PMID- 34129135
OWN - NLM
STAT- MEDLINE
DCOM- 20210621
LR  - 20210727
IS  - 1530-9932 (Electronic)
IS  - 1530-9932 (Linking)
VI  - 22
IP  - 5
DP  - 2021 Jun 15
TI  - Fabrication and Evaluation of Celecoxib Oral Oleogel to Reduce the Inflammation 
      of Ulcerative Colitis.
PG  - 180
LID - 10.1208/s12249-021-02042-6 [doi]
AB  - Oleogel consists of hydrophobic solvent and an oleogelator. In this study, 
      attempts were made to study the influence of Celecoxib solubility, concentration 
      and dispersability on its release, absorption, and biological performance. 
      Oleogels were prepared to study the formulation variables on its stability and 
      release. Castor oil was selected as the oil and the oleogelator concentration was 
      4.5% w/w. F3 revealed the highest release and stability compared to other 
      formulae. The percent permeated across the rat intestine showed a 7.5-fold 
      increase over free Celecoxib, and its lifetime was found to be greater than 18 
      months. The efficacy of free Celecoxib and oleogel formulae to treat rats with 
      ulcerative colitis was done via the induction of ulcerative colitis (UC) through 
      administration of 5% dextran sodium sulphate (DSS). Celecoxib besides its 
      formulae significantly reduced the release of Leucine rich 2 glycoprotein (LRG), 
      Myeloperoxidase (MPO), Tumor necrosis factor-alpha (TNF-alpha), proinflammatory cytokine 
      expression, High mobility group box 1 (HMGB1), Nuclear factor kappa B (NF-KappaB), 
      Trefoil Factor 3 (TFF3), Metalloproteinase-3 (MMP3), and miRNA31. Moreover, F3 
      significantly increased the colonic cAMP in DSS treated rats and reduced the 
      intestinal inflammation beside healing of mucosa and restitution of the 
      epithelium of the gastrointestinal tract.
FAU - Sheta, Nermin M
AU  - Sheta NM
AD  - Pharmaceutics Department, Faculty of Pharmacy, October 6 University, 6th of 
      October City, Central Axis, Part 1/1, Behind Sixth October City Authority, Giza, 
      12585, Egypt. nerminsheta@o6u.edu.eg.
FAU - Boshra, Sylvia A
AU  - Boshra SA
AD  - Biochemistry Department, Faculty of Pharmacy, October 6 University, 6th of 
      October City, Central Axis, Part 1/1, Behind Sixth October City Authority, Giza, 
      12585, Egypt.
LA  - eng
PT  - Journal Article
DEP - 20210615
PL  - United States
TA  - AAPS PharmSciTech
JT  - AAPS PharmSciTech
JID - 100960111
RN  - 0 (Anti-Inflammatory Agents, Non-Steroidal)
RN  - 0 (NF-kappa B)
RN  - 0 (Organic Chemicals)
RN  - 0 (Tumor Necrosis Factor-alpha)
RN  - 0 (oleogels)
RN  - 9042-14-2 (Dextran Sulfate)
RN  - JCX84Q7J1L (Celecoxib)
SB  - IM
MH  - Animals
MH  - Anti-Inflammatory Agents, Non-Steroidal/chemical 
      synthesis/pharmacokinetics/*therapeutic use
MH  - Celecoxib/chemical synthesis/pharmacokinetics/*therapeutic use
MH  - Colitis, Ulcerative/chemically induced/*drug therapy/metabolism
MH  - Colon/drug effects/metabolism
MH  - Dextran Sulfate/toxicity
MH  - Drug Evaluation, Preclinical/methods
MH  - Inflammation/chemically induced/drug therapy/metabolism
MH  - Male
MH  - NF-kappa B/metabolism
MH  - Organic Chemicals/chemical synthesis/pharmacokinetics/therapeutic use
MH  - Rats
MH  - Rats, Wistar
MH  - Tumor Necrosis Factor-alpha/metabolism
OTO - NOTNLM
OT  - TFF3
OT  - celecoxib
OT  - miRNA31
OT  - oral oleogel capsule
OT  - ulcerative colitis
EDAT- 2021/06/16 06:00
MHDA- 2021/06/22 06:00
CRDT- 2021/06/15 13:39
PHST- 2021/02/19 00:00 [received]
PHST- 2021/05/06 00:00 [accepted]
PHST- 2021/06/15 13:39 [entrez]
PHST- 2021/06/16 06:00 [pubmed]
PHST- 2021/06/22 06:00 [medline]
AID - 10.1208/s12249-021-02042-6 [pii]
AID - 10.1208/s12249-021-02042-6 [doi]
PST - epublish
SO  - AAPS PharmSciTech. 2021 Jun 15;22(5):180. doi: 10.1208/s12249-021-02042-6.