PMID- 28847666
OWN - NLM
STAT- MEDLINE
DCOM- 20180110
LR  - 20181202
IS  - 1873-3476 (Electronic)
IS  - 0378-5173 (Linking)
VI  - 531
IP  - 1
DP  - 2017 Oct 5
TI  - Nanosuspensions of a new compound, ER-beta005, for enhanced oral bioavailability and 
      improved analgesic efficacy.
PG  - 246-256
LID - S0378-5173(17)30821-9 [pii]
LID - 10.1016/j.ijpharm.2017.08.103 [doi]
AB  - Estrogen receptor-beta005 (ER-beta005) is a novel compound developed by our group; 
      however, its application has been greatly hindered due to its low solubility. A 
      nanosuspension of insoluble drugs is a nanoscale colloidal dispersion that has 
      extremely higher drug-loading compared with other nanomedicines. In this study, 
      nanosuspensions of ER-beta005 (Nano-ER-beta005) stabilized by a food protein, beta-casein 
      (beta-CN), were prepared via an antisolvent-precipitation method to improve oral 
      absorption and thus promote therapeutic efficacy. Nano-ER-beta005, which has a 
      diameter of 110nm and drug-loading of 50%, was developed. Analyses of 
      fluorescence and circular dichroism (CD) spectra demonstrated a strong 
      interaction between beta-CN and drug particles in Nano-ER-beta005, indicating that beta-CN 
      is a potent nanosuspension stabilizer. The oral bioavailability of Nano-ER-beta005 
      was 1.6-fold greater than that of raw drug particles. Additionally, ER-beta005 was 
      confirmed to have a strong therapeutic effect against pain reactions in animal 
      models, and inhibition of this effect was significantly increased with 
      Nano-ER-beta005 treatment. In conclusion, by using beta-CN as a stabilizer, 
      nanosuspensions of ER-beta005 were developed and oral absorption was enhanced. 
      Moreover, ER-beta005 is a powerful drug that inhibits pain reactions, and its 
      therapeutic efficacy was markedly increased in the Nano-ER-beta005.
CI  - Copyright (c) 2017 Elsevier B.V. All rights reserved.
FAU - Ye, Ling
AU  - Ye L
AD  - Key Lab of Drug Metabolism & Pharmacokinetics, China Pharmaceutical University, 
      Nanjing 210009, PR China; School of Pharmaceutical Sciences, Southern Medical 
      University, Guangzhou 510515, PR China; School of Traditional Chinese Medicine, 
      Guangzhou University of Chinese Medicine, Guangzhou 51006, PR China.
FAU - Miao, Mingxing
AU  - Miao M
AD  - Key Lab of Drug Metabolism & Pharmacokinetics, China Pharmaceutical University, 
      Nanjing 210009, PR China; National Experimental Teaching Demonstration Center of 
      Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.
FAU - Li, Suning
AU  - Li S
AD  - China National Center for Biotechnology Development, Beijing 100039, PR China. 
      Electronic address: lisn@cncbd.org.cn.
FAU - Hao, Kun
AU  - Hao K
AD  - Key Lab of Drug Metabolism & Pharmacokinetics, China Pharmaceutical University, 
      Nanjing 210009, PR China. Electronic address: haokun@cpu.edu.com.
LA  - eng
PT  - Journal Article
DEP - 20170825
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Analgesics)
RN  - 0 (Drug Carriers)
RN  - 0 (Estrogen Receptor beta)
RN  - 0 (Suspensions)
SB  - IM
MH  - Administration, Oral
MH  - Analgesics/*administration & dosage
MH  - Animals
MH  - Biological Availability
MH  - Drug Carriers/*chemistry
MH  - Estrogen Receptor beta/*chemistry
MH  - Male
MH  - Mice
MH  - Nanostructures/*chemistry
MH  - Rats, Sprague-Dawley
MH  - Solubility
MH  - Suspensions
OTO - NOTNLM
OT  - Analgesic efficacy
OT  - Bioavailability
OT  - ER-beta005 (PubChem CID: 16450315)
OT  - Estrogen receptor agonist
OT  - Interaction
OT  - Nanosuspensions
OT  - Stabilizer
OT  - acetone (PubChem CID: 180)
OT  - capsaicin (PubChem CID: 1548943)
OT  - dimethyl sulfoxide (PubChem CID: 679)
OT  - ethyl acetate (PubChem CID: 8857)
OT  - isoliquiritigenin (PubChem CID: 638278)
OT  - morphine (PubChem CID: 5288826)
OT  - phenylephrine (PubChem CID: 6041)
OT  - sodium dodecyl sulfate (PubChem CID: 3423265)
OT  - sulprostone (PubChem CID: 5312153)
EDAT- 2017/08/30 06:00
MHDA- 2018/01/11 06:00
CRDT- 2017/08/30 06:00
PHST- 2017/05/12 00:00 [received]
PHST- 2017/07/31 00:00 [revised]
PHST- 2017/08/21 00:00 [accepted]
PHST- 2017/08/30 06:00 [pubmed]
PHST- 2018/01/11 06:00 [medline]
PHST- 2017/08/30 06:00 [entrez]
AID - S0378-5173(17)30821-9 [pii]
AID - 10.1016/j.ijpharm.2017.08.103 [doi]
PST - ppublish
SO  - Int J Pharm. 2017 Oct 5;531(1):246-256. doi: 10.1016/j.ijpharm.2017.08.103. Epub 
      2017 Aug 25.