PMID- 37268093
OWN - NLM
STAT- MEDLINE
DCOM- 20230621
LR  - 20230621
IS  - 1879-0720 (Electronic)
IS  - 0928-0987 (Linking)
VI  - 187
DP  - 2023 Aug 1
TI  - A novel deformable liposomal hydrogel loaded with a SREBP-1-inhibiting 
      polypeptide for reducing sebum synthesis in golden hamster model.
PG  - 106483
LID - S0928-0987(23)00113-6 [pii]
LID - 10.1016/j.ejps.2023.106483 [doi]
AB  - Excessive sebum is the major factor involved in the pathophysiology of seborrheic 
      diseases. Chemical medicines can result in mild to severe side effects. 
      Polypeptides with much less side effects make them ideal for reducing sebum 
      synthesis. Sterol regulatory element-binding proteins-1 (SREBP-1) is necessary 
      for the biosynthesis of sterols. A SREBP-1-inhibiting polypeptide (SREi), which 
      competitively inhibits the ubiquitination of Insig-1 so as to suppress the 
      activation of SREBP-1 was selected as an active ingredient and formulated into 
      skin topical preparations. The SREi anionic deformable liposomes contained sodium 
      deoxycholate (SDCh) at the concentration of 4.4 mg/mL (SREi-ADL3) and SREi-ADL3 
      in 0.3% (w/v) carbomer hydrogel (SREi-ADL3-GEL) were prepared and characterized. 
      The SREi-ADL3 presented a high entrapment efficiency of 92.62 +/- 6.32%, a particle 
      size of 99.54 +/- 7.56 nm and a surface charge of -19.18 +/- 0.45 mV. SREi-ADL3-GEL 
      exhibited a sustained release behavior, a higher stability, a much more cellular 
      uptake ability and transdermal absorption. In vivo golden hamster model confirmed 
      that SREi-ADL3-GEL presented the strongest inhibitory effect on sebaceous gland 
      growth and sebum synthesis by down-regulating the mRNA and protein expression of 
      SREBP-1, fatty acid synthase (FAS) and acetyl-coenzyme A carboxylase 1 (ACC1). As 
      confirmed by histological analysis, only a small amount of sebaceous gland lobes 
      with the lightest staining intensity and the smallest dyeing area could be 
      observed in the SREi-ADL3-GEL group. Taken together, SREi-ADL3-GEL displayed 
      potential applications in sebum excessive production related diseases.
CI  - Copyright (c) 2023. Published by Elsevier B.V.
FAU - Lv, Zhe
AU  - Lv Z
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Bao, Han
AU  - Bao H
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Zhu, Ming
AU  - Zhu M
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Xie, Yizhuo
AU  - Xie Y
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Tang, Huan
AU  - Tang H
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Miao, Dongfanghui
AU  - Miao D
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Guo, Xin
AU  - Guo X
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Zhai, Xinhui
AU  - Zhai X
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Wang, Shanshan
AU  - Wang S
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Chen, Hongli
AU  - Chen H
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Cong, Dengli
AU  - Cong D
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Liu, Xin
AU  - Liu X
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China.
FAU - Pei, Jin
AU  - Pei J
AD  - Department of Biopharmacy, School of Pharmaceutical Sciences, Jilin University, 
      Changchun, PR China. Electronic address: peijin@jlu.edu.cn.
LA  - eng
PT  - Journal Article
DEP - 20230531
PL  - Netherlands
TA  - Eur J Pharm Sci
JT  - European journal of pharmaceutical sciences : official journal of the European 
      Federation for Pharmaceutical Sciences
JID - 9317982
RN  - 0 (CCAAT-Enhancer-Binding Proteins)
RN  - 0 (Liposomes)
RN  - 0 (Sterol Regulatory Element Binding Protein 1)
RN  - 0 (Hydrogels)
RN  - 0 (Peptides)
SB  - IM
MH  - Cricetinae
MH  - Animals
MH  - Mesocricetus
MH  - *Sebum/metabolism
MH  - *CCAAT-Enhancer-Binding Proteins/genetics/metabolism
MH  - Liposomes
MH  - Sterol Regulatory Element Binding Protein 1/genetics
MH  - Hydrogels
MH  - Peptides
OTO - NOTNLM
OT  - Deformable liposome
OT  - Hydrogel
OT  - Polypeptide
OT  - Sebum
OT  - Transdermal delivery
COIS- Declaration of Competing Interest The authors declare that they have no competing 
      financial interests or personal relationships that could have appeared to 
      influence the work reported in this paper.
EDAT- 2023/06/03 11:42
MHDA- 2023/06/21 06:42
CRDT- 2023/06/02 19:22
PHST- 2023/02/09 00:00 [received]
PHST- 2023/05/10 00:00 [revised]
PHST- 2023/05/30 00:00 [accepted]
PHST- 2023/06/21 06:42 [medline]
PHST- 2023/06/03 11:42 [pubmed]
PHST- 2023/06/02 19:22 [entrez]
AID - S0928-0987(23)00113-6 [pii]
AID - 10.1016/j.ejps.2023.106483 [doi]
PST - ppublish
SO  - Eur J Pharm Sci. 2023 Aug 1;187:106483. doi: 10.1016/j.ejps.2023.106483. Epub 
      2023 May 31.