 
      Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia.
FAU - Shaaban, Ahmed Abdel Aziz
AU  - Shaaban AAA
AD  - Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura 
      University, Mansoura, Egypt.
FAU - El-Sheakh, Ahmed Ramadan
AU  - El-Sheakh AR
AD  - Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura 
      University, Mansoura, Egypt.
FAU - Hamed, Mohammed Fawzy
AU  - Hamed MF
AD  - Department of Pathology, Faculty of Veterinary Medicine, Mansoura University, 
      Mansoura, Egypt.
FAU - Badria, Farid Abd Elreheem
AU  - Badria FAE
AD  - Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura, 
      Egypt.
LA  - eng
PT  - Journal Article
DEP - 20180219
PL  - New Zealand
TA  - Int J Nanomedicine
JT  - International journal of nanomedicine
JID - 101263847
RN  - 0 (Anti-Ulcer Agents)
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Drug Carriers)
RN  - 0 (Flavanones)
RN  - 0 (Micelles)
RN  - 106392-12-5 (Poloxamer)
RN  - N7TD9J649B (naringin)
SB  - IM
MH  - Animals
MH  - Anti-Ulcer Agents/administration & dosage/chemistry/*pharmacology
MH  - Antineoplastic Agents/administration & dosage/chemistry/*pharmacology
MH  - Biological Availability
MH  - Cell Line, Tumor
MH  - Drug Carriers/*chemistry/pharmacokinetics
MH  - Drug Liberation
MH  - Female
MH  - Flavanones/administration & dosage/chemistry/*pharmacology
MH  - Humans
MH  - Male
MH  - Mice
MH  - Micelles
MH  - Particle Size
MH  - Poloxamer/chemistry
MH  - Rats, Sprague-Dawley
MH  - Solubility
MH  - Ulcer/chemically induced/drug therapy
PMC - PMC5823073
OTO - NOTNLM
OT  - antitumor activity
OT  - antiulcer
OT  - in vitro cytotoxicity
OT  - naringin
OT  - pluronic F68
OT  - polymeric micelles
COIS- Disclosure The authors report no conflicts of interest in this work.
EDAT- 2018/03/03 06:00
MHDA- 2018/04/26 06:00
PMCR- 2018/02/19
CRDT- 2018/03/03 06:00
PHST- 2018/03/03 06:00 [entrez]
PHST- 2018/03/03 06:00 [pubmed]
PHST- 2018/04/26 06:00 [medline]
PHST- 2018/02/19 00:00 [pmc-release]
AID - ijn-13-1009 [pii]
AID - 10.2147/IJN.S154325 [doi]
PST - epublish
SO  - Int J Nanomedicine. 2018 Feb 19;13:1009-1027. doi: 10.2147/IJN.S154325. 
      eCollection 2018.